Niosomal Gel Research Articles

Niosomes based formulation containing tenoxicam: A newer solution for the rheumatic diseases

This investigation aimed to explore the potential of non-ionic surfactant based niosomal vesicles encapsulating tenoxicam (TN; anti-rheumatic drug) for the treatment of rheumatic diseases. Mechanical dispersion technique with controlled pressure was employed to prepare different niosomal formulations. The effects of different ratios of surfactant (span-60), lipid, and sodium deoxycholate on noisome's physicochemical properties have been examined. Moreover, inhibition of TNF-α in lipopolysaccharide-activated cultured Human leukemia monocytic (THP-1) cells were demonstrated to assess the in vitro inflammation profile. Finally, the optimized niosomal formulation (TN3) was prepared in gel matrix consist of carbopol 934 (termed as TN34) and stability was also tested at 4±2̊C, 25±2̊C, 37±2̊C and 45±2̊C for 6months. The optimized niosomal formulation exhibited a small vesicle size (165±14nm) and high drug encapsulation (79.64±1.5%). Niosomal gel formulation TN34 showed pH (6.7), viscosity (6810±3.34cps), spreadability (19.11±1.87gm.cm/sec) and also displayed sustained release pattern of drug release (98.16±0.07% TN released from gel matrix in 24h) in vitro release study. TN34 exhibited substantial anti-inflammatory response, with ∼75% inhibition of TNF-α in 48h. Stability investigation revealed that refrigerator temperature is most suitable for the storage of niosomal gel. Transdermal niosomal formulation displayed promising potential in the treatment of rheumatic diseases.

DEVELOPMENT AND CHARACTERIZATION OF FLURBIPROFEN LOADED NIOSOMAL IN-SITU GEL FOR OPHTHALMIC DRUG DELIVERY SYSTEM

Niosome are non-ionic surfactant-based liposomes, obtained in the hydration of artificial non-ionic surfactants, without or with addition of cholesterol or additional lipids. The intention of the current study was to organize and evaluate the in-situ niosomal gel loaded with flurbeprofen for the ophthalmic drug delivery system. Flurbeprofen, a nonsteroidal anti- infammatory drug (NSAIDs) is used to relief pain and inflammation. It carries out anti- inflammatory, analgesic and antipyretic activities. Flurbeprofen loaded Niosomes investigate the connection among the non-ionic drug / surfactant ratio with the adding of cholesterol was successfully organized with the thin film hydration way and compare the result of different grade of span used (20, 40 and 60) with the different ratio of cholesterol. Niosomes have been identified by drug entrapment efficiency, drug content, particle size and in-vitro diffusion study. Niosomes prepared using span 60 and cholesterol in the ratio (1:1) f4 showed greater entrapment efficiency (79.2%).

Development and Evaluation of Curcumin-loaded Niosomal Gel for Wound Healing in Rats

Background: The process of wound healing is a complicated series of organized biochemical and cellular phenomena that restore the integrity of the skin and subcutaneous tissue. A drug molecule can be transported to the site of action through a variety of carriers, including niosomes or non-ionic surfactant vesicles. They can trap medications that are both hydrophilic and hydrophobic. It has been demonstrated that curcumin has strong analgesic, anti-inflammatory, and wound-healing qualities. Methods: In the current study, an effort has been made to create a curcumin-loaded niosomal gel for efficient wound healing therapy. Utilizing non-ionic surfactants (Span 60, Span 20, Tween 20, and Tween 60) and cholesterol at various concentrations, a modified thin-film hydration process was used to create niosomal gels containing curcumin. Particle size, shape, entrapment effectiveness, deformability, and in vitro skin penetration were used to describe the vesicles. The 1% carbopol 940 gel was then made using the improved formulation. In wound-induced rats, the effectiveness of the in vivo wound healing was assessed. Results: The manufactured niosomes were discovered to be homogeneous in size and spherical in shape. According to the IR spectrum study, the medication and formulation additives did not interact. It was discovered that the niosomal gel (S-3) loaded with curcumin was not irritating to the skin. According to studies on in vivo wound healing, curcumin-loaded niosomal gel exhibited the highest percentage of wound contraction. Following 21 days of niosomal gel treatment, the histopathological evaluation found a noticeable improvement in the skin's histological architecture. Curcumin-loaded niosomal gel was easily made using the thin film hydration process. Conclusion: The results of this study demonstrate the potential of niosomal gel as a cutting-edge therapeutic strategy for wound healing.

