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Drug Deliv. 2017 Nov;24(1):1056-1066. doi: 10.1080/10717544.2017.1346001.

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

Author information

1
a Department of Pharmacy , Chungbuk National University , Cheongju , Republic of Korea.
2
b Dong-a Pharmaceutical Research Laboratory , Yongin , Republic of Korea.
3
c Department of Pharmaceutical Engineering , Cheongju University , Cheongju , Republic of Korea.
4
d College of Pharmacy and Research Institute of Pharmaceutical Sciences , Gyeongsang National University , Jinju , Republic of Korea.
5
e College of Pharmacy , Woosuk University , Wanju-gun , Republic of Korea.
6
f School of Pharmacy , Sunkyunkwan University , Suwon , Republic of Korea.

Abstract

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.

KEYWORDS:

Chitosan-based film-forming gel; anti-inflammatory and analgesic effects; chitosan; dermal drug delivery systems; ketoprofen; oleic acid

PMID:
28687046
DOI:
10.1080/10717544.2017.1346001
[Indexed for MEDLINE]

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