| 引用本文: | 华育晖,汪维佳,王刚,郑小丽,沈雁.奥沙利铂长循环脂质体的制备和体内外评价[J].中国现代应用药学,2018,35(3):335-339. |
| HUA Yuhui,WANG Weijia,WANG Gang,ZHENG Xiaoli,SHEN Yan.Preparation and Evaluation of Oxaliplatin Long-circulating Liposomes[J].Chin J Mod Appl Pharm(中国现代应用药学),2018,35(3):335-339. |
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| 奥沙利铂长循环脂质体的制备和体内外评价 |
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华育晖1, 汪维佳1, 王刚2, 郑小丽1, 沈雁3
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1.杭州市第一人民医院集团, 杭州市肿瘤医院药剂科, 杭州 310002;2.杭州市第一人民医院药剂科, 杭州 310006;3.中国药科大学, 南京 211198
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| 摘要: |
| 目的 制备奥沙利铂长循环脂质体（long-circulating liposome，LCL），并考察其在体内外的性质。方法 利用逆相蒸发法制备奥沙利铂LCL，观察其形态，测定粒径电位、包封率、载药量等理化性质。采用SD大鼠进行药动学研究，考察脂质体在动物体内的药动学参数与生物利用度。结果 奥沙利铂LCL的平均粒径为（195.1±1.8）nm，电位为（-29.53±0.57）mV，包封率为18%，载药量为2.4%。药动学研究结果显示，奥沙利铂的血浆清除率是LCL的71倍，LCL能够显著降低奥沙利铂的血浆清除率，延长药物体内滞留时间，LCL的药时曲线下面积（AUC）是奥沙利铂溶液的70倍，显著提高了生物利用度。结论 本研究选择逆相蒸发法制备并筛选出具有合适包封率，低毒性和高药效的奥沙利铂LCL。 |
| 关键词: 奥沙利铂 长循环脂质体 理化性质 药动学 |
| DOI：10.13748/j.cnki.issn1007-7693.2018.03.007 |
| 分类号:R941 |
| 基金项目: |
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| Preparation and Evaluation of Oxaliplatin Long-circulating Liposomes |
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HUA Yuhui1, WANG Weijia1, WANG Gang2, ZHENG Xiaoli1, SHEN Yan3
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1.Pharmacy Department of Hangzhou Cancer Hospital, Hangzhou First People's Hospital Group, Hangzhou 310002, China;2.Pharmacy Department of Hangzhou First People's Hospital, Hangzhou 310006, China;3.China pharmaceutical university, Nanjing 211198, China
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| Abstract: |
| OBJECTIVE To prepare oxaliplatin long-circulating liposomes(LCL) and perform evaluations in vitro and in vivo. METHODS Oxaliplatin-loaded LCL were prepared by reverse phase evaporation method. Physicochemical properties of LCL were investigated, including particle size and encapsulation efficiency(EE). Pharmacokinetic study was conducted on rat model. RESULTS The average particle size of oxaliplatin LCL was (195.1±1.8) nm and the potential was (-29.53±0.57) mV. In addition, the encapsulation efficiency was 18% and the drug loading was 2.4%. Pharmacokinetic studies showed that the plasma clearance rate of oxaliplatin is 71-fold LCL, so LCL could significantly reduce the plasma clearance rate of oxaliplatin and prolong drug the residence time in vivo. The AUC of LCL was 70-fold of that for oxaliplatin solution which significantly improved the bioavailability. CONCLUSION This study select reverse phase evaporation method to prepare and obtain the optimal oxaliplatin LCL with suitable entrapment efficiency, low toxicity and high efficacy. |
| Key words: oxaliplatin long-circulating liposome physicochemical property pharmacokinetic |
