Microencapsulation of antibiotic rifampicin in poly(3-hydroxybutyrate-co-3-hydroxyvalerate)

• Published in: Archives of pharmacal research 2008, 31(11), , pp.1509-1516
• Main Authors: Durán, N., Alvarenga, M. A., Da Silva, E. C., Melo, P. S., Marcato, P. D.
• Format: Article
• Language: English
• Subjects: Animals; Antibiotics, Antitubercular - administration & dosage; Antibiotics, Antitubercular - chemistry; Antibiotics, Antitubercular - pharmacology; Cell Line; Cricetinae; Drug Compounding; Excipients; Medicine; Microbial Sensitivity Tests; Microscopy, Electron, Scanning; Nanoparticles; Neutral Red; Nucleic Acid Synthesis Inhibitors - administration & dosage; Nucleic Acid Synthesis Inhibitors - chemistry; Nucleic Acid Synthesis Inhibitors - pharmacology; Particle Size; Pharmacology/Toxicology; Pharmacy; Polyesters - chemistry; Research Article; Rifampin - administration & dosage; Rifampin - chemistry; Rifampin - pharmacology; Staphylococcus aureus - drug effects; Tetrazolium Salts; Thiazoles; 약학
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/s12272-001-2137-7

The aim of this study was the preparation of microparticles containing rifampicin using a biodegradable polymer poly(3-hydroxybutyrate-co-3-hydroxyvalerate) for oral administration produced by a bacteria. The poly(3-hydroxybutyrate-co-3-hydroxyvalerate) microparticles with and without rifampicin were prepared by the emulsification and solvent evaporation method, in which chloroform and polyvinyl alcohol are used as the solvent and emulsifier, respectively. Microparticles were obtained within a size range of 20-60 μm by changing the initial poly(3-hydroxybutyrate-co-3-hydroxyvalerate), polyvinyl alcohol and rifampicin concentrations. An encapsulation efficiency value of 14% was obtained. The optimized total yield of 60% of the poly(3-hydroxybutyrate-co-3-hydroxyvalerate)/ rifampicin was obtained. A load of 0.035 mg/1 mg of PHBV was reached. Almost 90% of the drug loaded in the microparticles was released after 24 h. The size, encapsulation efficiency and ribampicin release of the microparticles varied as a function of the initial poly(3-hydroxybutyrate-co-3-hydroxyvalerate), polyvinyl alcohol and rifampicin concentrations. It was demonstrated that the microencapsulated rifampicin, although was not totally available in the medium, exhibited a similar inhibition value as free rifampicin at 24 h of incubation with S. aureus. Cytotoxicity assays demonstrated a reduction of the toxicity when rifampicin was microencapsulated in poly(3-hydroxybutyrate-co-3-hydroxyvalerate) while maintaining its antibacterial activity.