Carbopol Gel Base Research Articles

Characterization and Evaluation of the Cytotoxicity of Pregabalin Gels for Oral Application.

The efficacy of pregabalin in pain treatment has led to the search for new formulations for its use through different routes of administration. This study aimed to prepare, characterize, and evaluate the cytotoxicity of pregabalin (PG) gels for topical application in the oral cavity. Solutions with three different concentrations of PG were prepared and added to a 1.0% carbopol gel base. Thermal analyses (TG and DSC) and FTIR were performed on the gel and pure pregabalin. Stability (preliminary and accelerated) and rheology studies were also conducted on the gels. Cytotoxicity was evaluated in human gingival fibroblasts in the following groups: WG (1.0% carbopol gel base), PG2G (2.0% pregabalin gel), PG5G (5.0% pregabalin gel), and PG10G (10% pregabalin gel). A transparent and homogeneous gel with a pH of 6 was obtained. The formulations showed stability, and the different drug concentrations did not influence the product's characteristics. None of the tested groups showed cytotoxicity for the analyzed cells. The pregabalin gels exhibited favorable and non-toxic characteristics for human gingival fibroblasts in vitro. Therefore, this product may be a promising therapeutic alternative for topical application in the oral mucosa.

Dermal Delivery of Hypericum perforatum (L.) Loaded Nanogel: Formulation to Preclinical Psoriasis Assessment.

Nanophytosomes represent an effective choice for topical drug delivery systems thanks to their small size, general non-toxicity, ease of functionalization and high surface to volume ratio. The goal of the current study was to investigate the potential benefits of using Hypericum perforatum extract nanogel as a means of improving skin penetration and prolonging skin deposition in dermatitis similar to psoriasis. Nanophytosomes (NPs) were developed, optimised and thoroughly characterised. The optimised NPs were then placed in a Carbopol gel base matrix and tested ex-vivo (skin penetration and dermatokinetic) and in-vivo (antipsoriatic activity in an Imiquimod-induced psoriatic rat model). The optimised NPs had a spherical form and entrapment efficiency of 69.68% with a nanosized and zeta potential of 168 nm and -10.37mV, respectively. XRD spectra and transmission electron microscopy tests confirmed the plant botanical encapsulation in the NPs. Following 60 days of storage at 40 ± 2°C/75 ± 5% RH, the optimised formula remained relatively stable. As compared to extract gel, nano-gel showed a much-improved ex vivo permeability profile and considerable drug deposition in the viable epidermal-dermal layers. When developed nano-gel was applied topically to a rat model of psoriasis, it demonstrated distinct in vivo anti-psoriatic efficacy in terms of drug activity and reduction of epidermal thickness in comparison to other formulations and the control. ELISA and histopathologic studies also demonstrated that nano-organogel had improved skin integrity and downregulated inflammatory markers (IL-17, IL-6, IFN-γ and MCP-1). Findings suggest that a developed plant botanicals-based nanogel has a potential for the treatment of psoriasis-like dermatitis with better skin retention and effectiveness.

FORMULATION AND EVALUATION OF HERBAL GEL CONTAINING DIMOCARPUS LONGAN LOUR SEEDS EXTRACT FOR TREATMENT OF SKIN ACNE

The present research work focuses on skin acne with the aim of developing an effective and safe herbal gel using Dimocarpus longan Lour. The ethanol extract of Dimocarpus longanLour was incorporated into an optimized Carbopol gel base. Physical characterization and phytochemical testing of the extract have been carried out. Antimicrobial studies showed no detectable microbial contamination and demonstrated good areas of inhibition. Overall, this research report concludes that herbal gel formulation can provide effective and safe formulations leading to patient tolerance and treatment compliance.

