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

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. ARTICLE HISTORY

Nanosystems for the Encapsulation of Natural Products: The Case of Chitosan Biopolymer as a Matrix

“…Oh et al [ 65 ] evaluated the physicochemical characteristics of chitosan-based film forming gel containing ketoprofen (CbFG). More specifically, CbFG was prepared with chitosan, lactic acid and various skin permeation enhancers.…”

<p>Film-Forming Sprays for Topical Drug Delivery</p>

“…Polymers can also prevent the transformation of molecules, such as the formation of unexpected crystals. 50 General considerations in the selection of polymers are its ease of being washed away by water, stability, biodegradability, and non-irritating properties. 10 Polymers used in FFS can be natural or synthetic (see Tables 1 and 2 ), as long as they have in situ gel or viscoelastic properties.…”

Controlled Release Film Forming Systems in Drug Delivery: The Potential for Efficient Drug Delivery

“…Another strategy that has been used to control drug release is a modification of the film-forming polymer as a functional excipient. Oh et al successfully grafted oleic acid on chitosan to increase drug skin permeation [72]. The inhibition of drug crystallinity formation and modulation of polymeric globules on the film caused by these grafts led to the improvement in drug permeability [72].…”

“…Oh et al successfully grafted oleic acid on chitosan to increase drug skin permeation [72]. The inhibition of drug crystallinity formation and modulation of polymeric globules on the film caused by these grafts led to the improvement in drug permeability [72]. In another study, Hazel et al used lipidic medium-chain triglycerides in a hydrophobic polymer (Eudragit ® and Dermacryl ® ) or hydrophilic polymer (hydroxypropyl cellulose) for an FFS to investigate betamethasone-17-valerate uptake into the skin [73].…”