Abstract In recent years, the incidence of skin cancer has increased worldwide, presenting a significant burden on healthcare services. Chemotherapy intervention is often not appropriate for all patients due to localized adverse effects on skin physiology. The aim of this study was, therefore, to consider the development of a novel phytochemical-based deformable liposomal formulation suspended in an

Abstract The barrier properties of lipid membranes are often determined by investigating their solute permeability with the help of spectroscopic methods and the use of liposome-encapsulated self-quenching fluorescent dyes, for example, Carboxyfluorescein (CF). It was shown previously that liposome–surface interactions, and thus the choice of cuvette material, influence the result of such spectroscopic

Abstract The aim of this research was the development and optimization of nanoniosomes for delivery of glibenclamide (Gbn) as hypoglycaemic agent to the lung in an inhaler dosage form. Fifteen formulae of niosomal dispersions were prepared according to Box–Behnken design. The effect of drug amount, Cholesterol molar ratio, and Hydrophilic lipophilic balance (HLB) values of the surfactant on the mean

Abstract Thymoquinone (TH), a naturally occurring moiety shows excellent anticancer properties and in the present study, TH loaded polymer hybrid lipid vesicles (TH PLH Vesicles) were formulated and in-vitro cytotoxicity towards breast cancer cell lines (MCF-7 and MBD –MB 231 cells) was determined. Thymoquinone Polymer Lipid Hybrid Vesicles (TH PLH Vesicles) was primed by ethanol spraying method and

Abstract Cilostazole (CLZ) is an anti-platelet drug that suffers from extensive first pass-metabolism and gastrointestinal side effects. This study aimed to prepare spanlastics for enhancing the transdermal delivery of CLZ to avoid its oral problems. CLZ-loaded spanlastic dispersions were prepared by ethanol injection technique according to a 413121 full factorial design to investigate the effect of

Abstract The markedly low oral bioavailability of domperidone (anti-emetic drug) is associated with rapid first-pass metabolism in the intestine and liver. To counteract such affects, there is a need to devise a strategy to enhance absorption and subsequently bioavailability. Thus, the current study was aimed at synthesizing phytosomes consisting of phosphatidylcholine and piperine (a P-glycoprotein

Abstract Sickle cell disease (SCD) is a mortal erythrocyte-based disease which is hard to treat effectively. Development of a treatment method that can prevent deoxygenation of erythrocytes or reduce the oxidative stress of sickle erythrocytes is one of the important issues towards SCD. Among a wide variety of potential drug carriers, liposomes are advantageous and preferable with their easy preparation

Abstract The aim of the research work was to investigate the efficacy of cream loaded with lipid nanocarriers (ethosomes) of piperine for the management of atopic dermatitis (AD) in comparison to conventional cream. Ethosomes of piperine were formulated with varying concentration of phosphatidylcholine and ethanol; and evaluated for entrapment efficiency (EE), sedimentation behaviour, vesicle size

Abstract The current research was undertaken to design stealth liposomes of 5-Fluorouracil for reducing its cardiotoxicity and prolong the half-life by developing long-circulating liposomes. The liposomes were prepared by the NH4EDTA gradient method, where EDTA is used as a cardioprotectant. Ascorbyl-6-palmitate was also used which helped for the synergistic effect of 5-Fluorouracil to counteract the

Abstract Cancer is a broad term used to describe a group of diseases that have more than 270 types. Today, due to the suffering of patients from the side effects of existing methods in the treatment of cancer such as chemotherapy and radiotherapy, the employment of targeted methods in the treatment of this disease has been received much consideration. In recent years, nanoparticles have revolutionized

Abstract The present work reports the development of doxorubicin (DOX) encapsulated α-Tocopherol polyethylene glycol 1000 succinate (TPGS) coated liposomal system (DOX-LIPO-TPGS) by quality by design (QbD) approach and evaluated for its anticancer and hemocompatibility potential. The screening and optimization of formulation variables were performed by the systematic design of experiments (DoE), using

Abstract The purpose of this study is to prepare stimuli-responsive chimeric liposomes (i.e. hybrid polymer-lipid liposomes) containing functional copolymers and conduct aqueous solution studies in order to determine their properties and potential as drug-delivery nanocarriers. Two random copolymers, composed of the hydrophilic, pH and thermo-responsive 2-(dimethyl amino) ethyl methacrylate (DMAEMA)

