Non-ionic Surfactant Vesicles Research Articles

PH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models

pH-sensitive nonionic surfactant vesicles (niosomes) by polysorbate-20 (Tween-20) or polysorbate-20 derivatized by glycine (added as pH sensitive agent), were developed to deliver Ibuprofen (IBU) and Lidocaine (LID). For the physical-chemical characterization of vesicles (mean size, size distribution, zeta potential, vesicle morphology, bilayer properties and stability) dynamic light scattering (DLS), small angle X-ray scattering and fluorescence studies were performed. Potential cytotoxicity was evaluated on immortalized human keratinocyte cells (HaCaT) and on immortalized mouse fibroblasts Balb/3T3. In vivo antinociceptive activity (formalin test) and anti-inflammatory activity tests (paw edema induced by zymosan) in murine models were performed on drug-loaded niosomes. pH-sensitive niosomes were stable in the presence of 0 and 10% fetal bovine serum, non-cytotoxic and able to modify IBU or LID pharmacological activity in vivo. The synthesis of stimuli responsive surfactant, as an alternative to add pH-sensitive molecules to niosomes, could represent a promising delivery strategy for anesthetic and anti-inflammatory drugs.

The effects of hydration media on the characteristics of non-ionic surfactant vesicles (NISV) prepared by microfluidics

Non-ionic surfactant vesicles (NISV) are colloidal particles that provide a useful delivery system for drugs and vaccines. One of the methods that is used for NISV preparation is microfluidics in which the lipid components dissolved in organic phase are mixed with an aqueous medium to prepare the particles through self-assembly of the lipids. In this work, we examined the effect of using different types of aqueous media on the characteristics of the NISV prepared by microfluidics. Five aqueous media were tested: phosphate buffered saline, HEPES buffer, Tris buffer, normal saline and distilled water. The resulting particles were tested for their physical characteristics and cytotoxicity. The aqueous media were found to have significant effects on the physical characteristics of the particles, as well as their overall stability under different conditions and their cytotoxicity to different human cell lines. Careful consideration should be taken when choosing the aqueous media for preparing NISV through microfluidics. This is an important factor that will also have implications with respect to the entrapped material, but which in addition may help to design vesicles for different uses based on changing the preparation medium.

Development of a biocompatible creatinine-based niosomal delivery system for enhanced oral bioavailability of clarithromycin

Context: Nonionic surfactant vesicles have gained increasing scientific attention for hydrophobic drugs delivery due to their biocompatibility, stability and low cost.Objective: The aim of the present study was to synthesize and evaluate a novel creatinine-based nonionic surfactant in terms of its ability to generate biocompatible niosomal system for the delivery of Clarithromycin.Materials and Methods: The surfactant was synthesized by reacting creatinine with lauroyl chloride followed by characterization using 1HNMR and MS. The drug-loaded niosomal vesicles of the surfactant were characterized for drug encapsulation efficiency (EE) using LC-MS, vesicle size using dynamic light scattering (DLS) and vesicle shape using atomic force microscopy (AFM). The surfactant was also investigated for blood hemolysis, in vitro cytotoxicity against different cell lines and in vivo acute toxicity in mice. Furthermore, the in vivo bioavailability of Clarithromycin encapsulated in the novel niosomal formulation was investigated using rabbits and quantified through validated LC-MS/MS method.Results and discussion: Findings showed that vesicles were able to entrap up to 67.82 ± 1.27% of the drug, and were rounded in shape with a size around 202.73 ± 5.30 nm and low polydispersity. The surfactant caused negligible blood hemolysis, very low cytotoxicity and was found to be safe up to 2500 mg/kg body weight using mice. The niosomal formulation showed twofold enhanced oral bioavailability of Clarithromycin as compared to commercial formulations of the drug.Conclusion: The study has shown that the creatinine-based niosomes developed in our laboratory were biocompatible, safe and increased the oral bioavailability of the model hydrophobic Clarithromycin using experimental animals.

