Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

International Journal of Nanomedicine
Dong Woo YeomYoung Wook Choi

Abstract

A novel, supersaturable self-microemulsifying drug delivery system (S-SMEDDS) was successfully formulated to enhance the dissolution and oral absorption of valsartan (VST), a poorly water-soluble drug, while reducing the total quantity for administration. Poloxamer 407 is a selectable, supersaturating agent for VST-containing SMEDDS composed of 10% Capmul(®) MCM, 45% Tween(®) 20, and 45% Transcutol(®) P. The amounts of SMEDDS and Poloxamer 407 were chosen as formulation variables for a 3-level factorial design. Further optimization was established by weighting different levels of importance on response variables for dissolution and total quantity, resulting in an optimal S-SMEDDS in large quantity (S-SMEDDS_LQ; 352 mg in total) and S-SMEDDS in reduced quantity (S-SMEDDS_RQ; 144.6 mg in total). Good agreement was observed between predicted and experimental values for response variables. Consequently, compared with VST powder or suspension and SMEDDS, both S-SMEDDS_LQ and S-SMEDDS_RQ showed excellent in vitro dissolution and in vivo oral bioavailability in rats. The magnitude of dissolution and absorption-enhancing capacities using quantity-based comparisons was in the order S-SMEDDS_RQ > S-SMEDDS_LQ > SMEDDS > VST powder or susp...Continue Reading

Citations

Jun 20, 2019·Recent Patents on Nanotechnology·Dilpreet SinghNeena Bedi
Apr 30, 2020·International Journal of Nanomedicine·Heshu Sulaiman RahmanNoorjahan Banu Alitheen
Oct 10, 2020·Pharmaceutical Development and Technology·Sun Young ParkYoung Wook Choi
Jul 10, 2020·Pharmaceutical Nanotechnology·Adella AparnaDarna V R N Bhikshapathi

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