Vesicular Gel Research Articles

Nigella sativa Oil-loaded Ethanolic Vesicular Gel for Imiquimod-induced Plaque Psoriasis: Physicochemical Characterization, Rheological Studies, and In vivo Efficacy.

The therapeutic effect of NS oil in mild to moderate psoriasis is limited owing to low play load of thymoquinone ( < 15 %w/w), irritation, dripping, low viscosity and thus, less contact time on the lesions. This study aimed at developing and characterizing the ethanolic vesicular hydrogel system of Nigella sativa (NS) oil (NS EV hydrogel) for the enhancement of anti-psoriatic activity. The objective of this study was to develop NS EV hydrogel and evaluate its anti-psoriatic activity. The identification and quantification of TQ content in different NS seed extracts and marketed oil were measured by an HPTLC method using n-hexane and ethyl acetate as solvent systems. Preparation of ethanolic vesicles (EVs) was performed by solvent injection method, while its antipsoriatic activity was evaluated employing an Imiquad (IMQ)-induced plaque psoriasis animal model. A compact HPTLC band was obtained for TQ at an Rf value of 0.651. The calibration plot was linear in the range of 1-10 μg/spot, and the correlation coefficient of 0.990 was indicative of good linear dependence of peak area on concentration. From the different NS sources, the high TQ content was obtained in the marketed cold press oil, i.e., 1.45±0.08mg/ml. Out of various NS oilloaded EVs, the F6 formulation revealed the smallest particle size (278.1nm), with log-normal size distribution (0.459) and adequate entrapment efficiency. A non-uniform shape was observed in the transmission electron microscopy. The viscosity of F6 formulation hydrogel was 32.34 (Pa·s), which exhibited plastic behavior. In vivo, efficacy studies demonstrated decreased inflammation of the epidermis and dermis and a marked decrease in the levels of IL-17 by NS EV hydrogel compared to plain NS oil and standard drugs (Betamethasone and Dr. JRK Psorolin Oil). It may be concluded from the findings that NS-loaded EV gel was as good as betamethasone cream but more efficacious than the other treatments.

Formulation development and in vitro evaluation of provesicular gel of ketoprofen for management of Arthritis

The fundamental principles and uses of transdermal drug delivery, which is a method for therapeutic drug delivery through the skin as an alternative to oral, intravascular, subcutaneous, and transmucosal routes. Arthritis is a chronic condition that affects nearly a quarter of the United States population. Osteoarthritis (OA) and rheumatoid arthritis (RA) are two major forms of arthritis associated with severe joint pain and reduced quality of life. Various pharmacological interventions may be utilized for arthritis treatment when non-pharmacological therapy is insufficient. However, pharmacological therapy can be associated with serious side effects and high costs. Therefore, alternative therapies have been under investigation. Some (details in tables) medications have shown the potential for safe and effective management of arthritis. this review, we attempt to summarize the mechanisms, diagnosis, treatments, clinical significant for OA and RA and all type of arthritis. The present study aims to formulate and evaluate the effectiveness of vesicular gel of ketoprofen in induced animal model. In the present work, optimization formulations of vesicular gel were prepared. Lecithin was used as polymers. The vesicular gel containing drugs and excipients were subjected to various evaluation test such as Preformulation study of drug, Particle size distribution, Morphology, Photomicroscope, Transfusion, SEM,TEM, In vitro, and Kinetic release. Various kinetic models to evaluate correlation coefficient and release rate constant. It was found that for the formulation, value of correlation coefficientof Korsemmayer Peppas equation is nearer to 1.0 and hence it can be predicted that the release from prodeformable vesicles follow Korsemmayer Peppas kinetics.

Formulation of Miconazole-Loaded Chitosan-Carbopol Vesicular Gel: Optimization to In Vitro Characterization, Irritation, and Antifungal Assessment.

Miconazole nitrate (MN) is a poorly water-soluble and antifungal drug used for fungal infections. The present research work was designed to develop topical MN-loaded bilosomes (BSs) for the improvement of therapeutic efficacy. MZBSs were prepared by using the thin-film hydration method and further optimized by using the Box-Behnken statistical design (BBD). The optimized miconazole bilosome (MZBSo) showed nano-sized vesicles, a low polydispersity index, a high entrapment efficiency, and zeta potential. Further, MZBSo was incorporated into the gel using carbopol 934P and chitosan polymers. The selected miconazole bilosome gel (MZBSoG2) demonstrated an acceptable pH (6.4 ± 0.1), viscosity (1856 ± 21 cP), and spreadability (6.6 ± 0.2 cm2). Compared to MZBSo (86.76 ± 3.7%), MZBSoG2 showed a significantly (p < 0.05) slower drug release (58.54 ± 4.1%). MZBSoG2 was found to be a non-irritant because it achieved a score of zero (standard score) in the HET-CAM test. It also exhibited significant antifungal activity compared to pure MZ against Candida albicans and Aspergillus niger. The stability study results showed no significant changes after stability testing under accelerated conditions. MZ-loaded gels could serve as effective alternative carriers for improving therapeutic efficacy.

