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载多聚电解质的聚合物胶束用于多西紫杉醇的控制释放。

Polyelectrolyte coated polymeric nanoparticles for controlled release of docetaxel.

机构信息

Department of Biosciences and Bioengineering, IIT Bombay, Powai, Mumbai 400076, India.

出版信息

J Biomed Nanotechnol. 2012 Feb;8(1):19-28. doi: 10.1166/jbn.2012.1355.

DOI:10.1166/jbn.2012.1355
PMID:22515091
Abstract

Polyelectrolyte coatings are effective means of minimizing the rate of release of small molecules from a nanoparticle system. The current investigation aim at developing biodegradable drug delivery carriers composed of three types of polymers viz poly(lactide-co-glycolic) acid [PLGA], poly(lactide-co-glycolic) acid-polyethylene imine [PLGA-PEI] and poly lactic acid [PLA]. The PLGA and PLGA-PEI nanoparticles were in the size range approximately 150 nm while PLA nanoparticles were approximately 80 nm in size respectively. The nanoparticles were found to encapsulate 66%, 62% and 65% of the hydrophobic drug, Docetaxel (DOCE) respectively. "Layer by Layer (LbL)" self assembly technique was then performed to coat these particles with polyelectrolyte thin films (PEs). DLS studies showed hydrodynamic diameter of 330 nm, 350 nm and 310 nm for the coated PLGA, PLGA-PEI and PLA nanoparticles respectively, while SEM and TEM studies demonstrated that after coating the particle sizes were approximately 200 nm for all the three nanoparticles. In vitro drug release studies demonstrated that at the end of 24 hours, about 83%, 90% and 88% of drug was released from uncoated PLA, PLGA-PEI and PLGA nanoparticles respectively. Using LbL coating, the same amount of the drug was found to be released in a sustained way for up to 7 days for PLGA and up to 6 days for PLGA-PEI and PLA nanoparticles. In vitro cytocompatibility studies were carried out with each system and the cell viability at end of 48 hours was found to be in the range of 70% to 100%. Current approach of sustained drug delivery can help in improving the therapeutic efficiency of the breast cancer drug, DOCE.

摘要

聚电解质涂层是最小化纳米颗粒系统中小分子释放速率的有效手段。本研究旨在开发由三种聚合物组成的可生物降解药物输送载体,即聚(丙交酯-乙交酯)酸[PLGA]、聚(丙交酯-乙交酯)酸-聚乙烯亚胺[PLGA-PEI]和聚乳酸[PLA]。PLGA 和 PLGA-PEI 纳米颗粒的粒径约为 150nm,而 PLA 纳米颗粒的粒径约为 80nm。研究发现,这些纳米颗粒分别包封了 66%、62%和 65%的疏水性药物多西他赛(DOCE)。然后,采用“层层自组装(LbL)”技术在这些颗粒上涂覆聚电解质薄膜(PEs)。DLS 研究表明,涂覆后的 PLGA、PLGA-PEI 和 PLA 纳米颗粒的水动力直径分别为 330nm、350nm 和 310nm,而 SEM 和 TEM 研究表明,涂覆后,三种纳米颗粒的粒径均约为 200nm。体外药物释放研究表明,在 24 小时结束时,未涂覆的 PLA、PLGA-PEI 和 PLGA 纳米颗粒分别释放了约 83%、90%和 88%的药物。使用 LbL 涂层,发现相同量的药物能够以持续的方式释放,PLGA 可持续 7 天,PLGA-PEI 和 PLA 可持续 6 天。对每个系统进行了体外细胞相容性研究,发现 48 小时结束时的细胞存活率在 70%至 100%之间。这种持续药物输送的方法可以帮助提高乳腺癌药物多西他赛的治疗效率。

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