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.

Development of tunable biodegradable polyhydroxyalkanoates microspheres for controlled delivery of tetracycline for treating periodontal disease

“…26,27 Bacterial PHAs are typically produced with high molecular weight (M w ; i.e., 10 5 210 6 g/mol) and low polydispersity index. [33][34][35][36][37] Coimbra et al 33 prepared polymeric microspheres from biodegradable P(HB-6HV) copolymers and showed controlled release of a non-steroidal anti-inflammatory drug, flurbiprofen. 28 In addition, they can be produced with different side chain compositions, which alter their physical properties and render them useful for a wide range of applications.…”

Association of the anti-tuberculosis drug rifampicin with a PAMAM dendrimer

“…[13,14] In order to improve the bioavailability of RIF and the other tuberculostatic drugs, several research groups have been developing drug delivery systems (DDS). [12] Suggested formulations involve hydrosoluble polymers, [15][16][17][18][19] solid dispersions, [20] microparticles, [9] liposomes, [21,22] inclusion complexes [23,24] and dendrimers [25]. Ideally, a DDS would transport the active compounds to their targets, reducing the therapeutic dosage while keeping the desired drug level for a long period of time, minimizing adverse effects and simplifying the treatment.…”

Microparticles prepared from biodegradable polyhydroxyalkanoates as matrix for encapsulation of cytostatic drug

“…PHA microparticles, films, and 3D matrices are promising carriers for antibiotics, enabling the sustained release of the drug [13][14][15][16]. Incorporation of protein compounds in composite microparticles consisting of PHAs and polyethylene glycol and polylactides was reported by Lionzo et al [9].…”