Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin.

Huiyi WU; Xiaoying Long; Fei Yuan; Li Chen; Sujing Pan; Yunjun Liu; Yoshiko Stowell; Xiaoling LI

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Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin.

Author: Huiyi WU ¹ ; Xiaoying LONG ¹ ; Fei YUAN ¹ ; Li CHEN ¹ ; Sujing PAN ¹ ; Yunjun LIU ¹ ; Yoshiko STOWELL ² ; Xiaoling LI ²
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1. School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, China.
2. Department of Pharmaceutics, Thomas J Long School of Pharmacy & Health Sciences, University of the Pacific, CA 95211, USA.
Publication Type:Journal Article
Keywords: Baicalin; Bioavailability; Caco-2 cell; Phospholipid complex; SMEDDS; Single-pass intestinal perfusion
From: Acta Pharmaceutica Sinica B 2014;4(3):217-226
CountryChina
Language:English
Abstract: The aim of this study was to develop a formulation to improve the oral absorption of baicalin (BA) by combining a phospholipid complex (PC) and self-emulsifying microemulsion drug delivery system (SMEDDS), termed BA-PC-SMEDDS. BA-PC was prepared by a solvent evaporation method and evaluated by complexation percentage (CP). The physicochemical properties of BA-PC were determined. The synergistic effect of PC and SMEDDS on permeation of BA was studied in vitro with Caco-2 cells and in situ with a single pass intestinal perfusion model. The improved bioavailability of BA in BA-PC-SMEDDS was confirmed in an in vivo rat model. The CP of BA-PC reached 100% when the molar ratio of drug to phospholipid (PP) was ≥1:1. The solubility of BA-PC increased in both water and octanol, and the log P o/w of BA-PC was increased significantly. BA-PC-SMEDDS could be dispersed more evenly in water, compared to BA and BA-PC. Both the Caco-2 cell uptake and single-pass intestinal perfusion models illustrated that transport of BA in BA-PC was lower than that of free BA, while improved significantly in BA-PC-SMEDDS. The relative bioavailability of BA-PC(1:2)-SMEDDS was 220.37%. The combination system of PC and SMEDDS had a synergistic effect on improving the oral absorption of BA.