摘要
目的以脂溶性药物盐酸利多卡因为模型药，制备载药传递体，即盐酸利多卡因柔性纳米脂质体，并对其质量进行评价。方法以磷脂、胆固醇为膜材，加入表面活性剂胆酸钠，采用真空旋转蒸发法制备盐酸利多卡因柔性纳米脂质体。用马尔文激光粒度分析仪测盐酸利多卡因柔性纳米脂质体粒度分布，原子力显微镜观察盐酸利多卡因柔性纳米脂质体形态，以高效液相色谱法测定盐酸利多卡因含量，并对制剂的回收率、精密度和包封率进行研究，以离心法测定利多卡因柔性纳米脂质体的包封率。结果利多卡因柔性纳米脂质体为乳白色、近透明的胶体溶液，原子力显微镜下呈规则圆形或椭圆形，利多卡因柔性纳米脂质体的粒径为106±6.88nm。文中建立了盐酸利多卡因柔性纳米脂质体含量的测定方法。用美国戴安公司BDSC18柱（4.6×200mm，5μm），流动相甲醇∶冰醋酸∶三乙胺∶水为50∶2∶1∶47，流速是0.8ml/min。结果显示利多卡因检测浓度线性范围为20-500μg/ml（r=0.99995），回收率为100.4%±0.44%（n=3），包封率为80.1%±1.02%（n=5）。利多卡因柔性纳米脂质体具有良好的稳定性，对皮肤无刺激性。结论利多卡因柔性纳米脂质体制备工艺可行，质量控制方法简便、可靠。
Objective To prepare drug loading transfersomes （lidocaine ultradeformable nano-liposomes） with lidocaine hydrochloride （LDH）, a lipophilic drug, as model, and to evaluate their qualities. Methods Phosphatidylcholine and cholesterol were used as liposome materials, then sodium cholate was added as a surface acting agent. Lidocaine ultradeformable nano-liposomes were prepared by using a vacuum rotary evaporation method. The particle size distribution of lidocaine ultradeformable nano-liposomes was determined by Malvem laser particle size analysator, the morphology of lidocaine ultradeformable nano-liposomes was identified by atomic force microscope, the concentration of lidocaine hydrochloride was determined by high efficiency liquid chromatography. The recovery rate, precision rate, and the entrapment efficiency of lidocaine ultradeformable nano-liposomes were studied, and the lidocaine ultradeformable nano-liposomes entrapment efficiency was determined by centrifngation. Results Lidocaine ultradeformable nano-liposomes was a colloid solution in ivory white color, nearly transparent, and appeared as regular, round or elliptical under atomic force microscope. Mean diameter of the lidocaine ultradeformable nano-liposomes was （106±6. 88） nm. A high performance liquid chromatography （HPLC） method for the measurement of lidocaine ultradeformable nano-liposomes was developed, h was performed by using BDS C18 column （4. 6×200 mm, 5μm）. On the mobile phase, colonial spirit： glacial acetic acid： triethylamine： water was 50： 2：1：47; the flow rate was 8ml/min, The linear detection concen tration range of lidocaine was 20- 500μg/ml （ r=0. 999 95） with average recovery rate at （100. 4±0.44） % （n=3）, and entrapment efficiency at （80. 1±1.02）% （n=5）. The lidocaine ultradeformable nano-liposomes had a good stability, and it showed no skin irritation. Conclusion The technique of preparing lidocaine ultradeformable nano-liposome is suitable, convenient and reliable in quality.
出处
《解放军医学杂志》
CAS
CSCD
北大核心
2007年第10期1091-1093,共3页
Medical Journal of Chinese People's Liberation Army
基金
国家863计划资助项目(2003AA217072)
关键词
利多卡因
柔性纳米脂质体
含量测定
高效液相色谱法
lidocaine
ultradeformable nano-liposomes
content determination
high efficiency liquid chromatography
