Screening of process variables using Box-Behnken design in the fabrication of Berberine-hydrochloride loaded transethosomes for enhanced transdermal delivery:TJPS-2021-0201.R1

The objective of the present work was to develop, optimize and characterize berberine hydrochloride loaded transethosomes. In this study, screening of formulation and process variables was conducted by using Box-Behnken design approach to observe significant and insignificant influence on the transethosomes. The transethosomes was developed by homogenization technique (hot method). The optimized berberine hydrochloride loaded transethosomes were evaluated for its vesicle size, polydispersity index, zeta potential, loading capacity and entrapment efficiency. Characterization was done by P-XRD, DSC and TEM. Further, in-vitro drug release study and stability study was also performed. The berberine hydrochloride loaded transethosomes are developed by using soya lecithin as phospholipid, oleic acid as edge activator and cholesterol as stabilizer. Developed transethosomes showed acceptable desired vesicle size (185-435 nm), excellent colloidal dispersion characteristics (polydispersity index- 0.141 to 0.321, z.p -17.34 to -24.35 mV) and high drug entrapment (67.05-85.21%). P-XRD and DSC results suggested that berberine hydrochloride encapsulated in amorphous state within transethosomes. In-vitro release study show prolonged release of drug for 24 hr. Results of stability studies showed transethosomes are more stable in refrigerated temperature. The results suggested that transethosomes could be better alternative to deliver drugs across the skin and potential carrier for efficient transdermal drug delivery.