Development of topical thymoquinone loaded polymer–lipid hybrid vesicular gel: in-vitro and ex-vivo evaluation

Thymoquinone (TH), a naturally occurring moiety shows excellent anticancer properties and in the present study, TH loaded polymer hybrid lipid vesicles (TH PLH) were formulated, and in-vitro cytotoxicity towards breast cancer cell lines (MCF-7 and MBD–MB 231 cells) was determined. TH PLH was primed by the ethanol spraying method and were characterized for various attributes like particle size, morphology, percentage drug entrapment, elasticity, rheological, zeta potential, etc. The prepared TH PLH Vesicles showed an average particle size from 344.7 ± 3.7 nm to 351.9 ± 2.3 nm and showed very narrow distribution with polydispersity index ranging from 0.245 ± 0.36 to 0.271 ± 0.66. The surface charge on the vesicles was confirmed by zeta potential (þ −21.3 ± 1.08 mV to þ −19.98 ± 3.4 mV). The globular moulded vesicles were in the nano-size range and had high flexibility and an approximately 10-fold increase in elasticity properties. TH PLH Vesicular gel was formulated by means of Carbopol 934 and was evaluated for physical appearance, pH, rheological behaviour, and skin irritation test. Cytotoxicity study reveals paramount inhibition on cells by TH vesicle-loaded gel. These results showed the high potential of TH PLH vesicles for topical anticancer application.

Oleic Acid Vesicles for Transdermal Delivery of Propranolol Hydrochloride: Development and Characterization

Background: Pharmaceutical scientists are exploring transdermal route for treatment of various systemic diseases nowadays. Transdermal nanocarrier systems show various advantages like bioavailability enhancement of drugs, avoidance of first pass hepatic metabolism, and reduction of dosing frequency of bioactive therapeutic molecules. Objective: The objective of the present research work was to encapsulate Propranolol hydrochloride into oleic acid vesicles and carry out in-vitro and in-vivo evaluation of oleic acid vesicular gel containing Propranolol hydrochloride. Method: Propranol hydrochloride loaded oleic acid vesicles were prepared by exploring thin film hydration method. Developed vesicles were evaluated for morphology, size, zeta potential and polydispersity index (PDI). Thermal behavior of drug loaded vesicles was checked using differential scanning calorimetry (DSC) and depth of skin penetration was determined using confocal laser scanning microscopy (CLSM). Oleic acid vesicles dispersed in Carbopol 934R gel were subjected to in-vivo evaluation in male Sprague Dawley rats through measurement of plasma concentration and tissue distribution of Propranolol hydrochloride. Results: Optimized formulation having oleic acid : Propranol hydrochloride in the ratio 7 : 3 showed highest entrapment (56.1 ± 0.7%), acceptable size (291.3 ± 2.2 nm), the optimum value of PDI (0.219 ± 0.043) and zeta potential (-27.13 ± 0.25 mV). The results of DSC analysis showed effective encapsulation of drug inside the vesicles and CLSM analysis revealed penetration of vesicles upto stratum spinosum layer of skin. The results of in-vivo study revealed capability of vesicular gel to prolong the release of Propranolol hydrochloride upto 24 h with a Cmax value of 83.6 ± 3.0 ng/mL which was higher compared to the marketed tablet of Propranolol hydrochloride [InderalR (40 mg), Abbott India Ltd.] (45.6 ± 3.1 ng/mL). Tissue distribution studies revealed higher percentage of Propranolol hydrochloride in various organs after 24 h of administration of vesicular gel compared to marketed tablet. Conclusion: Developed oleic acid vesicular gel could be effective to reduce dosing frequency and avoid side effects of oral Propranol hydrochloride.

