PROTOTYPE SELF EMULSIFYING SYSTEM OF ETRAVIRINE: DESIGN, FORMULATION AND IN VITRO EVALUATION


G. B. Preethi, H. N. Shivakumar, M Ravi Kumar, N Sweta

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 surfactant and Transcutol HP as the co-surfactant were selected. SEDDS with drug etravirine was formulated and evaluated for emulsifying ability, dilution potential and were found to be satisfactory. The emulsion area for each of the combination of Oil and Smix was determined by the construction of pseudo ternary phase diagrams.

Results Based on the studies, Oil(Gelucire 44/14) and Smix(Labrasol:Transcutol HP, 6:1) in a ratio of 2:8 was selected and evaluated for parameters like drug content, percentage transmittance, dilution potential, emulsification time and was found to be optimized formulation. The optimized formulation 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 percentage drug release from the final formulation was improved compared to that of pure drug indicating good solubilization of the drug.

 


Keywords


Etravirine, Self emulsifying system, Gelucire44/14, BCS class IV, Antiretroviral

References


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