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Article # : SC25

Sema alış, Ph.D.

Professor

 

Diclofenac sodium incorporated PLGA (50:50) microspheres: formulation considerations and in vitro:in vivo evaluation

 

M. Tunaya ,S.alışa , H.S. Kaşa, M.T. Ercanb, İ. Peksoyb, A.A. Hincala

 

aDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, 06100 Ankara, Turkey

b Department of Nuclear Medicine, Faculty of Medicine, Hacettepe University, 06100 Ankara, Turkey

 

Summary

Recently, considerable interest has been focused on the use of biodegradable polymers for specialized applications such as controlled release of drug formulations; meanwhile, microsphere drug-delivery systems using various kinds of biodegradable polymers have been studied extensively during the past two decades. Poly (lactide-co-glycolide) (PLGA) polymers have been proven to be excellent drug carriers for microparticulate systems due to their advantages, e.g. biocompatibility and regulatory approval. The administration of nonsteroidal anti-inflammatory drugs (NSAIDs) into the intra-articular cavity in patients with chronic inflammatory disease is complicated due to the short duration of effect. In the present study, controlled-release parenteral formulations of diclofenac sodium (DS), a commonly used NSAID, were prepared for intra-articular administration, and evaluated in vitro for particle size, yield, drug loading, surface morphology and release characteristics. For in vivo studies, Technetium-99m labelled polyclonal human immunogammaglobulin ( 99m Tc-HIG) was used as the radiopharmaceutical to demonstrate arthritic lesions by gamma scintigraphy. Evaluation of arthritic lesions post-therapy in rabbits showed no significant difference in the group treated with PLGA (50:50) (mw 34 000) DS microspheres compared to control groups.

 

Key words

Poly (lactide-co-glycolic acid) microspheres; Diclofenac sodium; Solvent-evaporation method; Experimental arthritis; Scintigraphic imaging