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Related Experiment Videos

Solvent influence on spray-dried biodegradable microspheres.

D F Bain1, D L Munday, A Smith

  • 1School of Pharmacy, Robert Gordon University, Aberdeen, UK.

Journal of Microencapsulation
|July 27, 1999
PubMed
Summary

Solvent choice critically impacts poly(D,L-lactic acid) microsphere properties and rifampicin release. Denser microspheres from stronger solvents show slower drug release, highlighting the need for careful solvent selection in spray-drying.

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Area of Science:

  • Pharmaceutics
  • Materials Science
  • Chemical Engineering

Background:

  • Poly(D,L-lactic acid) (PDLLA) microspheres are utilized for controlled drug delivery.
  • Spray-drying is a common method for microsphere fabrication, but solvent choice influences characteristics.

Purpose of the Study:

  • To investigate the effect of various solvents on the characteristics of rifampicin-loaded PDLLA microspheres produced by spray-drying.
  • To understand the relationship between solvent properties, microsphere morphology, and drug release kinetics.

Main Methods:

  • Spray-drying of PDLLA microspheres with a fixed composition (Resomer R104:R202H, 30:70) containing 20% rifampicin.
  • Utilized solvents including acetone, dichloromethane, chloroform, and halothane, and their mixtures.
  • Evaluated microsphere characteristics such as morphology, density, glass transition temperature (Tg), residual solvent content, and drug release rates.

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Main Results:

  • Solvent power, determined by viscosity, influenced polymer deposition and microsphere matrix structure (e.g., acetone yielded porous structures, while stronger solvents produced denser matrices).
  • Denser microspheres exhibited elevated Tg and significantly retarded rifampicin release.
  • Yield and residual solvent content increased with solvent strength and particle density.
  • Drug release rate correlated positively with Tg after accounting for specific surface area (r² = 0.963).

Conclusions:

  • Solvent selection during spray-drying profoundly affects PDLLA microsphere characteristics, including morphology, density, and drug release profiles.
  • Residual solvent content and Tg are directly linked to solvent affinity for the polymer composite.
  • Technological and toxicological considerations are paramount when selecting solvents for microsphere production.