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Microsphere preparation using the untoxic solvent glycofurol.

Daniela Allhenn1, Alf Lamprecht

  • 1Laboratory of Pharmaceutical Engineering, Institute of Pharmacy, University of Bonn, Gerhard-Domagk-Str 3, 53121 Bonn, Germany.

Pharmaceutical Research
|November 5, 2010
PubMed
Summary
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This study introduces glycofurol as a non-toxic solvent for preparing poly(lactide-co-glycolide) microspheres. The novel method effectively encapsulates lipophilic drugs for controlled release, offering a safer alternative for microencapsulation.

Area of Science:

  • Biomaterials Science
  • Pharmaceutical Technology
  • Drug Delivery Systems

Background:

  • Traditional microencapsulation methods often rely on toxic organic solvents.
  • Developing safer, non-toxic alternatives is crucial for therapeutic applications.

Purpose of the Study:

  • To introduce glycofurol as a non-toxic solvent for poly(lactide-co-glycolide) (PLGA) microsphere preparation.
  • To evaluate a quasi-emulsion extraction method for microencapsulation using glycofurol.
  • To assess the encapsulation efficiency and in-vitro release of lipophilic drugs.

Main Methods:

  • PLGA and lipophilic drugs were dissolved in glycofurol to form the internal phase.
  • This internal phase was emulsified into an external phase to form microspheres.

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  • Microspheres were characterized for particle size, morphology, and drug encapsulation.

    • Main Results:

    • Spherical microspheres (100-200 μm) with monomodal size distribution were produced.
    • Encapsulation efficiency increased with higher drug partition coefficients, ranging from 1.9% for Ibuprofen to 28.3% for Sudan III.
    • In-vitro drug release varied from 4 hours (Ritonavir) to 3 weeks (Sudan III).

    Conclusions:

    • Glycofurol is a suitable non-toxic solvent for PLGA microsphere preparation.
    • The method allows for effective entrapment of lipophilic active pharmaceutical ingredients.
    • Controlled release of encapsulated drugs can be achieved using this novel approach.