| Autor: |
Amin MM; a Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy , Cairo University , Cairo , Egypt., El Gazayerly ON; a Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy , Cairo University , Cairo , Egypt., Abd El-Gawad NA; b Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy , October 6 University , Sixth of October City , Egypt , and., Abd El-Halim SM; b Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy , October 6 University , Sixth of October City , Egypt , and., El-Awdan SA; c Department of Pharmacology , National Research Center , Cairo , Egypt. |
| Abstrakt: |
Valsartan is a specific angiotensin II antagonist used for the treatment of hypertension. It suffers from low aqueous solubility and high variability in its absorption after oral administration. The aim of this study was to improve the dissolution and thereby the bioavailability of Valsartan through the development of self nano-emulsifying drug delivery systems. Four ternary phase diagrams were constructed to identify the self-emulsification region of Capmul® MCM, Labrafil® M1944, Capryol™ 90 and Labrafac® PG together with Cremophore® RH 40 and Transcutol™ HP as oil, surfactant and co-surfactant, respectively. The effect of oil type, oil and surfactant concentration on droplet size and in vitro Valsartan dissolution were studied. The protective effect of the optimum formula F5 in adrenaline-induced oxidative stress in rats during myocardial infarction was determined. Formula F5 exhibited globule size of (13.95 nm) with 76.07% ± 1.10 of Valsartan dissolved after five minutes compared to Disartan 80 mg capsules (13.43%). Results revealed a significant reduction (p < 0.05) in serum aspartate transaminase, creatine kinase myocardial band and malondialdehyde levels, while a significant increase (p < 0.05) in serum glutathione in F5. Therefore, self nano-emulsifying drug delivery systems could be considered as a promising approach to improve the dissolution and thereby the bioavailability of Valsartan. |
