Preparation and pharmacokinetics in vivo of linarin solid dispersion and liposome

Yingying Huang; Lihua Xu; Fangping Zhang; Yang Liu; Yunyu Wang; Fangfeng Meng; Shuang Li; Xintao Cheng; Yuefeng Bi

doi:10.1016/j.chmed.2021.12.004

Preparation and pharmacokinetics in vivo of linarin solid dispersion and liposome

Chin Herb Med. 2022 Apr 2;14(2):310-316. doi: 10.1016/j.chmed.2021.12.004. eCollection 2022 Apr.

Authors

Yingying Huang¹, Lihua Xu¹, Fangping Zhang¹, Yang Liu^{1

2}, Yunyu Wang¹, Fangfeng Meng¹, Shuang Li¹, Xintao Cheng¹, Yuefeng Bi^{1

2}

Affiliations

¹ School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
² Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou 450001, China.

Abstract

Objective: The current investigation aimed to determine the appropriate dosage form by comparing solid dispersion and liposome to achieve the purpose of improving the solubility and bioavailability of linarin.

Methods: Linarin solid dispersion (LSD) and linarin liposome (LL) were developed via the solvent method and the thin film hydration method respectively. The Transwell chamber model of Caco-2 cells was established to evaluate the absorption of drug. The pharmacokinetics of linarin, LSD and LL in rats after ig administration were carried out by high performance liquid chromatography (HPLC) method.

Results: The solubility of LSD and LL was severally 3.29 times and 3.09 times than that of linarin. The permeation coefficients of LSD and LL were greater than 10^-6, indicating that the absorption of LSD and LL were both better than linarin. The bioavailability of the LSD was 3.363 times higher than that of linarin, and the bioavailability of LL was 0.9886 times higher than that of linarin.

Conclusion: The linarin was more suitable for making solid dispersion to enhance its solubility and bioavailability.

Keywords: bioavailabilit; intestinal absorption; linarin; liposome; pharmacokinetics; solid dispersion.