A Novel Stable Crystalline Triamcinolone Acetonide-loaded PLGA Microsphere for Prolonged Release After Intra-Articular Injection
- Authors
- Ho, Myoung Jin; Kim, Sung Rae; Choi, Young Wook; Kang, Myung Joo
- Issue Date
- Sep-2016
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- Triamcinolone acetonide; Microsphere; PLGA; Intra-articular injection; Sustained release
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.37, no.9, pp 1496 - 1500
- Pages
- 5
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 37
- Number
- 9
- Start Page
- 1496
- End Page
- 1500
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/6567
- DOI
- 10.1002/bkcs.10897
- ISSN
- 1229-5949
1229-5949
- Abstract
- The aim of this study was to fabricate novel poly(lactic-co-glycolic acid) microspheres (PLGA MSs) containing triamcinolone acetonide (TA), a potent corticosteroid, to achieve the sustained release profile in joints after intra-articular injection. The TA-loaded MSs were prepared by layering the suspended drug crystals with PLGA using spray-drying. The MS consisting of the drug crystals, PLGA, and lecithin was spherical with size 9.7-10.3 mu m. Hyperspectral analysis (CytoViva (R)) and powder X-ray diffraction studies revealed that the drug crystals were predominantly located in the inner compartment of MS in a stable crystalline form. In an in vitro release test under sink condition, over 90% of TA was released from drug powder within 1 h. However, the MS system released only 35% of the drug during 1 h, achieving 80% drug release after 48 h. Moreover, the steroid-embedded MS was stable for 6 months under long-term storage condition (25 degrees C/60% RH) with no physicochemical changes. These findings suggest that PLGA-based MSs of TA can be a sustained release formula for the treatment of chronic diseases with less frequent intra-articular injection and improved patient compliance.
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