Enhanced oral bioavailability of valsartan using a polymer-based supersaturable selfmicroemulsifying drug delivery system
- Authors
- Yeom, Dong Woo; Chae, Bo Ram; Son, Ho Yong; Kim, Jin Han; Chae, Jun Soo; Song, Seh Hyon; Oh, Dongho; Choi, Young Wook
- Issue Date
- May-2017
- Publisher
- DOVE MEDICAL PRESS LTD
- Keywords
- valsartan; SMEDDS; supersaturation; factorial design; optimization; bioavailability
- Citation
- INTERNATIONAL JOURNAL OF NANOMEDICINE, v.12, pp 3533 - 3545
- Pages
- 13
- Journal Title
- INTERNATIONAL JOURNAL OF NANOMEDICINE
- Volume
- 12
- Start Page
- 3533
- End Page
- 3545
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/6224
- DOI
- 10.2147/IJN.S136599
- ISSN
- 1178-2013
1178-2013
- 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 (R) MCM, 45% Tween (R) 20, and 45% Transcutol (R) 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 suspension. Thus, we concluded that, in terms of developing an effective SMEDDS preparation with minimal total quantity, S-SMEDDS_RQ is a promising candidate.
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