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Rifampicin-carrying poly(D,L-lactide) microspheres: loading and release
E B Denkbaş1, X Kaitian, A Tuncel
1Chemical Engineering Department, Hacettepe University, Ankara, Turkey.
Journal of Biomaterials Science. Polymer Edition
|January 1, 1995
Summary
Poly(D,L-lactide) (PDLLA) microspheres loaded with rifampicin were developed. Release rates were influenced by microsphere degradation, which accelerated in basic pH and high temperatures, indicating combined control mechanisms.
Area of Science:
- Biomaterials Science
- Polymer Chemistry
- Pharmaceutical Technology
Background:
- Poly(D,L-lactide) (PDLLA) is a biodegradable polymer frequently used in drug delivery systems.
- Rifampicin is a crucial antibiotic for treating tuberculosis.
- Controlling the release rate of rifampicin from polymeric microspheres is essential for effective therapeutic outcomes.
Purpose of the Study:
- To prepare and characterize rifampicin-loaded PDLLA microspheres.
- To investigate the impact of various formulation parameters on rifampicin loading and release.
- To evaluate the influence of environmental conditions (pH and temperature) on microsphere degradation and drug release.
Main Methods:
- Modified solvent evaporation technique for microsphere preparation.
- Varied solvents (methylene chloride, chloroform, carbon tetrachloride), solvent/polymer ratios, emulsifiers (methyl cellulose, gelatin, Tween-20), and drug/polymer ratios.
- Assessed microsphere degradation and rifampicin release profiles at different pH and temperature conditions.
Main Results:
- Rifampicin-loaded PDLLA microspheres were successfully prepared in the size range of 0.8-8.0 microns.
- Microsphere degradation and rifampicin release were significantly accelerated at basic pH (9.8) and elevated temperatures (55°C).
- Formulation parameters like solvent type, emulsifier, and drug/polymer ratio influenced rifampicin loading.
Conclusions:
- Rifampicin release from PDLLA microspheres is governed by both polymer degradation and drug diffusion mechanisms.
- Environmental factors such as pH and temperature play a critical role in modulating the release kinetics.
- The developed microspheres offer potential for controlled rifampicin delivery, with release rates tunable by formulation and environmental conditions.