Chitosan-Modified PLGA Nanoparticles for Control-Released Drug Delivery
Chitosan-Modified PLGA Nanoparticles for Control-Released Drug Delivery
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DOI：
10.3390/polym11020304
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发表时间：
2019-02-01
期刊：
影响因子：
5
通讯作者：
Le, Yuan
中科院分区：
文献类型：
--
作者：
Lu, Boting;Lv, Xikun;Le, Yuan
聚乳酸-乙醇酸纳米粒子（PLGA NP）因其生物相容性和生物降解性而被公认为理想的药物递送载体。为了克服药物突释的缺点，采用壳聚糖(CS)对PLGA纳米粒子进行修饰。在这项工作中，利用高重力旋转填充床（RPB）制备了不同CS与PLGA比例的CS-PLGA纳米粒子。随着CS用量的增加，粒径从132.8±1.5 nm增加到172.7±3.2 nm，zeta电位从-20.8±1.1 mV增加到25.6±0.6 mV，药物包封率从65.8%增加到87.1%。 CS修饰后PLGA NPs的初始突释量降低，2 h后累积释放量分别为66.9%、41.9%、23.8%和14.3%。 CS修饰的PLGA NPs在pH5.5下的药物释放比在pH 7.4下更快。与 PLGA NP 相比，CS 修饰的 PLGA NP 的细胞摄取增加，但细胞活力降低。总之，这些结果表明CS修饰的负载PTX的PLGA NPs具有药物持续释放和增强药物毒性的优点，表明CS修饰的NPs可以用作抗癌药物的载体。
Poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs) are well recognized as an ideal drug delivery carrier for their biocompatibility and biodegradability. In order to overcome the disadvantage of drug burst release, chitosan (CS) was used to modify the PLGA nanoparticles. In this work, CS-PLGA nanoparticles with different ratio of CS to PLGA were prepared using high-gravity rotating packed bed (RPB). With the increase of amount of CS, the particle size increased from 132.8 +/- 1.5 nm to 172.7 +/- 3.2 nm, zeta potential increased from -20.8 +/- 1.1 mV to 25.6 +/- 0.6 mV, and drug encapsulation efficiency increased from 65.8% to 87.1%. The initial burst release of PLGA NPs reduced after being modified by CS, and the cumulative release was 66.9%, 41.9%, 23.8%, and 14.3%, after 2 h, respectively. The drug release of CS-modified PLGA NPs was faster at pH5.5 than that at pH 7.4. The cellular uptake of CS-modified PLGA NPs increased compared with PLGA NPs, while cell viability was reduced. In conclusion, these results indicated that CS-modified, PTX-loaded PLGA NPs have the advantages of sustained drug release and enhanced drug toxicity, suggesting that CS-modified NPs can be used as carriers of anticancer drugs.