Antibiotic release from biodegradable PHBV microparticles

Sendil D., Gursel I., Wise D., Hasirci V.

JOURNAL OF CONTROLLED RELEASE, vol.59, no.2, pp.207-217, 1999 (Peer-Reviewed Journal) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 59 Issue: 2
  • Publication Date: 1999
  • Doi Number: 10.1016/s0168-3659(98)00195-3
  • Journal Indexes: Science Citation Index Expanded, Scopus
  • Page Numbers: pp.207-217
  • Keywords: polyhydroxybutyrate-co-hydroxyvalerate (PHBV), tetracycline, controlled release, microencapsulation, periodontal diseases, DRUG-RELEASE, TETRACYCLINE, PERIODONTITIS, MICROSPHERES, MORPHOLOGY, ACID)


For the treatment of periodontal diseases, design of a controlled release system seemed very appropriate for an effective, long term result. In this study a novel, biodegradable microbial polyester, poly(3-hydroxybutyrate-co-3-hydroxyvalerate), PHBV of various valerate contents containing a well established antibiotic, tetracycline, known to be effective against many of the periodontal disease related microorganisms, was used in the construction of a controlled release system. Tetracycline was loaded in the PHBV microspheres and microcapsules both in its acidic (TC) and in neutral form (TCN). Microcapsules of PHBV were prepared under different conditions using w/o/w double emulsion and their properties such as encapsulation efficiency, loading, release characteristics, and morphological properties were investigated. It was found that concentration of emulsifiers polyvinyl alcohol (PVA) and gelatin (varied between 0-4%) influenced the encapsulation efficiency appreciably. In order to increase encapsulation efficiency (from the obtained range of 18.1-30.1%) and slow down the release of the highly soluble tetracycline. HCl, it was neutralized with NaOH. Encapsulation efficiency of neutralized tetracycline was much higher (51.9-65.3%) due to the insoluble form of the drug used during encapsulation. The release behaviour of neither of the drugs was found to be of zero order. Rather the trends fitted reasonably well to Higuchi's approach for release from spherical micropheres. Biodegradability was not an appreciable parameter in the release from microcapsules because release was complete before any signs of degradation were observed. (C) 1999 Elsevier Science B.V. All rights reserved.