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Synthesis and Characterization of ZIF-90 Nanoparticles as Potential Brain Cancer Therapy Pharmaceutics (IF 5.4) Pub Date : 2024-03-18 Lorenzo Monarca, Francesco Ragonese, Paola Sabbatini, Concetta Caglioti, Matteo Stamegna, Federico Palazzetti, Paolo Sportoletti, Ferdinando Costantino, Bernard Fioretti
Human glioblastoma is probably the most malignant and aggressive among cerebral tumors, of which it represents approximately 80% of the reported cases, with an overall survival rate that is quite low. Current therapies include surgery, chemotherapy, and radiotherapy, with associated consistent side effects and low efficacy. The hardness in reaching the site of action, and overcoming the blood–brain
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Preparation of Nanoparticles Loaded with Membrane-Impermeable Peptide AC3-I and Its Protective Effect on Myocardial Ischemia and Reperfusion Pharmaceutics (IF 5.4) Pub Date : 2024-03-18 Yi Liu, Yingyi Niu, Wenjie Zhang, Kaikai Wang, Tianqing Liu, Weizhong Zhu
Purpose: It is well known that inhibition of Ca2+/calmodulin-dependent protein kinase II (CaMKII) provides cardiac protection in cases of myocardial ischemia–reperfusion injury. However, there are currently no cytoplasm-impermeable drugs that target CaMKII. The aim of this study was to develop curcumin albumin nanoparticles (HSA-CCM NPs) containing AC3-I and investigate their protective effects on
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The Physicochemical Compatibility of Sildenafil Injection with Parenteral Medications Used in Neonatal Intensive Care Settings Pharmaceutics (IF 5.4) Pub Date : 2024-03-18 D. Thisuri N. De Silva, Tobias Strunk, Michael Petrovski, Madhu Page-Sharp, Brioni R. Moore, Kevin T. Batty
Sildenafil is used to treat pulmonary hypertension in neonatal intensive care unit (NICU) settings. As multiple intravenous (IV) medications are co-administered in NICU settings, we sought to investigate the physicochemical compatibility of sildenafil with a range of IV drugs. Sildenafil 600 mcg/mL or 60 mcg/mL was mixed 1:1 with the secondary drug solution to simulate Y-site co-administration procedures
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Cannabinoid-Induced Inhibition of Morphine Glucuronidation and the Potential for In Vivo Drug–Drug Interactions Pharmaceutics (IF 5.4) Pub Date : 2024-03-18 Shelby Coates, Keti Bardhi, Philip Lazarus
Opioids are commonly prescribed for the treatment of chronic pain. Approximately 50% of adults who are prescribed opioids for pain co-use cannabis with their opioid treatment. Morphine is primarily metabolized by UDP-glucuronosyltransferase (UGT) 2B7 to an inactive metabolite, morphine-3-glucuronide (M3G), and an active metabolite, morphine-6-glucuronide (M6G). Previous studies have shown that major
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Fundamentals and Applications of Focused Ultrasound-Assisted Cancer Immune Checkpoint Inhibition for Solid Tumors Pharmaceutics (IF 5.4) Pub Date : 2024-03-16 Sepideh Jahangiri, François Yu
Despite spectacular clinical successes across several cancer types, immune checkpoint inhibition is effective only in subgroups of patients and suffers from significant systemic toxicities, highlighting the need to understand and locally overcome the mechanisms of therapeutic resistance. Similarly to other therapeutics, immunotherapies face delivery challenges (for example, antibodies need to reach
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Natural Stabilizers and Nanostructured Lipid Carrier Entrapment for Photosensitive Compounds, Curcumin and Capsaicin Pharmaceutics (IF 5.4) Pub Date : 2024-03-17 Wipanan Jandang, Chadarat Ampasavate, Kanokwan Kiattisin
Capsaicin and curcumin, the active components of chili and turmeric, are prone to instability when exposed to light. Therefore, this research aimed to enhance the photostability of both extracts via the use of antioxidants, natural sunscreen, and nanostructured lipid carriers (NLCs). NLCs were chosen for this this study due to their advantages in terms of stability, drug loading capacity, occlusive
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AMPK Activation by Cimicifuga racemosa Extract Ze 450 Is Associated with Metabolic Effects and Cellular Resilience against Age-Related Pathologies in Different Tissue Cell Types Pharmaceutics (IF 5.4) Pub Date : 2024-03-13 Madeline Günther, Peter Schnierle, Thorsten Rose, Jonathan Schlegel, Georg Boonen, Jürgen Drewe, Eduardo Muñoz, Bernd L. Fiebich, Carsten Culmsee
Cimicifuga racemosa extracts (CREs) have gained well-established use for the treatment of menopausal symptoms such as hot flushes and excessive sweating, and weight gain. While the clinical effects of CREs have been well documented, the mechanisms underlying these effects are largely unknown. More recently, the metabolic effects of the CRE Ze 450 were demonstrated in cultured cells in vitro and in
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Real-Time Cone-Growth Model for Determination of Pharmaceutical Powder Flow Properties Pharmaceutics (IF 5.4) Pub Date : 2024-03-15 Gyula Farkas, Sándor Nagy, Attila Dévay, Aleksandar Széchenyi, Szilárd Pál
