| 引用本文: | 时军,张慧迪,吴秀君,陈桂添,吴艳婷,郭思旖.基于pH梯度载药技术的咪喹莫特脂质体的制备工艺研究[J].中国现代应用药学,2018,35(3):325-329. |
| SHI Jun,ZHANG Huidi,WU Xiujun,CHEN Guitian,WU Yanting,GUO Siyi.Study of Preparation Technology of Imiquimod Liposomes Based on pH Gradient Active Drug Loading Method[J].Chin J Mod Appl Pharm(中国现代应用药学),2018,35(3):325-329. |
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| 摘要: |
| 目的 根据咪喹莫特的理化性质，利用pH梯度主动载药技术制备脂质体，考察其性状、粒径、表面电荷及体外释药特征。方法 葡聚糖凝胶滤过法测定脂质体的包封率，以包封率与成型性为主要指标筛选制备方法，考察水化液的种类、pH值、离子强度及pH梯度载药、磷脂-胆固醇比例、脂药比、维生素E用量对包封率的影响；正交试验优化咪喹莫特脂质体的处方，考察脂质体样品在0~4℃下的稳定性。结果 按处方咪喹莫特50 mg、大豆卵磷脂400 mg、胆固醇130 mg、油酸10 mg、维生素E 5 mg、柠檬酸pH 2.5缓冲液5 mL，采用薄膜分散法工艺制备脂质体样品，并进行pH梯度主动载药，pH值调至7.0。制得的咪喹莫特脂质体呈白色均匀的混悬液，脂质体微粒圆整，分散性好，粒径（347±21）nm，包封率（81.2±1.9）%，Zeta电位（-12.19±1.7）mV。结论 pH梯度主动载药技术适于咪喹莫特脂质体的制备。 |
| 关键词: 咪喹莫特脂质体 pH梯度主动载药技术 正交试验设计 体外释药特征 |
| DOI：10.13748/j.cnki.issn1007-7693.2018.03.005 |
| 分类号:R943 |
| 基金项目:广东省科技计划项目（2014A020212417）；广东省高等学校优秀青年教师培养计划资助项目（YQ2015099） |
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| Study of Preparation Technology of Imiquimod Liposomes Based on pH Gradient Active Drug Loading Method |
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SHI Jun1, ZHANG Huidi1, WU Xiujun2, CHEN Guitian1, WU Yanting1, GUO Siyi1
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1.Department of Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, China;2.Guangdong Women and Children Hospital, Guangzhou 511400, China
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| Abstract: |
| OBJECTIVE To prepare imiquimod(Imiq) liposomes using pH gradient active drug loading technology based on the physicochemical properties of Imiq, and investigate the characters, particle size, surface charge and release characteristics in vitro. METHODS To determine the encapsulation efficiency by gel filtration method, and use encapsulation efficiency and formability as the main index of preparation screening. To study the impact on entrapment efficiency of the factors involving hydration liquid type, pH value, ionic strength and pH gradient drug loading, phospholipid and cholesterol ratio, drug lipid ratio and the dosage of VE. To optimize the prescription composition of imiquimod liposomes by orthogonal test prescription, and then to observe the stability of liposome samples at 0-4℃. RESULTS The prescription composition of imiquimod liposomes were 50 mg of Imiq, 400 mg of soybean soft phospholipid, 130 mg of cholestorol, 10 mg of oleic acid, 5 mg of vitamin E, 5 mL of citric acid pH 2.5 buffer, and use THF-pH gradient active loading technology, the pH value was adjusted to 7.0. The prepared Imiq liposomes showed white uniform suspension, had round and well dispersed particles, and the particle size was (347±21)nm, encapsulation efficiency was (81.2±1.9)%, Zeta potential was (-12.19±1.7)mV. CONCLUSION The pH gradient active drug delivery technique is suitable for the preparation of Imiq liposomes. |
| Key words: imiquimod liposomes pH gradient active drug loading technology orthogonal experimental design release characteristics in vitro |
