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Preparation and Characterization of Triamcinolone Acetonide-loaded Poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) (PHBHx) Microspheres

Hacettepe University, Chemistry Department, Biochemistry Division Beytepe, Ankara, Turkey

Emir Baki Denkba

Hacettepe University, Chemistry Department, Biochemistry Division Beytepe, Ankara, Turkey, denkbas{at}hacettepe.edu.tr

Ebru Kiliçay

Karaelmas University, Chemistry Department, Physical Chemistry Division, Zonguldak, Turkey

Baki Hazer

Karaelmas University, Chemistry Department, Physical Chemistry Division, Zonguldak, Turkey

Hasan Basri Çakmak

Ministry of Health, Atatürk Training Hospital, Ophthalmology Clinics, Ankara, Turkey

Isao Noda

The Procter and Gamble Company,West Chester, Ohio, USA

Triamcinolone acetonide loaded in poly(3-hydroxybutyrate-co-3 hydroxyhexanoate) (PHBHx) microspheres were prepared to treat cystoid macular oedema (CMO) and acute posterior segment inflammation associated with uveitis. The PHBHx microspheres were prepared by solvent evaporation technique using methylene chloride as the solvent and aqueous poly(vinyl alcohol) emulsifier as the dispersion medium. The PHBHx microspheres obtained were well formed with narrow size distribution; the average size prepared ranged from 40—200 µm depending on the formulation used. The stirring rate of the dispersion medium, emulsifier concentration, and polymer/solvent ratio parameters were varied to determine their effect on the size and size distribution of the PHBHx microspheres. Increasing the stirring rate and emulsifier concentration decreased the size and the size distribution of the microspheres, while increasing the polymer/solvent ratio caused the opposite effect. The polymer/drug ratio was the most effective parameter for controlling drug loading and release properties. More than 90% of the loaded drug was released within the first 24 h; after that, the release rate was slower for all formulations.

Key Words: triamcinolone acetonide • PHBHx • cystoid macular oedema • uveitis • microspheres • controlled drug delivery • controlled drug release.

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