The flow properties of pellets or granules are crucial for further processing drug dosage forms. Optimal compression or filling of multiparticulate dosage forms into capsules is influenced by forces between discrete particles, which could be partially characterized by flow properties. Several techniques have been developed to examine flowability, including static and dynamic methods applying empirical
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Nanomedicine for the Treatment of Viral Diseases: Smaller Solution to Bigger Problems Pharmaceutics (IF 5.4) Pub Date : 2024-03-16 Suvankar Ghorai, Harshita Shand, Soumendu Patra, Kingshuk Panda, Maria J. Santiago, Md. Sohanur Rahman, Srinivasan Chinnapaiyan, Hoshang J. Unwalla
The continuous evolution of new viruses poses a danger to world health. Rampant outbreaks may advance to pandemic level, often straining financial and medical resources to breaking point. While vaccination remains the gold standard to prevent viral illnesses, these are mostly prophylactic and offer minimal assistance to those who have already developed viral illnesses. Moreover, the timeline to vaccine
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Revolutionizing Three-Dimensional Printing: Enhancing Quality Assurance and Point-of-Care Integration through Instrumentation Pharmaceutics (IF 5.4) Pub Date : 2024-03-16 Javier Suárez-González, Eduardo Díaz-Torres, Cecilia N. Monzón-Rodríguez, Ana Santoveña-Estévez, José B. Fariña
Three-dimensional printing in the field of additive manufacturing shows potential for customized medicines and solving gaps in paediatric formulations. Despite successful clinical trials, 3D printing use in pharmaceutical point-of-care is limited by regulatory loopholes and a lack of Pharmacopoeia guidelines to ensure quality. Semi-solid extrusion is a 3D printing technology that stands out for its
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Effects of Combined Treatment with Sodium Dichloroacetate and Sodium Valproate on the Genes in Inflammation- and Immune-Related Pathways in T Lymphocytes from Patients with SARS-CoV-2 Infection with Pneumonia: Sex-Related Differences Pharmaceutics (IF 5.4) Pub Date : 2024-03-16 Donatas Stakišaitis, Linas Kapočius, Vacis Tatarūnas, Dovydas Gečys, Auksė Mickienė, Tomas Tamošuitis, Rasa Ugenskienė, Arūnas Vaitkevičius, Ingrida Balnytė, Vaiva Lesauskaitė
The study presents data on the anti-inflammatory effects of a combination of sodium dichloroacetate and sodium valproate (DCA–VPA) on the expression of inflammation- and immune response-related genes in T lymphocytes of SARS-CoV-2 patients. The study aimed to assess the effects of DCA–VPA on the genes of cytokine activity, chemokine-mediated signaling, neutrophil chemotaxis, lymphocyte chemotaxis,
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Role of Biofunctionalized Nanoparticles in Digestive Cancer Vaccine Development Pharmaceutics (IF 5.4) Pub Date : 2024-03-16 Razvan Zdrehus, Cristian Delcea, Lucian Mocan
Nanotechnology has provided an opportunity for unparalleled development of the treatment of various severe diseases. The unique properties of nanoparticles offer a promising strategy for enhancing antitumor immunity by enhancing immunogenicity and presentation of tumor autoantigens for cancer immunotherapy. Polymeric, liposomal, carbon or silica-based nanoparticles are among those with major immunomodulatory
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Lipid Nanocarriers-Enabled Delivery of Antibiotics and Antimicrobial Adjuvants to Overcome Bacterial Biofilms Pharmaceutics (IF 5.4) Pub Date : 2024-03-14 Anam Ahsan, Nicky Thomas, Timothy J. Barnes, Santhni Subramaniam, Thou Chen Loh, Paul Joyce, Clive A. Prestidge
The opportunistic bacteria growing in biofilms play a decisive role in the pathogenesis of chronic infectious diseases. Biofilm-dwelling bacteria behave differently than planktonic bacteria and are likely to increase resistance and tolerance to antimicrobial therapeutics. Antimicrobial adjuvants have emerged as a promising strategy to combat antimicrobial resistance (AMR) and restore the efficacy of
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Liposome-Based Drug Delivery Systems in Cancer Research: An Analysis of Global Landscape Efforts and Achievements Pharmaceutics (IF 5.4) Pub Date : 2024-03-14 Islam Hamad, Amani A. Harb, Yasser Bustanji
Lipid-bilayer-based liposomes are gaining attention in scientific research for their versatile role in drug delivery. With their amphiphilic design, liposomes efficiently encapsulate and deliver drugs to targeted sites, offering controlled release. These artificial structures hold great promise in advancing cancer therapy methodologies. Bibliometric research analyzes systematic literary data statistically
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Drug Repurposing of Metformin for the Treatment of Haloperidol-Related Behavior Disorders and Oxidative Stress: A Preliminary Study Pharmaceutics (IF 5.4) Pub Date : 2024-03-15 George Jîtcă, Zsolt Gáll, Carmen-Maria Jîtcă, Mădălina-Georgiana Buț, Erzsébet Májai
A particular attribute of the brain lies in the ability to learn, acquire information from the environment, and utilize the learned information. Previous research has noted that various factors (e.g., age, stress, anxiety, pathological issues), including antipsychotic medications, affect the brain and memory. The current study aimed to reveal the effects of chronic metformin treatment on the cognitive