Fluconazole-loaded niosomal gels as a topical ocular drug delivery system for corneal fungal infections

Non-ionic surfactant vesicles containing fluconazole (FLZ) were prepared using, span 60 or span 80 and cholesterol in weight ratios of 1:1, 2:1 and 1:2. The prepared vesicles were characterized for size, entrapment efficiency, and in vitro drug release. The drug encapsulation efficiencies varied from 40.0% to 84.35%. The particle size ranged from 140 to 280 nm. Higher encapsulation was obtained by the span 60: cholesterol ratio of 2:1, which showed the best drug release. The selected niosomal formulations were incorporated into poloxamer 407 and chitosan gel formulations. Drug release from niosomal dispersions and niosomal gels, permeation of drug from niosomal gels through goat cornea and its antifungal activity were evaluated. Results showed that the surfactant: cholesterol ratio had a significant effect on the encapsulation efficiency and the size of vesicles. The niosomes prepared with 2:1 surfactant: cholesterol showed superior release over the other niosomal formulations. The drug release and permeation from poloxamer gel were higher than that from chitosan gel. Permeation study showed that, the flux of drug was dependent on the viscosity of the gel. The selected niosomal gels had excellent antifungal activity where the poloxamer niosomal gel was more effective compared to chitosan niosomal gel.

Development and optimization of boswellic acid-loaded proniosomal gel

Context: Boswellic acids (BAs) are isolated from oleo gum of Boswellia serrata and are mainly used as potential anti-inflammatory, hypolipidemic, immunomodulatory, and antitumor agents. Pharmacokinetic investigations of BAs uncover its poor bioavailability through digestive system thus creates a need for improved therapeutic responses which can possibly be achieved by developing formulations through novel delivery system.Objective: Present study was conducted to design topical BA-loaded proniosomal gel for the management of inflammatory disorders with enhanced bioavailability.Materials and methods: Nonionic surfactant vesicles were prepared using the coacervation phase separation method. A central composite design was employed to statistically optimize formulation variables using Design-Expert software. Three independent variables were evaluated: amount of surfactant (X1), amount of soya lecithin (X2), and amount of cholesterol (X3). The encapsulation efficiency percentage (Y1) and particle size (Y2) were selected as dependent variables.Results and discussion: The optimum formulation (F10) displayed spherical bi-layered vesicles under transmission electron microscopy with optimum particle size of 707.9 nm and high entrapment efficiency as 98.52%. In vitro skin permeation study demonstrated the most sustained release of 84.83 ± 0.153 mg/cm2 in 24 h. Anti-inflammatory activity of the gel showed a significant (p < 0.001) higher percentage inhibition as compared to the marketed gel at the same dose.Conclusion: The present study exhibited that BA-loaded proniosomal gel was better in terms of absorption, bioavailability, and release kinetics.

Molecular structure and dynamical properties of niosome bilayers with and without cholesterol incorporation: A molecular dynamics simulation study

Niosomes are non-ionic surfactant vesicles having a bilayer structure formed by self-assembly of hydrated surfactants, usually with cholesterol incorporation. Stability and mechanical properties of niosomes strongly depend on type of non-ionic surfactants and compositions used. In this study we present the structural and dynamical properties of niosome bilayers composed of sorbitan monostearate (Span60) with 0% and 50% cholesterol compositions which are investigated by using molecular dynamics simulations. The simulations reveal that niosome bilayer without cholesterol prefer to form in the gel phase with a higher order structure, while in the presence of cholesterol the bilayer exhibits more fluidity having a less ordered structure. The niosome bilayer with 50% cholesterol inclusion shows an increase of area per lipid (∼11%) and thickness (∼39%) compared with the niosome bilayer without cholesterol. The Span60 tailgroup orientation of the niosome bilayers without cholesterol exhibits more tilt (34.5o±0.5) than that of the bilayer with 50% cholesterol (15.4o±0.8). Additionally, our results show that the addition of cholesterol to the bilayer causes the higher in lateral and transverse diffusion, as well as an increase in the hydrogen bond number between Span60 and water. Such characteristics not only enhance the niosome stability but also increase the fluidity, which are necessary for the niosomal drug delivery.

