紫杉醇脂质体凝胶剂的制备及其镇痛抗炎作用

Preparation of Taxol-liposome Gel and Its Analgesic and Anti-inflammatory Effects

关键词:  紫杉醇  脂质体凝胶剂  镇痛  抗炎

Key words:  taxol  liposome gel  analgesic  anti-inflammatory

摘要:

目的 制备紫杉醇脂质体凝胶剂，对其镇痛抗炎作用进行初步研究。方法 薄膜分散法制备紫杉醇脂质体，用透射电镜观测其形态，用激光纳米粒度仪测定粒径大小及分布，用HPLC测定其包封率。脂质体进一步制成凝胶剂后，体外透皮实验测定其不同时间的体外透皮量，考察其体外透皮情况。大鼠角叉菜胶致足肿胀模型及小鼠甲醛致痛模型，考察紫杉醇脂质体凝胶剂的镇痛抗炎作用。结果 制得的紫杉醇脂质体形态规则、分布均匀，平均包封率为(73.6±0.3)% (n=3)，所得凝胶呈半透明状；体外透皮实验中，紫杉醇脂质体凝胶剂符合一级动力学方程，起到较好的缓释作用。抗炎实验中，与模型组比较，各给药组在一定时间内均能显著性减轻致炎足趾的肿胀程度(P<0.05)，并呈现明显的量效关系。甲醛致痛实验中，给药组与模型组比较，小鼠舔足次数明显减少(P<0.05)。结论 紫杉醇脂质体凝胶具有明显镇痛抗炎作用。

Abstract:

OBJECTIVE To prepare a liposome hydrogel taxol, study the analgesic and anti-inflammatory effects. METHODS Taxol-liposome gel was obtained by thin film dispersion method. The shape, size, size distribution and encapsulation efficiency were detected by transmission electron microscope(TEM), nano-particle size analyzer and HPLC, respectively. The gel was then prepared based on the liposome. The in vitro release of taxol-liposome gel in different time was detected with transdermal experiments. Observe its effect on mouse inflammatory model induced by carrageenin and the pain model induced by formaldehyde. RESULTS The shape of taxol-liposome was regular and narrowly-distributed, and its encapsulation efficiency was (73.6±0.3)%. The prepared gel was semitransparent. After that, transdermal experiments, taxol-liposome gel met a kinetic equation, played better sustained release. In vitro transdermal experiments, after 12 h taxol-liposome through maximum amount, played better sustained action. In inflammatory experiment, compared with the model group, the taxol-liposome gel produced significant inhibition on rat paw edema in a dose-dependent manner(P<0.05). In mouse formalin test, taxol-liposome gel reduced the number of writhing induced by acetic acid, significantly(P<0.05). CONCLUSION The taxol-liposome gel has significant analgesic and anti-inflammatory effects.