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Molecular Imaging for Lung Cancer: Exploring Small Molecules, Peptides, and Beyond in Radiolabeled Diagnostics Pharmaceutics (IF 5.4) Pub Date : 2024-03-15 Meliha Ekinci, Tais Monteiro Magne, Luciana Magalhães Rebelo Alencar, Pierre Basilio Almeida Fechine, Ralph Santos-Oliveira, Derya Ilem-Özdemir
It is evident that radiolabeled drug delivery systems hold great promise in the field of lung cancer management. The combination of therapeutic agents with radiotracers not only allows for precise localization within lung tumors but also enables real-time monitoring of drug distribution. This approach has the potential to enhance targeted therapy and improve patient outcomes. The integration of advanced
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Useful Role of a New Generation of Dexamethasone, Vitamin E and Human Serum Albumin Microparticles in the Prevention of Excitotoxicity Injury in Retinal Ocular Diseases Pharmaceutics (IF 5.4) Pub Date : 2024-03-15 Javier Rodríguez Villanueva, Pedro de la Villa, Rocío Herrero-Vanrell, Irene Bravo-Osuna, Manuel Guzmán-Navarro
Excitotoxicity has been linked to the pathogenesis of several serious degenerative ocular diseases. Long-term overactivation of the NMDA receptor by glutamate in retinal ganglion cells (RGCs) results in degeneration, apoptosis and loss of function leading to blindness. NMDA receptor antagonists have been proposed as a pharmacological blockage of glutamate excitotoxicity. However, an inhibition of the
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In Vivo Predictive Dissolution and Biopharmaceutic-Based In Silico Model to Explain Bioequivalence Results of Valsartan, a Biopharmaceutics Classification System Class IV Drug Pharmaceutics (IF 5.4) Pub Date : 2024-03-13 Isabel Gonzalez-Alvarez, Alejandro Ruiz-Picazo, Ruben Selles-Talavera, Andres Figueroa-Campos, Virginia Merino, Marival Bermejo, Marta Gonzalez-Alvarez
The purpose of this study was to predict the in vivo bioequivalence (BE) outcome of valsartan (VALS, BCS class IV) from three oral-fixed combination products with hydrochlorothiazide (HCTZ, BCS class III) (Co-Diovan® Forte as reference and two generic formulations in development) by conducting in vivo predictive dissolution with a gastrointestinal simulator (GIS) and a physiologically based biopharmaceutic
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Amide-to-Triazole Switch in Somatostatin-14-Based Radioligands: Impact on Receptor Affinity and In Vivo Stability Pharmaceutics (IF 5.4) Pub Date : 2024-03-13 Xabier Guarrochena, Panagiotis Kanellopoulos, Anna Stingeder, Lisa-Maria Rečnik, Irene V. J. Feiner, Marie Brandt, Wolfgang Kandioller, Theodosia Maina, Berthold A. Nock, Thomas L. Mindt
The use of metabolically stabilized, radiolabeled somatostatin (SST) analogs ([68Ga]Ga/[177Lu]Lu-DOTA-TATE/TOC/NOC) is well established in nuclear medicine. Despite the pivotal role of these radioligands in the diagnosis and therapy of neuroendocrine tumors (NETs), their inability to interact with all five somatostatin receptors (SST1–5R) limits their clinical potential. [111In]In-AT2S is a radiolabeled
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Development of a Semi-Mechanistic Modeling Framework for Wet Bead Milling of Pharmaceutical Nanosuspensions Pharmaceutics (IF 5.4) Pub Date : 2024-03-13 Donald J. Clancy, Gulenay Guner, Sayantan Chattoraj, Helen Yao, M. Connor Faith, Zahra Salahshoor, Kailey N. Martin, Ecevit Bilgili
This study aimed to develop a practical semi-mechanistic modeling framework to predict particle size evolution during wet bead milling of pharmaceutical nanosuspensions over a wide range of process conditions and milling scales. The model incorporates process parameters, formulation parameters, and equipment-specific parameters such as rotor speed, bead type, bead size, bead loading, active pharmaceutical
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Designing a Placebo Microneedle Stamp: Modeling and Validation in a Clinical Control Trial Pharmaceutics (IF 5.4) Pub Date : 2024-03-14 Seung-Yeon Jeong, Ye-Seul Lee, Ji-Yeun Park, Jung-Hwan Park, Hi-Joon Park, Song-Yi Kim
Recently, several clinical studies have been conducted using microneedles (MNs), and various devices have been developed. This study aimed to propose and confirm the feasibility of a placebo control for activating MN clinical research. A 0.5 mm MN stamp with 42 needles was used as a treatment intervention, and a placebo stamp with four acupressure-type needles that did not penetrate was proposed and
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Cellular Uptake and Transport Mechanism Investigations of PEGylated Niosomes for Improving the Oral Delivery of Thymopentin Pharmaceutics (IF 5.4) Pub Date : 2024-03-14 Mengyang Liu, Darren Svirskis, Thomas Proft, Jacelyn Loh, Yuan Huang, Jingyuan Wen
Background: Although its immunomodulatory properties make thymopentin (TP5) appealing, its rapid metabolism and inactivation in the digestive system pose significant challenges for global scientists. PEGylated niosomal nanocarriers are hypothesized to improve the physicochemical stability of TP5, and to enhance its intestinal permeability for oral administration. Methods: TP5-loaded PEGylated niosomes
