Recent Advances in the Surface Functionalization of PLGA-Based Nanomedicines

Abstract

Therapeutics are habitually characterized by short plasma half-lives and little affinity for targeted cells. To overcome these challenges, nanoparticulate systems have entered into the disease arena. Poly(d,l-lactide-co-glycolide) (PLGA) is one of the most relevant biocompatible materials to construct drug nanocarriers. Understanding the physical chemistry of this copolymer and current knowledge of its biological fate will help in engineering efficient PLGA-based nanomedicines. Surface modification of the nanoparticle structure has been proposed as a required functionalization to optimize the performance in biological systems and to localize the PLGA colloid into the site of action. In this review, a background is provided on the properties and biodegradation of the copolymer. Methods to formulate PLGA nanoparticles, as well as their in vitro performance and in vivo fate, are briefly discussed. In addition, a special focus is placed on the analysis of current research in the use of surface modification strategies to engineer PLGA nanoparticles, i.e., PEGylation and the use of PEG alternatives, surfactants and lipids to improve in vitro and in vivo stability and to create hydrophilic shells or stealth protection for the nanoparticle. Finally, an update on the use of ligands to decorate the surface of PLGA nanomedicines is included in the review.

Applications of mannose-binding lectins and mannan glycoconjugates in nanomedicine

“…Solanum tuberosum lectin-conjugated PLGA-NPs being biodegradable have the potential to serve as nose to brain DDS [ 99 ]. PLGA-based NP conjugated with tumour-specific antigens also served as cancer nanovaccines in APC-like DCs and improves the transfection activity of the targeted gene delivery [ 100 – 102 ].…”

Targeting anti-inflammatory immunonanocarriers to human and murine neutrophils via the Ly6 antigen for psoriasiform dermatitis alleviation

“…PEG is frequently used to coat PLGA nanoparticles for escaping the RES. 44 Although our nanoparticles were decorated by PEG, a complete prevention against RES could not be achieved. It is possible that PEGylation could further activate the complement system for the rapid clearance of nanoparticles.…”

Research Status and Prospect of Non-Viral Vectors Based on siRNA: A Review

“…As PLGA is easily cleared by the immune system and lacks a specific targeting effect, it has limited its clinical application. PEG has been shown to protect PLGA from degradation, increasing drug permeability and thus enhancing gene transfection efficiency [ 150 ]. At the same time, chemotherapy drugs, siRNA, and PLGA can be used in combination to treat cancer [ 151 ].…”