Formulation and evaluation of embelin loaded nanoliposomes: Optimization, in vitro and ex vivo evaluation

Abstract

The present research work designed to prepare and optimize Embelin (EMB) loaded liposomes. The liposomes were prepared by solvent evaporation method and optimized using 3-factors at 3- levels Box-Behnken design (Design-Expert software., Version 12, Stat-Ease, USA). The effect of independent variables was taken as Leciva-S70 (X1), cholesterol (X2), sonication time (X3) and their individual as well combined effects were observed on vesicle size (Y1), entrapment efficiency (Y2), and in-vitro release (Y3). The optimized formulation (EMB-NLop) was further characterized for drug release, DPPH assay, confocal laser scanning microscopy (CLSM), and ex-vivo permeation study. EMB-NLop depicted the vesicle size of 70.36 nm, PDI (0.11), entrapment efficiency of 78.22 ± 0.93% and drug release of 86.41 ± 3.34%. A better antioxidant activity of 89.27% was found as compared to standard ascorbic acid. Ex-vivo permeation studies showed significantly enhanced permeation from EMB-NLop (75.02 ± 2.05%) than EMB suspension (34.56 ± 1.73%). Further, the CLSM image of the nasal mucosa suggested rhodamine B loaded EMB-NLop showed better penetration as compared to control (rhodamine B- solution). From all experimental data, it was concluded that EMB-NLop is a promising and effective formulation for intranasal delivery.