Effect of different types of surfactants on the physical properties and stability of carvedilol nano-niosomes.

Background:Niosomes are non-ionic surfactant vesicles used as drug carriers for encapsulating both hydrophobic and hydrophilic drugs. The aim of this study is to evaluate the effect of different surfactants on the physical properties and stability of carvedilol niosomes designed to improve oral bioavailability.Materials and Methods:Different niosomal formulations were prepared using a film hydration method, with various mixtures of different non-ionic surfactants including Span 20, 40, and 60, and also Tween 20, 40, and 60, along with cholesterol. The physicochemical characteristics of the formulations were evaluated in vitro.Results:The drug encapsulation efficiency was reduced by using lauryl (C12) chain containing surfactants, that is, Span/Tween. Cholesterol content and drug entrapment were the main factors affecting the mean particle size of the niosomes. The drug release profiles from most of the formulations were fitted well with the Baker-Lonsdale model, indicating a diffusion-based drug release mechanism. Niosomes prepared from 50 and 40% of the cholesterol with 25 or 30% of Span/Tween 60 showed the highest stability due to their high transition temperature and solid state feature of these surfactants.Conclusions:From the results obtained, it may be concluded that nanoniosomes are promising stable carriers for the oral delivery of carvedilol.

Preparation of Nonionic Vesicles Using the Supercritical Carbon Dioxide Reverse Phase Evaporation Method and Analysis of Their Solution Properties.

We have previously reported a new preparation method for liposomes using supercritical carbon dioxide (scCO2) as a solvent, referred to as the supercritical carbon dioxide reverse phase evaporation (scRPE) method. In our previous work, addition of ethanol to scCO2 as a co-solvent was needed, because lipid molecules had to be dissolved in scCO2 to form liposomes. In this new study, niosomes (nonionic surfactant vesicles) were prepared from various nonionic surfactants using the scRPE method. Among the nonionic surfactants tested were polyoxyethylene (6) stearylether (C18EO6), polyoxyethylene (5) phytosterolether (BPS-5), polyoxyethylene (6) sorbitan stearylester (TS-106V), and polyoxyethylene (4) sorbitan stearylester (Tween 61). All these surfactants have hydrophilic-lipophilic balance values (HLBs) around 9.5 to 9.9, and they can all form niosomes using the scRPE method even in the absence of ethanol. The high solubility of these surfactants in scCO2 was shown to be an important factor in yielding niosomes without ethanol addition. The niosomes prepared with the scRPE method had higher trapping efficiencies than those prepared using the conventional Bangham method, since the scRPE method gives a large number of unilamellar vesicles while the Bangham method gives multilamellar vesicles. Polyoxyethylene-type nonionic surfactants with HLB values from 9.5 to 9.9 were shown to be optimal for the preparation of niosomes with the scRPE method.

Nioplexes encapsulated in supramolecular hybrid biohydrogels as versatile delivery platforms for nucleic acids

Supramolecular hydrogels based on N-protected phenylalanine (Fmoc–Phe–OH) were used to encapsulate non-ionic surfactant vesicles (niosomes).

Novel synthesis of biologically active CdS nanoclusters in cell-mimicking vesicles

ABSTRACTStable cadmium sulphide (CdS) nanoclusters have been synthesised in non-ionic surfactant vesicles (niosomes). The nanocluster characteristics show strong dependence on the Cd2+ precursor concentration. At low precursor concentration, aggregates comprising fine nanocrystals of CdS with diameter 2–5 nm are formed. At high precursor concentrations, crystalline CdS nanoclusters (15–20 nm in diameter) are formed. Interestingly, these nanoclusters reside exclusively in the vesicular bilayer. Moreover, these nanoclusters are highly photoluminescent and exhibit cytotoxicity towards cancerous HeLa cells. As the vesicular bilayer mimics the cell membrane, the present work is extremely relevant to the use of the CdS nanoclusters for diagnostic and therapeutic purpose.

