Purpose The study was aimed at exploring the feasibility of LIPOID SPC-3 as a coprecipitate carrier to enhance the aqueous solubility and permeability of ranolazine, a BCS class II drug. Methods LIPOID SPC-3-based coprecipitates of ranolazine (RNZ-SPC-CP) were developed using the solvent method. The developed formulation was physico-chemically characterized using scanning electron microscopy (SEM)

Purpose The active ingredient recovery from the vegetable is a very attractive research field for the development of a sustainable economy; to revalue the jujube fruit (Zizyphus lotus) polysaccharide (ZLPS), an optimized green microwave-assisted method was used for the recovery and enrichment of the antioxidants present in a distilled water extract. Methods A series of 17 experiments including microwave

Purpose The size was a key factor influencing the drug loading, release, and delivery efficacies of poly (lactic-co-glycolic) acid (PLGA) microspheres (MS). The purpose of the study was to explore a novel and simple method to prepare uniform-sized PLGA MS for drug delivery. Methods Different from routine homogenizer, a vortex shaker was employed for emulsification during the preparation of PLGA MS

Purpose The purpose of the study was to develop a model to predict the critical quality attribute (CQA) of tablets during continuous and batch manufacturing using only critical material attributes (CMAs). Methods Experiments were performed using ethenzamide as the active pharmaceutical ingredient processed with batch and continuous high-shear granulators. The disintegration time of tablets was defined

Abstract The design of multiparticulate systems is a high-impact technological strategy in the formulation of immunomodulators for oral administration, fluid bed coating being a technique used due to its versatility and relatively low cost. Purpose The objective of this work was to cover a solid support (Suglets® of Colorcon®) with an extract of cell wall of Saccharomyces cerevisiae through a fluidized

Purpose Less local availability and higher skin permeation restrict wide application of silver sulfadiazine (SSD) formulations against infectious burn wound. Aim We aimed to develop β-cyclodextrin inclusion complex-based in situ pluronic gel of SSD (β-CD-ssd P-Gel). Methods Formation of inclusion complex was confirmed by FT-IR, DSC, SEM, and XRD and checked for improved solubility. Results and Discussion

Purpose The purpose of this paper is to unveil two novel statistical strategies to decide on the acceptability of an analytical and bioanalytical method transfer. These new approaches, namely the uncertainty assessment approach and the risk-based approach, are based on the measurement uncertainty as a decision-making tool. Methods At first, we illustrate step by step all the calculations required to

Background and Introduction Piroxicam is an NSAID (non-steroidal anti-inflammatory drug) persisting antipyretic and analgesic effects and being usually implied in managing and treating osteoarthritis, rheumatoid arthritis, soft tissue disorders, ankylosing spondylitis, and acute gout and also in post-operative pain management. Aim The present research was undertaken aiming to formulate Piroxicam encompassing

Purpose Clofazimine displays high intersubject variability in absorption after oral administration because of its extremely low water solubility and high lipophilicity. The present investigation was aimed to prepare self micro emulsifying drug delivery system (SMEDDS) of clofazimine for improving its dissolution properties by using design of experiment (DoE) approach. Methods Various lipid, surfactant

Purpose Lean stability is a science- and risk-based initiative which utilizes the enhanced understanding of drug substance and drug product physical and chemical characteristics to (1) reduce and optimize the design of standard stability protocols; (2) expedite the generation of stability data without impact to safety, efficacy, or quality of the product; and (3) decrease time to market for innovative

Purpose Infectious diseases caused by Candida sp. have high drug resistance due to the uncontrolled use of antibiotics. Among the natural products, ursolic acid (UA), a triterpene, has been increasing interest due to its antimicrobial effects. However, the physicochemical properties of UA, such as its low aqueous solubility, lead to failure of therapeutic application. Because of this, drug release

Purpose The present study explored biochemical transformation and optimization of fermentation method for enhanced content of flavonoids in a composite extract of Syzygium cumini seed, Mangifera indica seed, Momordica charantia fruit, and Gymnema sylvestre leaf along with the fermentation kinetics. Methods The herbs were mixed and extracted in hot water. The extract was fermented using Wickerhamomyces

