Csóka G, Gelencsér A, Makó A, Marton S, Zelkó R, Klebovich I, Antal I
Department of Pharmaceutics, Semmelweis University, Hogyes E. Street 7, H-1092 Budapest, Hungary.
Int J Pharm. 2007 Jun 29;338(1-2):15-20. doi: 10.1016/j.ijpharm.2007.01.018. Epub 2007 Jan 19.
The purpose of the present study was to formulate a novel thermoresponsive membrane controlled therapeutic system from Metolose for possible transdermal application. Metolose gel shows thermal gelation property, which can be characterized by two (T(1), T(2)) temperatures. A sharp decrease of viscosity can be measured at T(1), but gelation can be observed at T(2). Different types of Metolose polymers were compared considering their thermoresponsive behaviour. Only thermal gelation was observed in the case of Metolose SM, while Metolose SH showed a sudden decrease of viscosity at T(1). Since this temperature is above the body temperature, so it should be shifted to the skin temperature in case of possible transdermal application. Modulation of thermoresponsibility was followed by rheological method, and the thermoresponsive drug release from Metolose gel was studied by static liberation test. Our results demonstrated that the effect of different salts (NaCl, NaHCO(3), KCl) of various concentrations in Metolose SH gel reduced T(1) to the skin temperature, which enabled enhanced drug release.
本研究的目的是用羟丙基甲基纤维素(Metolose)制备一种新型的热响应性膜控治疗系统,用于可能的透皮给药。Metolose凝胶具有热凝胶化特性,其可由两个温度(T(1)、T(2))来表征。在T(1)时可测得粘度急剧下降,但在T(2)时可观察到凝胶化现象。考虑到它们的热响应行为,对不同类型的Metolose聚合物进行了比较。在Metolose SM的情况下仅观察到热凝胶化,而Metolose SH在T(1)时粘度突然下降。由于该温度高于体温,因此在可能进行透皮给药的情况下应将其调节至皮肤温度。采用流变学方法对热响应性进行调节,并通过静态释放试验研究了Metolose凝胶的热响应性药物释放。我们的结果表明,Metolose SH凝胶中不同浓度的不同盐(氯化钠、碳酸氢钠、氯化钾)的作用将T(1)降低至皮肤温度,从而实现了增强的药物释放。