title: Microencapsulation of antibiotic rifampicin in poly(3-hydroxybutyrate-co-3-hydroxyvalerate).
abstract: 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 microm 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.
authors.affiliation: Instituto de Quimica, Biological Chemistry Laboratory, Universidade Estadual de Campinas, C.P. 6154, Campinas CEP 13083-970, S.P, Brazil. duran@iqm.unicamp.br
authors.forename: N
authors.initials: N
authors.lastname: Durán
authors.forename: M A
authors.initials: MA
authors.lastname: Alvarenga
authors.forename: E C
authors.initials: EC
authors.lastname: Da Silva
authors.forename: P S
authors.initials: PS
authors.lastname: Melo
authors.forename: P D
authors.initials: PD
authors.lastname: Marcato
mesh_terms: D000818:Animals; D000904:Antibiotics, Antitubercular / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D006224:Cricetinae; D004339:Drug Compounding; D005079:Excipients; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D009499:Neutral Red; D019384:Nucleic Acid Synthesis Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D012293:Rifampin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013778:Tetrazolium Salts; D013844:Thiazoles; D000094122:Polyhydroxybutyrates
chemical_list: D000904:Antibiotics, Antitubercular; D005079:Excipients; D009499:Neutral Red; D019384:Nucleic Acid Synthesis Inhibitors; D011091:Polyesters; D012293:Rifampin; D013778:Tetrazolium Salts; D013844:Thiazoles; C052620:poly(3-hydroxybutyrate)-co-(3-hydroxyvalerate); D000094122:Polyhydroxybutyrates; C022616:thiazolyl blue