Design and characterisation of topical emulgel containing neem oil for its antidandruff properties

Emulgel is a novel drug delivery system for controlled release of drug. It is suitable for the dual release of drugs. This study focuses on the development and characterization of topical emulgel containing neem oil for its anti-dandruff properties. Neem oil is emulsified using suitable surfactant in the ratio 4:2:1 and the prepared emulsion is incorporated with Carbopol gel base in ratio1:1. A total of 5 formulations were prepared using the polymer carbopol-934. Topical emulgel of neem oil was formulated and subjected to evaluation studies such as organoleptic properties, pH, Viscosity, Spreadibility, Invitro diffusion studies, Accelerated stability studies using ultracentrifugation, SEM analysis and Invitro antifungal properties. Formulation F5 subjected to in vitro oil diffusion study had shown a total release of 65.27% after 8 hours. Korsmeyer-Peppa’s plot had shown that the mechanism of diffusion was non-fickian. Emulgel of neem oil shown zone of inhibition on invitro antifungal study using Candida albicans as fungi. Formulation F5 show highest zone of inhibition of 12mm as compared to other formulations. It was concluded that, formulation of neem oil as a semi solid dual release control emulgel formulation with a time dependant oil diffusion, also add up all the advantage of a semisolid dosage compared to liquids with optimum Spreadibility, stability, aesthetic appearance, adherence to the affected scalp area and with pH that is similar scalp.

Formulasi Sistem Vesikel Elastik Surfaktan Nonionik Ekstrak Etanol Rimpang Etlingera alba dalam Sediaan Gel

Etlingera alba is a plant in Southeast Sulawesi that has antioxidant activity. Natural ingredients such as herbal medicine require a delivery system that facilitates them to reach the site of drug action, especially for transdermal delivery. The elastic vesicle system is a transdermal delivery system that can increase the penetration of active substances at the skin through the act of phospholipids on the skin's lipid bilayer and the deformability of the vesicles. This study aims to formulate and evaluate Etlingera alba rhizome ethanolic extract's elastic vesicle gel to obtain the optimal concentration of Tween 60 as a vesicle former and carbopol as a gel base. Preparation of elastic vesicles of Etlingera alba ethanolic extract using the heat method through variations Tween 60's concentration, namely 5%(F1); 10%(F2); 15%(F3); and 20%(F4). Meanwhile, elastic vesicle gel formulation of the ethanol extract of Etlingera alba rhizome used various concentrations of 0.5% carbopol gel base (FGel 1); 1% (FGel 2); 1.5% (FGel 3); and 2% (FGel 4). The results obtained were the optimum concentration of Tween 60 as a constituent of elastic vesicles of 15% (F4) with spherical morphology using an optical microscope, vesicle size of 10.45 nm, and polydispersity index of 0.280 using a Particle Size Analyzer. In addition, the optimal concentration of carbopol as a base for elastic vesicle gel is a concentration of 0.5% (GGel 1) with white color, distinctive aroma, and thick texture, and has a pH of 6, a viscosity of 2,366 cPs, spread of 6.8 cm, and physically stable through cycling test.

Solubility Enhancement, Formulation Development, and Antibacterial Activity of Xanthan-Gum-Stabilized Colloidal Gold Nanogel of Hesperidin against Proteus vulgaris.

The objective of the study was to develop a transdermal nanoformulation of hesperidin (HSP) against Proteus vulgaris (P. vulgaris). Based on the low water solubility of HSP, we prepared HSP-enabled AuNPs stabilized with xanthan gum (XA), referred to as HSP@XA@AuNPs. The HSP@XA@AuNP formulation was evaluated for particle size (43.16 nm), PDI (0.565), zeta potential (−31.9 mV), and entrapment efficiency (56.7%). The HSP@XA@AuNPs gel was developed by incorporating selected formulation grades into a 1% Carbopol gel base and characterized by physical evaluation and rheological studies. The color of the HSP@XA@AuNP gel was light pink, and the texture was very smooth and non-greasy. The gel was shown to be odorless. A field emission scanning electron microscope (FESEM) was used to investigate the shape of HSP@XA@AuNPs further. The drug release was 73.08% for the HSP@XA@AuNPs and 86.26% for the HSP@XA@AuNPs gel in 500 min. The prepared gel showed antimicrobial activity against P. vulgaris with an MIC of 1.78 μg/mL. In conclusion, the HSP@XA@AuNPs gel could be an advanced modality for treating P. vulgaris.

