Characterization of herpetrione amorphous nanoparticles stabilized by hydroxypropylmethyl cellulose and its absorption mechanism in vitro.

Autor: Wang F; Department of Pharmacy, Air Force Medical Center, Air Force Medical University, Beijing 100142, China; School of Medicine, Huaqiao University, Quanzhou 362021, China., Hang L; Department of Pharmacy, Air Force Medical Center, Air Force Medical University, Beijing 100142, China., Dai B; Department of Pharmacy, Air Force Medical Center, Air Force Medical University, Beijing 100142, China., Li F; Department of Pharmacy, Air Force Medical Center, Air Force Medical University, Beijing 100142, China., Zhu Y; Department of Pharmacy, Air Force Medical Center, Air Force Medical University, Beijing 100142, China., Jia H; Department of Pharmacy, Air Force Medical Center, Air Force Medical University, Beijing 100142, China; School of Medicine, Huaqiao University, Quanzhou 362021, China., Ai Y; Bohai (Tianjin) Medical Laboratory, Tianjin 300400, China., Wang L; School of Medicine, Huaqiao University, Quanzhou 362021, China. Electronic address: wlq1599@163.com., Xue Y; Department of Pharmacy, Air Force Medical Center, Air Force Medical University, Beijing 100142, China. Electronic address: 1585414032@qq.com., Yuan H; Department of Pharmacy, Air Force Medical Center, Air Force Medical University, Beijing 100142, China. Electronic address: yhlpharm@126.com.
Jazyk: angličtina
Zdroj: International journal of biological macromolecules [Int J Biol Macromol] 2024 May; Vol. 268 (Pt 1), pp. 131744. Date of Electronic Publication: 2024 Apr 23.
DOI: 10.1016/j.ijbiomac.2024.131744
Abstrakt: Herpetrione(HPE) is an effective compound that has been used in the treatment of liver diseases. To improve its dissolution and absorption, herpetrione nanosuspensions was prepared. Nanosuspensions were proved to achieve intact absorption in vivo. However, the transport mechanisms are not fully understood, especially lack of direct evidence of translocation of particulates. In this study, an environment-responsive dye, P4, was loaded into herpetrione amorphous nanoparticles (HPE-ANPs) to elucidate the absorption and transport mechanism of the nanoparticles. And the amount of HPE and nanoparticles in the samples were quantified using HPLC/LC-MS/MS and IVIS with the model of Caco-2 and Caco-2/HT29-MTX. Results demonstrated that HPE is mainly taken up by passive diffusion in the form of free drugs, while HPE-ANPs are internalized by an energy dependent active transport pathway or intracellular endocytosis. It is speculated that HPE-ANPs may change the original entry pathway of drug molecules. Furthermore, the presence of mucus layer and the use of HPMC E15 may contribute to drug absorption to some extent. Transcellular transport study indicates that HPE-ANPs has a poor absorption. In conclusion, the differences in the absorption behavior trends of HPE-ANPs are caused by the difference in particle properties and the form of existence of the drug.
Competing Interests: Declaration of competing interest 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.
(Copyright © 2024 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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