Formulation and Evaluation of Niosomal Gel for Treatment of Acne

A skin disease, like acne, is very common and normally happens to everyone at least once in their lifetime. The structure of the stratum corneum is often compared with a brick wall, with corneocytes surrounded by the mortar of the intercellular lipid lamellae. Acne vulgaris is a chronic inflammatory dermatosis which is notable for open and/or closed comedones (blackheads and whiteheads), and inflammatory lesions including papules, pustules, or nodules. It is a disorder of sebaceous follicles which are special pilosebaceous units located on the face, chest, and back. Skin is one of the most readily available organs on human body for topical management and is the major route of topical drug delivery system. Topical drug administration is a localized drug delivery system everywhere in the body during ophthalmic, vaginal, rectal and skin as topical routes. SA niosomes gel delivery system (SANG1 to SANG5) as a dispersed system, which consists of small droplets and well distributed in to immiscible vehicle. Niosome salicylic acid was prepared by Reverse phase evaporation method using cholesterol and span 80 and tween 20. Niosome were evaluated for vesicle shape, size determination, Entrapment efficiency and in-vitro drug release study. The result concluded that SANG5 was best formulation with Carbopol 940 (2g), PVP, nutmeg oil base. The drug release profile and release kinetics are two important characteristics of the dosage forms, which play an important role for describing dissolution profile of dosage form.
 Keywords: Topical drug delivery, Acne vulgaris, Niosomes, Gel, Carbopol 940, nutmeg oil

FORMULATION AND EVALUATION OF NIOSOMAL GEL OF AZELAIC ACID FOR ANTIACNE ACTIVITY

Objective: This study aimed to develop niosomes loaded with azelaic acid (AA) to administer in gel form. The primary objective was to achieve controlled and sustained release of the drug while minimizing potential side effects. Methods: Niosomes were fabricated using a combination of various non-ionic surfactants and cholesterol through the application of thin film hydration technique. Furthermore, the processing parameters were optimized and drug excipient compatibility study was conducted using FTIR spectroscopy. The formulations were extensively characterized in terms of entrapment efficiency, particle size, shape, and in vitro release. Subsequently, the improved niosomal dispersions were employed to formulate gels, which underwent analysis to evaluate their visual properties, pH, and rheological behavior. Stability study was also conducted. Results: Total 15 formulations were prepared, out of which 3 formulations F3, F9 and F15 were found to exhibit maximum entrapment efficiency. These formulation were having particle size 260.1 nm, 272.3 nm and 226.3 nm respectively. In vitro drug release was found to be maximum in F9 formulation. The release was found to be dose-dependent across all formulations, with regression values between 0.97 and 0.99, confirming first-order release kinetics. FTIR spectra indicated the absence of any drug-cholesterol-nonionic surfactant interaction in the formulation. The niosomal gel formulations exhibited optimal performance when stored within the temperature range of 4 to 8 °C. Conclusion: This investigation demonstrates the utility of the thin film hydration technique in effectively incorporating poorly water-soluble medications such as azelaic Acid (AA) into niosomes, resulting in high entrapment efficiency. These findings suggest that niosomes containing AA, when topically applied as a gel, have the potential to be an efficacious treatment for acne.