Background Topical drug delivery offers improved therapeutic effect and reduced systemic adverse effects of the administered compounds. Objective The present work was aimed at developing and comparing levocetirizine loaded polymeric nanoparticles and niosomal formulation(s), respectively, against dinitrochlorobenzene-induced atopic dermatitis animal model. Methods The niosome and chitosan nanoparticle

Purpose The aim of this work is to study the metal–drug–amino acid ternary complex formation kinetically, thermodynamically and computationally and explore the possibility of developing some potent new drugs for biological applications. Methods Metal(II)–ciprofloxacin–glycine ternary complexes (metal = MnII, CuII, ZnII) were synthesized. The slow kinetics and thermodynamics of imine formation were

Purpose Objective of present work was to develop microfluidic-based technique for continuous production of drug (luliconazole)-loaded microemulsion. Methods Pseudo-ternary phase diagrams were constructed, and optimization of concentration of selected formulation components like Capmul MCM, Tween 20 and Transcutol P was done using the Box-Behnken design (BBD). Batch process and microfluidic process

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Purpose The present study was aimed to formulate and evaluate fast-disintegrating tablets (FDTs) having Flurbiprofen (FP) and Metoclopramide HCl (MHCl) in combination. Method Direct compression was used to formulate FDTs of FP and MHCl as a combination regimen in six formulations. FDTs are defined as solid oral dosage form that disintegrates rapidly within seconds when placed in the oral cavity. FDT-1

Purpose The study was aimed to formulate eugenol-loaded polymeric microsponges using eugenyl methacrylate (Eg-MA) incorporated in situ gelling system for the treatment of periodontitis. Method Eg-MA monomer was first synthesized by reacting eugenol with methacryloyl chloride, which acted as a monomer and cross-linking agent for preparing microsponges of Eg-MA using suspension polymerization method

Purpose The prevalence of rheumatic disease patients was estimated at 25% of the population. Rheumatic diseases are the leading cause of disability. The main objective of the study was to investigate the kinetic drug release characteristics of aceclofenac sustained-release (SR) matrix tablets for the management of rheumatic diseases. Methods The novel formulation of aceclofenac was prepared by using

Purpose Implementation of Process Analytical Technologies (PAT) is an important consideration to increase process knowledge during pharmaceutical manufacturing. Currently used batch sampling methods, however, are limited in terms of temporal resolution when compared with continuous process sampling. Here, we show the importance of fluid dynamic characterization when repurposing available batch sampling

Drug delivery through the skin by transdermal patches has a long history. Subsequent growth of transdermal science proved prominent utility of transdermal systems meant for passive diffusion of the drug. It was followed by the development of iontophoresis- and sonophoresis-based transdermal delivery systems. Microneedle array has now caught attention of the investigators owing to its immense utility

Purpose A pulsatile drug delivery system containing dexketoprofen trometamol was designed by combining immediate release and colon-targeted mini tablets into a capsule. Methods Both immediate release and colon-targeted mini tablets were prepared by wet granulation. Furthermore, colon-targeted mini tablets were coated with Eudragit L 100, Eudragit S 100, Eudragit RS 30D, and ethylcellulose (Surelease®)

Purpose The present work describes the systematic development of ganoderic acid (GA)–loaded solid lipid nanoparticles (SLNs) for the treatment of hepatocellular carcinoma (HCC). Methods A full factorial design was employed for optimization of the GA-loaded SLNs prepared by hot-homogenization method, where Capmul MCMC10 and soy lecithin were used as solid lipid and surfactant, while poloxamer 188 was

Purpose Light-induced fluorescence was evaluated as a process analytical tool in the development of quantitative models for the monitoring of a low-dose formulation manufacturing process. Method The system, equipped with a probe, was positioned in a tablet press feed-frame to monitor the active pharmaceutical ingredient content of the flowing powder before compression. Results Modeling errors of 1

