Oh Dong-Won, Kang Ji-Hyun, Lee Hyo-Jung, Han Sang-Duk, Kang Min-Hyung, Kwon Yie-Hyuk, Jun Joon-Ho, Kim Dong-Wook, Rhee Yun-Seok, Kim Ju-Young, Park Eun-Seok, Park Chung-Woong
a Department of Pharmacy , Chungbuk National University , Cheongju , Republic of Korea.
b Dong-a Pharmaceutical Research Laboratory , Yongin , Republic of Korea.
Drug Deliv. 2017 Nov;24(1):1056-1066. doi: 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.
这种成膜凝胶在应用时粘附于皮肤表面并形成薄膜,在皮肤上具有为应用部位提供保护和持续药物释放的优势。本研究旨在制备含酮洛芬的壳聚糖基成膜凝胶(CbFG),并评估CbFG及其形成的薄膜(CbFG-薄膜)。CbFG由壳聚糖、乳酸和各种皮肤渗透促进剂制备而成。通过质地分析、粘度测定、扫描电子显微镜(SEM)、差示扫描量热法(DSC)、X射线衍射(XRD)和傅里叶变换红外光谱(FT-IR)对其理化特性进行评估。为确定皮肤渗透机制,使用Franz扩散池以及切除的SD大鼠和无毛小鼠背部皮肤进行体外皮肤渗透研究。还在单碘乙酸(MIA)诱导的类风湿性关节炎动物模型中进行了体内疗效评估。成功制备了CbFG,将CbFG应用于切除的大鼠背部皮肤后,CbFG-薄膜也形成良好。在无催化剂的情况下,油酸接枝到壳聚糖上可解释CbFG和CbFG-薄膜的理化特性。此外,与任何其他候选促进剂相比,含油酸的CbFG具有更高的皮肤渗透速率。体内疗效研究也证实了其显著的抗炎和镇痛作用。因此,我们报道成功制备了含酮洛芬的壳聚糖基成膜凝胶,其具有优异的机械性能、皮肤渗透性以及抗炎和镇痛作用。