الفهرس | Only 14 pages are availabe for public view |
Abstract The objective of this study was to formulate and evaluate Valsartan (VLT) ethosomes in order to prepare an optimized formula of VLT-entrapped ethosomes that could be incorporated into a sustained release transdermal gel dosage form. The formulation of the prepared ethosomal gel was investigated and subjected to in vitro drug release studies, ex-vivo test and in vivo studies to assess the effectiveness of ethosomal formulation in enhancing the availability and bioavailability of VLT as a poorly soluble drug and in controlling its release from the transdermal gel dosage form. The acquired results are as follows: 1- As dependent responses, particle size, polydispersity index, zeta potential, and entrapment efficiency. The optimized VLT-ETHs had a nanometric diameter (45.8 ± 0.5nm), a negative surface charge (-51.4 ± 6.3mV), and a high drug encapsulation (94.24 ± 0.2). 2- The permeation of VLT from all the prepared ethosomal formulations and VLT-ethogel preparation followed Higuchi’s diffusion model. 3- VLT-ethogel preparation showed very good gel evaluation, the best in-vitro drug permeation, and good ex-vivo permeation of drug. 4- The prepared VLT ethosomal gel (VLT-ethogel) showed a high peak plasma concentration and enhanced bioavailability in rats compared with oral solution of valsartan presented in the higher AUC (0-∞). The AUC (0–∞) with oral treatment was 7.0 ± 2.94 (μg.h/ml), but the AUC (0–∞) with topical application of the VAL nanoethosomal gel was 137.2 ± 49.88 (μg.h/ml), provides the sustained release pattern of VLT from the tested ethosomal gel. So, ethosomes were shown to be effective as a VLT carrier for topical formulation and application |