Recent advances in the formulation of PLGA microparticles for controlled drug delivery
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REVIEW PAPER
Recent advances in the formulation of PLGA microparticles for controlled drug delivery Elena Lagreca1 · Valentina Onesto1 · Concetta Di Natale1,3 · Sara La Manna2 · Paolo Antonio Netti1,3,4 · Raffaele Vecchione1,3 Received: 13 July 2020 / Accepted: 28 September 2020 © The Author(s) 2020
Abstract Polymeric microparticles (MPs) are recognized as very popular carriers to increase the bioavailability and bio-distribution of both lipophilic and hydrophilic drugs. Among different kinds of polymers, poly-(lactic-co-glycolic acid) (PLGA) is one of the most accepted materials for this purpose, because of its biodegradability (due to the presence of ester linkages that are degraded by hydrolysis in aqueous environments) and safety (PLGA is a Food and Drug Administration (FDA)-approved compound). Moreover, its biodegradability depends on the number of glycolide units present in the structure, indeed, lower glycol content results in an increased degradation time and conversely a higher monomer unit number results in a decreased time. Due to this feature, it is possible to design and fabricate MPs with a programmable and time-controlled drug release. Many approaches and procedures can be used to prepare MPs. The chosen fabrication methodology influences size, stability, entrapment efficiency, and MPs release kinetics. For example, lipophilic drugs as chemotherapeutic agents (doxorubicin), anti-inflammatory non-steroidal (indomethacin), and nutraceuticals (curcumin) were successfully encapsulated in MPs prepared by single emulsion technique, while water-soluble compounds, such as aptamer, peptides and proteins, involved the use of double emulsion systems to provide a hydrophilic compartment and prevent molecular degradation. The purpose of this review is to provide an overview about the preparation and characterization of drug-loaded PLGA MPs obtained by single, double emulsion and microfluidic techniques, and their current applications in the pharmaceutical industry. Graphic abstract
Elena Lagreca and Valentina Onesto contributed equally. Extended author information available on the last page of the article
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Vol.:(0123456789)
Progress in Biomaterials
Keywords PLGA MPs · Double emulsion · Single emulsion · Drug encapsulation · Drug release Abbreviations PLGA Poly(lactic-co-glycolic acid) MPs Polymeric microparticles NPs Polymeric nanoparticles MW Molecular weight PGA Poly(glycolic acid) PLA Poly(lactic acid) FDA Food and Drug Administration EMA European Medicine Agency SPG Shirasu porous glass PRINT Particle replication in non-wetting templates EHDA Electrohydrodynamic atomization PEG Polyethylene glycol PVA Polyvinyl alcohol RM Rasagiline mesylate PDI Polydispersity index DMSO Dimethyl sulfoxide PVP Polyvinylpyrrolidone SDS Sodium dodecyl sulfate ICH International Conference on Harmonization PDE Permitted daily exposure W/O Water in oil W/O/W Water in oil in water LbL Layer-by-layer PDMS Poly(dimethyl siloxane) PMMA Poly(methyl methacrylate) PC Polycarbonate SEM Scanning el
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