Biodegradable microparticles for sustained delivery of tetracycline to the periodontal pocket: formulatory and drug release studies

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Abstract
This paper describes the production and characterization of biodegradable microparticles containing tetracycline, designed for periodontal disease therapy. The influence of production parameters on microparticle characteristics and antibiotic release modality was studied. Microparticles were made by using different preparation procedures and different polyesters, namely poly(L-lactide), [L-PLA] poly(DL-lactide), [DL-PLA] and poly(DL-lactide-co-glycolide) 50:50, [DL-PLG]. A double emulsion preparation method together with a concentrated salt solution as external phase gave the best results in terms of tetracycline incorporation efficacy. In vitro release experiments demonstrated that tetracycline is slowly and appropriately released from microparticles. Release kinetics were found to be influenced by the type of polymer utilized for microparticle production. In vitro experiments, simulating in vivo conditions were carried out for up to 30 days. Only DL-PLG microparticles showed significant changes in their morphology, whereas L-PLA and DL-PLA were found almost intact after the same period of time.