Niosomes as transdermal drug delivery system for celecoxib: in vitro and in vivo studies

Nonionic surfactant vesicles containing celecoxib (CXB) as an anti-inflammatory drug were prepared using, Span 60 or Span 40 and cholesterol in the ratios of 1:0, 1:1 and 1:2. Prepared vesicles were characterized for encapsulation efficiency, particle size and drug release. The drug encapsulation efficiencies varied from 60.55 to 80.35 %. The vesicle size ranged from 170 to 235 nm. The high encapsulation was achieved by the ratio 1:1 of span 60:cholesterol and this formula showed significant in vitro release of the drug (80 %) as compared to other forms (P < 0.05). Among niosomal gels investigated, poloxamer 407 niosomal gel showed significant drug release (72 % after 12 h) over the other forms (P < 0.05). The results also showed that the release of CXB from the niosomes and niosomal gels obeyed the Higuchi’s diffusion model. The anti-inflammatory activity of the drug from different niosomal gel formulations was also studied using Carrageenan-induced rat paw edema method. The results showed that there is significant anti-inflammatory activity (75.45 %) of the poloxamer niosomal gel on rat paw edema (P < 0.05).

Abstract 3677: Enhanced targeted delivery of paclitaxel to tumor cells of epithelial and neuroectodermal origin using chlorotoxin-chitosan nanodelivery system

Abstract We report a development of a novel localized nanodelivery system featuring an enhanced targeted and controlled paclitaxel (PTX) delivery to epithelial and neuroectodermal origin tumor cells. The presented drug delivery system consists of a chitosan hydrogel embedded with PTX loaded non-ionic surfactant vesicles (PTX-niosomes) and chlorotoxin (CTX). We found a higher accumulation of chitosan on the surface of ovarian epithelial carcinoma cells known to overexpress MUC1 antigen as compared to normal ovarian epithelial cells. We therefore hypothesized that besides serving as a localized drug delivery platform, chitosan hydrogel can actively target MUC1 overexpressing tumor cells. To further improve the tumor-specific delivery of PTX, we have incorporated CTX, a 36-amino acid peptide, which binds to tumor cells of neuroectodermal origin, but not to non-transformed cells. Using a High Performance Liquid Chromatography (HPLC) assay, we have measured the in-vitro release profiles of PTX from chitosan hydrogel embedded with PTX-niosomes and CTX. We have assessed the morphology of CTX and PTX-nisomes as well as chitosan hydrogel embedded with PTX-niosomes and CTX using Transmission Electron Microscopy (TEM). We have used Attenuated Total Reflectance-Fourier Transform Infra-Red (ATR-FTIR) spectroscopy to investigate the possible molecular interactions between chitosan hydrogel and various tumor cells. To better understand the mechanism involved in interactions between chitosan and specific tumor cells, we have developed a new Cell based Enzyme Linked Immunosorbent Assay (Cell ELISA) allowing us to quantify the expression level of MUC1 in epithelial and neuroectodermal origin tumor cells. Our Cell ELISA results revealed higher expression level of MUC1 (around 1.5 fold) in ovarian epithelial carcinoma cell line (OV2008) when compared to normal ovarian epithelial cell line (MCC3). The ATR-FTIR results showed a specific interaction of chitosan with OV2008 cells implying the mucoadhesive property of chitosan and its potential in targeting of MUC1 overexpressing tumor cells. We observed a sustained PTX release from chitosan hydrogel embedded with PTX-niosomes (&amp;lt; 40% of cumulative release occurred within two weeks). Release studies in cell-free system also indicated that embedding CTX along with the niosomes does not have any adverse effect on the controlled release of PTX from the chitosan network. In fact, attachment of CTX to the surface of PTX-niosomes shown by TEM imaging improves the stability of PTX-niosomes resulting in extended release rates. Together these findings indicate that the proposed drug delivery system with the distinctive tumor targeting features and extended release profiles would improve the specific delivery of PTX to epithelial and neuroectodermal origin tumor cells. Citation Format: Rana Falahat, Eva Williams, Marzenna Wiranowska, Ryan Toomey, Norma Alcantar. Enhanced targeted delivery of paclitaxel to tumor cells of epithelial and neuroectodermal origin using chlorotoxin-chitosan nanodelivery system. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 3677. doi:10.1158/1538-7445.AM2015-3677

