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
Highlights
Polymeric microparticles (MPs) are gaining more and more interest as drug delivery systems (Karp et al 2019), and in biosensing and tissue engineering (Martins et al 2018; Qodratnama et al 2015)
The focus is on a random copolymer of poly-(glycolic acid) (PGA) and poly-(lactic acid) (PLA) (Fig. 1), which employment is mostly due to the possibility to achieve a controlled drug release by governing its bio-degradation which is ruled by the polymer chemistry such as glycoside units content, initial molecular weight (MW) (Amoyav et al 2019; Xia, Li, and Gao 2017; Hussain et al 2017), stereochemistry (Makadia and Siegel 2011) or end-group functionalization (Wang et al 2019)
Degradation time and morphological characteristics of poly-(lactic-co-glycolic acid) (PLGA) MPs can be modified by monomer composition, MW and end-group functionalization
Summary
Polymeric microparticles (MPs) are gaining more and more interest as drug delivery systems (Karp et al 2019), and in biosensing and tissue engineering (Martins et al 2018; Qodratnama et al 2015). MPs can be used for the controlled release of drugs (Choi et al 2011; Guo et al 2015) that can be modulated by choosing the kind of polymer and its chemical and molecular features such as molecular weight (MW), monomer composition (Takeuchi et al 2017), crystallinity, glass transition temperature (Tg), and inherent viscosity (Ansary et al 2014) In this scenario, a lot of biodegradable polymers can be used to formulate MPs as alginate (Strobel et al 2020), dextran (Shah et al 2019), chitosan (Batista et al 2019), gelatin (da Silva and Pinto et al 2019) and poly-(lactic-co-glycolic acid) (PLGA) (Kapoor et al 2015). Emulsification solvent diffusion method Supercritical fluid emulsion Coacervation Spray drying Hydrogel template method Microfluidic systems Membrane extrusion emulsification Particle replication in non-wetting templates (PRINT) technique Electro hydrodynamic atomization (EHDA) or electro-spraying Particles from gas saturated solutions (PGSS) method
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