Tailoring and Evaluation of Berberine Loaded Transethosomal Gel for Effective Transdermal Delivery: Optimization, Characterization, and in vitro Evaluation.

Berberine is an isoquinolone alkaloid present in a wide variety of plants. Other than Type 2 diabetes and hypertension it is also found to have an effect in lowering blood cholesterol levels. However, because of its poor oral bioavailability and substantial first pass hepatic metabolism it is consumed in higher dosage leading to side effects. To reduce dosage and avoid adverse effects, transdermal delivery is investigated using transethosomal gel as a carrier. Transethosomes are ethanolic nanocarriers that are specifically designed for the dermal or transdermal delivery route as it has enhanced permeation of the vesicles. In our study we have successfully investigated the potential use of berberine loaded transethosomal gel (BBR-TE) as a carrier for transdermal delivery. Three-level three-factorial Box Behnken Design was used to optimize BBR-TE (Opt-BBR-TE). The optimized formulation was further evaluated and found to have a particle size of 165.70 nm with entrapment efficiency of 79.60±4.07%. The in vitro drug release study suggested the non-Fickian transport mechanism. The ex vivo skin permeation was found to be 94.35±3.64% when compared to berberine conventional formulation. Berberine has also shown promising antioxidant activity when compared to the standard solution and was entrapped inside TE vesicles in non-crystalline form. The Opt-BBR-TE was converted into gel form. Various parameters of the gel such as pH, Drug Content, Spreadability and extrudability were found to have promising results. Present study data revealed that the developed transethosomal gel formulation was found to be a potentially useful drug carrier for transdermal delivery of berberine. [ABSTRACT FROM AUTHOR]