Computer-based formulation design and optimization using Hansen Solubility Parameters to enhance the delivery of ibuprofen through the skin

Publication date: Available online 5 August 2019Source: International Journal of PharmaceuticsAuthor(s): Bshaer M. Jameel, An Huynh, Aastha Chadha, Sujata Pandey, Jacalyn Duncan, Mark Chandler, Gabriella BakiAbstractTrial-and-error approach to formulation development is long and costly. With growing time and cost pressures in the pharmaceutical industry, the need for computer-based formulation design is greater than ever. In this project, emulgels were designed and optimized using Formulating for EfficacyTM (FFE) for the topical delivery of ibuprofen. FFE helped select penetration enhancers, design and optimize emulgels and simulate skin penetration studies. pH, viscosity, spreadability, droplet size and stability of emulgels were evaluated. Franz cell studies were performed to test in vitro drug release on regenerated cellulose membrane, drug permeation in vitro on Strat-M® membrane and ex vivo on porcine ear skin, a marketed ibuprofen gel served as control. Emulgels had skin compatible pH, viscosity and spreadability comparable to a marketed emulgel, were opaque and stable at 25°C for 6 months. Oleyl alcohol (OA), combined with either dimethyl isosorbide (DMI) or diethylene glycol monoethyl ether (DGME) provided the highest permeation in 24 hours in vitro, which was significantly higher than the marketed product (p<0.01). OA+DGME significantly outperformed OA ex vivo (p<0.05). The computer predictions, in vitro and ex vivo p...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research