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The Processing Space of the Spray-Dried Mannitol-Leucine System for Pulmonary Drug Delivery Pharmaceutics (IF 5.4) Pub Date : 2024-03-14 Riley T. Schweizer, Mani Ordoubadi, Cody A. Prather, Reinhard Vehring, Kimberly B. Shepard
Designing spray-dried particles for inhalation aims at specific physicochemical properties including a respirable aerodynamic diameter and adequate powder dispersibility. Leucine, an amphiphilic amino acid, has been shown to aid in optimizing bulk powder properties. Mannitol, a model crystalline active and common bulking agent, was co-sprayed with leucine at several excipient ratios, ethanol/water
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Impact of Polyvinylpyrrolidone-Vinyl Acetate Copolymer and Sodium Starch Glycolate Excipients on Phenolic Extraction from Red Clover: Enhancing Biological Activity and Antioxidant Potential Pharmaceutics (IF 5.4) Pub Date : 2024-03-14 Jurga Andreja Kazlauskaite, Mindaugas Marksa, Jurga Bernatoniene
Adding certain excipients during the extraction process can enhance the concentration of target compounds, leading to potentially increased biological properties of the plant extract. This study explores the impact of PVP/VAC and SSG excipients on red clover bud extracts, aiming to enhance their concentration of target compounds and, consequently, their biological properties. The antioxidative potential
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Combination of Betulinic Acid Fragments and Carbonic Anhydrase Inhibitors—A New Drug Targeting Approach Pharmaceutics (IF 5.4) Pub Date : 2024-03-14 Matthias Bache, Niels V. Heise, Andreas Thiel, Anne Funtan, Franziska Seifert, Marina Petrenko, Antje Güttler, Sarah Brandt, Thomas Mueller, Dirk Vordermark, Iris Thondorf, René Csuk, Reinhard Paschke
Human carbonic anhydrase IX (hCA IX) is a zinc(II)-dependent metalloenzyme that plays a critical role in the conversion of carbon dioxide and water to protons and bicarbonate. It is a membrane-bound protein with an extracellular catalytic center that is predominantly overexpressed in solid hypoxic tumors. Sulfamates and sulfonamides, for example acetazolamide (AZA), have been used to inhibit hCA IX
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Combined Delivery of miR-15/16 through Humanized Ferritin Nanocages for the Treatment of Chronic Lymphocytic Leukemia Pharmaceutics (IF 5.4) Pub Date : 2024-03-14 Francesca Romana Liberati, Sara Di Russo, Lorenzo Barolo, Giovanna Peruzzi, Maria Vittoria Farina, Sharon Spizzichino, Federica Di Fonzo, Deborah Quaglio, Luca Pisano, Bruno Botta, Alessandra Giorgi, Alberto Boffi, Francesca Cutruzzolà, Alessio Paone, Paola Baiocco
Chronic lymphocytic leukemia (CLL) is a widespread type of leukemia that predominantly targets B lymphocytes, undermining the balance between cell proliferation and apoptosis. In healthy B cells, miR-15/16, a tandem of microRNAs, functions as a tumor suppressor, curbing the expression of the antiapoptotic B cell lymphoma 2 protein (Bcl-2). Conversely, in CLL patients, a recurring deletion on chromosome
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Enhanced Skin Permeation of 5-Fluorouracil through Drug-in-Adhesive Topical Patches Pharmaceutics (IF 5.4) Pub Date : 2024-03-10 Sangseo Kim, Souha H. Youssef, Kyung Min Kirsten Lee, Yunmei Song, Sachin Vaidya, Sanjay Garg
5-fluorouracil (5-FU), commercially available as a topical product, is approved for non-melanoma skin cancer (NMSC) treatment with several clinical limitations. This work aimed to develop 5-FU-loaded topical patches as a potential alternative to overcome such drawbacks. The patches offer accurate dosing, controlled drug release and improved patient compliance. Our study highlights the development of
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A New Algorithm Integrating Molecular Response, Toxicity, and Plasma Level Measures for Ponatinib Dose Choice in Patients Affected by Chronic Myeloid Leukemia Pharmaceutics (IF 5.4) Pub Date : 2024-03-11 Sara Galimberti, Elisabetta Abruzzese, Giacomo Luci, Claudia Baratè, Luigia Luciano, Alessandra Iurlo, Giovanni Caocci, Riccardo Morganti, Fabio Stefanelli, Antonello Di Paolo
Ponatinib may be effective in chronic myeloid leukemia (CML) patients after failure of first/second line therapies. Although its efficacy for minimum plasma concentrations (Cmin) is >21.3 ng/mL (equal to 40 nM), ponatinib may cause adverse events (AE) that require dose optimization. The present study was aimed at investigating any possible correlations among ponatinib dose, plasma concentration, molecular
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Weekly Oral Tenofovir Alafenamide Protects Macaques from Vaginal and Rectal Simian HIV Infection Pharmaceutics (IF 5.4) Pub Date : 2024-03-11 Ivana Massud, Kenji Nishiura, Susan Ruone, Angela Holder, Chuong Dinh, Jonathan Lipscomb, James Mitchell, George M. Khalil, Walid Heneine, J. Gerardo Garcίa-Lerma, Charles W. Dobard