COMPARATIVE STUDY OF SEMI-SOLID BASES OF NAPROXEN: PHARMACEUTICAL TECHNOLOGY ASPECTS

Objective: The main objectives of the present investigation work included that the preparation of a suitable naproxen semi-solid dosage form by using different types of semi-solid bases (gel bases, ointment bases) for topical application for the effective treatment of muscle aches. Methods: Different types of semi-solid bases (gel bases and ointment bases) were successfully prepared by the incorporation method to know the effect of semi-solid bases on drug release from topical semi-solid formulations. In all formulations, the drug was added by the levigation method. An evaluation study of prepared formulations, includes physical appearance, spreadability, extrudability, pH was conducted according to official methods. Results: Percent drug release of all formulations was conducted by taking diffusion cells with cellophane membrane and results showed that gel-based formulations showed more drug release than ointment-based formulations. Carbopol gel base (F1) showed more drug release (98.76 %), simple ointment base formulation (F8) showed least drug release (25.11%). From the stability studies reports at various temperature and humidity conditions it is evident that all formulations are stable for one month. In all the formulations, the drug content was observed at 95.75%. Conclusion: Finally concluded that the NXN topical dosage forms can be prepared by using gel-type bases preferably than ointment bases to release more drug from formulations.

Preparation of Luliconazole loaded silver nanoparticles Topical gel

After optimization of the luliconazole loaded silver nanoparticles formulation it was given a gel base for topical delivery the silver nanoparticles have a very low viscosity. The gel was formed by varying the concentration of carbopol 940 as 0.75%, 1. %, 2%. The optimized luliconazole loaded silver nanoparticles formulation LSN14 was incorporated into different concentration carbopol gel base of different concentrations of carbopol and evaluated for various in vitro characterization parameters homogeneity, grittiness, measurement of pH, drug content, viscosity study, Spreadibility, in - vitro drug release studies and drug release kinetics. All prepared gel formulation having different concentration of carbopol was homogenous and uniform in appearance and free from grittiness except the formulation LSN14G1Have not sufficient thickness and thus it was not used further evaluation. On the basis of result of above parameters LSN14G3 was selected for further in-vitro drug release study. Comparison of In vitro Percentage drug release study of Control gel of Luliconazole and luliconazole loaded silver nanoparticle gel formulations LSN14G3 and in - vitro drug release profile the Percentage drug release of prepared silver nanoparticle gel was found to be higher in sustained manner93.36±0.56 after 24 hr as compare to control gel 38.50±1.21.
 Keywords: optimization, silver-nanoparticles, carbopol, kinetics, luliconazole

Betamethasone Dipropionate Nanocrystals: Investigation, Feasibility and In Vitro Evaluation.

Corticosteroids, such as betamethasone dipropionate (BMD), have been the mainstay in topical therapy as potent glucocorticoid receptor agonist with immune suppression, anti-proliferative, and anti-inflammatory effects. Moreover, they have poor skin penetration, which is a hurdle against its potential therapeutic benefits. In present investigation, nanocrystals as carrier for effective topical delivery of BMD were explored using wet milling as technique and polysorbate 80 as a non-ionic stabilizer. Upon optimizing different process parameters, promising results were observed at stabilizer concentration of 0.9% w/v having particle size analysis (PSA) and PDI as 284 nm and 0.299, respectively. These results were supported by the FTIR and PXRD spectra of BMD-API and BMD nanocrystals, suggesting strong crystal lattice structure of BMD being reduced due to milling. The reduction in particle morphology was evident from the FESEM images. The optimized batch of BMD nanocrystals was incorporated into Carbopol gel base, showing pH 6.2 ± 0.2 and viscosity 87.00 ± 5.2 Pa s at 25°C. A drug diffusion study using Franz diffusion cell proclaimed around ~86% BMD release from nanogel across the membrane. Also, it was observed that the BMD permeation across the skin was 2.39-fold higher with marketed formulation in contrast to BMD nanogel, suggesting prolonged drug release. The skin permeation flux with nanogel was at a much lower rate along with ~50.27% drug retention in different strata of skin, resulting in retention of drug nanocrystals. Thus, in nutshell the prolonged drug release from nanogel would fulfill the aim of once a day application and would aid in reducing the adverse events associated with repeated drug applications.

