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用于提高口服生物利用度的液晶相。

Liquid Crystalline Phases for Enhancement of Oral Bioavailability.

机构信息

Department of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, 510632, China.

Center for Medical Research and Innovation, Shanghai Pudong Hospital, Fudan University Pudong Medical Center, Shanghai, 201399, China.

出版信息

AAPS PharmSciTech. 2021 Feb 22;22(3):81. doi: 10.1208/s12249-021-01951-w.

Abstract

Liquid crystalline phases (LCPs) are generated upon lipolysis of ingested lipids in the gastrointestinal tract. The breaking off and subsequent evolution of LCPs produce more advanced vesicular and micellar structures which facilitate oral absorption of lipids, as well as co-loaded drug entities. Owing to sustained or controlled drug release, bioadhesiveness, and capability of loading drugs of different properties, LCPs are promising vehicles to implement for enhancement of oral bioavailability. This review aims to provide an overview on the classification, preparation and characterization, in vivo generation and transformation, absorption mechanisms, and encouraging applications of LCPs in enhancement of oral bioavailability. In addition, we comment on the merits of LCPs as oral drug delivery carriers, as well as solutions to industrialization utilizing liquid crystalline precursor and preconcentrate formulations.

摘要

在胃肠道中摄入的脂质发生脂解时会产生液晶相 (LCPs)。LCPs 的断裂和随后的演变产生了更先进的囊泡和胶束结构,这有助于脂质的口服吸收以及共载药物实体。由于持续或控制药物释放、生物黏附性以及装载不同性质药物的能力,LCPs 是一种很有前途的载体,可用于提高口服生物利用度。本综述旨在概述 LCPs 在提高口服生物利用度方面的分类、制备和表征、体内生成和转化、吸收机制以及令人鼓舞的应用。此外,我们还评论了 LCPs 作为口服药物递送载体的优点,以及利用液晶前体和预浓缩制剂实现工业化的解决方案。

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