Pre-exposure prophylaxis (PrEP) with a weekly oral regimen of antiretroviral drugs could be a suitable preventative option for individuals who struggle with daily PrEP or prefer not to use long-acting injectables. We assessed in macaques the efficacy of weekly oral tenofovir alafenamide (TAF) at doses of 13.7 or 27.4 mg/kg. Macaques received weekly oral TAF for six weeks and were exposed twice-weekly
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Exploring Variability in Rifampicin Plasma Exposure and Development of Anti-Tuberculosis Drug-Induced Liver Injury among Patients with Pulmonary Tuberculosis from the Pharmacogenetic Perspective Pharmaceutics (IF 5.4) Pub Date : 2024-03-12 Agnija Kivrane, Viktorija Ulanova, Solveiga Grinberga, Eduards Sevostjanovs, Anda Viksna, Iveta Ozere, Ineta Bogdanova, Maksims Zolovs, Renate Ranka
Genetic polymorphisms can exert a considerable impact on drug pharmacokinetics (PK) and the development of adverse drug reactions (ADR). However, the effect of genetic polymorphisms on the anti-tuberculosis (anti-TB) drug, and particularly rifampicin (RIF), exposure or anti-TB drug-induced liver injury (DILI) remains uncertain. Here, we evaluated the relationship between single nucleotide polymorphisms
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The Effect of Formulation Variables on the Manufacturability of Clopidogrel Tablets via Fluidized Hot-Melt Granulation—From the Lab Scale to the Pilot Scale Pharmaceutics (IF 5.4) Pub Date : 2024-03-13 Béla Kovács, Erzsébet-Orsolya Tőkés, Éva Katalin Kelemen, Katalin Zöldi, Francisc Boda, Edit Suba, Boglárka Kovács-Deák, Tibor Casian
Solid pharmaceutical formulations with class II active pharmaceutical ingredients (APIs) face dissolution challenges due to limited solubility, affecting in vivo behavior. Robust computational tools, via data mining, offer valuable insights into product performance, complementing traditional methods and aiding in scale-up decisions. This study utilizes the design of experiments (DoE) to understand
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Modulation of Heat Shock Protein Expression in Alveolar Adenocarcinoma Cells through Gold Nanoparticles and Cisplatin Treatment Pharmaceutics (IF 5.4) Pub Date : 2024-03-11 Bashiru Ibrahim, Taiwo Hassan Akere, Swaroop Chakraborty, Eugenia Valsami-Jones, Hanene Ali-Boucetta
Heat-shock proteins (HSPs) are stress-responsive molecules belonging to the family of evolutionary molecular chaperones known to be crucial in many cancer types, including human alveolar adenocarcinoma cells (A549). These proteins are highly overexpressed in cancers to support their ability to accommodate imbalances in cell signalling, DNA alterations, proteins, and energy metabolism associated with
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Stem Cell-Derived Extracellular Vesicles in the Treatment of Cardiovascular Diseases Pharmaceutics (IF 5.4) Pub Date : 2024-03-11 Jennifer McDonald, Sidhesh Mohak, Zsolt Fabian
Cardiovascular disease constitutes a noteworthy public health challenge characterized by a pronounced incidence, frequency, and mortality rate, particularly impacting specific demographic groups, and imposing a substantial burden on the healthcare infrastructure. Certain risk factors, such as age, gender, and smoking, contribute to the prevalence of fatal cardiovascular disease, highlighting the need
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Metformin-Mediated Improvement in Solubility, Stability, and Permeability of Nonsteroidal Anti-Inflammatory Drugs Pharmaceutics (IF 5.4) Pub Date : 2024-03-11 Qi An, Cheng Xing, Zhipeng Wang, Shuang Li, Wenwen Wang, Shiying Yang, Linglei Kong, Dezhi Yang, Li Zhang, Guanhua Du, Yang Lu
Nonsteroidal anti-inflammatory drugs (NSAIDs) are class II biopharmaceutics classification system drugs. The poor aqueous solubility of NSAIDs can lead to limited bioavailability after oral administration. Metformin (MET), a small-molecule compound, can be used in crystal engineering to modulate the physicochemical properties of drugs and to improve the bioavailability of orally administered drugs
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In Vitro Profile of Hydrocortisone Release from Three-Dimensionally Printed Paediatric Mini-Tablets Pharmaceutics (IF 5.4) Pub Date : 2024-03-11 Chrystalla Protopapa, Angeliki Siamidi, Siva Satyanarayana Kolipaka, Laura Andrade Junqueira, Dennis Douroumis, Marilena Vlachou
Three-dimensional (3D) printing is quickly being adopted in pharmaceutics due to the many advantages it offers, including treatment, adaptability, the reduction in waste and the accelerated development of new formulations. In this study, micro-extrusion printing was implemented for the production of modified-release hydrocortisone (HCT) mini-tablets for paediatric patients. For the developed formulations
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Mesoporous Silica as an Alternative Vehicle to Overcome Solubility Limitations Pharmaceutics (IF 5.4) Pub Date : 2024-03-12 Tim Becker, Jan Heitkötter, Anna K. Krome, Andrea Schiefer, Kenneth Pfarr, Alexandra Ehrens, Miriam Grosse, Birthe Sandargo, Ingo Stammberger, Marc Stadler, Marc P. Hübner, Stefan Kehraus, Achim Hoerauf, Karl G. Wagner
