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.

Highlights

  • Published: 22 January 2022In recent decades, nanomedicine has received significant interest for its biomedical applications, including prevention, diagnosis, and treatment of diseases

  • Folic acid (FA)-modified NPs labelled with indocyanine green (ICG), a near-infrared fluorescence dye, administered intravenously to mice xenografted with MDA-MB-231 human breast cancer cells, showed a significant accumulation in tumor compared to nonmodified particles

  • Owing to their versatility and unique properties, PLGA NPs represent an effective platform with exciting opportunities in the delivery of therapeutics

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Summary

Introduction

Nanomedicine has received significant interest for its biomedical applications, including prevention, diagnosis, and treatment of diseases. Polymers, which can be synthetic, such as poly(D,L-lactide) (PLA), poly(D,L-lactide-co-glycolide) (PLGA) copolymers, poly (ε-caprolactone) (PCL) and poly(amino acids), or naturally occurring, such as alginate, chitosan (CS) and gelatin, have been widely used as NP-forming biomaterials due to their diverse characteristics, flexibility of design, synthesis, functionalization and, more importantly, favorable safety profile and low toxicity. Amongst these polymers, PLGA copolymers, which are approved for medical application by the United States Food and. The background of the properties and biodegradation of the copolymer is provided, as well as a brief discussion on the methods of fabrication and in vivo fate of PLGA NPs

Physicochemical Properties of PLGA
Biodegradation of the PLGA Copolymer
Preparation of PLGA NPs
Procedure
Emulsion Evaporation Method
Nanoprecipitation Method
Solvent Diffusion Method
Salting Out Method
Emerging Production Methods
Biological Fate of PLGA NPs
Surface Modification Strategies
Surfactants
PEGylation of PLGA
PEG Alternatives
Lipids
Surface Functionalization with Targeting Ligands
Antibodies
Biotin
Bisphosphonate
Folate
Lectins
Mannan
Nucleotides
Peptides
Sialic Aid
6.5.10. Transferrin
Findings
Conclusions
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