Bioerodable PLGA-based microparticles for producing sustained-release drug formulations and strategies for improving drug loading

Han, Felicity Y., Thurecht, Kristofer J., Whittaker, Andrew K. and Smith, Maree T. (2016) Bioerodable PLGA-based microparticles for producing sustained-release drug formulations and strategies for improving drug loading. Frontiers in Pharmacology, 7 JUN: 1-11. doi:10.3389/fphar.2016.00185


Author Han, Felicity Y.
Thurecht, Kristofer J.
Whittaker, Andrew K.
Smith, Maree T.
Title Bioerodable PLGA-based microparticles for producing sustained-release drug formulations and strategies for improving drug loading
Journal name Frontiers in Pharmacology   Check publisher's open access policy
ISSN 1663-9812
Publication date 2016-06-28
Year available 2016
Sub-type Critical review of research, literature review, critical commentary
DOI 10.3389/fphar.2016.00185
Open Access Status DOI
Volume 7
Issue JUN
Start page 1
End page 11
Total pages 11
Place of publication Lausanne, Switzerland
Publisher Frontiers Research Foundation
Collection year 2017
Language eng
Abstract Poly(lactic-co-glycolic acid) (PLGA) is the most widely used biomaterial for microencapsulation and prolonged delivery of therapeutic drugs, proteins and antigens. PLGA has excellent biodegradability and biocompatibility and is generally recognized as safe by international regulatory agencies including the United States Food and Drug Administration and the European Medicines Agency. The physicochemical properties of PLGA may be varied systematically by changing the ratio of lactic acid to glycolic acid. This in turn alters the release rate of microencapsulated therapeutic molecules from PLGA microparticle formulations. The obstacles hindering more widespread use of PLGA for producing sustained-release formulations for clinical use include low drug loading, particularly of hydrophilic small molecules, high initial burst release and/or poor formulation stability. In this review, we address strategies aimed at overcoming these challenges. These include use of low-temperature double-emulsion methods to increase drug-loading by producing PLGA particles with a small volume for the inner water phase and a suitable pH of the external phase. Newer strategies for producing PLGA particles with high drug loading and the desired sustained-release profiles include fabrication of multi-layered microparticles, nanoparticles-in-microparticles, use of hydrogel templates, as well as coaxial electrospray, microfluidics, and supercritical carbon dioxide methods. Another recent strategy with promise for producing particles with well-controlled and reproducible sustained-release profiles involves complexation of PLGA with additives such as polyethylene glycol, poly(ortho esters), chitosan, alginate, caffeic acid, hyaluronic acid, and silicon dioxide.
Keyword PLGA microparticles
Drug delivery system
Hydrophilic molecule
Biodegradation mechanisms
Tuneable release
Microfluidics
Supercritical carbon dioxide
Hydrogel template
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

 
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