Preparation and Optimization of Amorphous Ursodeoxycholic Acid Nano-suspensions by Nanoprecipitation based on Acid-base Neutralization for Enhanced Dissolution

Author(s): Yike Xie, Zhongjian Chen, Rui Su, Ye Li, Jianping Qi, Wei Wu, Yi Lu*.

Journal Name: Current Drug Delivery

Volume 14 , Issue 4 , 2017

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Abstract:

Background: Ursodeoxycholic acid, usually used to dissolve cholesterol gallstones in clinic, is a typical hydrophobic drug with poor oral bioavailability due to dissolution rate-limited performance. The objective of this study was to increase the dissolution of ursodeoxycholic acid by amorphous nanosuspensions.

Methods: Nanoprecipitation based on acid-base neutralization was used to prepare the nanosuspensions with central composite design to optimize the formula. The nanosuspensions were characterized by particle size, morphology, crystallology and dissolution.

Results: The ursodeoxycholic acid nanosuspensions showed mean particle size around 380 nm with polydispersion index value about 0.25. Scanning electron microscope observed high coverage of HPMC-E50 onto the surface of the nanosuspensions. Differential scanning calorimetry and powder X-ray diffractometry revealed amorphous structure of the ursodeoxycholic acid nanosuspensions. A significant increase of dissolution in acidic media was achieved by the amorphous nanosuspensions compared with the physical mixture.

Conclusion: It can be predicted that the amorphous nanosuspensions show great potential in improving the oral bioavailability of ursodeoxycholic acid.

Keywords: Acid-base neutralization, amorphous, dissolution, nanosuspensions, oral bioavailability, ursodeoxycholic acid.

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Article Details

VOLUME: 14
ISSUE: 4
Year: 2017
Page: [483 - 491]
Pages: 9
DOI: 10.2174/1567201813666160902152122
Price: $58

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