用于癌症治疗的靶向促性腺激素释放激素的纳米颗粒。

LHRH-targeted nanoparticles for cancer therapeutics.

作者信息

Minko Tamara, Patil Mahesh L, Zhang Min, Khandare Jayant J, Saad Maha, Chandna Pooja, Taratula Oleh

机构信息

Department of Pharmaceutics, Rutgers, The State University of New Jersey, Piscataway, NJ, USA.

出版信息

Methods Mol Biol. 2010;624:281-94. doi: 10.1007/978-1-60761-609-2_19.

DOI:10.1007/978-1-60761-609-2_19

PMID:20217603

Abstract

Synthesis and evaluation of a novel cancer cell's receptor-targeted internally quaternized and surface neutral poly(amidoamine) (PAMAM) generation four dendrimer as well as PAMAM-paclitaxel conjugate are described. The advantages of developed nanocarriers include but are not limited to (1) internal cationic charges for the complexation with small interfering RNA or antisense oligonucleotides and their protection from the degradation in systemic circulation; (2) neutral-modified surface for low cytotoxicity of empty unloaded dendrimers; (3) efficient internalization by cancer cells; and (4) preferential accumulation in the tumor and the prevention of adverse side effects of chemotherapy.

摘要

本文描述了一种新型的靶向癌细胞受体的内部季铵化且表面中性的第四代聚酰胺-胺（PAMAM）树枝状大分子以及PAMAM-紫杉醇共轭物的合成与评估。所开发的纳米载体的优点包括但不限于：（1）内部阳离子电荷可与小干扰RNA或反义寡核苷酸络合并保护它们在体循环中不被降解；（2）表面中性修饰可使空载树枝状大分子的细胞毒性较低；（3）癌细胞可有效内化；（4）在肿瘤中优先积累并预防化疗的不良副作用。