Formulation and Evaluation of Clotrimazole Niosomal Gel for Topical Application

Objective: In the present investigation, an attempt is made to develop and characterize niosomal gel formulation of clotrimazole to increase retention time in the dermis layer through controlled release of the drug. Methodology: Clotrimazole niosomes were prepared by thin film hydration method using span 40 (as non-ionic surfactant) and cholesterol (as stable vesicle forming agent). The niosomal dispersion was evaluated for vesicle size, surface morphology, percent entrapment efficiency and in vitro drug release. Results: Among the five formulations prepared, the formulation CN3 (containing 100 mg drug, 200 mg surfactant) was found to be promising. Selected niosomal suspension (CN3) containing clotrimazole equivalent to 2 % w/w was incorporated into gel base composed of carbopol (1%), triethanolamine 0.3% and distilled water quantity sufficient. The gel was studied for it’s different parameters such as pH, in vitro drug release, anti-fungal activity and skin irritation effect. Conclusion: The studies suggest that encapsulating clotrimazole in nonionic surfactant vesicles would provide better patient compliance by achieving prolonged release of the drug to the dermis with improved efficacy.

Novel method of niosome generation using supercritical carbon dioxide part I: process mechanics

A novel method for the production of non-ionic surfactant vesicles (niosomes) using an rapid expansion of supercritical solution (RESS)-based process coupled with a gas ejector is presented along with an investigation of parameters affecting niosome morphology, size and encapsulation efficiency of a 0.2 M d-glucose solution in Tris buffer at physiological pH. The solubility of the non-ionic surfactant polyoxyethylene(4) sorbitan monostearate in SC-CO2 was determined at three pressures (10, 15 and 20 MPa) and three temperatures (40, 50 and 60 °C). Mole fraction of Tween61 in the vapor phase increased with pressure at 40 °C, but did not change with pressure at 50 or 60 °C. Solubility data were correlated using the Peng–Robinson equation of state (PREOS) with the Panagiotopoulos and Reid mixing rule. Vesicles were either multilamellar or unilamellar, depending on the degree of precipitation of the lipid formulation at the point of aqueous cargo introduction. Vesicle particle size distributions were bimodal, with the 80–99% of the liposomal volume contributed niosomes ranging in size from 3 to 7 μm and the remaining niosomes ranging from 239 to 969 nm, depending on the system configuration. Encapsulation efficiency as high as 28% using the gas ejector to introduce the glucose cargo solution was achieved. Vesicle particle size and encapsulation efficiency were shown to be dependent on cargo droplet formation.