Abstract The selectivity of chemotherapeutic agents for liver cancer is poor. When they kill tumor cells, they produce serious adverse reactions in the whole body and multidrug resistance (MDR) is also a major hurdle in liver cancer chemotherapy. Combination therapy is a useful method for overcoming MDR and reducing toxic and side effects. In this study, we developed a long-circulating codelivery system

Abstract The selectivity of chemotherapeutic agents for liver cancer is poor. When they kill tumor cells, they produce serious adverse reactions in the whole body and multidrug resistance (MDR) is also a major hurdle in liver cancer chemotherapy. Combination therapy is a useful method for overcoming MDR and reducing toxic and side effects. In this study, we developed a long-circulating codelivery system

Chronic wounds are a serious problem that could cause severe morbidity and even death. The ability of statins including rosuvastatin calcium (RVS) to enhance wound healing was well reported. However, RVS is poorly soluble and has low bioavailability. Thus, the current study aimed to prepare and evaluate RVS loaded nanocubics to enhance its skin performance. In addition, silver nanoparticles (AgNPs)

The interactions of egg yolk phosphatidylcholine liposomes with F108 and F127 triblock copolymers, in the monomer state, were analysed by isothermal titration calorimetry (ITC) at 37 °C. According to the results, the critical micelle concentration were determined to be 0.4 wt.% and 0.04 wt.% for F108 and F127, respectively, by surface tension at 37 °C. According to the results, liposomes/poloxamers

The aim of this study was to establish the mechanisms of action of a novel liposomal nitric oxide (NO) carrier on large-conductance Ca2+-activated channels (BKCa or Maxi-K) expressed in vascular smooth muscle cells (VSMC) isolated from the rat main pulmonary artery (MPA). Experimental design comprised of both whole-cell and cell-attached single-channel recordings using the patch-clamp techniques. The

The natural vesicles, microscopic spherical structures defined by a single or many lipid bilayer membranes, not only entrap but are also dispersed in the aqueous environment. The space division between inner and outer compartments is also the basic characteristics of cell membranes playing several essential functions in all living organisms. Thus, vesicles are a simple model system for studying various

Conventional formulations can not sufficiently control seizures and influence on cognitive corruption and oxidative stress with chronic usage in patients with epilepsy. To defeat this issue, it was planned to develop polymeric liposome formulations that are using for their bioavailability and enhancer impact in oral epilepsy treatment. In this study, chitosan-coated liposomal formulations that encapsulate

Background- The aim of the current study was to develop the phytosomal gel of aloe-vera extract for improved topical delivery. Methodology- Aloe-vera extract loaded phytosomal system was developed by fixing the amount of aloe-vera extract and ethanol and by varying the concentration of lecithin (0.15-0.25% w/v) and speed of rotation (80-120 rpm). Different formulation batches were prepared as per the

Docetaxel (DTX) is a highly lipophilic, BCS class IV drug with poor aqueous solubility (12.7 µg/mL). Presently, only injectable formulation is available in the market which uses a large amount of surfactant (Tween 80) and dehydrated alcohol as a solubilizer. High concentrations of Tween 80 in injectable formulations are associated with severe consequences i.e. nephrotoxicity, fluid retention, and hypersensitivity

The aim of present study was to evaluate the oral bioavailability of liposomal vitamin C and non-liposomal vitamin C in healthy, adult, human subjects under fasting conditions through an open label, randomized, single dose, two-treatment, two sequence, two-period, two way crossover, study. The vitamin C loaded liposome was well characterized using transmission electron microscopy (TEM), dynamic light

Cancer vaccines have been developed as an additional method of treatment in the fight against cancer. However, an important barrier to an effective vaccine is the inefficient presentation of exogenous antigen by dendritic cells to cytotoxic CD8 T cells. In this study, DPPC liposomes were modified with channels and loaded with polyethyleneimine (PEI) and 5,6-dimethylxanthenone-4-acetic acid (DMXAA)

Abstract β-sitosterol (BS), a phytosterol, exhibits ameliorative effects on hepatocellular carcinoma (HCC) due to its antioxidant activities. However, its poor aqueous solubility and negotiated bioavailability and short elimination half-life is a huge limitation for its therapeutic applications. To overcome these two shortcomings, BS-loaded niosomes were made to via, film hydration method and process