Statistical development and in vivo evaluation of resveratrol-loaded topical gel containing deformable vesicles for a significant reduction in photo-induced skin aging and oxidative stress

Objective The present study aims to formulate and evaluate a novel vesicular formulation of resveratrol to achieve its dermatological benefits in terms of antiphotoaging and antioxidant. Method In this study, resveratrol-loaded deformable vesicular gel was prepared and optimized using Box–Behnken design. Selected critical material attributes were amount of phospholipid (X1), concentration of ethanol (X2), and amount of sodium cholate (X3). The prepared transethosomal vesicles were incorporated into carbopol gel base and evaluated. Ultraviolet radiation-induced skin aging and oxidative stress model in Swiss Albino mice was used to evaluate the clinical potential of the developed formulation and compared with conventional gel. Levels of Super Oxide Dismutase (SOD), catalase, glutathione peroxidase, protein content, and malondialdehyde were measured to assess the extent of lipid peroxidation and reactive oxygen species inhibition in different groups. Result DoE was successfully employed to optimize the vesicular formulation. Vesicle size was found to be 158.9 ± 7.65 nm, while values of entrapment efficiency and skin deposition were found to be 77.83 ± 2.87% and 371.84 ± 5.12 µg cm−2, respectively. Visual skin grading and histopathological studies confirmed the higher efficacy of transethosomal resveratrol against oxidative stress. Significant enhancement in the levels of antioxidant enzymes and protein content confirmed the ameliorated potential of flexible transethosomal resveratrol as compared to the plain gel of resveratrol. Conclusion Restoration of first-line defense mechanism in chronic UV-exposed animal model has proved that transethosomal resveratrol can be developed as an innovative cosmetic product for significant improvement and repair of photo-aged skin.

English

English

Oleic Acid Nanovesicles of Minoxidil for Enhanced Follicular Delivery.

Current topical minoxidil (MXD) formulations involve an unpleasant organic solvent which causes patient incompliance in addition to side effects in some cases. Therefore, the objective of this work was to develop an MXD formulation providing enhanced follicular delivery and reduced side effects. Oleic acid, being a safer material, was utilized to prepare the nanovesicles, which were characterized for size, entrapment efficiency, polydispersity index (PDI), zeta potential, and morphology. The nanovesicles were incorporated into the emugel Sepineo® P 600 (2% w/v) to provide better longer contact time with the scalp and improve physical stability. The formulation was evaluated for in vitro drug release, ex vivo drug permeation, and drug deposition studies. Follicular deposition of the vesicles was also evaluated using a differential tape stripping technique and elucidated using confocal microscopy. The optimum oleic acid vesicles measured particle size was 317 ± 4 nm, with high entrapment efficiency (69.08 ± 3.07%), narrow PDI (0.203 ± 0.01), and a negative zeta potential of −13.97 ± 0.451. The in vitro drug release showed the sustained release of MXD from vesicular gel. The skin permeation and deposition studies revealed superiority of the prepared MXD vesicular gel (0.2%) in terms of MXD deposition in the stratum corneum (SC) and remaining skin over MXD lotion (2%), with enhancement ratios of 3.0 and 4.0, respectively. The follicular deposition of MXD was 10-fold higher for vesicular gel than the control. Confocal microscopy also confirmed the higher absorption of rhodamine via vesicular gel into hair follicles as compared to the control. Overall, the current findings demonstrate the potential of oleic acid vesicles for effective targeted skin and follicular delivery of MXD.

Sertaconazole nitrate loaded nanovesicular systems for targeting skin fungal infection: In-vitro, ex-vivo and in-vivo evaluation

The aim of this study was to develop different vesicular systems for sertaconazole nitrate and evaluate the ability of targeting deep skin layers to treat dermal fungal infection. Therefore, different phospholipid based nanovesicles, namely liposomes, glycerosomes, transferosmes and ethosomes were prepared and in-vitro evaluated for morphology, entrapment efficiency, vesicle size and zeta potential value, followed by ex-vivo evaluation through skin penetration and permeation. The selected vesicular formula was incorporated into gel base system and assessed by ex-vivo permeation visualization study using confocal laser scanning microscopy (CLSM). In-vivo study was performed to compare antifungal efficacy of STZL loaded vesicular gel with commercial cream (Dermofix®). All nanovesicles were unilamller and almost spherical in shape. Entrapment efficiency, vesicle size and zeta potential were dependent upon vesicle composition. Vesicular formulae promoted drug permeation compared to commercial cream where transferosomal system containing 3% soyphospholipid (SPC) and 0.15% sodium deoxychloate (SDC) exhibited highest flux (645μg/cm2/h). The CLSM images confirmed the penetration of the developed probe-loaded tansferosomal system to viable epidermis layers with fluorescence intensity greater than unencapsulated probe. The in-vivo study revealed significant prevention effect in immunecompromised rat model. Furthermore, the antifungal activity with lowest histopathological changes was significantly observed in the developed STZL-loaded transferosomal gel compared to commercial cream using immunecompromised rat model with fungal skin infection.

