Abstract
The blood–brain barrier (BBB) is a natural obstacle for drug delivery into the human brain, hindering treatment of central nervous system (CNS) disorders such as acute ischemic stroke, brain tumors, and human immunodeficiency virus (HIV)-1-associated neurocognitive disorders. Poly(lactic-co-glycolic acid) (PLGA) is a biocompatible polymer that is used in Food and Drug Administration (FDA)-approved pharmaceutical products and medical devices. PLGA nanoparticles (NPs) have been reported to improve drug penetration across the BBB both in vitro and in vivo. Poly(ethylene glycol) (PEG), poly(vinyl alcohol) (PVA), and poloxamer (Pluronic) are widely used as excipients to further improve the stability and effectiveness of PLGA formulations. Peptides and other linkers can be attached on the surface of PLGA to provide targeting delivery. With the newly published guidance from the FDA and the progress of current Good Manufacturing Practice (cGMP) technologies, manufacturing PLGA NP-based drug products can be achieved with higher efficiency, larger quantity, and better quality. The translation from bench to bed is feasible with proper research, concurrent development, quality control, and regulatory assurance.
Highlights
Introduction ofPhysical, Chemical, and Biological Characteristics of Poly(lactic-co-glycolic acid) (PLGA) Polymer3.1
Trimethylated chitosan (TMC)-modified PLGA NPs loaded with coumarin exhibited increased uptake in mouse brains vs. PLGA-NPs
Neuroprotective effects of Q10 displayed by mice in TMC PLGA NPs were superior to Angiopep-2 modified PLGA NPs improved
Summary
Several strategies have been used to improve drug delivery to the brain. Efforts have been made for the development of inhibitors for ABC transporters due to their high expressions on the BBB [2,12,13]. Studies showed that blocking ABC transporters may significantly improve drug penetrations across the BBB. This method has not been used clinically due to the wide distribution of ABC transporters throughout the body, the potential toxicity of inhibitors, and unexpected drug–drug interactions [12]. Another approach is the “BBB opening” approach. The. NP-based delivery system can cross the BBB through membrane transcytosis, bypass efflux transporters, and effectively deliver the therapeutic molecule to the CNS [3].
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