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Routine Screening Method for Microparticles in Platelet Transfusions
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Microparticle preparation by a propylene carbonate emulsification-extraction method.

Daris Grizić1, Alf Lamprecht2

  • 1Department of Pharmaceutics, Institute of Pharmacy, University of Bonn, Gerhard-Domagk-Str. 3, 53121 Bonn, Germany.

International Journal of Pharmaceutics
|April 10, 2018
PubMed
Summary
This summary is machine-generated.

This study introduces propylene carbonate (PC) as a safer solvent for poly(lactic-co-glycolic-acid) (PLGA) microparticle formulation. An enhanced extraction method significantly reduces residual PC, improving microparticle properties and stability.

Keywords:
Enhanced solvent extractionMicroparticlesPLGAPropylene carbonate

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Area of Science:

  • Materials Science
  • Polymer Chemistry
  • Pharmaceutical Technology

Background:

  • Conventional organic solvents used in microparticle formulation pose significant health and environmental risks.
  • Poly(lactic-co-glycolic-acid) (PLGA) microparticles are widely used in drug delivery but their preparation often involves hazardous solvents.
  • Developing safer and more efficient methods for microparticle production is crucial for sustainable pharmaceutical manufacturing.

Purpose of the Study:

  • To evaluate propylene carbonate (PC) as a low-toxicity alternative solvent for PLGA microparticle preparation.
  • To develop and validate an enhanced solvent extraction method for PC from PLGA microparticles.
  • To assess the impact of residual PC on microparticle properties, including solidification and thermal characteristics.

Main Methods:

  • PLGA microparticles were prepared using an emulsification-solvent extraction method with PC as the solvent.
  • An additional solvent extraction step utilizing hydrolytic solvent cleavage was incorporated.
  • Microparticle morphology, size distribution, residual solvent content, and glass transition temperature (Tg) were analyzed.

Main Results:

  • Spherical PLGA microparticles with a volume median diameter of 20-60 µm were successfully produced.
  • The enhanced PC extraction step reduced residual PC content from 8.8% to 2.7%.
  • This reduction in residual PC significantly improved microparticle solidification, shifting Tg from 8.2°C to 37.7°C, indicating a reduced plasticizing effect.

Conclusions:

  • Propylene carbonate (PC) is a viable low-toxicity solvent for PLGA microparticle formulation.
  • The enhanced hydrolytic solvent cleavage extraction method effectively removes residual PC without compromising PLGA stability.
  • This approach offers a significant advancement in developing safer and more efficient microparticle preparation techniques, replacing conventional harmful organic solvents.