Ethosomal gel for rectal transmucosal delivery of domperidone: design of experiment, in vitro, and in vivo evaluation

Despite high efficiency of domperidone (DOM) in prophylaxis of emesis accompanied with radiotherapy and chemotherapy, it still can bother cancer patients by its powerful side effects and difficulty of its oral administration. The study was designed to develop and optimize DOM loaded ethosomal gel for rectal transmucosal delivery. Ethosomal formulations were prepared using a 21, 51 full-factorial design where the impact of lecithin concentration and additives were investigated. The optimum ethosomal vesicles were subsequently incorporated in Carbopol gel base where rheological behavior, spreadability, mucoadhesion, and in vivo pharmacokinetic parameters were studied. Based on Design Expert® software (Stat Ease, Inc., Minneapolis, MN), the optimum formulation illustrated entrapment efficiency of 70.02%±5.52%, and vesicular size of 112 ± 3.3 nm, polydispersity index of 0.32 ± 0.01, zeta potential of −59 ± 0.28 mV, and % drug released after 6 h of 76.30%±2.45%. Moreover, ex vivo permeation through rabbit intestinal mucosa increased four times compared to free DOM suspension. The gel loaded with ethosomes showed excellent mucoadhesion to rectal mucosa. DOM ethosomal gel showed a raise in C max and AUC0–48 of DOM by twofolds compared to free DOM gel. The study suggested that ethosomes incorporated in gels could be an efficient candidate for rectal transmucosal delivery of DOM.

Optimisasi Carbopol Sebagai Basis Gel pada Gel Antiseptik Berbasis Alkohol

Alcohol-based antiseptic gels are considered to be able to replace washing hands with soap and can inhibit the growth of viruses. Alcohol-based gels have the disadvantage of being difficult to mix with gel-based ingredients. Carbopol as an alcohol-soluble gel base was chosen to be the base for this alcohol-based antiseptic gel. The concentrations used were 0.5%, 0.75%, 1%, 1.25%, 1.5%, 1.75%, and 2%. The physical test of the gel was carried out to see the optimum carbopol gel base for alcohol-based antiseptic gel. Physical test includes organoleptic observation, pH value, viscosity determination spreadability test and homogeneity test. The results obtained from organoleptic observation showed that the gel was clear, smelled antiseptic, two concentrations had a slightly sticky and sticky consistency. The pH value yields a pH range of 4.65 - 6.06. The viscosity results showed a viscosity range of 10.48725 - 21.18107 Pa.S. The Spreadability test shows the spreadability range of 6.07 - 7.03 cm. The homogeneity test resulted in an alcohol-based antiseptic gel without coarse particles. Hedonic organoleptic test produced the most preferred antiseptic gel was the antiseptic gel with a carbopol concentration of 1.25%. The results showed that the optimal carbopol was used as a gel base in an alcohol-based antiseptic gel 1.25% carbopol.

Development of Topical Nanoemulgel Using Combined Therapy for Treating Psoriasis.

This study focuses on the development of topical formulation of methoxsalen using Babchi oil as formulation component that can be applied at body surfaces providing sustained delivery and enhanced penetration of methoxsalen leading to significant epidermal localization and better anti-psoriatic activity. The combination of psoralens, that is, methoxsalen (synthetic) and Babchi oil (natural) has been developed into nanoemulgel formulations. A total of four nanoemulsion formulations was developed using Babchi oil as oil phase and Tween 80 as surfactant by high-pressure homogenization method. The prepared nanoemulsions were characterized for entrapment efficiency, mean droplet size, and zeta potential. Based on characterization results, the optimized nanoemulsion formulation(s) were incorporated into the carbopol gel base to make a nanoemulgel. The prepared nanoemulgel formulations were analyzed for pH, drug content determination, spreadability, viscosity, ex vivo skin permeation, and in vivo studies. The nanoemulsions showed droplet size between 51.3 and 146.7 nm, entrapment efficiency of 92.76%-98.10%, and zeta potential of -28.1 to -54.89 mev. The nanoemulsions showed varied in vitro drug release. In ex vivo skin permeation, nanoemulgel (NG2) showed increased penetration and localized accumulation of methoxsalen across the skin compared with plain gel. Ex vivo results were substantiated by in vivo results showing significant amelioration of hyperproliferative skin symptoms. The promising results suggested that nanoemulgel system is a suitable carrier for the topical delivery of methoxsalen-Babchi oil.