Purpose Teriparatide (PTH(1–34)), as one of the FDA-approved anabolic medications for postmenopausal osteoporosis treatment, shows anabolic effects in intermittent administration. In the current study, a multilayer implantable device was developed by spin-coating and dip-coating techniques for providing pulsatile pattern release of teriparatide, composed of polymeric and hydrogel layers. Methods Copolymers

Purpose Tizanidine (TZN) is used for the management of muscle spasms. Oral TZN is liable to first-pass metabolism and interindividual variation. Transdermal drug delivery systems (TDDS) are gaining research attention as an alternative route. The aim of this study is the bioanalytical comparison of the oral route and two TDDS, bilosomes and aspasomes. Methods TZN-loaded bilosomes and aspasomes were

Purpose The current investigation explores the enhanced biopharmaceutical attributes of solid supersaturable self-microemulsifying drug delivery system (Solid SS SMEDDS) for poorly water soluble drug canagliflozin (CFZ). Methods Solid SS SMEDD formulation was prepared by spray drying using Neusilin US2 as an adsorbent. The developed SS SMEDDS were characterized for physicochemical and solid state characterizations

Purpose Due to the exceptionally high standards for accuracy and data integrity in scientific regulatory reporting, it is vital that any tool that aims to streamline this process is as efficient or more in gathering data as a team of scientists, without higher cost in terms of time or resources. For this reason, an artificial intelligence-based tool with parallel search, document creation, and data

Purpose This study was performed to explore the physicochemical and anti-biofilm properties of rifampin (Rif) and cis-2-decenoic acid (C2DA) co-entrapped in solid lipid nanoparticles, Rif-C2DA-SLN, against staphylococcal biofilm. Methods The formulation was prepared by high-shear homogenization and ultrasound methods and characterized for size, zeta potentials, encapsulation efficacy, drug lipid interaction

Purpose Loss-in-weight feeders play a vital role in assuring blend and content uniformity as well as lot-to-lot powder traceability in continuous manufacturing. Irregular flow from the feeders propagates through the system, potentially resulting in out-of-specification product. Powder properties such as density, cohesion, and adhesion can cause large variability in the flow rate of ingredients from

Purpose The present study focused on synthesis and characterization of polymeric nanocarrier for the hydrophobic drug, naringenin (Nar), using chitosan (CS) and dextran sulfate (DS). Method CSDS-Nar and blank CSDS nanoparticles were prepared by complex coacervation technique. The nanoparticles were characterized by scanning electron microscopy (SEM), Fourier transform-infrared spectroscopy (FTIR),

Purpose Conventional and novel drug delivery systems encompass therapeutic effects for treatment and management of various conditions like cancer, diabetes, and Alzheimer’s disease but mostly show side or adverse effects. To overcome such undesirable effects, new approaches like functionalized polymers, biocarriers, drug-free particles, and metallic nanocomposite display potential applications in healthcare

Purpose Roll compaction/dry granulation is established in manufacturing of solid oral dosage forms and, within the context of continuous manufacturing, it has sparked interest as material is fed, processed, and ejected continuously while also providing large possible throughputs. However, this amount of material has to be adequately controlled in real time to assure quality. Methods This research aimed

Purpose The current study entails the design, development, and optimization of nasal mucoadhesive microspheres of lercanidipine with improved systemic bioavailability for the management of hypertension. Methods Mucoadhesive microspheres of lercanidipine were prepared by solvent evaporation and polymerization method using bovine serum albumin (BSA) as the carrier and glutaraldehyde as the chelating

Purpose The objective of present work was to develop fibroin-sodium alginate floating microspheres of felodipine (FD) showing modified release. Method Binary polymer system of fibroin-sodium alginate was used to prepare microspheres by spray drying technique. Thus, FD loaded microspheres obtained were evaluated for % drug content, % entrapment efficacy, particle size, micromeritics, FT-IR, DSC, XRD

Purpose Glycine has been widely used as pharmaceutical excipients and synthesis reagents, and commercial glycine has a significant amount of aggregation and wide particle size distribution. A simple but reproducible process for generating uniform glycine crystals is always desired for both product quality and process efficiency purposes. Methods Continuous cooling crystallization of glycine has been

