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KMID : 0369820080380010063
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Jorunal of Korean Pharmaceutical Sciences
2008 Volume.38 No. 1 p.63 ~ p.72
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Preparation and Evaluation of Meloxicam-loaded Poly(D,L-lactic acid) Microspheres
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Im Jong-Seub
Oh Dong-Hoon
Lee Dong-Hoon
Sung Jung-Hoon
Yoo Bong-Kyu
Kim Jung-Ae
Woo Jong-Soo
Lee Yong-Bok
Kim Se-Mi
Choi Han-Gon
Yong Chul-Soon
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Abstract
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Meloxicam-loaded microspheres were prepared with poly(D,L-lactic acid)(PLA) by a solvent-emulsion evaporation method. The morphology, particle size, drug loading capacity, drug entrapment efficiency (EE) and release patterns of drug were investigated in vitro. Various batches of micro spheres with different size and drug content were obtained by changing the ratio of meloxicam to with different molecular weight, PLA concentration in the dispersed phase and stirring rate. Meloxicam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. Microspheres prepared with smaller molecular weight produced faster drug release rate. The release rate of meloxicam for long-acting injectable delivery system in vitro, which would aid in predicting in vivo release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres. Blood concentration-time profile of meloxicam after intramuscular injection of meloxicam-loaded microspheres in rabbits showed possibility of long term application of this system in clinical settings.
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KEYWORD
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Meloxicam, Poly(D, L-lactic acid), Microspheres, Injectable delivery system
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