Mupirocin Loaded Niosomal Gel for Topical Wound Healing Applications

Mupirocin Loaded Niosomal Gel for Topical Wound Healing Applications

Formulation optimization, in vitro and in vivo evaluation of niosomal nanocarriers for enhanced topical delivery of cetirizine

Cetirizine hydrochloride (CTZ), a second-generation anti-histaminic drug, has been recently explored for its effectiveness in the treatment of alopecia. Niosomes are surfactant-based nanovesicular systems that have promising applications in both topical and transdermal drug delivery. The aim of this study was to design topical CTZ niosomes for management of alopecia. Thin film hydration technique was implemented for the fabrication of CTZ niosomes. The niosomes were examined for vesicle size, surface charge, and entrapment efficiency. The optimized niosomal formulation was incorporated into a hydrogel base (HPMC) and explored for physical characteristics, ex vivo permeation, and in vivo dermato-kinetic study. The optimized CTZ-loaded niosomal formulation showed an average size of 403.4 ± 15.6 nm, zeta potential of − 12.9 ± 1.7 mV, and entrapment efficiency percentage of 52.8 ± 1.9%. Compared to plain drug solution, entrapment of CTZ within niosomes significantly prolonged in vitro drug release up to 12 h. Most importantly, ex-vivo skin deposition studies and in vivo dermato-kinetic studies verified superior skin deposition/retention of CTZ from CTZ-loaded niosomal gels, compared to plain CTZ gel. CTZ-loaded niosomal gel permitted higher drug deposition percentage (19.2 ± 1.9%) and skin retention (AUC0-10h 1124.5 ± 87.9 μg/mL.h) of CTZ, compared to 7.52 ± 0.7% and 646.2 ± 44.6 μg/mL.h for plain CTZ gel, respectively. Collectively, niosomes might represent a promising carrier for the cutaneous delivery of cetirizine for the topical management of alopecia.

Preparation and physicochemical properties of coenzyme Q10 loaded niosomal hydrogels based on carbomer and scleroglucan

AbstractIn this study, the blank hydrogels and the niosomal hydrogels loading coenzyme Q10 (CoQ10) were prepared by carbomer (CBM) and scleroglucan (SCL), and their physicochemical properties were characterized in terms of rheological and texture measurement, FTIR, SEM, DSC, and DLS. First, the blank hydrogels CBM‐SCL‐Gel were prepared. With the increase of SCL concentration, the viscosity and modulus increased, displaying better shear thinning behavior of pseudoplastic fluid. A dense network structure was formed in CBM‐SCL‐Gel, especially for CBM/SCL at 5/4 and 5/5, due to hydrogen bonding between CBM and SCL. The swelling behaviors of the composite gels conformed to pseudo‐second‐order kinetics, and CBM/SCL at 5/1 exhibited the highest swelling capability. The addition of SCL made the water absorption mechanism tend to a non‐Fickian diffusion mode. Then, the niosomal hydrogel was prepared by the optimized gel formulation with the CoQ10‐loaded niosome. It was found that the gel properties were insignificantly affected by the CoQ10 niosomes. The particle sizes of the niosomes in the gel were a little larger than that in aqueous suspension. After storage for 30 days, the CoQ10 retention rate in the niosomal gel remained at 92% (4°C, N‐Gel), representing high stability of CoQ10.

DEVELOPMENT AND EVALUATION OF LULICNAZOLE NIOSOMAL TRANSDERMAL DRUG DELIVERY SYSTEM

According to earlier research, using niosomes as drug carriers, particularly for antifungal drugs, produces greater results than using alternative carriers. Niosomes has the capacity to encapsulate both hydrophilic and hydrophobic pharmaceuticals, as well as their prolonged stability in circulation. This work aimed to prepare and evaluate luliconazole niosomal gel for antifungal activity. In this study, niosomes containing luliconazole were prepared by thin film hydration technique using non-ionic surfactant (Span 60 and Tween 80) and cholesterol at different concentrations. The prepared formulations were evaluated for optical microscopy, drug entrapment efficiency, drug content, in-vitro drug release study, and stability studies. The ratio 2:1 of span 60 and cholesterol showed better results. Hence it was optimized as the final vesicle formulation. The FTIR study concluded there was no interaction between Luliconazole and any of the excipients. The niosomes gel was evaluated for various parameters of all the formulations. The 1% Carbopol 934 gel shows the best and most promising results. The niosomal gel formulation could be a useful dosage form to increase efficacy by the transdermal route. The potential of a secure and efficient therapy for difficult clinical applications is made possible by the development of niosomes with target specificity. Therefore, niosomes gel may be considered the best vesicular carrier for the effective delivery of luliconazole through the skin.

