Design and development of a self-microemulsifying drug delivery system of Olmesartan Medoxomil for enhanced bioavailability.

Design and development of a self-microemulsifying drug delivery system of Olmesartan Medoxomil for enhanced bioavailability. Drug Dev Ind Pharm. 2019 Apr 15;:1-40 Authors: Komesli Y, Ozkaya AB, Ergur BU, Kirilmaz L, Karasulu E Abstract Olmesartan Medoxomil (OM) is a hydrophobic antihypertensive drug with low bioavailability (26%) and is known to have adverse effects such as celiac disease and enteropathy. The purpose of this study was to develop SMEDDS to increase bioavailability and decrease potential side effects of OM. Hydrophilic lipophilic balance was calculated by testing solubility of OM in different oils, surfactants and cosurfactants to obtain the most suitable combination of SMEDDS. Pseudoternary phase diagram was used to select the better oil/water formulation of SMEDDS. After a test for 3-month stability, dissolution tests and Parallel Artificial Membrane Permeability Assay (PAMPA) were conducted to investigate drug solubility and permeability. Biodistribution of fluorescent marked SMEDDS was observed by using In Vivo Imaging System. The pharmacodynamics of the drug were determined by measuring blood pressure from tails of rats. At the end of the experiment, intestines were examined for adverse effects of OM. Compared with tablet formulation according to the dissolution study, SMEDDS formulation showed 1.67 times improvement in solubility of OM. PAMPA studies suggested a much faster permeability rate for OM SMEDDS compare...
Source: Drug Development and Industrial Pharmacy - Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research