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分别采用去溶剂化法和乳化交联法制备多柔比星牛血清白蛋白(BSA)纳米粒,以BSA收率、包封率、载药量和粒径等为评价指标,优选处方工艺,并比较两种制备工艺所得制品的差异。结果表明,去溶剂化法和乳化交联法所得纳米粒外观均呈球形,差异不大,BSA收率、包封率、载药量、粒径及电位分别为96.5%、92.9%,98.5%、97.4%,4.3%、3.6%,132.4、172.9 nm,-27.7、-19.9 mV。但制备工艺对体外释放行为和大鼠体内药动学行为影响较大,去溶剂化法和乳化交联法制备的多柔比星BSA纳米粒在生理盐水中48 h累积释放率分别为44.2%、63.8%;大鼠尾静脉给药后,去溶剂化法和乳化交联法所得制品的AUC分别是原药的1.5倍(P<0.05)和1.1倍(P>0.05),前法所得纳米粒在大鼠体内具有一定的缓释效果,而后法所得制品没有。
The preparation of doxorubicin bovine serum albumin (BSA) nanoparticles by desolvation and emulsification cross-linking respectively was used as the evaluation index for BSA yield, entrapment efficiency, drug loading and particle size, The differences between the two preparations were also compared. The results showed that the appearance of the nanoparticles obtained by the desolvation and emulsification cross-linked were spherical, the difference was not significant, BSA yield, entrapment efficiency, drug loading, particle size and potential were 96.5%, 92.9%, 98.5% , 97.4%, 4.3%, 3.6%, 132.4, 172.9 nm, -27.7, -19.9 mV. However, the preparation process had a great effect on in vitro release behavior and pharmacokinetics in rats. The release rates of doxorubicin BSA nanoparticles prepared by desolvation and emulsification cross-linking in saline for 48 h were 44.2% , 63.8% respectively. The AUC of desolvated and emulsified cross-linked products after the tail vein injection in rats was 1.5 times (P <0.05) and 1.1 times (P> 0.05) Granules in rats with a sustained release effect, and after the law derived products did not.