Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Preparation and pre-clinical characterization of sustained-release ketoprofen implants for the management of pain and inflammation in osteoarthritis

Jian Zhang¹, Xiaoping Xu², Lin Zhu³, Xiaofan Fei¹ , Zhaohui Jin¹

¹Department of Clinical Pharmacy; ²Drug Analysis Teaching and Research Office; ³Department of Integrated Traditional Chinese and Western Medicine, West China Hospital, Sichuan University, Chengdu 610041, China.

For correspondence:- Xiaofan Fei Email: x116k3@163.com Tel:+862885422664

Accepted: +862885422664 Published: 30 April 2018

Citation: Zhang J, Xu X, Zhu L, Fei X, Jin Z. Preparation and pre-clinical characterization of sustained-release ketoprofen implants for the management of pain and inflammation in osteoarthritis. Trop J Pharm Res 2018; 17(4):577-582 doi: 10.4314/tjpr.v17i4.2

© 2018 The authors.
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Abstract

Purpose: To prepare and evaluate sustained-release ketoprofen implants for prolonged drug release and activity.

Methods: Ketoprofen implants were prepared with poly (lactic-co-glycolic acid) (PLGA) and chitosan in the form of tablets. The implants were analyzed for drug loading, thickness, hardness, swelling, in vitro drug release, as well as in vivo analgesic and anti-inflammatory activities.

Results: The implants were round, smooth in appearance, uniform in thickness and showed no cracks or physical defects on the surface. Their friability was < 1 % while drug content ranged from 89.98 ± 2.06 to 92.95 ± 1.65 %. In vitro drug release ranged from 70.23 to 92.04 % at the end of 5 days. Implants containing higher amounts of PLGA produced the highest swelling (40.24 ± 1.08 %). Implant IKT3 showed maximum analgesic activity (7.75 ± 1.00 s) and shortest time of maximum analgesia (2.5 h) in hot plate method. Inhibition of rat paw edema for IKT1, IKT2 and IKT3 was 79.95, 69.98 and 82.24 %, respectively, after 24 h.

Conclusion: Ketoprofen-loaded implant IKT3 (4:4:2 ratio of PLGA, chitosan and ketoprofen) provides relatively quick onset and prolonged duration of analgesic effect. Thus, ketoprofen implants have a potential for development into therapeutic products for prolonged management of pain and inflammation in osteoarthritis.

Keywords: Osteoarthritis, Ketoprofen implant, Prolonged analgesia, Poly(lactic-co-glycolic acid), Chitosan