Development, Characterization, and Evaluation of α-Mangostin-Loaded Polymeric Nanoparticle Gel for Topical Therapy in Skin Cancer.

The aim of this study was to prepare and evaluate α-mangostin-loaded polymeric nanoparticle gel (α-MNG-PLGA) formulation to enhance α-mangostin delivery in an epidermal carcinoma. The poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) were developed using the emulsion–diffusion–evaporation technique with a 3-level 3-factor Box–Behnken design. The NPs were characterized and evaluated for particle size distribution, zeta potential (mV), drug release, and skin permeation. The formulated PLGA NPs were converted into a preformed carbopol gel base and were further evaluated for texture analysis, the cytotoxic effect of PLGA NPs against B16-F10 melanoma cells, and in vitro radical scavenging activity. The nanoscale particles were spherical, consistent, and average in size (168.06 ± 17.02 nm), with an entrapment efficiency (EE) of 84.26 ± 8.23% and a zeta potential of −25.3 ± 7.1 mV. Their drug release percentages in phosphate-buffered solution (PBS) at pH 7.4 and pH 6.5 were 87.07 ± 6.95% and 89.50 ± 9.50%, respectively. The release of α-MNG from NPs in vitro demonstrated that the biphasic release system, namely, immediate release in the initial phase, was accompanied by sustained drug release. The texture study of the developed α-MNG-PLGA NPs gel revealed its characteristics, including viscosity, hardness, consistency, and cohesiveness. The drug flux from α-MNG-PLGA NPs gel and α-MNG gel was 79.32 ± 7.91 and 16.88 ± 7.18 µg/cm2/h in 24 h, respectively. The confocal study showed that α-MNG-PLGA NPs penetrated up to 230.02 µm deep into the skin layer compared to 15.21 µm by dye solution. MTT assay and radical scavenging potential indicated that α-MNG-PLGA NPs gel had a significant cytotoxic effect and antioxidant effect compared to α-MNG gel (p < 0.05). Thus, using the developed α-MNG-PLGA in treating skin cancer could be a promising approach.

Composition of carbopol 940 and HPMC affects antibacterial activity of beluntas (Pluchea indica (L.)) leaves extract gel

Indonesia is a country known for its source of biological wealth, one of which is beluntas leaves. Beluntas leaves have the potential to be an antibacterial, so it is appropriate to be formulated in the form of medicinal preparations, especially gels. This study aims to find out the influence of variations between carbopol gel base 940 and Methylcellulose Hydroxypropyl (HPMC) on the physical properties of gel preparations beluntas leaf extract ( Pluchea indica (L.), and know the influence of gel of extract of beluntas leaves on antibacterial activity. The extract is obtained by the maceration method using ethanol solvent 96%. Each formula uses 15% of the extract of beluntas leaves. Gels are made in four gel base variations namely F0 (0.5% carbopol, 1% HPMC), FI (1% carbopol, 1.5% HPMC), FII (1.5% carbopol, 2.5% HPMC), and FIII (2% carbopol, 3% HPMC). Gels evaluated for their physical properties include organoleptic, viscosity, pH, homogeneity, scattering power, adhesion and Freeze-thaw cycling . Then the gel tested antibacterial activity against bacteria Staphylococcus aureus and Pseudomonas aeruginosa by cup-plate diffusion method . The data obtained were analyzed with One Way Anova and LSD with a 95% confidence level. The results showed that beluntas leaf extract gel meets the organoleptic requirements, homogeneity, good gel adhesion (&gt; 4sec), good gel viscosity (2000-50.000 cps), and good gel pH (4.5-6.5). However, the gel does not meet the requirements of good scattering power (5-7 cm) and Freeze-thaw cycling. Based on the test results that have been done with some of the parameters above, The best composition of carbopol 940 and HPMC in the beluntas leaf extract gel which has antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa is 1% carbopol and 1.5% HPMC. The antibacterial activity of the formula is categorized as strong.