Purpose There is a growing interest in continuous biopharmaceutical processing due to the advantages of small footprint, increased productivity, consistent product quality, high process flexibility and robustness, facility cost-effectiveness, and reduced capital and operating cost. To support the decision making of biopharmaceutical manufacturing, comparisons between conventional batch and continuous

Purpose There is a continuous search for efficient optimization methods in the production of biopharmaceuticals, with a special focus on reducing production time and costs. Pharmaceutical production is currently dominated by batch production processes that have a relatively long downtime for cleaning and reconfiguration of the plant equipment when the product or its format size is changed. The geometry

Purpose The main objective of the present investigation was to develop transdermal films of ondansetron HCl (OS) with polyvinyl alcohol (PVA) using Box-Behnken design and to optimize them employing Derringer’s optimization tool. Methods Design-Expert software was used to investigate the effect of independent variables such as concentration (%, w/w) of glycerol and 1,8-cineole, and number of Freeze-Thaw

Purpose With the applications of more advanced manufacturing technologies being applied to the pharmaceutical industry, continuous processes are at the forefront of innovation. One area that is highly desired to be systematically investigated is material traceability in continuous manufacturing systems. By following federal guidelines already in place, the goal was to address the issue of material

Purpose This study is concerned with encapsulation of the anti-cancer drug (berberine hydrochloride (BH)) in nanocarriers as cubosomes, which is, then, formulated in solid form to ease its incorporation into different drug delivery systems, improve its solubility, and improve its anti-cancer activity. Methods BH cubosomes were prepared using glyceryl mono-oleate (GMO) and poloxamer 407 (PF127). Polyvinyl

Purpose Scholars often associate Operational Excellence (OPEX) enablers with high operational performance. Several studies have concluded that advancing OPEX enablers helps improve organizational performance. This paper aims to better understand the relation between OPEX enablers and a robust quality control lab. Integral to pharmaceutical quality systems, robust quality control labs ensure effective

Purpose Zoledronic acid (ZA) is one of the drugs used clinically for the treatment of osteoporosis, and its therapeutic effect is due to the inhibition of osteoclastic cells leading to bone resorption. The aim of this study is developing an optimization method for poly(lactide-co-glycolide) (PLGA) nanoparticles of ZA which is intended for local application to enable guided bone regeneration. Methods

Objective Solid lipid nanoparticles (SLN) mainly consist of lipids and surfactants. However, the toxicity of surfactant cannot be ignored, as the surfactant may cause unexpected side effect. This study established model SLN with different surfactants, Tween 80 (T80) and poloxamer 188 (P188). It was aimed to establish ultraviolet-visible (UV-Vis) spectroscopy methods for quantifying the contents of

Purpose Chromium species in higher oxidation states are toxic and carcinogenic. But lower oxidation state as Cr(III) microelement shows potential antimicrobial properties. Cefoperazone sodium is a parenteral bactericidal third-generation cephalosporin antibiotic effective in treating Pseudomonas bacterial infections. A new drug formed with the complexation of metal and drug. Hence, newer coordinated

Purpose Antimicrobial activity of drug products containing antibiotics is often measured using microbiological assays. However, the high values of measurement uncertainty associated with the analytical results obtained from microbiological assays may be an issue to conformity decisions. Methods The aim of this work was to estimate the risk of false decisions in conformity assessment due to measurement

Purpose The objective of this article is to review the critical material attributes of pharmaceutical excipients employed in solid dosage manufacturing and link them to critical quality attributes (CQAs). Material attributes can have a profound impact on CQAs of product. Methods The importance of particle size, particle morphology, density, moisture content, and polymorphism to product CQAs is discussed

Purpose A new Circulaire II (holding chamber) was designed to be used with VixOne nebulizer to increase the inhalable doses reaching the patient. The aim of this study was to evaluate the efficacy of this holding chamber with VixOne nebulizer and determine its usability with other nebulizers. Methods The aerodynamic characteristics of emitted dose of 2 ml salbutamol solution, 5000 μg/ml, were evaluated

