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

Preparation and pharmacokinetics in vivo of linarin solid dispersion and liposome

Yingying Huang  1 , Lihua Xu  1 , Fangping Zhang  1 , Yang Liu  1   2 , Yunyu Wang  1 , Fangfeng Meng  1 , Shuang Li  1 , Xintao Cheng  1 , Yuefeng Bi  1   2
Affiliations

Preparation and pharmacokinetics in vivo of linarin solid dispersion and liposome

Yingying Huang et al. Chin Herb Med. .

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.

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Conflict of interest statement

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Figures

Fig. 1
Fig. 1
Chemical structure of linarin.
Fig. 2
Fig. 2
A: DSC diagram of linarin (a), PVPK30 (b), physical mixture (c) and LSD (d); B: FTIR map of linarin (a), PVPK30 (b), physical mixture (c) and LSD(d); C: Transmission electron micrograph of PVPK30 (a), linarin (b), physical mixture (c) and LSD (d); D: X-ray diffractograms (PXRD) of linarin (a), PVPK30 (b), physical mixture (c) and LSD (d).
Fig. 3
Fig. 3
Dissolution of linarin, LSD and physical mixture.
Fig. 4
Fig. 4
Transmission electron micrograph of LL.
Fig. 5
Fig. 5
Particle size (A) and electric potential (B) distribution of LL.
Fig. 6
Fig. 6
Caco-2 cell transport experiment of linarin, LSD and LL. AP-BL side transshipment of LSD-LL-linarin (A); BL-AP side transshipment of LSD-LL-linarin (B).
Fig. 7
Fig. 7
Plasma drug concentration–time curve of linarin, LSD and LL after ig administration in rats (mean ± SD, n = 6).
Fig. 8
Fig. 8
Method specificity (A: blank plasma; B: blank plasma with linarin; C: 2 h plasma sample of rat; a: linarin).
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