Herein an Ir(III) complex [Ir(Hppy)2(HMNPIP)](PF6) (Ir1, Hppy =2-phenylpyridine, HMNPIP =2-(1H-imidazo[4,5-f][1,10]phenanthroline-3-yl)-6-methoxy-4-nitrophenol) was prepared and characterized. Due to the low anticancer activity of Ir1 when administered free drug, we prepared a liposome Ir1Lipo encapsulated form of Ir1 to improve the antitumor effect, furthermore we explored the antitumor mechanism

Abstract The anti-inflammatory property of ratite oils as well as its ability to act as a penetration enhancer makes it an ideal agent to be used in transdermal formulations. The present study aims to develop an effective transfersomal delivery of 4-hydroxytamoxifen (4-OHT), an anti-cancer drug, using ratite oil as a carrier agent for the treatment of breast cancer (BC). The 4-OHT transfersomes were

Abstract Osthole (Ost) is a coumarin compound and a potential drug for Alzheimer’s disease (AD). However, the effectiveness of Ost is limited by solubility, bioavailability, and low permeability of the blood-brain barrier. In this study, we constructed Ost liposomes with modified CXCR4 on the surface (CXCR4-Ost-Lips), and investigated the intracellular distribution of liposomes in APP-SH-SY5Y cells

Topotecan (TPT)is a semi-synthetic, water-soluble derivative of camptothecin, which inhibits the action of topoisomerase I in the S-phase of the cell cycle leading to cell death. For the effective delivery of TPT to cancer cells, pH-sensitive sialic acid modified liposomes were developed. These liposomes were prepared by the thin-film hydration method using the active loading technique. Vesicle size

Abstract A novel method for electroformation of liposomes and phytosomes using copper electrode is described. Liposomes made at 2 V and 10 Hz AC field from L-α-egg-phosphatidylcholine (egg-PC), K. pneumoniae phosphatidylethanolamine, K. pneumoniae polar lipids and E. coli polar lipids on copper electrode were (777.9 ± 118.4), (370.2 ± 100.5), (825.3 ± 21.54), and (281.3 ± 42.3) nm in diameter, respectively

Abstract Archaeosomes, composed of sulphated lactosyl archaeol (SLA) glycolipids, have been proven to be an effective vaccine adjuvant in multiple preclinical models of infectious disease or cancer. In addition to efficacy, the stability of vaccine components including the adjuvant is an important parameter to consider when developing novel vaccine formulations. To properly evaluate the potential of

Abstract The aim of the present study was to develop a topical liposomal formulation as a transdermal delivery of rivastigmine for the treatment of Alzheimer’s disease as an alternative to the oral dosage form and to achieve smooth continuous drug delivery and maintain plasma levels within the therapeutic window. Rivastigmine-loaded liposomes were prepared by a thin layer hydration technique that was

Abstract We have previously developed ammonium sulphate gradient loaded liposomes to encapsulate dibucaine. Thus, the purpose of this study was to evaluate the pre-clinical safety and effectiveness of this novel ionic liposomal formulation of dibucaine (DBC), as described in previous work. Effectiveness was evaluated in vivo on Wistar rats (n = 8) that received plain DBC or liposomal DBC (DBCLUV).

Curcumin is known as an effective anticancer herbal medicine but unfortunately, its bioavailability is poor which necessitate efforts for developing more efficient and specific delivery systems. Human epidermal growth factor receptor 2 (HER 2) due to its overexpression in various types of cancers, is demonstrated to be a good candidate as a target for anticancer therapy. In this study, cytotoxicity

A novel antioxidant glutathione liposomes (GSH-LIP) were prepared and applied for diabetic nephropathy therapy. GSH-LIP not only improve the bioavailability and antioxidant capacity of glutathione to scavenge redundant ROS inducing by oxidative stress, but also effectively inhibit the activity of AR and sorbitol accumulation in polyol pathway. The imaging in vivo showed that GSH-LIP could target kidney

Here, the retinal targeting SA-g-AA coated multilamellar liposomes carrier synthesized to deliver the bioactive agents into the retinal region of the eye. The multilayered targeting macromolecules of liposomes prepared using a layer-by-layer assembly. The curcumin (CUR) and Rhodamine B (RhB) dyes loaded in a multilamellar vesicle (MLV) were synthesized by the Lipid film hydration method. The Sodium