Vesicular self-assembly of a natural triterpenoid arjunolic acid in aqueous medium: study of entrapment properties and in situ generation of gel–gold nanoparticle hybrid material

Formation of vesicular gel and gel–gold nanoparticle hybrid material from arjunolic acid extractable from the saw-dust of Terminalia arjuna.

Formulation and evaluation of meloxicam niosomes as vesicular carriers for enhanced skin delivery

Context: Skin delivery of Meloxicam (MX) offers several advantages over the oral route which is associated with potential side effects.Objectives: The aim of this study was to develop transdermal MX in niosomes.Materials and Methods: Vesicles prepared by thin film hydration method were characterized and the acute anti-inflammatory activity of 0.5% MX niosomal hydrogel was evaluated using carrageenan induced rat paw edema method. Results: The results revealed that niosomes prepared from span 60 and cholesterol at 6:4 molar ratio using 20 mg of MX were of the highest entrapment efficiency (> 55%) and with particle size (187.3 nm). There was a marked increase in the percentage inhibition of edema in animals treated with MX vesicular gel compared to those treated with free MX and piroxicam gels.Discussion: There was an inverse proportionality between vesicle size and cholesterol content. With increased cholesterol molar ratio the bilayer stability increased and permeability decreased leading to efficiently trapping the MX. In contrast, higher amounts of cholesterol may compete with the drug for packing space within the bilayer. The inhibitory effect of MX niosomal gel may be attributed to its superior skin permeation.Conclusions: The results suggest that niosomes may be promising vehicles for transdermal delivery of MX.

Efficacy study of vesicular gel containing methotrexate and menthol combination on parakeratotic rat skin model

Methotrexate (MTX) is indicated in the symptomatic control of severe, recalcitrant, and disabling psoriasis. The oral or parenteral route of administration causes systemic toxicity. The topical route of delivery, though, reduces systemic toxicity and has limited applicability due to restricted permeability. Liposomal and niosomal MTX topical formulations have also been investigated with limited success to achieve drug localization in the skin. Menthol has been suggested in conditions of psoriasis, in addition to its skin-penetration–enhancing effect on drugs. The present work aimed at investigating the potential benefits of combining menthol with MTX in a vesicular gel base for not only improving the penetration and dermal availability of MTX, but also to render such a formulation more effective with greater patient acceptability. MTX liposomes were prepared by thin-film hydration, and the vesicles were characterized for drug-entrapment efficiency, size, and morphology. These liposomal vesicles were incorporated in a gel base, and this vesicular gel was evaluated for transdermal drug permeation and extent of drug accumulation in the skin, using a rat skin ex vivo model. Skin histology studies were carried out to investigate any structural changes caused by the permeation enhancers. Antipsoriatic efficacy of the formulations was tested in vivo, using the rat tail model. The results indicated that the vesicular gel containing menthol could cause maximum drug retention in the skin. The skin treated with menthol had a disrupted epidermis and microcavities. The in vivo studies also ascertained the effectiveness of the formulation in inducing a normal pattern of differentiation in the rat tail skin that initially showed parakeratosis, which is also characteristic of psoriatic epidermis. These results show the potential of vesicular gel containing MTX and menthol to improve penetration into the skin and cause drug retention in skin appendages.

Effect of Amphiphile Size on the Transformation from a Lyotropic Gel to a Vesicular Dispersion

The sequence of phases formed by amphiphilic copolymers on dilution in water has been studied for two poly(ethylene oxide)-co-poly(butylene oxide) copolymers with the same hydrophobe−hydrophile ratio but different molecular weights. The size of the amphiphile significantly affects both the formation of lyotropic phase and dispersed vesicles. The evolution from the bulk solid to lyotropic liquid shows that the low molecular weight copolymer assembles first into an inverted hexagonal structure and then lamellae, whereas the high molecular weight dissolves directly to the lamellar phase. The transition from lamellae to the sponge phase is essentially unaffected by the molecular weight of the amphiphiles. In contrast, however, the evolution of the sponge phase into vesicles is qualitatively different depending on the size of the amphiphile. The smaller amphiphile forms dispersed vesicles at quite high concentrations, whereas the high molecular weight polymer initially forms peculiar vesicular gel clusters, wh...