ROLE OF NIOSOMES AND PRONIOSOMES FOR ENHANCING BIOAVAILABILITY OF DRUGS

Niosome are non-ionic surfactant vesicles obtained on hydration of synthetic nonionic surfactants, with or without incorporation of cholesterol or their lipids. They are vesicular systems similar to liposomes that can be used as carriers of amphiphilic and lipophilic drugs. Noisome are promising vehicle for drug delivery and being non-ionic; and Niosomes are biodegradable, biocompatible nonimmunogenic and exhibit flexibility in their structural characterization. Niosomes can entrap both hydrophilic and lipophilic drugs and can prolong the circulation of the entrapped drug in body. Proniosomes are dry formulation of water soluble carrier particles that are coated with surfactant. They are rehydrated to form niosomal dispersion immediately before use on agitation in hot aqueous media within minutes. Proniosomes and niosomes are physically stable during the storage and transport. Drug encapsulated in the vesicular structure of proniosomes prolong the existence of drug in the systematic circulation and enhances the penetration into target tissue and reduce toxicity. From a technical point of view, niosomes and proniosomes are promising drug carriers as they possess greater chemical stability and lack of many disadvantages associated with liposomes, such as high- cost and variable purity problems of phospholipids. The present review emphasizes on overall methods of preparation characterization and applicability of niosomes and proniosomes in targeted drug delivery. KEYWORDS: proniosomes, targeted , Niosome,

Immunization of Female Mice with a Plasmid DNA Vaccine Coding Eight Repeats of Gonadotrophin Releasing Hormone(Gnrh-I) and Eight T-Helper Epitopes Suppress Fertility In Vivo

Induction of an appropriate immune response against gonadotrophin releasing hormone (GnRH-I) disrupt fertility, reduce fecundity and regress tumours of reproductive system.To disrupt fertility a plasmid DNA vaccine was engineered coding eight repeats of GnRH-I and eight T-helper epitopes. Translation efficiency of the vaccine was evaluated in undifferentiated COS1 cells and found to release GnRH-I fusion protein in culture supernatant. Swiss albino female mice (N=24) were immunized with 50μg plasmid DNA construct in study weeks 0, 3, 6, 9 and 12. Group 2 mice were primed with the plasmid DNA in hemagglutinating virus of japanese envelope (HVJE) vector and subsequent boosts were carried out in phosphate buffer saline. Group 3 mice were immunized with the plasmid DNA in non-ionic surfactant vesicles (NISV) and Group 1 was served as untreated control. The effect of immunization was studied in terms of anti-GnRH-I antibody response (OD value at A540 ± SD), suppression of ovarian folliculogenesis, altered uterine histoarchitecture and impaired fertility in vivo in mating trials. In study week 24 OD values of anti- GnRH-I antibody response were 0.982 ± 0.231 in Group 3 mice, followed by 0.783 ± 0.191 in Group 2 in comparison with no response in Group 1 controls (0.237 ± 0.147). Results of mating trials showed conception failure in vaccinated mice; 51, 18 and 05 pups were seen in the uteri of Groups 1, 2 and 3 mice respectively. There was significant (p>0.001) reduction in the weight of ovaries in Group 2 (8.50 ± 2.38 mg) and Group 3 (7.25 ± 0.95 mg) mice compared to Group 1 control (15.00 ± 1.41 mg). Significant reduction of ovarian folliculogenesis was seen in Group 2 (p>0.001) and Group 3 mice (p>0.01). In conclusion, the plasmid DNA vaccine delivered in female mice with HVJE and NISV induced significantly (p>0.001) higher levels of anti-GnRH-I antibody response, suppressed ovarian and uterine function and impaired fertility in vivo.

English

Nanotechnology has offered enormous improvement in field of therapeutics by means of designing of nano-carriers that can cross biological barriers and are able to target cellular reservoirs. The aim of the present investigation was to formulate and evaluate Niosomes, a synthetic microscopic non-ionic surfactant vesicles formed on the admixture of a non-ionic surfactant, cholesterol and phosphate with subsequent hydration in aqueous media. The delivery of drugs by “vesicular drug delivery system” such as niosomes provides several important advantages over conventional drug therapy. Ofloxacin was selected as a suitable drug for the present study because it is a potent secondgeneration fluoroquinolone active against a broad range of gram positive and gram-negative aerobic and anaerobic bacteria. In the present investigation three formulations of Niosomal drug delivery system of ofloxacin with non ionic surfactant, span 60, in various proportions were prepared and evaluated for Morphological characterization, Encapsulation efficiency, In-vitro drug release study. The Ofloxacin niosomes were prepared by lipid film hydration method. The prepared ofloxacin niosomes showed a vesicle size of 100-300 nm, the entrapment efficiency was 78.4%. The partition coefficient value of ofloxacin was found to be 0.5.