Mupirocin Niosomal Gel with Bee Honey & Curcumin as Nano-Drug Delivery in Wound Healing Applications

Mupirocin Niosomal Gel with Bee Honey & Curcumin as Nano-Drug Delivery in Wound Healing Applications

Quality-by-Design-Assisted Optimization of Carvacrol Oil-Loaded Niosomal Gel for Anti-Inflammatory Efficacy by Topical Route.

Niosomes are multilamellar vesicles that effectively transfer active ingredients into the skin's layers. To improve the active substance's penetration across the skin, these carriers are frequently utilized as topical drug delivery systems. Essential oils (EOs) have garnered significant interest in the field of research and development owing to their various pharmacological activities, cost-effectiveness, and simple manufacturing techniques. However, these ingredients undergo degradation and oxidation over time, leading to a loss of functionality. Niosome formulations have been developed to deal with these challenges. The main goal of this work was to create a niosomal gel of carvacrol oil (CVC) to improve its penetration into the skin for anti-inflammatory actions and stability. By changing the ratio of drug, cholesterol and surfactant, various formulations of CVC niosomes were formulated using Box Behnken Design (BBD). A thin-film hydration technique using a rotary evaporator was employed for the development of niosomes. Following optimization, the CVC-loaded niosomes had shown: 180.23 nm, 0.265, -31.70 mV, and 90.61% of vesicle size, PDI, zeta potential, and EE%. An in vitro study on drug release discovered the rates of drug release for CVC-Ns and CVC suspension, which were found to be 70.24 ± 1.21 and 32.87 ± 1.03, respectively. The release of CVC from niosomes best fit the Higuchi model, and the Korsmeyer-Peppas model suggests that the release of the drug followed the non-Fickian diffusion. In a dermatokinetic investigation, niosome gel significantly increased CVC transport in the skin layers when compared to CVC-conventional formulation gel (CVC-CFG). Confocal laser scanning microscopy (CLSM) of rat skin exposed to the rhodamine B-loaded niosome formulation showed a deeper penetration of 25.0 µm compared to the hydroalcoholic rhodamine B solution (5.0 µm). Additionally, the CVC-N gel antioxidant activity was higher than that of free CVC. The formulation coded F4 was selected as the optimized formulation and then gelled with carbopol to improve its topical application. Niosomal gel underwent tests for pH determination, spreadability, texture analysis, and CLSM. Our findings imply that the niosomal gel formulations could represent a potential strategy for the topical delivery of CVC in the treatment of inflammatory disease.

Formulation And In Vitro Evaluation Of Fluconazole Niosomal Gel For Topical Drug Delivery

Fluconazole, a macrolide antibiotic, is employed to treat certain susceptible bacteria. Niosomes play a significant role in drug delivery since they can alter pharmacokinetics and bioavailability characteristics, as well as minimise toxicity. Niosomes are becoming more and more crucial in the administration of drugs. While decreasing the drug's systemic absorption, topically administered niosomes can lengthen the duration that medications remain in the stratum corneum and epidermis. Fluconazole-loaded topical gel niosomes are intended to be developed and evaluated in this study. Span 20, 40, 60 (as a non-ionic surfactant) and cholesterol were used to create niosomes by the thin film hydration method (as stable vesicle forming agent). Different dosages of the drugs, surfactants, and cholesterol were used to make niosomes (0.30:1:0.6, 0.6:1:0.6, 0.9:1:0.6). The vesicle size, surface shape, % entrapment effectiveness, drug content, and in vitro drug release of the niosomal dispersion were examined. Using a UV spectrophotometer, the drug concentration and entrapment efficiency were determined at 262 nm. A range of 77.650.25 to 94.120.48 was discovered for the entrapment efficiency. A maximum entrapment efficiency of 94.120.48 was shown for Formulation FS5, which contains Span 60, and 93.900.70 was shown for Formulation FT4, which contains Tween 60. Carbopol 940, glycerol, triethanolamine, and distilled water were used to make fluconazole niosomal gel. Niosomal gel's evaluation was based on its outward appearance, pH, viscosity, drug content, entrapment effectiveness, and in-vitro permeation investigations. The amount of medication released from the niosomal gel was discovered to be 80.76%. The aforementioned data show that encapsulating a fluconazole-loaded niosomal topical gel lengthens drug release, increases drug retention in skin, and enhances cellular permeability.

