Design, Formulation, and Evaluation of Aloe vera Gel-Based Capsaicin Transemulgel for Osteoarthritis.

Topical treatments are a potential therapeutic option for the therapy of osteoarthritis, with significant data supporting the effectiveness and safety of topical formulation. Topical gel formulations may offer an alternative to oral formulations to relieve osteoarthritis (OA) pain while decreasing systemic exposure. Topical capsaicin transemulgel may represent an effective and safe alternative. The transemulgel was prepared from aqueous Aloe vera gel and Carbopol 934 with capsaicin in clove oil emulsion. The optimized transemulgel of capsaicin showed a pH of 6.1 ± 0.1 and viscosity of 15263-998 cps. Data from in vitro diffusion demonstrated improved permeability properties. The formulation caused no skin irritation when applied topically. The optimal transemulgel spreadability was found to be 20.23 g·cm/s. In vitro and ex vivo studies of the optimized formulation were performed. The skin irritant test was performed on rat skin with an optimized and marketed formulation. Both showed no irritation on the skin. The transemulgel of the capsaicin with Aloe vera gel was proven to be effective for osteoarthritis therapy.

Development and evaluation of the effect of ethanol and surfactant in vesicular carriers on Lamivudine permeation through the skin.

The skin embodies a relatively large and readily accessible surface area to absorb a drug through a non-invasive procedure. The vesicular carrier systems such as liposomes, ethosomes, and transethosomes have been explored as non-invasive systems for transdermal delivery of drugs. In the present study, different vesicular carriers were prepared by the thin-film hydration method with modification, and various parameters like size, elasticity, and release profiles were evaluated. Ethosomes and transethosomes have shown the smaller size of 362.21 ± 55.76 and 314.34 ± 41.21 nm, with deformity of 19.34% and 25.04%, respectively, compared with liposomes. The FTIR study of the skin before and after the application of vesicular formulation was performed. The ethosomes and transethosomes changed the orthorhombic phase to the liquid crystalline phase to move the vesicular carrier with the drug to cross the stratum corneum (SC) of the skin. The thermotropic behaviour of drug and vesicular carrier ingredients was studied using differential scanning calorimetry (DSC). Fluorescence images of vesicular-skin permeation have revealed that ethosome and transethosome formulation have shown deeper penetration across the SC and epidermis. The in vitro drug release from the ethosomes and transethosomes has shown 93.34 ± 1.23% and 95.45 ± 2.67% of drug release using Franz diffusion cell and porcine skin as a membrane. The nanostructured flexible vesicular carrier containing ethanol alone and a combination of ethanol and edge activator is a perfect carrier for drug penetration to the deeper skin layer and maintaining the sustained release of drug for a prolonged time.

Microemulsion Based Gel of Sulconazole Nitrate for Topical Application.

OBJECTIVES: Sulconazole is a broad spectrum antifungal agent of the imidazole class used against dermatophytes and other fungi to treat skin infections. The aim of the present work was to formulate and evaluate a microemulsion-based topical sulconazole gel. MATERIALS AND METHODS: Microemulsion formulation of sulconazole nitrate was prepared by using oil, surfactant, cosurfactant and water at different ratios. This was then subjected to clarity and particle size analysis, a centrifugation test, a dilution test, and freeze thawing. RESULTS: The zeta potential of formulation F1 was -41.3 and stable. The pH of the microemulsion formulation was within the range of pH of skin. F1 showed a higher percentage amount of drug as compared with the other formulations. The viscosity showed that F1 was optimum. The freezing and thawing results showed there was no phase separation and the formulation was stable. In vitro drug release showed that the drug release from the microemulsion of F1 was higher when compared to the other formulations. It revealed F1 had the highest drug content of 95.88±0.3% and % cumulative drug release was 88.75% release in 8 h. The in vivo skin irritation study on rats confirmed that formulation was nontoxic and nonirritant. CONCLUSION: The present study confirmed the safety of the formulated sulconazole loaded microemulsion gel for topical application.