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Nanoparticles of esterified polymalic acid for controlled anticancer drug release

机译:用于控制抗癌药物释放的酯化聚苹果酸纳米颗粒

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摘要

Esterification of microbial poly(malic acid) is performed with either ethanol or 1-butanol to obtain polymalate conjugates capable to form nanoparticles (100–350 nm). Degradation under physiological conditions takes place with release of malic acid and the corresponding alcohol as unique degradation products. The anticancer drugs Temozolomide and Doxorubicin are encapsulated in nanoparticles with efficiency of 17 and 37%, respectively. In vitro drug release assays show that Temozolomide is almost completely discharged in a few hours whereas Doxorubicin is steadily released along several days. Drug-loaded nano-particles show remarkable effectiveness against cancer cells. Partially ethylated poly(malic acid) nano-particles are those showing the highest cellular uptake.
机译:用乙醇或1-丁醇对微生物聚(苹果酸)进行酯化,以获得能够形成纳米颗粒(100-350 nm)的聚苹果酸结合物。在生理条件下降解发生,苹果酸和相应的醇作为独特的降解产物释放出来。将抗癌药替莫唑胺和阿霉素分别封装在纳米颗粒中,效率分别为17%和37%。体外药物释放试验表明,替莫唑胺在数小时内几乎完全排出,而阿霉素则在数天内稳定释放。载有药物的纳米颗粒显示出对癌细胞的显着功效。部分乙基化的聚(苹果酸)纳米颗粒是显示出最高细胞摄取的颗粒。

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