Evaluation of physicochemical, in vivo analgesic and antiinflammatory activities of Brachystegia eurycoma gum-based naproxen loaded niosomal gels

Protracted oral Naproxen administration for acute and chronic conditions, such as rheumatoid arthritis treatment, may cause peptic ulcers. The topical application of Naproxen will circumvent this effect. This research aims to assess the physicochemical, anti-inflammatory and analgesic properties of Naproxen-loaded niosomal gels formulated using Brachystegia eurycoma gum (BEG) as the gelling polymer. BEG was isolated by acetone precipitation of filtrate produced by cold maceration of Brachystegia eurycoma seeds powder. Naproxen and BEG compatibility was evaluated using Fourier transform infrared FTIR) spectroscopy. Naproxen-loaded niosomes were produced with cholesterol, surfactant (tween 80) and water using a modified ethanol injection method. Theformulated niosomes were incorporated into either BEG (5, 7.5 or 10%) or HPMC (1.5, 5%) gel base to produce the respective Naproxen-loaded niosomal gels. The niosomal gels were assessed for their physicochemical, antiinflammatory and analgesic properties using a commercially available gel as a positive control. There was no incompatibility between BEG and Naproxen. The formulated gels’ pH ranged from 6.4 to 7.3, while the viscosity ranged from 1476.2 to 2980 mPas. The formulated gels had good extrudability and spreadability compared to the commercially available gel (1%). In-vivo studies using white albino rats showed that gels from the optimized formulation (F1) had comparable anti-inflammatory (26.5% inhibition) and analgesic properties to the commercially available gel (31.3% inhibition). Naproxen-loaded niosomal gels having good physicochemical, analgesic and anti-inflammatory properties were successfully formulated using BEG as a gelling agent.

Formulation and Evaluation of Niosomal Gel Loaded with Asparagus racemosus Extract for Anti-inflammatory Activity

Abstract: Background/Aim: Inflammation typically occurs when infectious microorganisms enter the body, settle in specific tissues, and/or circulate in the blood. Asparagus racemosus extract contains various saponins and flavonoids and plant-origin drugs have fewer side effects and toxicity. The phytoconstituents have less permeability through the skin; to enhance their permeability and effectiveness it was loaded in niosomes. Therefore, the study aimed to formulate and characterize the niosomal gel loaded with Asparagus racemosus extract for anti-inflammatory activity. Materials and Methods: The niosomes containing saponins in the extract were prepared using thin film hydration method and 23 full factorial design was employed to assess the influence of independent variables span 60 and cholesterol on vesicle size, PDI, zeta potential, and percentage entrapment efficiency. 10% of niosomal and conventional gels were prepared by incorporating optimized niosomes and extract containing total saponin in 1% carbopol gel. Ex vivo permeability studies of prepared gels were performed through goat skin using Franz diffusion cell. An anti-inflammatory study was conducted on albino rat. Results: The statistical analysis revealed the significant effect of independent variables on vesicle size, PDI, entrapment efficiency and zeta potential. SEM image shows vesicles are spherical in shape and uniform in size. The niosomal gel provided a significantly higher amount of steady-state flux and permeability coefficient into the skin than conventional gel. The animal model proved that niosomal gel loaded with total saponins in extract showed significant anti-inflammatory compared to the control. Conclusion: It was concluded that the niosomal gel had better efficacy than the conventional gel. Keywords: Asparagus racemosus, Niosomes, Span 60, Cholesterol, Factorial design, Carbopol 934.

Qbd-Based Approach to Optimize Niosomal Gel of Levosulpiride for Transdermal Drug Delivery.

