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载柔红霉素和汉防己甲素的聚乳酸羟基乙酸-聚赖氨酸-聚乙二醇纳米粒的制备
  • ISSN号:1001-2494
  • 期刊名称:中国药学杂志
  • 时间:2014.10.22
  • 页码:1820-1826
  • 分类:R944[医药卫生—药剂学;医药卫生—药学]
  • 作者机构:[1]南京工业大学药学院,南京211816, [2]东南大学医学院,南京210009
  • 相关基金:国家自然科学基金资助项目(81170492);江苏省博士后科研资助计划(1301012A);江苏政府留学奖学金(2013)
  • 相关项目:化疗药和中药与转铁蛋白纳米载体的设计及逆转白血病耐药的机制研究
中文摘要:

目的制备包载柔红霉素-汉防己甲素的聚乳酸羟基乙酸-聚赖氨酸-聚乙二醇(PLGA-PLL-PEG)纳米粒。方法以合成高分子聚合物聚乳酸羟基乙酸-聚赖氨酸-聚乙二醇作为载体,采用复乳化溶剂挥发法制备包载柔红霉素与汉防己甲素的纳米粒;动态光散射粒径仪和透射电镜测定纳米粒的粒径分布、Zeta电位及表面形态;紫外分光光度计测定柔红霉素的包封率及载药量,HPLC测定汉防己甲素的包封率及载药量;以pH 7.4磷酸盐缓冲液(PBS)作为释放介质,考察载药纳米粒的体外释放行为。结果纳米粒平均粒径为(213.0±12)nm,Zeta电位为-19.16 mV,柔红霉素载药量为(3.63±0.15)%,包封率为(70.23±1.91)%,汉防己甲素载药量为(4.27±0.12)μg·mg-1,包封率为(86.5±0.7)%,7 d两药累积释放率大于80%。结论复乳化溶剂挥发法工艺简便可行,结果稳定,且制备的柔红霉素-汉防己甲素聚乳酸羟基乙酸-聚赖氨酸-聚乙二醇纳米粒在体外具有一定缓释效果。

英文摘要:

OBJECTIVE To prepare PLGA-PLL-PEG nanoparticles simultaneously loaded with daunorubicln (DNR) and tetran- drine (Tet). METHODS A functional polymer composed of PLGA, PLL and PEG was synthesized and used as a carrier material for a drug delivery system of nanoparticles. A modified double-emulsion solvent evaporation/diffusion method was used to prepare the nan- oparticles. A Zetasizer 3000HS system and transmission electron microscopy were used to determine the particle size distribution, Zeta potential and surface morphology of the nanopartieles. UV spectrophotometer and HPLC were used to determine the encapsulation efficiency and drug loading of daunorubicin. HPLC was used to determine the encapsulation efficiency and drug loading of tetrandrine, respectively. The release rates of DNR and Tet from DT-PLCA-PLL-PEG-NPs in vitro were evaluated at ( 37 ± 0. 5 )℃ using the dialysis bag technique in pH 7. 4 phosphate buffered saline (PBS). RESULTS The mean particle size of the nanoparticles produced by the optimized process was (213.0 ± 12) nm ( n = 3 ) with a relatively low polydispersity index [ ( 0. 075± 0. 023 ) , n = 3 ]. TEM examination showed that the nanoparticles were spherical with a smooth surface. The drug loadings were (3.63 ± 0. 15 )% for DNR and (4. 27 ± 0. 13)% for Tet (n =3). The entrapment efficieneies were(70. 23 ± 1.91 )% for DNR and(86. 5 ±0. 7)% for Tet (n =3) , respectively. DNR and Tet could be sustainedly released over one week. CONCLUSION Double emulsion solvent evaporation method is simple and feasible. The prepared PLGA-PLL-PEG nanoparticles loaded with DNR and Tet have significant sustained release effect.

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期刊信息
  • 《中国药学杂志》
  • 中国科技核心期刊
  • 主管单位:中国科学技术协会
  • 主办单位:中国药学会
  • 主编:桑国卫
  • 地址:北京市朝阳区建外大街四号建外SOHO九号楼18层
  • 邮编:100022
  • 邮箱:zgyxzz@cpa.org.cn
  • 电话:010-58698009
  • 国际标准刊号:ISSN:1001-2494
  • 国内统一刊号:ISSN:11-2162/R
  • 邮发代号:2-232
  • 获奖情况:
  • 首届国家期刊奖,第一、二届全国优秀科技期刊一等奖,中国期刊方阵“双高”期刊
  • 国内外数据库收录:
  • 美国国际药学文摘,美国化学文摘(网络版),荷兰文摘与引文数据库,荷兰医学文摘,日本日本科学技术振兴机构数据库,中国中国科技核心期刊,中国北大核心期刊(2004版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版),英国英国皇家化学学会文摘,中国北大核心期刊(2000版)
  • 被引量:54982