Formulation and Evaluation of Hydrogels containing Liposomes Entrapped with Antifungal Agent

Background: The main aim of the present study was to formulate and evaluate prolonged release Fluconazole liposomal gel for the transdermal delivery. Fluconazole, α-(2.4-diflurofenil)-α-(1H-triazole-1-methyl)-1H-1, 2, 4-triazole-1-ethanol, is a class of antifungal of triazole. It shows the action against species of Candida sp., and it is specified in cases of or pharyngeal candidiasis, esophageal, vaginal, and deep infection. Materials and Method: Fluconazole liposomal gel was prepared by thin film hydration method using phosphatidyl choline and cholesterol. Liposomes were characterized for entrapment efficiency, particle size, and surface charge. Liposomes were then dispersed into a Carbopol gel base to form liposomal gel and evaluated for drug content, pH, spreadability, viscosity and in-vitro drug release. Results: The results indicated that concentration of cholesterol in the formulations affected the particle size and entrapment efficiency. When the concentration of cholesterol increased particle size was also increased but decrease in entrapment efficiency. The viscosity of Fluconazole liposomal gel decreases with increasing rate of shear. Hence it was showed that with non-Newtonian flow. In-vitro diffusion studies were carried out using cellophane membrane, results showed that liposomal gel formulation F1 (91.36%) showed highest cumulative percent of drug release and formulation F8 (76.98%) showed lowest cumulative percent of drug release. Conclusion: Therefore, Fluconazole liposomal gel sustained the drug release for the longer duration, hence decreases the number of application of drugs and also improves patient compliance.

Formulation and Evaluation of Clarithromycin Loaded Nanostructured Lipid Carriers for the Treatment of Acne

Background: Clarithromycin is a macrolide antibiotic used in acne treatment, but it has poor solubility, which decreases its permeability through lipid barriers such as skin. Nanostructured lipid carriers can enhance the permeability of clarithromycin through the skin, thus improving its potential for controlling acne.&#x0D; Aim: To formulate and evaluate Nanostructured lipid carriers of clarithromycin for topical delivery in acne treatment&#x0D; Methods: Nanostructured lipid carriers were prepared by emulsification and ultrasonication methods using lipids such as glycerol monostearate and oleic with poloxamer 188 as stabilizer. These nano-carriers were optimized with the help of the Quality by Design (QbD) approach employing Design-Expert® software. The nanoparticles were characterized for particle size analysis, zeta potential, drug-excipient compatibility, entrapment efficiency, and surface morphology by Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The nano-carriers were also investigated for in vitro drug release and ex vivo permeation through excised goat skin. The optimized formulation was incorporated into topical carbopol gel base, formulated and examined for pH, viscosity, spreadability, in vitro drug release, ex vivo permeation, and stability under accelerated conditions.&#x0D; Results: The average particle size of the optimized nanoparticles was 164.8 nm, and zeta potential was -39.2 mV. FTIR studies showed that drug and lipids are compatible with each other. The morphology study by SEM and TEM showed spherical shaped particles. The entrapment efficiency of the optimized formulation was found to be 88.16%. In vitro drug release studies indicated sustained release from the formulation due to diffusion through the lipid matrix of the particles. The ex vivo permeation study using goat skin produced greater permeation from the NLC gel (89.5%) than marketed gel (65%) due to the lipid solubility of the nanoparticles in the skin. The formulation was stable under accelerated conditions.&#x0D; Conclusion: The optimized formulation can be considered as promising nano-carriers suitable for the sustained release of clarithromycin into the skin for effective control of acne.

Development and Characterization of Apremilast Transethosomal Gel for Transdermal Delivery

