Prototype Self Emulsifying System of Etravirine: Design, Formulation and in Vitro Evaluation

Abstract

Objective: Lipid-based formulations have gained much attention, particularly on self-emulsifying drug delivery systems (SEDDS), to improve the oral bioavailability of lipophilic drugs. In the present study, an attempt was made to develop and evaluate prototype SEDDS of poorly soluble antiviral BCS class IV drug etravirine.Methods: Various oils, surfactants and co-surfactants were screened for their suitability in the formulation of SEDDS. Based on the screening, gelucire 44/14, as the oil, labrasol as a surfactant and transcutol HP as the co-surfactant were selected. SEDDS with drug etravirine was formulated and evaluated for emulsifying ability, dilution potential and microscopic properties. The emulsion area for each of the combination of oil and surfactant co-surfactant mixture (Smix) was determined by the construction of pseudo-ternary phase diagrams.Results: The optimized formulation with oil (gelucire 44/14) and Smix (labrasol: transcutol HP, 6:1) in a ratio of 2:8 exhibited a rapid emulsification rate and a good polydispersibility index of 0.103±0.012 indicating uniformity of the formed droplets. The size of the droplets was determined by zetasizer and was found to be in 200 nm range. The drug release from the final formulation after 2hr was found to be 41.15%±0.5 compared to 19.3%±3.8 of pure drug indicating enhanced dissolution profile of the drug.Conclusion: In vitro study illustrated enhanced dissolution rate of formulated prototype SEDDS of BCS class IV drug etravirine for oral delivery.

Quality by Design Based Development of Etravirine Self Micro Emulsifying Drug Delivery System

“…Although several works have reported the formulation of ETV SEDDS by OFAT approach either to enhance bioavailability or to attain other formulation goals [20]. A rigorous development of ETV-SMEDDS by QbD approach was not present.…”

Design and Characterization of Nanospray With Self-Nanoemulsifying Drug Delivery System Using Sinergistic Combination of Melastoma Malabathricum L. Fraction and Gentamicin

“…These preparations increased the penetration of the drug into the skin, and because of their lipid properties, the drug penetrated into the skin layers and kept it for a long time, allowing the drug to be targeted on the skin. Another study of the SNEDDS, using the active compound etravirine (BCS class IV) using labrasol oil: transcutol HP, 6: 1 with a ratio of 2:8, showed the test results meeting the requirements, and in vitro studies illustrated an increase in the dissolution rate [66].…”

A Systematic Review on Self-Micro Emulsifying Drug Delivery Systems: A Potential Strategy for Drugs With Poor Oral Bioavailability

“…The purpose of level-A is to achieve candidate systems for further screening and evaluation. This begins with the choice of prominent excipients and blends [61,62]. Usually, excipients possess diverse functionalities in blends e. g. being an oil, surfactant, co-surfactant or the additive can be a solvent.…”