Formulation and in vitro/in vivo evaluation of chitosan-based film forming gel containing ketoprofen

• Main Authors: Dong-Won Oh, Ji-Hyun Kang, Hyo-Jung Lee, Sang-Duk Han, Min-Hyung Kang, Yie-Hyuk Kwon, Joon-Ho Jun, Dong-Wook Kim, Yun-Seok Rhee, Ju-Young Kim, Eun-Seok Park, Chung-Woong Park
• Format: Article
• Language: English
• Published: Taylor & Francis Group 2017-01-01
• Series: Drug Delivery
• Subjects: chitosan-based film-forming gel; chitosan; oleic acid; ketoprofen; dermal drug delivery systems; anti-inflammatory and analgesic effects
• Online Access: http://dx.doi.org/10.1080/10717544.2017.1346001

The film forming gel, adhered to skin surfaces upon application and formed a film, has an advantage onto skin to provide protection and continuous drug release to the application site. This study aimed to prepare a chitosan-based film forming gel containing ketoprofen (CbFG) and to evaluate the CbFG and film from CbFG (CbFG-film). CbFG were prepared with chitosan, lactic acid and various skin permeation enhancers. The physicochemical characteristics were evaluated by texture analysis, viscometry, SEM, DSC, XRD and FT-IR. To identify the mechanism of skin permeation, in vitro skin permeation study was conducted with a Franz diffusion cell and excised SD-rat and hairless mouse dorsal skin. In vivo efficacy assessment in mono-iodoacetate (MIA)-induced rheumatoid arthritis animal model was also conducted. CbFG was successfully prepared and, after applying CbFG to the excised rat dorsal skin, the CbFG-film was also formed well. The physicochemical characteristics of CbFG and CbFG-film could be explained by the grafting of oleic acid onto chitosan in the absence of catalysts. In addition, CbFG containing oleic acid had a higher skin permeation rate in comparison with any other candidate enhancers. The in vivo efficacy study also confirmed significant anti-inflammatory and analgesic effects. Consequently, we report the successful preparation of chitosan-based film forming gel containing ketoprofen with excellent mechanical properties, skin permeation and anti-inflammatory and analgesic effects.