Poor aqueous solubility besides extensive hepatic first effect significantly decreases the oral absorption of levosulpiride, which in turn minimizes its therapeutic effectiveness. Niosomes have been extensively investigated as a transdermal vesicular nanocarrier to increase the delivery of low permeable compounds into and across the skin. This research work was to design, develop and optimize levosulpiride-loaded niosomal gel and to evaluate its prospects for transdermal delivery. The Box-Behnken design was used to optimize niosomes by analyzing the impact of three factors (cholesterol; X1, Span 40; X2, and sonication time; X3) on the responses (particle size, Y1, and entrapment efficiency, Y2). Optimized formulation (NC) was incorporated into gel and evaluated for pharmaceutical properties, drug release study, ex vivo permeation, and in vivo absorption. The design experiment data suggest that all three independent variables influence both response variables significantly (p < 0.01). Pharmaceutical characteristics of NC vesicles showed the absence of drug excipient interaction, nanosize (~102.2 nm), narrow distribution (~0.218), adequate zeta potential (-49.9 mV), and spherical shape, which are suitable for transdermal therapy. The levosulpiride release rates varied significantly (p < 0.01) between niosomal gel formulation and control. Greater flux (p < 0.01) was observed with levosulpiride-loaded niosomal gel than with control gel formulation. Indeed, the drug plasma profile of niosomal gel was significantly higher (p < 0.005), with ~3 folds higher Cmax and greater bioavailability (~500% higher; p < 0.0001) than its counterpart. Overall, these findings imply that the use of an optimized niosomal gel formulation can increase the therapeutic efficacy of levosulpiride and may represent a promising alternative to conventional therapy.

Formulation and characterisation of lacidipine niosomal gel for transdermal delivery

Abstract The present study aimed to enhance the transdermal delivery of lacidipine by niosomal vesicles. Lacidipine niosomes were generated using the ultrasonic method, and Span 60 was used as a nonionic surfactant. Formulations were prepared containing Span 60 and cholesterol in 1:1 and 2:1 ratios, respectively, with essential oils added at increasing concentrations. The formulated niosomes had nano-vesicles with entrapment efficiency ranging from 75.81% to 91.25% and in-vitro drug release ranging from 80.61% to 89.81%. The optimal formulation was selected based on particle size, entrapment efficiency and in-vitro drug release. Optical microscopy and high-resolution transmission electron microscopy studies revealed a spherical shape of the niosomal vesicles. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction studies confirmed complete encapsulation of the drug in the niosomal vesicles. The optimized formulation was also incorporated into a gel base, which was then evaluated for appearance, pH, viscosity, spreadability, in vitro drug release and stability. Overall, the results indicated that the developed niosomal lacidipine vesicles may provide an alternative to existing delivery systems for this drug.

An Eco-Friendly and Hopeful Promise Platform for Delivering Hydrophilic Wound Healing Agents in Topical Administration for Wound Disorder: Diltiazem-Loaded Niosomes

PurposesCalcium channel blockers, such as diltiazem (DLZ), are important drugs for wound repair treatment. This current study used an ultrasonic method to increase the cutaneous delivery of (DLZ) niosomes.MethodsThe impact of the cholesterol:surfactant ratio on the DLZ-loaded niosome formulations was investigated. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, drug release, skin sensitivity, animal wound repair model, and histopathological assessment were applied to investigate the characteristics, morphology, and therapeutic effectiveness of the DLZ noisome.ResultsThe results showed that changes in the cholesterol:surfactant ratio can influence the zeta potential and the size of the niosome. The maximum entrapment efficiency was observed to be about 94% when the cholesterol content in the formulation was high. The DLZ release studies revealed that the niosomal formulation was released slowly over the course of 24 h. Macroscopic observations of the wound demonstrated that wound closure in the DLZ-niosome-treated group and the commercial brand was equal and higher than in the other groups (gel base, placebo gel, and negative control). Pathological studies described that the wound repair in the DLZ-niosomal gel group was greater than in the other treatment. All the preparations tested for cutaneous irritation on Wistar rats showed the DLZ niosomal gels to be non-irritating.ConclusionThe findings of this study revealed that the prepared DLZ-niosome could be used as a possible nano-vesicle for DLZ cutaneous delivery thus potentially opening up new prospects for the treatment of wound disorders.