Purpose In the biopharmaceutical industry, in vitro models are not commonly used to assess formulation risks of injectables. With limited knowledge, their impact on predicting altered pharmacokinetic (PK) or injection site responses is modest. In this paper, we address this gap by testing five injectable therapeutic modalities in the subcutaneous injection site simulator (SCISSOR). The goal was to

With the advent of novel biotherapeutics in indications such as oncology, the attention has moved to making these therapies patient centric, potentially available for self-administration. Given the volume limitations of the other convenient routes of administration such a subcutaneous, intramuscular, there is a need for high concentration drug products. Along with the concerns of inherent protein instability

Purpose Biologic molecules constitute a major part of the therapeutics portfolio across the pipeline of several biotech and pharmaceutical companies. They have the advantage of being more target-specific, and recent progress in protein engineering has allowed product designs on various platforms that befit the therapeutic indication and allow differentiation from competitor molecules. They are fundamentally

Purpose Advancements in genetic engineering have profoundly impacted the biotherapeutic industry and shaped many of the methods and strategies used today for both bioproduction and therapeutic design. Improvements in production yield and quality have been achieved by manipulating the expression of genes involved in cell survival, metabolism, secretion, and glycosylation, among others, and recent breakthroughs

Purpose Biotherapeutics are a large and rapidly growing class of drugs being produced by pharmaceutical companies to treat a diverse range of clinical indications. The overall efficacy and safety of these products can be greatly impacted by their capacity to induce undesired immune responses. This review discusses in vitro cell-based methods used to assess the T cell mediated immunogenicity risk of

Purpose Current in vitro disintegration methods for polymeric films are qualitative and introduce significant user bias. The goal of these studies is to develop a novel, quantitative disintegration technique which can be used to characterize polymeric films in vitro. Methods A method was developed using a Texture Analyzer instrument to evaluate film disintegration. Solvent casted, clinically advanced

Purpose The main objective of this present study was the investigation of potential novel transdermal patch technology (TEPI®) delivering ibuprofen as the active pharmaceutical ingredient (API) using a novel poly(ether-urethane)-silicone crosslinked pressure-sensitive adhesive (PSA) as the drug reservoir in a solvent-free manufacturing process. Methods The patch was synthesized utilizing the hot-melt

The sterility test described in pharmacopoeial compendia requires a 14-day incubation period to obtain a valid analytical result. Therefore, the use of alternative methods to evaluate the sterility of pharmaceuticals, such as the BacT/Alert® 3D system, is particularly interesting, because it allows a reduced incubation period and lower associated costs. Considering that the BacT/Alert® 3D system offers

PURPOSE 5-chloro-3-[phenylsulfonyl] indole-2-carboxamide (CSIC) is a highly potent non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 which has been shown to have a more desirable resistance profile than other NNRTIs in development as HIV prevention strategies. This work involves generation of preformulation data for CSIC and systematic development of a cosolvent system to effectively

PURPOSE "Me-too" drugs are new pharmaceuticals with the mechanism of action of an existing drug and are considered less innovative than breakthrough drugs. The objective of this study was to evaluate whether the adoption patterns of the breakthrough drug sitagliptin and the "me-too" drug saxagliptin differed; and to assess whether the patterns differed between Medicare stand-alone (PDP) and Medicare-Advantage

Continuous processing in pharmaceutical manufacturing is a relatively new approach that has generated significant attention. While it has been used for decades in other industries, showing significant advantages, the pharmaceutical industry has been slow in its adoption of continuous processing, primarily due to regulatory uncertainty. This paper aims to help address these concerns by introducing methods

Small-interfering RNA (siRNA) is both a powerful tool in research and a promising therapeutic platform to modulate expression of disease-related genes. Malignant tumors are attractive disease targets for nucleic acid-based therapies. siRNA directed against oncogenes, and genes driving metastases or angiogenesis have been evaluated in animal models and in some cases, in humans. The outcomes of these