PLGA-based biodegradable microspheres in drug delivery: recent advances in research and application

Drug Deliv. 2021 Dec;28(1):1397-1418. doi: 10.1080/10717544.2021.1938756.


Biodegradable microspheres have been widely used in the field of medicine due to their ability to deliver drug molecules of various properties through multiple pathways and their advantages of low dose and low side effects. Poly (lactic-co-glycolic acid) copolymer (PLGA) is one of the most widely used biodegradable material currently and has good biocompatibility. In application, PLGA with a specific monomer ratio (lactic acid and glycolic acid) can be selected according to the properties of drug molecules and the requirements of the drug release rate. PLGA-based biodegradable microspheres have been studied in the field of drug delivery, including the delivery of various anticancer drugs, protein or peptide drugs, bacterial or viral DNA, etc. This review describes the basic knowledge and current situation of PLGA biodegradable microspheres and discusses the selection of PLGA polymer materials. Then, the preparation methods of PLGA microspheres are introduced, including emulsification, microfluidic technology, electrospray, and spray drying. Finally, this review summarizes the application of PLGA microspheres in drug delivery and the treatment of pulmonary and ocular-related diseases.

Keywords: Biodegradable microspheres; PLGA; applications; drug delivery; preparation methods.

Publication types

  • Review

MeSH terms

  • Biocompatible Materials / chemistry*
  • Brain Neoplasms / drug therapy
  • Chemistry, Pharmaceutical
  • Drug Delivery Systems / methods*
  • Drug Liberation
  • Eye Diseases / drug therapy
  • Lung Diseases / drug therapy
  • Microspheres*
  • Neoplasms / drug therapy
  • Particle Size
  • Peptides / administration & dosage
  • Polylactic Acid-Polyglycolic Acid Copolymer / chemistry*
  • Proteins / administration & dosage
  • Technology, Pharmaceutical


  • Biocompatible Materials
  • Peptides
  • Proteins
  • Polylactic Acid-Polyglycolic Acid Copolymer

Grants and funding

This work was supported by the National Natural Science Foundation of China [Nos. 81202378 and 81311140268]; the Project of Hunan Science and Technology [No. 2020JJ9011 and 2020JJ9020]; the Graduate Independent Exploration and Innovation Project Foundation of Central South University [No. 2020zzts817]; and the Hunan Graduate Research and Innovation Project Foundation [No. CX20200119].