Department of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, People's Republic of China.
ASD Medical Rehabilitation Center, the Second People's Hospital of Guangdong Province, Guangzhou, People's Republic of China.
Int J Nanomedicine. 2022 Oct 17;17:4861-4877. doi: 10.2147/IJN.S382192. eCollection 2022.
Bioavailability is an eternal topic that cannot be circumvented by peroral drug delivery. Adequate blood drug exposure after oral administration is a prerequisite for effective treatment. Nanovesicles as pleiotropic oral vehicles can solubilize, encapsulate, stabilize an active ingredient and promote the payload absorption via various mechanisms. Vesicular systems with nanoscale size, such as liposomes, niosomes and polymersomes, provide a versatile platform for oral delivery of drugs with distinct nature. The amphiphilicity of vesicles in structure allows hydrophilic and lipophilic molecule(s) either or both to be loaded, being encapsulated in the aqueous cavity or the inner core, respectively. Depending on high oral transport efficiency based on their structural flexibility, gastrointestinal stability, biocompatibility, and/or intestinal epithelial affinity, nanovesicles can markedly augment the oral bioavailability of various poorly absorbed drugs. Vesicular drug delivery systems (VDDSs) demonstrate a lot of preferences and are becoming more prominent of late years in biomedical applications. Equally, these systems can potentiate a drug's therapeutic index by ameliorating the oral absorption. This review devotes to comment on various VDDSs with special emphasis on the peroral drug delivery. The classification of nanovesicles, preparative processes, intestinal transport mechanisms, in vivo fate, and design rationale were expounded. Knowledge on vesicles-mediated oral drug delivery for bioavailability enhancement has been properly provided. It can be concluded that VDDSs with many merits will step into an energetic arena in oral drug delivery.
生物利用度是口服药物递送无法回避的永恒话题。口服给药后充分的血液药物暴露是有效治疗的前提。纳米囊泡作为多效口服载体，可以通过多种机制增溶、包封、稳定活性成分并促进载药吸收。具有纳米级尺寸的囊泡系统，如脂质体、非诺体和聚合物体，为具有不同性质的药物提供了口服递送的多功能平台。囊泡在结构上的两亲性允许亲水和疏水分子（或两者）被加载，分别包封在水腔或内核中。基于其结构灵活性、胃肠道稳定性、生物相容性和/或肠上皮亲和力的高口服转运效率，纳米囊泡可以显著提高各种吸收不良药物的口服生物利用度。囊泡药物递送系统 (VDDS) 在生物医学应用中表现出许多优势，近年来越来越受到关注。同样，这些系统可以通过改善口服吸收来提高药物的治疗指数。本文专门评论了各种 VDDS，特别强调了口服药物递送。阐述了纳米囊泡的分类、制备工艺、肠道转运机制、体内命运和设计原理。适当提供了关于通过囊泡介导的口服药物递送提高生物利用度的知识。可以得出结论，具有多种优点的 VDDS 将在口服药物递送领域中崭露头角。