Co-delivery of amphotericin B and pentamidine loaded niosomal gel for the treatment of Cutaneous leishmaniasis

Topical drug delivery is preferable route over systemic delivery in case of Cutaneous leishmaniasis (CL). Among the available agents, amphotericin B (AmB) and pentamidine (PTM) showed promising result against CL. However, monotherapy is associated with incidences of reoccurrence and resistance. Combination therapy is therefore recommended. Thin film hydration method was employed for amphotericin B-pentamidine loaded niosomes (AmB-PTM-NIO) preparation followed by their incorporation into chitosan gel. The optimization of AmB-PTM-NIO was done via Box Behnken Design method and in vitro and ex vivo analysis was performed. The optimized formulation indicated 226 nm particle size (PS) with spherical morphology, 0.173 polydispersity index (PDI), −36 mV zeta potential (ZP) and with entrapment efficiency (EE) of 91% (AmB) and 79% (PTM), respectively. The amphotericin B-pentamidine loaded niosomal gel (AmB-PTM-NIO-Gel) showed desirable characteristics including physicochemical properties, pH (5.1 ± 0.15), viscosity (31870 ± 25 cP), and gel spreadability (280 ± 26.46%). In vitro release of the AmB and PTM from AmB-PTM-NIO and AmB-PTM-NIO-Gel showed more prolonged release behavior as compared to their respective drug solution. Higher skin penetration, greater percentage inhibition and lower IC50 against the promastigotes shows that AmB-PTM-NIO has better antileishmanial activity. The obtained findings suggested that the developed AmB-PTM-NIO-Gel has excellent capability of permeation via skin layers, sustained release profile and augmented anti-leishmanial outcome of the incorporated drugs.

Niosomes for Topical Application of Antioxidant Molecules: Design and In Vitro Behavior

In the present study, gels based on xanthan gum and poloxamer 407 have been developed and characterized in order to convey natural antioxidant molecules included in niosomes. Specifically, the studies were conducted to evaluate how the vesicular systems affect the release of the active ingredient and which formulation is most suitable for cutaneous application. Niosomes, composed of Span 20 or Tween 20, were produced through the direct hydration method, and therefore, borate buffer or a micellar solution of poloxamer 188 was used as the aqueous phase. The niosomes were firstly characterized in terms of morphology, dimensional and encapsulation stability. Afterwards, gels based on poloxamer 407 or xanthan gum were compared in terms of spreadability and adhesiveness. It was found to have greater spreadability for gels based on poloxamer 407 and 100% adhesiveness for those based on xanthan gum. The in vitro diffusion of drugs studied using Franz cells associated with membranes of mixed cellulose esters showed that the use of a poloxamer micellar hydration phase determined a lower release as well as the use of Span 20. The thickened niosomes ensured controlled diffusion of the antioxidant molecules. Lastly, the in vivo irritation test confirmed the safeness of niosomal gels after cutaneous application.

Preparation and Characterization of Patch Loaded with Clarithromycin Nanovesicles for Transdermal Drug Delivery

Clarithromycin (CLR), categorized as a Biopharmaceutical Classification System class II drug, has several gastrointestinal tract side effects and an extremely unpalatable bitter taste. The current study aimed to design transdermal patch-embedded CLR niosomes to overcome the aforementioned CLR-related challenges. Various niosomal formulations were successfully fabricated and characterized for their morphology, size, in vitro release, and antimicrobial efficacy. Subsequently, the CLR niosomes were loaded into transdermal patches using the solvent casting method. The polydispersity index of the niosomes ranged from 0.005 to 0.360, indicating the uniformity of the niosomes. The encapsulating efficiency (EE)% varied from 12 to 86%. The optimal Chol: surfactant ratio for drug release was found to be 0.5:1. In addition, the encapsulation of CLR into niosomal nanovesicles did not reduce the antibacterial activity of the CLR. The niosomal patch had a significantly higher permeability coefficient of CLR than the conventional patch. In addition to that, a shear-thinning behavior was observed in the niosomal gels before loading them into a niosomal patch. The flux (Jss) of the niosomal patch was significantly higher than the conventional patch by more than 200 times. In conclusion, niosome-based transdermal patches could be a promising method for the transdermal drug delivery of class II drugs and drugs experiencing GIT side effects.