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›› 2004, Vol. 4 ›› Issue (2): 155-159.

• 过程与工艺 • 上一篇    下一篇

白蛋白纳米球药物载体的制备及表征

王恺,马光辉   

  1. 中国科学院过程工程研究所生化工程国家重点实验室
  • 出版日期:2004-04-20 发布日期:2004-04-20

Preparation and Characterization of Albumin Nanospheres as Drug Carrier

WANG Kai,MA Guang-hui   

  1. 中国科学院过程工程研究所生化工程国家重点实验室
  • Online:2004-04-20 Published:2004-04-20

摘要: 以超声乳化-化学交联方法制备了粒径为60~100 nm的负载丝裂霉素的白蛋白纳米球. 含有丝裂霉素和白蛋白的水相经超声乳化,在油相中形成纳米乳滴,然后加入戊二醛,使纳米乳滴发生交联形成纳米球. 通过比较形成乳液的稳定性选择了最适的乳化剂,系统考察了交联剂戊二醛的用量对所制纳米球性质的影响. 结果表明,戊二醛用量增加,则纳米球产率、载药量和药物包封率均增加,而粒径和溶胀度下降,体外释药速度亦下降. 戊二醛用量使醛基与白蛋白氨基摩尔比为16:1时最佳. 纳米球的体外释药为双相释药,两个释药相均符合Higuchi方程.

关键词: 白蛋白纳米球, 制备, 体外释药, 丝裂霉素

Abstract: Mitomycin-loaded albumin nanospheres sized between 60 and 100 nm were prepared by the ultrasonic emulsification-crosslinking method. After the albumin aqueous phase containing mitomycin was emulsified into the oil phase by the ultrasonifier to obtain the nanodroplets, glutaraldehyde was added to crosslink the nanodroplets. The optimal emulsifier was chosen by comparing the stability of emulsion prepared with various emulsifiers. It was found that the most stable W/O emulsion was obtained when Arlacel 83 was used as the emulsifier. The influence of the amount of glutataldehyde on the properties of the albumin nanospheres was investigated. It was found that the yield and drug content of nanospheres and loading efficiency of the drug increased, while the diameter and swelling degree of nanospheres, and the rate of drug release in vitro decreased, with the increase of the amount of gluataraldehyde. The optimal amount of glutaraldehyde corresponds to the ratio of aldehyde group to amino group being 16:1. The drug release in vitro can be divided into two phases, both of which can be expressed with the Higuchi equation.

Key words: albumin nanospheres, preparation, in vitro drug release, mitomycin