The apremilast is anti-inflammatory drug and PDE-4 inhibitor, used in treatment of psoriasis. The oral route of apremilast has limitation of GI irritation and frequent dosage regimen.The objective of the present work was aimed to prepare transethosomal gel of apremilast to achieve more skin permeation, more drug entrapment efficiency and sustained release. The transethosome vesicle containing apremilast was prepared by using Rotary vacuum evaporator, followed by probe sonication. The Box-Behnken design was used to optimize the formulation by taking quantity of lipoid S 100, sodium cholate and ethanol as independent variable and vesicle size, entrapment efficiency and cumulative drug release as dependent variable. The optimized batch of transethosome vesicle was incorporated in 1 % of Carbopol gel base. The prepared optimized batch was evaluated for size, zeta potential, surface morphology, pH, viscosity, spreadability, extrudability, drug content and ex-vivo permeation studies. The result showed that optimized batch of transethosome was found to have vesicle size of 130.8 nm, entrapment efficiency of 62.83 % and cumulative drug release of gel 73.13 %. The transethosome vesicles were found to be spherical and uniform in size based on TEM analysis. The ex-vivo permeation studies were performed for 24 hrs through the rat skin. The formulation was found to show better skin permeation and sustained release. The formulation showed satisfactory result with respect to pH, gel characteristics and stability. Thus, can concluded that transethosomal gel containing apremilast could be an effective option for treatment of psoriasis.

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.

Eudragit RS100 based microsponges for dermal delivery of clobetasol propionate in psoriasis management

Clobetasol propionate (CP), a super potent dihalogenated topical corticosteroid for psoriasis, displays common side effects like allergic contact dermatitis, steroid acne, skin atrophy, hypo-pigmentation and systemic absorption, on topical application. Hence, entrapment of CP in an appropriate carrier system could minimise the aforementioned side effects, while controlling its percutaneous absorption. Therefore, motive behind current work was to fabricate and evaluate CP loaded microsponges (MS). The microsponges were successfully crafted by employing quasi-emulsion solvent diffusion method. For preparation of MS, organic phase comprising CP, Eudragit RS 100 and dichloromethane was added to aqueous phase (polyvinyl alcohol solution), while stirring. During optimization of MS formulations, factors (drug: polymer ratio, aqueous and organic phase volume) affecting the physical properties of microsponges were also investigated. The prepared microsponges were found to possess particle size in the range 12.2 ± 8.2–45.80 ± 12.3 μm, entrapment efficiency: 60.00 ± 0.06 to 96.37 ± 0.04 % and drug release: 60.60 ± 0.13 to 92.82 ± 0.15 %. Additionaly, CP loaded microsponges were evaluated for topography, thermal and photostability. Finally, optimized CPMS were incorporated into Carbopol gel base, which was subsequently evaluated. In vitro release of CPMS was compared with plain CP and release results were fitted into different kinetic models. CPMS formulation followed zero order kinetics indicating release of drug at constant rate, with absence of initial burst release. This delivery system resulted in extended CP release and its maximum therapeutic activity, with minimum toxic effects. In vivo antipsoriatic activity of CPMS gel performed using mouse tail model exhibited significant therapeutic efficacy in comparison to plain CP gel, which was further supported by the histopathological findings.

Antimicrobial and Wound Healing Potential of Dietary Flavonoid Naringenin

Background: Naringenin belongs to the class flavanones, and chemically it is known as 5,7-dihydroxy-2-(4-hydroxyphenyl) chroman-4-one. It is one of the dietary poly-phenolic constituents of the citrus fruits and vegetables. Naringenin possesses excellent antioxidant, antiinflammatory, and antimicrobial activities. These activities promote wound healing activity. Naringenin has been incorporated in the gel base to be applied on the wounded skin. The wound healing property of naringenin gel has not been studied extensively in the literature to date. &lt;/P&gt;&lt;P&gt; Objective: The present study aims to unveil the wound healing property of naringenin gel formulation on excision and incision model. &lt;/P&gt;&lt;P&gt; Materials and Methods: 0.5% and 1% naringenin was incorporated in a carbopol gel base formulation and evaluated for physicochemical parameters. Incision and excision wound models were used to study wound contraction, tensile strength, healing index, the period of epithelization and histopathological parameters. Antimicrobial activity was performed using agar plate method. Results: Naringenin (0.5% and 1%) treatment shows a significant increase in the percentage of wound contraction, good healing index and shorter epithelization period. Histopathology of naringenin gel treated wound tissue showed more fibroblasts, less macrophage infiltration, and wellformed collagen fibers as compared to control. In incision wound model, the animals were treated with 0.5% and 1% naringenin gel for nine days and showed a significant increase in the tensile strength. Naringenin exerts antimicrobial activity against fungus and E. coli. Conclusion: The present study explored potent wound healing activity of naringenin gels.