Toxicological studies are a part of the drug development process and the preclinical stages, for which suitable vehicles ensuring easy and safe administration are crucial. However, poor aqueous solubility of drugs complicates vehicle screening for oral administration since non-aqueous solvents are often not tolerable. In the case of the anti-infective corallopyronin A, currently undergoing preclinical
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Validated LC-MS/MS Assay for the Quantitative Determination of Fenretinide in Plasma and Tumor and Its Application in a Pharmacokinetic Study in Mice of a Novel Oral Nanoformulation of Fenretinide Pharmaceutics (IF 5.4) Pub Date : 2024-03-12 Cristina Matteo, Isabella Orienti, Adriana Eramo, Ann Zeuner, Mariella Ferrari, Alice Passoni, Renzo Bagnati, Marianna Ponzo, Ezia Bello, Massimo Zucchetti, Roberta Frapolli
We describe the development and validation of a HPLC-MS/MS method to assess the pharmacokinetics and tumor distribution of fenretinide, a synthetic retinoid chemically related to all-trans-retinoic acid, after administration of a novel oral nanoformulation of fenretinide, called bionanofenretinide (BNF). BNF was developed to overcome the major limitation of fenretinide: its poor aqueous solubility
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Tobramycin Reduces Pulmonary Toxicity of Polymyxin B via Inhibiting the Megalin-Mediated Drug Uptake in the Human Lung Epithelial Cells Pharmaceutics (IF 5.4) Pub Date : 2024-03-12 Maizbha Uddin Ahmed, Jian Li, Qi (Tony) Zhou
Accumulation of polymyxins in the lung epithelial cells can lead to increased mitochondrial oxidative stress and pulmonary toxicity. Aminoglycosides and polymyxins are used, via intravenous and pulmonary delivery, against multidrug-resistant Gram-negative pathogens. Our recent in vitro and animal studies demonstrated that the co-administration of polymyxins with aminoglycosides decreases polymyxin-induced
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Gelatin-/Alginate-Based Hydrogel Scaffolds Reinforced with TiO2 Nanoparticles for Simultaneous Release of Allantoin, Caffeic Acid, and Quercetin as Multi-Target Wound Therapy Platform Pharmaceutics (IF 5.4) Pub Date : 2024-03-07 Marija Babić Radić, Marija Vukomanović, Jasmina Nikodinović-Runić, Simonida Tomić
This study proposes synthesis and evaluation of gelatin-/alginate-based hydrogel scaffolds reinforced with titanium dioxide (TiO2) nanoparticles which, through their combination with allantoin, quercetin, and caffeic acid, provide multi-target therapy directed on all phases of the wound healing process. These scaffolds provide the simultaneous release of bioactive agents and concurrently support cell/tissue
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Continuous Microfluidic Antisolvent Crystallization as a Bottom-Up Solution for the Development of Long-Acting Injectable Formulations Pharmaceutics (IF 5.4) Pub Date : 2024-03-08 Snehashis Nandi, Laura Verstrepen, Mariana Hugo Silva, Luis Padrela, Lidia Tajber, Alain Collas
A bottom-up approach was investigated to produce long-acting injectable (LAI) suspension-based formulations to overcome specific limitations of top-down manufacturing methods by tailoring drug characteristics while making the methods more sustainable and cost-efficient. A Secoya microfluidic crystallization technology-based continuous liquid antisolvent crystallization (SCT-CLASC) process was optimized
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Safety and Tolerability of KIO-101 Eye Drops in Healthy Volunteers and Patients with Ocular Surface Disease—A Phase I Study Pharmaceutics (IF 5.4) Pub Date : 2024-03-05 Doreen Schmidl, Nikolaus Hommer, Martin Kallab, Andreas Schlatter, Clemens Nadvornik, Franz Obermayr, Stefan Sperl, Eric J. Daniels, Gerhard Garhöfer
Purpose: Inhibitors of dihydroorotate dehydrogenase (DHODH) have been found to be potent anti-inflammatory agents. Recently, a topical formulation (KIO-101 eye drops) of a DHODH inhibitor has been developed. The aim of the present study was to evaluate the safety and tolerability of KIO-101 eye drops in Healthy Volunteers (HVs) and patients with conjunctival hyperemia. Methods: The study was carried
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Silver Nanoparticles Selectively Treat Neurofibromatosis Type 1-Associated Plexiform Neurofibroma Cells at Doses That Do Not Affect Patient-Matched Schwann Cells Pharmaceutics (IF 5.4) Pub Date : 2024-03-07 Bashnona Attiah, Garrett Alewine, Mary-Kate Easter, Robert A. Coover, Cale D. Fahrenholtz
Neurofibromatosis Type 1 (NF1) is a common neurogenic condition characterized by heterozygous loss of function mutations in the neurofibromin gene. NF1 patients are susceptible to the development of neurofibromas, including plexiform neurofibromas (pNFs), which occurs in about half of all cases. Plexiform neurofibroma are benign peripheral nerve sheath tumors originating from Schwann cells after complete
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Cancer Therapy Resistance: Choosing Kinase Inhibitors Pharmaceutics (IF 5.4) Pub Date : 2024-03-07 Carmela Dell’Aversana, Federica Sarno, Rosaria Benedetti, Wouter Leonard Megchelenbrink, Donato Cappetta
Recent advances in comprehending the essential molecular mechanisms that govern cancer signaling have revealed the pivotal involvement of kinases in the development and progression of various cancer types [...]