Niosome nanoparticles can be prepared using different methods, each of which can affect the size and homogeneity of the prepared particles. The aim of this study was to establish if the method of preparation impacted on the prepared vesicles when loaded with a model protein and the type of immune responses induced to the vaccine antigen. Niosomes were prepared using both the traditional thin film hydration

Amphotericin B (AmB) is a very potent antibiotic which still remains as the gold standart for the treatment of systemic fungal infections. AmB is a member of Biopharmaceutical Classification System Class IV, mainly characterized by its poor solubility and low permeability. In this study, AmB/AmB-α cyclodextrin complex double loaded liposomes were developed using the design of experiments (DoE®) approach

Tumor metastasis is a major cause of cancer treatment failure and death, and chemotherapy efficiency for gastric cancer patients is usually unsatisfactory due to tumor cell metastasis, poor targeting and serious adverse reactions. In this study, a kind of R8GD modified epirubicin plus tetrandrine liposomes was prepared to enhance the antitumor efficiency via killing tumor cells, destroying tumor metastasis

Temozolomide is a drug approved for treating glioblastomas which has 100% oral bioavailability but gets degraded at physiological pH thus having very short half-life and only 20-30% brain bioavailability. Due to its amphiphilic nature, reported nanoformulations exhibits poor drug loading. The objective of the present work was to formulate lipid-based drug delivery systems to enhance the brain bioavailability

This study was to develop a combination of zedoary turmeric oil (ZTO) and tretinoin (TRE)-loaded liposomal gel as a topical drug delivery system. We used a combination of single factor experiment and orthogonal experiment to systematically optimize encapsulation process of the compound liposomes. The optimized liposome vesicles were incorporated into Carbopol gel matrix and studied by continuous in

Non-small cell lung cancer (NSCLC) is a malignant cancer characterized by easy invasion, metastasis and poor prognosis, so that conventional chemotherapy can't inhibit its invasion and metastasis. Doxorubicin, as a broad-spectrum antitumor drug, cannot be widely used in clinic because of its poor targeting, short half-life, strong toxicity and side effects. Therefore, the aim of our study is to construct

Leishmaniasis is a parasitic disease treatable and curable, however, the chemotherapeutic agents for their treatment are limited. In South American countries, pentavalent antimonials are still the first line of treatment for cutaneous leishmaniasis with an efficacy of about 75%, but the toxicity of the drug causes serious side effects and remains as the main obstacle for treatment. New knowledge aimed

The aim of the present study was production of nanostructured lipid carriers (NLCs) of curcumin and imatinib for co-administration in non-Hodgkin lymphoma cells. NLCs were prepared and conjugated to rituximab to target CD20 receptors of lymphoma cell lines. Oleic acid or Labrafac and glyceryl monostearate or lecithin were used for production of NLCs. The antibody coupling efficiency to NLCs and their

Vesicle structures primarily embody spherical capsules composed of a single or multiple bilayers, entrapping a pool of aqueous solution in their interior. The bilayers can be made by phospholipids or other amphiphiles (surfactants, block copolymers, etc.). Vesicles broad-spectrum applications in numerous scientific disciplines, including biochemistry, biophysics, biology, and various pharmaceutical

Recent treatment approaches of osteoarthritis (OA) face a number of obstacles due to the progressive multitude of pain generators, nociceptive mechanisms, first pass mechanism, less efficacy and compromised safety. The present study was aimed to bring a novel approach for the effective management of OA, by developing sublingual targeted nanovesicles (NVs) bearing tapentadol HCl (TAP), surface modified

pH responsive drug delivery systems are one of the new strategies to address the spread of bacterial resistance to currently used antibiotics. The aim of this study was to formulate liposomes with 'On' and 'Off'" pH responsive switches for infection site targeting. The vancomycin (VCM) loaded liposomes had sizes below 100 nm, at pH 7.4. The QL-liposomes had a negative zeta potential at pH 7.4 that

Abstract In this paper, two medusa-like ACyDs, modified at the primary rim bearing four (ACyD4) and eight carbons (ACyD8) acyl chain length, and one bouquet-like CyD, modified at primary side with thiohexyl and at secondary one with oligoethylene moiety (SC6OH), were investigated for their ability to assemble in nanostructures or to form hybrid dipalmitoylphosphatidylcholine (DPPC)/ACyDs systems. The

