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PLGA/聚合物脂质体用于靶向药物和基因共递药。

PLGA/polymeric liposome for targeted drug and gene co-delivery.

机构信息

Institute of Nanobiotechnology, School of Materials Science and Engineering, Tianjin University and Tianjin Key Laboratory of Composites and Functional Materials, Tianjin,300072, PR China.

出版信息

Biomaterials. 2010 Nov;31(33):8741-8. doi: 10.1016/j.biomaterials.2010.07.082. Epub 2010 Aug 19.

Abstract

Chemotherapy is one of the most effective approaches to treat cancers in the clinic, but the problems, such as multidrug resistance (MDR), low bioavailability and toxicity, severely constrain the further application of chemotherapy. Our group recently reported that cationic PLGA/folate coated PEGlated polymeric liposome core-shell nanoparticles (PLGA/FPL NPs). It was self-assembled from a hydrophobic PLGA core and a hydrophilic folate coated PEGlated lipid shell for targeting co-delivery of drug and gene. Hydrophobic drugs can be incorporated into the core and the cationic shell of the drug-loaded nanoparticles can be used to bind DNA. The drug-loaded PLGA/FPL NPs/DNA complexes offer advantages to overcome these problems mentioned above, such as co-delivery of drugs and DNA to improving the chemosensitivity of cancer cells at a gene level, and targeting delivery of drug to the cancer tissue that enhance the bioavailability and reduce the toxicity. The experiment showed that nanoparticles have core-shell structure with nanosize, sustained drug release profile and good DNA-binding ability. Importantly, the core-shell nanoparticles achieve the possibility of co-delivering drugs and genes to the same cells with high gene transfection and drug delivery efficiency. Our data suggest that the PLGA/FPL NPs may be a useful drug and gene co-delivery system.

摘要

化疗是临床上治疗癌症最有效的方法之一,但多药耐药性(MDR)、生物利用度低和毒性等问题严重限制了化疗的进一步应用。我们小组最近报道了阳离子 PLGA/叶酸修饰的聚乙二醇化聚合物脂质体核壳纳米粒(PLGA/FPL NPs)。它由疏水性 PLGA 内核和亲水性叶酸修饰的聚乙二醇化脂质外壳自组装而成,用于靶向共递送药物和基因。疏水性药物可以被包裹在核内,载药纳米粒的阳离子外壳可以用来结合 DNA。载药的 PLGA/FPL NPs/DNA 复合物具有克服上述问题的优势,例如共递送药物和 DNA 以提高癌细胞的化疗敏感性,以及靶向递送至癌症组织以提高生物利用度和降低毒性。实验表明,纳米粒具有核壳结构,纳米尺寸,具有持续的药物释放特性和良好的 DNA 结合能力。重要的是,核壳纳米粒实现了将药物和基因共递送至同一细胞的可能性,具有高基因转染和药物递送效率。我们的数据表明,PLGA/FPL NPs 可能是一种有用的药物和基因共递药系统。

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