Self-microemulsifying drug delivery system for improved oral bioavailability of dipyridamole: Preparation and evaluation |
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Authors: | Feng Guo Haijun Zhong Jing He Baogang Xie Fen Liu Helin Xu Minmin Liu Chunlian Xu |
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Institution: | (1) Dabur Research Foundation, Plot No. 22 Site IV, Sahibabad, 201010, Ghaziabad Uttar Pradesh, India;(2) Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), 110062 New Delhi, India;(3) Department of Dermatology, All India Institute of Medical Sciences, 110029 New Delhi, India;(4) ARA Healthcare Pvt Ltd., Plot No. 10 Electronic City, Sector 18, 122015 Gurgaon, Haryana, India |
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Abstract: | Dipyridamole shows poor and variable bioavailability after oral administration due to pHdependent solubility, low biomembrane
permeability as well as being a substrate of P-glycoprotein. In order to improve the oral absorption of dipyridamole, a self-microemulsifying
drug delivery system (SMEDDS) for dipyridamole was prepared and evaluated in vitro and in vivo. The optimum formulation was 18% oleic acid, 12% Labrafac lipophile WL 1349, 42% Solutol HS 15 and 28% isopropyl alcohol.
It was found that the performance of self-microemulsification with the combination of oleic acid and Labrafac lipophile WL
1349 increased compared with just one oil. The results obtained from an in vitro dissolution assay indicated that dipyridamole in SMEDDS dissolved rapidly and completely in pH 6.8 aqueous media, while the
commercial drug tablet was less soluble. An oral bioavailability study in rats showed that dipyridamole in the SMEDDS formulation
had a 2.06-fold increased absorption compared with the simple drug suspension. It was evident that SMEDDS may be an effective
approach to improve the oral absorption for drugs having pH-dependent solubility. |
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