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Article

Design and In Vivo Pharmacokinetic Evaluation of Triamcinolone Acetonide Microcrystals-Loaded PLGA Microsphere for Increased Drug Retention in Knees after Intra-Articular Injection

1
College of Pharmacy, Dankook University, 119, Dandae-ro, Dongnam-gu, Cheonan-si, Chungcheongnam-do 31116, Korea
2
College of Pharmacy, Chung-Ang University, 84, Heukseok-ro, Dongjak-gu, Seoul 06974, Korea
3
Department of Radiology, Seoul National University Bundang Hospital, 82, Gumi-ro 173beon-gil, Bundang-gu, Seongnam-si, Gyeonggi-do 13620, Korea
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(8), 419; https://doi.org/10.3390/pharmaceutics11080419
Received: 22 July 2019 / Revised: 9 August 2019 / Accepted: 12 August 2019 / Published: 19 August 2019
(This article belongs to the Special Issue PLGA Based Drug Carrier and Pharmaceutical Applications)
A novel polymeric microsphere (MS) containing micronized triamcinolone acetonide (TA) in a crystalline state was structured to provide extended drug retention in joints after intra-articular (IA) injection. Microcrystals with a median diameter of 1.7 μm were prepared by ultra-sonication method, and incorporated into poly(lactic-co-glycolic acid)/poly(lactic acid) (PLGA/PLA) MSs using spray-drying technique. Cross-sectional observation and X-ray diffraction analysis showed that drug microcrystals were evenly embedded in the MSs, with a distinctive crystalline nature of TA. In vitro drug release from the novel MSs was markedly decelerated compared to those from the marketed crystalline suspension (Triam inj.®), or even 7.2 μm-sized TA crystals-loaded MSs. The novel system offered prolonged drug retention in rat joints, providing quantifiable TA remains over 28 days. Whereas, over 95% of IA TA was removed from joints within seven days, after injection of the marketed product. Systemic exposure of the steroidal compound was drastically decreased with the MSs, with <50% systemic exposure compared to that with the marketed product. The novel MS was physicochemically stable, with no changes in drug crystallinity and release profile over 12 months. Therefore, the TA microcrystals-loaded MS is expected to be beneficial in patients especially with osteoarthritis, with reduced IA dosing frequency. View Full-Text
Keywords: triamcinolone acetonide; microcrystal; PLGA microsphere; local delivery; spray-drying technique; intra-articular injection; joint retention; systemic exposure triamcinolone acetonide; microcrystal; PLGA microsphere; local delivery; spray-drying technique; intra-articular injection; joint retention; systemic exposure
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MDPI and ACS Style

Ho, M.J.; Jeong, H.T.; Im, S.H.; Kim, H.T.; Lee, J.E.; Park, J.S.; Cho, H.R.; Kim, D.Y.; Choi, Y.W.; Lee, J.W.; Choi, Y.S.; Kang, M.J. Design and In Vivo Pharmacokinetic Evaluation of Triamcinolone Acetonide Microcrystals-Loaded PLGA Microsphere for Increased Drug Retention in Knees after Intra-Articular Injection. Pharmaceutics 2019, 11, 419. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11080419

AMA Style

Ho MJ, Jeong HT, Im SH, Kim HT, Lee JE, Park JS, Cho HR, Kim DY, Choi YW, Lee JW, Choi YS, Kang MJ. Design and In Vivo Pharmacokinetic Evaluation of Triamcinolone Acetonide Microcrystals-Loaded PLGA Microsphere for Increased Drug Retention in Knees after Intra-Articular Injection. Pharmaceutics. 2019; 11(8):419. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11080419

Chicago/Turabian Style

Ho, Myoung J., Hoe T. Jeong, Sung H. Im, Hyung T. Kim, Jeong E. Lee, Jun S. Park, Ha R. Cho, Dong Y. Kim, Young W. Choi, Joon W. Lee, Yong S. Choi, and Myung J. Kang 2019. "Design and In Vivo Pharmacokinetic Evaluation of Triamcinolone Acetonide Microcrystals-Loaded PLGA Microsphere for Increased Drug Retention in Knees after Intra-Articular Injection" Pharmaceutics 11, no. 8: 419. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11080419

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