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Phage Delivery Strategies for Biocontrolling Human, Animal, and Plant Bacterial Infections: State of the Art Pharmaceutics (IF 5.4) Pub Date : 2024-03-08 Marta M. D. C. Vila, Liliane M. N. Balcão, Victor M. Balcão
This review aims at presenting the main strategies that are currently available for the delivery of bacteriophages to combat bacterial infections in humans, animals, and plants. It can be seen that the main routes for phage delivery are topical, oral, systemic, and airways for humans. In animals, the topical and oral routes are the most used. To combat infections in plant species, spraying the plant’s
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Forecasting Fetal Buprenorphine Exposure through Maternal–Fetal Physiologically Based Pharmacokinetic Modeling Pharmaceutics (IF 5.4) Pub Date : 2024-03-08 Matthijs W. van Hoogdalem, Ryota Tanaka, Khaled Abduljalil, Trevor N. Johnson, Scott L. Wexelblatt, Henry T. Akinbi, Alexander A. Vinks, Tomoyuki Mizuno
Buprenorphine readily crosses the placenta, and with greater prenatal exposure, neonatal opioid withdrawal syndrome (NOWS) likely grows more severe. Current dosing strategies can be further improved by tailoring doses to expected NOWS severity. To allow the conceptualization of fetal buprenorphine exposure, a maternal–fetal physiologically based pharmacokinetic (PBPK) model for sublingual buprenorphine
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pH-Triggered Controlled Release of Chlorhexidine Using Chitosan-Coated Titanium Silica Composite for Dental Infection Prevention Pharmaceutics (IF 5.4) Pub Date : 2024-03-08 Mrinal Gaurav Srivastava, Nur Hidayatul Nazirah Kamarudin, Merve Kübra Aktan, Kai Zheng, Naiera Zayed, Derick Yongabi, Patrick Wagner, Wim Teughels, Aldo R. Boccaccini, Annabel Braem
Peri-implantitis is a growing pathological concern for dental implants which aggravates the occurrence of revision surgeries. This increases the burden on both hospitals and the patients themselves. Research is now focused on the development of materials and accompanying implants designed to resist biofilm formation. To enhance this endeavor, a smart method of biofilm inhibition coupled with limiting
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First Insights about Antiparasitic and Action Mechanisms of the Antimicrobial Peptide Hepcidin from Salmonids against Caligus rogercresseyi Pharmaceutics (IF 5.4) Pub Date : 2024-03-08 Paula A. Santana, Camila Arancibia, Laura Tamayo, Juan Pablo Cumillaf, Tanya Roman, Constanza Cárdenas, Cinthya Paillan Suarez, Claudio A. Álvarez, Fanny Guzman
Currently, one of the primary challenges in salmon farming is caligidosis, caused by the copepod ectoparasites Caligus spp. The infection process is determined by the copepod’s ability to adhere to the fish skin through the insertion of its chitin-composed filament. In this study, we examined several antimicrobial peptides previously identified in salmonid mucosal secretions, with a primary focus on
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Development and Evaluation of Two-Phase Gel Formulations for Enhanced Delivery of Active Ingredients: Sodium Diclofenac and Camphor Pharmaceutics (IF 5.4) Pub Date : 2024-03-05 Giedre Kasparaviciene, Yuliia Maslii, Nataliia Herbina, Daiva Kazlauskiene, Mindaugas Marksa, Jurga Bernatoniene
The formulation of biphasic gels as potential semi-solid carriers for hydrophilic and lipophilic active substances is promising for the development of pharmaceutical preparations. The aim of this study was to design a stable bigel composition and to determine the influence of the organogel/hydrogel ratio on the gel’s physical-chemical and structural-mechanical properties. The investigated compositions
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3D Screen Printing Offers Unprecedented Anticounterfeiting Strategies for Oral Solid Dosage Forms Feasible for Large Scale Production Pharmaceutics (IF 5.4) Pub Date : 2024-03-05 Nicolle Schwarz, Marcel Enke, Franka V. Gruschwitz, Daniela Winkler, Susanne Franzmann, Lisa Jescheck, Felix Hanf, Achim Schneeberger
A threat to human health in developed and, in particular, in developing countries, counterfeit medicines represent the largest identified fraud market worldwide. 3D screen printing (3DSP), an additive manufacturing technology that enables large-scale production, offers unique opportunities to combat counterfeit drugs. One such possibility is the generation of oral dosage forms with a distinct colored
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Preparation and Characterization of a Novel Salicin–Cyclodextrin Complex Pharmaceutics (IF 5.4) Pub Date : 2024-03-06 Adina Căta, Ioana Maria Carmen Ienaşcu, Adina Frum, Daniel Ursu, Paula Svera, Corina Orha, Gerlinde Rusu, Adriana Aurelia Chiș, Carmen Maximiliana Dobrea, Claudiu Morgovan, Oana-Raluca Pop
Bioactive compounds extracted from plants can provide wide health benefits. However, some molecules have limited applications as pharmaceuticals due to their limited solubility, poor bioavailability, and low stability when exposed to environmental factors. Their integration in formulations that can deliver them to physiological targets while preserving their biological activity can enhance their usage
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Alginate-Based Encapsulation Fabrication Technique for Drug Delivery: An Updated Review of Particle Type, Formulation Technique, Pharmaceutical Ingredient, and Targeted Delivery System Pharmaceutics (IF 5.4) Pub Date : 2024-03-06 Joanne Lai, Abul Kalam Azad, Wan Mohd Azizi Wan Sulaiman, Vinoth Kumarasamy, Vetriselvan Subramaniyan, Salah Abdalrazak Alshehade
Alginate is a natural biopolymer widely studied for pharmaceutical applications due to its biocompatibility, low toxicity, and mild gelation abilities. This review summarizes recent advances in alginate-based encapsulation systems for targeted drug delivery. Alginate formulations like microparticles, nanoparticles, microgels, and composites fabricated by methods including ionic gelation, emulsification
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Modeling Pharmacokinetics in Individual Patients Using Therapeutic Drug Monitoring and Artificial Population Quasi-Models: A Study with Piperacillin Pharmaceutics (IF 5.4) Pub Date : 2024-03-04 Gellért Balázs Karvaly, István Vincze, Michael Noel Neely, István Zátroch, Zsuzsanna Nagy, Ibolya Kocsis, Csaba Kopitkó
Population pharmacokinetic (pop-PK) models constructed for model-informed precision dosing often have limited utility due to the low number of patients recruited. To augment such models, an approach is presented for generating fully artificial quasi-models which can be employed to make individual estimates of pharmacokinetic parameters. Based on 72 concentrations obtained in 12 patients, one- and two-compartment
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Non-Invasive Device-Mediated Drug Delivery to the Brain across the Blood–Brain Barrier Pharmaceutics (IF 5.4) Pub Date : 2024-03-05 Toshihiko Tashima, Nicolas Tournier
We will be serving as the Guest Editor for this very interesting Special Issue on “Non-Invasive Device-Mediated Drug Delivery to the Brain Across the Blood–Brain Barrier” [...]
