Oral delivery of polyester nanoparticles for brain-targeting: Challenges and opportunities

Wang, P; Wang, Y; Li, P; Chen, C; Ma, SM; Zhao, LX; He, HB; Yin, T; Zhang, Y; Tang, X; Gou, JX

Abstract

Efficient oral delivery of drugs treating brain diseases has long been a challenging topic faced by the drug delivery community. Fortunately, polyester nanoparticles offer certain solutions to this problem. This re-view article firstly describes the main obstacles faced by oral administered brain targeting, including: (1) instability in the gastrointestinal tract; (2) poor penetration of the intestinal mucosa and epithelium; (3) blood clearance; and (4) restriction by the BBB. Then the key factors influencing brain-targeting efficiency of orally administered polyester nanoparticles are also discussed, such as size, shape and surface prop-erties. Finally, recent brain-targeting delivery strategies using oral polyester nanoparticles as carriers and their effects on brain drugs transport are reviewed, and the delivery 'as a whole' strategy of polyester nanoparticles will provide new insight for oral brain-targeting delivery. And by combination of multiple strategies, both the stability and permeability of polyester nanoparticles can be greatly improved for oral brain drug delivery.(c) 2023 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.

Keywords: Polyester nanoparticles; Oral brain drugs; Brain-targeted delivery; Physiological barrier; Absorption enhancement

Related products/services

Biopolymers & Synthetic Polymers

Oral delivery of polyester nanoparticles represents a promising approach for targeted drug delivery, capitalizing on the advantages of non-invasive administration and enhanced patient compliance. Polyester nanoparticles, such as those made from poly(lactic-co-glycolic acid) (PLGA), are engineered to protect drugs from degradation in the gastrointestinal tract and facilitate controlled release. These nanoparticles can be designed to release their payload in response to specific environmental conditions, such as pH changes or enzymatic activity, ensuring targeted delivery to the desired site of action. The use of polyester nanoparticles also allows for the encapsulation of a wide range of therapeutic agents, including poorly soluble drugs. Additionally, surface modifications can be employed to enhance cellular uptake and achieve precise targeting of disease sites, such as tumors or inflamed tissues. This approach not only improves drug bioavailability and efficacy but also minimizes systemic side effects, offering a significant advancement in oral drug delivery systems.