PLGA微米与纳米载药颗粒用于药物携带与递送的比较研究

 

目的 通过评价聚乳酸-羟基乙酸共聚物(polylactic acid-glycolic acid copolymer,PLGA)微米颗粒(micron particle,MP)与纳米颗粒(nanoparticle,NP)的表面特征、载药能力、药物缓释能力及细胞吞噬能力等方面来比较阐述PLGA纳米与微米颗粒在细胞预处理与修饰中的合理应用。方法 分别制备PLGA纳米颗粒与微米颗粒,并进行表征;随后,比较其载药能力,并对药物的释放特征进行测定;最后,在不同时间点通过荧光强度评价两种颗粒与细胞结合或进入细胞的能力。结果 所制备的纳米粒与微米颗粒粒径分别分布在200~300 nm和2~4 μm;两种颗粒载药量相当,分别为14.3%和14.1%;在药物缓释方面,纳米颗粒存在显著的早期突释现象;微米颗粒释放缓慢,持续缓释可达一周左右;粒径相对小的纳米粒更容易进入或与细胞结合,共孵育12 h即达到最大值,微米颗粒相对较慢,最大值出现在共孵育24 h后。结论 PLGA纳米颗粒作为药物载体更适合于急性组织或细胞保护,微米颗粒更适合于慢性持续性保护。

Comparison of PLGA Micron and Nano Drug-loaded Particles for Drug Carrier and Delivery

Objective The surface characteristics, drug delivery capacity, chemical drug delivery ability, nucleic acid sustained release ability and cell phagocytosis of poly (lactic acid-glycolic acid) (polylactic acid-glycolic acid copolymer,PLGA) microparticles (micron particle,MP) and nanoparticles (nanoparticle,NP) were evaluated to compare the application of PLGA nanoparticles and micron particles in cell pretreatment and modification.Methods PLGA nanoparticles and microparticles were prepared and characterized respectively. Then, drug loading capacity was compared and drug release characteristics were determined. Finally, the ability of PLGA nanoparticles to bind to cells or enter cells was evaluated by fluorescence intensity at different time points. Results The particle size of the prepared nanoparticles and microparticles were distributed at 200-300 nm and 2-4 μm, respectively. The loading of the two particles was 14.3% and 14.1%, respectively. In the aspect of drug sustained release, the nanoparticles exhibited significant early burst release; the release of microparticles was slow and sustained release could reach about one week; the relatively small nanoparticles were easier to enter or combine with cells, and incubated for 12 hours. That is to say, the micron particles are relatively slow to reach the maximum value, and the maximum value appears after 24 hours of incubation. Conclusions PLGA nanoparticles are more suitable for acute tissue or cell protection, and microparticles are more suitable for chronic persistent protection.