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The Effect of Microcrystalline Cellulose–CaHPO4 Mixtures in Different Volume Ratios on the Compaction and Structural–Mechanical Properties of Tablets Pharmaceutics (IF 5.4) Pub Date : 2024-03-05 Valentyn Mohylyuk, Artūrs Paulausks, Oskars Radzins, Liga Lauberte
Using microcrystalline cellulose (MCC) with plastic behaviour and calcium phosphate anhydrous (CaHPO4) with brittle behaviour under compaction is very popular in the pharmaceutical industry for achieving desirable structural–mechanical properties of tablet formulations. Thus, mixtures of specific grades of MCC and CaHPO4 were tested in volume proportions of 100-0, 75-25, 50-50, 25-75, and 0-100 at
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Pulsed Electric Fields Induce STING Palmitoylation and Polymerization Independently of Plasmid DNA Electrotransfer Pharmaceutics (IF 5.4) Pub Date : 2024-03-05 Amanda Sales Conniff, Julie Singh, Richard Heller, Loree C. Heller
Gene therapy approaches may target skeletal muscle due to its high protein-expressing nature and vascularization. Intramuscular plasmid DNA (pDNA) delivery via pulsed electric fields (PEFs) can be termed electroporation or electrotransfer. Nonviral delivery of plasmids to cells and tissues activates DNA-sensing pathways. The central signaling complex in cytosolic DNA sensing is the cyclic GMP-AMP synthase-stimulator
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Determination of the Absolute Configuration of Secondary Alcohols in a Compound Mixture via the Application of Competing Enantioselective Acylation Coupled with LC/MS Analysis Pharmaceutics (IF 5.4) Pub Date : 2024-03-05 Bum Soo Lee, Hoon Kim, Jiwon Baek, Rhim Ryoo, Seoung Rak Lee, Ki Hyun Kim
The determination of natural product stereochemistry plays a significant role in drug discovery and development. Understanding the stereochemistry of natural products is essential for predicting and optimizing their interactions with biological targets, which, in turn, influences their therapeutic efficacy, safety, and overall impact on living organisms. Here, we present the first application of competitive
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Anti-Inflammatory Effects of Chamaecyparis obtusa (Siebold & Zucc.) Endl. Leaf Extract Fermented by Ganoderma applanatum Mycelia Pharmaceutics (IF 5.4) Pub Date : 2024-03-05 Chae-Hyun Kim, Yong-Jin Kwon, Young-Ah Jang
Corticosteroids are commonly used anti-inflammatory agents. However, their prolonged use can lead to side effects. Therefore, the development of natural compounds with minimal side effects is necessary. This study was performed to investigate the anti-inflammatory effects and mechanisms of action of Chamaecyparis obtusa (Siebold & Zucc.) Endl. leaf (COL), bioconverted using Ganoderma applanatum (G
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Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation Pharmaceutics (IF 5.4) Pub Date : 2024-03-03 Rafaela de Andrade, Rita de Cássia dos Reis Schmidt, Leonardo Santos Gomes, Legna Colina-Vegas, Ruth Hinrichs, Marcos Antônio Zen Vasconcellos, Tania Maria Haas Costa, Monique Deon, Wilmer Villarreal, Edilson Valmir Benvenutti
Malaria is a dangerous tropical disease, with high morbidity in developing countries. The responsible parasite has developed resistance to the existing drugs; therefore, new drug delivery systems are being studied to increase efficacy by targeting hemozoin, a parasite paramagnetic metabolite. Herein, magnetic mesoporous silica (magMCM) was synthesized using iron oxide particles dispersed in the silica
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3D-Printed Chitosan-Based Scaffolds with Scutellariae baicalensis Extract for Dental Applications Pharmaceutics (IF 5.4) Pub Date : 2024-03-04 Magdalena Paczkowska-Walendowska, Ioanna Koumentakou, Maria Lazaridou, Dimitrios Bikiaris, Andrzej Miklaszewski, Tomasz Plech, Judyta Cielecka-Piontek
The plant material Scutellariae baicalensis radix, which is rich in flavones (baicalin), possesses antibacterial, antifungal, antioxidant, and anti-inflammatory properties. This work aimed to develop a 3D-printed chitosan-based hydrogel rich in Scutellariae baicalensis extract as an innovative approach for the personalized treatment of periodontal diseases. Chitosan-based hydrogels were prepared, and
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New MoS2/Tegafur-Containing Pharmaceutical Formulations for Selective LED-Based Skin Cancer Photo-Chemotherapy Pharmaceutics (IF 5.4) Pub Date : 2024-03-04 Miguel T. Campos, Filipa A. L. S. Silva, José Ramiro Fernandes, Susana G. Santos, Fernão D. Magalhães, Maria J. Oliveira, Artur M. Pinto
Non-melanoma skin cancer (NMSC) is one of the most common types of cancer worldwide. Despite the low mortality rate, rising incidence and recurrence rates are a burden on healthcare systems. Standard treatments such as chemotherapy, radiotherapy, and surgery are either invasive or toxic to healthy tissues; therefore, new, alternative, selective treatments are needed. In this work, a combined photothermal