Singh S, Gajra B, Rawat M, Muthu M S
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221005, India.
Pak J Pharm Sci. 2009 Apr;22(2):193-8.
The aim of this study was to evaluate and compare the in vitro and in vivo transdermal potential of bioadhesive gels of ketoprofen by using gelling polymers like sodium carboxymethylcellulose, xanthan gum, poloxamer 407 and carbopol 934P as bioadhesive polymer with and without penetration enhancer (oleic acid). The effect of oleic acid as a penetration enhancer was examined when it was added to the bioadhesive formulations. Gels were evaluated for bioadhesive force and viscosity. To study the in vitro potential of these formulations, permeation studies were performed with Franz diffusion cell using excised rat abdominal skin. Carrageenan induced rat paw edema model was used to investigate their in vivo performance. The commercial formulation of ketoprofen was used as a reference formulation. The in vitro permeation studies indicate that ketoprofen bioadhesive gel of poloxamer 407 with penetration enhancer was superior to gels of sodium carboxymethylcellulose and xanthan gum with penetration enhancer (oleic acid). The permeation rate of ketoprofen from poloxamer 407 based bioadhesive gel with 15% v/w penetration enhancer was higher (rat abdominal skin flux = 0.421 +/- 0.032 mg/cm(2)/h) than the permeation rate of sodium carboxymethylcellulose and xanthan gum based bioadhesive gel with 15% v/w penetration enhancer. In the paw edema test poloxamer 407 based bioadhesive gel with 15% v/w penetration enhancer showed the best permeation and effectiveness. The in vitro and in vivo studies showed that bioadhesive gels of ketoprofen could be used for effective therapy.
本研究的目的是通过使用羧甲基纤维素钠、黄原胶、泊洛沙姆407和卡波姆934P等胶凝聚合物作为生物黏附聚合物，在有和没有渗透促进剂（油酸）的情况下，评估并比较酮洛芬生物黏附凝胶的体外和体内透皮潜力。当将油酸作为渗透促进剂添加到生物黏附制剂中时，研究了其效果。对凝胶的生物黏附力和粘度进行了评估。为了研究这些制剂的体外潜力，使用Franz扩散池，采用切除的大鼠腹部皮肤进行了渗透研究。使用角叉菜胶诱导的大鼠足爪水肿模型来研究它们的体内性能。酮洛芬的市售制剂用作参比制剂。体外渗透研究表明，含有渗透促进剂的泊洛沙姆407酮洛芬生物黏附凝胶优于含有渗透促进剂（油酸）的羧甲基纤维素钠和黄原胶凝胶。含有15% v/w渗透促进剂的泊洛沙姆407基生物黏附凝胶中酮洛芬的渗透速率较高（大鼠腹部皮肤通量 = 0.421 +/- 0.032 mg/cm(2)/h），高于含有15% v/w渗透促进剂的羧甲基纤维素钠和黄原胶基生物黏附凝胶。在足爪水肿试验中，含有15% v/w渗透促进剂的泊洛沙姆407基生物黏附凝胶显示出最佳的渗透性和有效性。体外和体内研究表明，酮洛芬生物黏附凝胶可用于有效治疗。