The goal of the current study was to investigate the pharmacokinetic profile, tissue distribution and adverse effects of long-circulation liposomes (LCL) with curcumin (CURC) and doxorubicin (DOX), in order to provide further evidence for previously demonstrated enhanced antitumor efficacy in colon cancer models. The pharmacokinetic studies were carried out in healthy rats, following the i.v. injection

New generation of amphiphilic vesicles known as aspasomes were investigated as potential carriers for transdermal delivery of tizanidine (TZN). Using full factorial design, an optimal formulation was developed by evaluating the effects of selected variables on the properties of the vesicles with regards to entrapment efficiency, vesicle size and cumulative percentage released. The optimal formula (TZN-AS

In this study, we describe a novel synthesis of galactosylated lipids by lipase catalysis. Lactitol (Lac), galactose (Gal), or N-acetyl galactosamine (GalNAc) was coupled with cholesterol (CHS) as target head groups by enzyme-catalyzed regioselective esterification to produce three kinds of lipids: CHS-1-Gal, CHS-6-Gal, or CHS-6-GalNAc1. The biological effects of galactosylated lipids carrying different

Abstract Luliconazole is a new drug candidate for treatment of topical fungal infections. Its present therapy is associated with limitations of very poor and slow skin permeation, leading to required long term repeated administration for complete cure of disease. Lipid nanocarriers based elastic lipogel and ethogel formulations were developed in strength of 1% w/w and extensively characterized in vitro

Elastic liposomes consist of phospholipids andof surfactants,could be considered as promising nanotechnological platforms for skin drug delivery. The aim of the present study was the formation of elastic liposomes by thin film hydration method, using different phospholipids and surfactants, in order to determine the effect of the components on their physical characteristics and on theirphysical stability

Abstract Itraconazole (ITZ) is an FDA-approved antifungal agent that has recently been explored for novel biological properties. In particular, ITZ was identified as a potent inhibitor of the hedgehog (Hh) pathway, a cell signalling pathway that has been linked to a variety of cancers and accounts for ∼25% of paediatric medulloblastoma (MB) cases. To date, there is not a targeted therapeutic option

Abstract Liposomes (or lipid vesicles) are a versatile platform as carriers for the delivery of the drugs and other macromolecules into human and animal bodies. Though the method of using liposomes has been known since 1960s, and major developments and commercialization of liposomal formulations took place in the late nineties (or early part of this century), newer methods of liposome synthesis and

Abstract Background and objective: The combination of two or more different mechanisms of drugs in the treatment of cancer has become one of the effective methods. The purpose of this study was to successfully prepare a non-viral delivery system that could efficiently co-delivery siRNA and gambogenic acid (GNA) to improve the anti-cancer efficiency in HepG2 cells. Methods: The delivery system was prepared

Abstract The Malus hupehensis (Pamp.) Rehd. is a traditional medicine and edible plant. The previous study found that the extracts of M. hupehensis (Pamp.) Rehd. had a good antioxidant activity in vivo and in vitro. But its clinical application was limited by its poor solubility, rapidly metabolized and poor bioavailability. Hence, this article aimed at developing liposomes as a novel transdermal system

Abstract Oligonucleotide is emerging as a novel class of therapeutics due to its high specificity, and ability to manage the incorrigible diseases with targeted action. The expedited growth evident from past few decades unveils the potentiality of the oligonucleotide as the future medicine. Various studies based on the vector-based system have shown the superiority of the lipid over other non-viral

Abstract The present study was designed with an aim to develop and optimize naproxen proniosomes (NAPRNs) using Box–Behnken Design (BBD). The formulation was optimized using three independent variables [maltodextrin (X1), surfactant concentration (X2) and drug concentration (X3)] at three different levels (low, medium and high). The prepared fifteen formulations were evaluated for drug entrapment efficiency

Abstract Nonionic surfactants have an extraordinary fascination for the researchers in the field of drug delivery for enhancing drug bioavailability and therapeutic efficacy. Here, we are reporting the synthesis, characterization, drug entrapment efficiency (EE), critical micellar concentration, and biocompatibility evaluation of sulphanilamide based new nonionic surfactants. The surfactants were synthesized

Abstract Microbubble formulations have a long history for enhancement of ultrasound (US) imaging and recently also for therapeutic applications. Previously, a series of freeze-dried bubble formulations based on the lipids DSPC and DSPG were developed. Here, we have attempted to scale-up the production process for future more extensive studies. Bubbles were prepared by homogenization of a lipid dispersion