Nanovesicles-Mediated Drug Delivery for Oral Bioavailability Enhancement

Abstract

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.

Pharmacokinetics and Oral Bioavailability of Panax Notoginseng Saponins Administered to Rats Using a Validated UPLC–MS/MS Method

“…Our study shows that the total oral bioavailability of PNS is only 1.2% due to the chemical and biological complexity of PNS. Adequate blood drug exposure or high oral bioavailability is a prerequisite for effective treatment . Obviously, poor oral bioavailability should not support the in vivo pharmacological activity of PNS.…”

“…Adequate blood drug exposure or high oral bioavailability is a prerequisite for effective treatment. 36 Obviously, poor oral bioavailability should not support the in vivo pharmacological activity of PNS. As a traditional Chinese medicine, P. notoginseng has a long use history with good clinical curative effects.…”

Recent Developments in Oral Delivery of Vaccines Using Nanocarriers

“…Nanometric size, amphiphilic nature, high entrapment efficiency, and high stability are the unique features of phytosomes that make them suitable carriers for the delivery of pharmaceuticals through the enteral route. Attachment of pharmaceuticals with phospholipid molecules, a principal component of phytosomes offers several benefits that include prevention of drug leakage from the carrier and slow and sustained drug release that enhance the efficacy of delivered medications [ 109 ].…”

Olesya Gusachenko

“…Representing a naturally occurring communication route exosomes are likely to have better biocompatibility and exhibit fewer side effects than synthetic delivery formulations. Similarly, exosomes may possess higher bioavailability and consequently give more promise in accommodating different administration routes 15,16 . Exosomes have the intrinsic ability to pass the blood-brain barrier 17,18 which alleviates a major hurdle in the development of treatments for neuropathological conditions.…”