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Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations

Authors Jin X, Zhang Z, Sun, Qian, Tan, Jia X

Received 14 July 2012

Accepted for publication 17 August 2012

Published 13 September 2012 Volume 2012:7 Pages 4907—4916

DOI https://doi.org/10.2147/IJN.S35965

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 2


Xin Jin,1,2 Zhen-hai Zhang,1 E Sun,1 Qian Qian,1 Xiao-bin Tan,1 Xiao-bin Jia1

1Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, 2College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, People's Republic of China

Background: Baohuoside I is a potential anticancer drug for a variety of malignancies and has been approved for in vitro use. However, baohuoside I has very poor oral absorption.
Methods: In the present study, we prepared baohuoside I-phospholipid complexes of different diameters and determined their physicochemical properties using transmission electron microscopy, ultraviolet spectroscopy, and differential scanning calorimetry. The in vitro absorption of baohuoside I and baohuoside I-phospholipid complexes of different sizes were compared using the Caco-2 cell culture model, and subsequently, the bioavailability of baohuosidel and its complexes were estimated in vivo.
Results: Compared with the large-sized phospholipid complexes, a nanoscale phospholipid complex improved the oral bioavailability of baohuoside I. In addition, our results suggest that the smaller the particle size, the faster the complexes crossed the Caco-2 monolayer and the faster they were resorbed after oral administration in rats. The relative oral bioavailability of a nanoscale size 81 ± 10 nm baohuoside I-phospholipid complex (area under the concentration-time curve [AUC] 0–∞)was 342%, while that of baohuoside I and a 227.3 ± 65.2 µm baohuoside I-phospholipid complex was 165%.
Conclusion: We enhanced the oral bioavailability of baohuoside I by reducing the particle size of the phospholipid complex to the nanometer range, thereby improving its potential for clinical application.

Keywords: nanoscale phospholipid complex, Caco-2 cell monolayer, bioavailability, oral absorption

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