Pharmaceutical Applications of Nano-Niosomes in Drug, Vaccine and Gene Delivery

This review article describes recent advances in the field of nano-science related to niosomes, non-ionic surfactant vesicles (NSVs). Development trends in nanotechnology in health and medicine are expected to provide solutions to many of modern medicine's unsolved problems. Nanotechnology offers potential developments in therapeutics, diagnosis, cancer treatment, implantable materials, and tissue regeneration. The objective of this review is to provide a solid groundwork for anticipating the next phases of nanomedicine development, highlighting valuable perspective and find out the various areas where niosomes are applied. NSVs are the hydrated lipids composed mainly of different classes of non-ionic surfactants, introduced in the seventies as a cosmetic vehicle. Currently, niosomes are used as important new drug delivery systems by many research groups and also they are effective immunoadjuvants which some commercial forms are already available in the market. These vesicles are recently used as gene transfer vectors too. &#x0D;

Gel-embedded niosomes: Preparation, characterization and release studies of a new system for topical drug delivery

In the present paper physical gels, prepared with two polysaccharides, Xanthan and Locust Bean Gum, and loaded with non-ionic surfactant vesicles, are described. The vesicles, composed by Tween20 and cholesterol or by Tween85 and Span20, were loaded with Monoammonium glycyrrhizinate for release experiments. Size and zeta (ζ)-potential of the vesicles were evaluated and the new systems were characterized by rheological and dynamo-mechanical measurements. For an appropriate comparison, a Carbopol gel and a commercial gel for topical applications were also tested. The new formulations showed mechanical properties comparable with those of the commercial product indicating their suitability for topical applications.In vitro release experiments showed that the polysaccharide network protects the integrity of the vesicles and leads to their slow release without disruption of the aggregated structures. Furthermore, being the vesicles composed of molecules possessing enhancing properties, the permeation of the loaded drugs topically delivered can be improved. Thus, the new systems combine the advantages of matrices for a modified release (polymeric component) and those of an easier permeability across the skin (vesicle components).Finally, shelf live experiments indicated that the tested gel/vesicle formulations were stable over 1 year with no need of preservatives.

Preparation and evaluation of a buflomedil hydrochloride niosomal patch for transdermal delivery

Context: Niosomes are the non-ionic surfactant vesicles obtained on hydration of synthetic non-ionic surfactants. These are the promising vehicles for effective transdermal drug delivery.Objective: The present research work was aimed to develop niosomal-based transdermal buflomedil hydrochloride patch containing a stable formulation with improved drug permeation.Materials and methods: Niosomes were prepared by solvent evaporation method using 32 factorial design. All the formulations were evaluated for vesicle size, zeta potential and percent entrapment efficiency. Optimized niosomal and liposomal formulation were loaded into a patch system. All the patches were then characterized for drug–excipient interaction study, scanning electron microscopy, pharmacotechnical properties and in vitro permeation studies.Result: F9 formulation having optimum vesicle size (10.09 ± 1.2 µm), highest zeta potential (−85.4 ± 0.56 mV) and maximum percent entrapment efficiency (97.09 ± 0.11%) was selected as optimized formulation. In case of liposomes, formulation F12 was selected. Patches loaded with niosomes showed 95.12 ± 1.19% cumulative amount of drug permeated as compared to liposomal vesicle-loaded patches which showed 82.21 ± 1.24% and control patches 70.10 ± 1.33%. Discussion: Flux, permeation rate and permeability coefficient were found to be higher in case of niosomal patches as compared to liposomal patches and control patches. Surfactant present in niosomes act as a penetration enhancer which contribute in the permeation enhancement of buflomedil hydrochloride from niosomes.Conclusion: Thus, it was concluded that niosomal vesicles represented to be an efficient and stable vesicular carrier for transdermal delivery of buflomedil hydrochloride.