Formulation/preparation of functionalized nanoparticles for in vivo targeted drug delivery.

Targeted cancer therapy allows the delivery of therapeutic agents to cancer cells without incurring undesirable side effects on the neighboring healthy tissues. Over the past decade, there has been an increasing interest in the development of advanced cancer therapeutics using targeted nanoparticles. Here we describe the preparation of drug-encapsulated nanoparticles formulated with biocompatible and biodegradable poly(D,L-lactic-co-glycolic acid)-block-poly(ethylene glycol) (PLGA-b-PEG) copolymer and surface functionalized with the A10 2-fluoropyrimidine ribonucleic acid aptamers that recognize the extracellular domain of prostate-specific membrane antigen (PSMA), a well-characterized antigen expressed on the surface of prostate cancer cells. We show that the self-assembled nanoparticles can selectively bind to PSMA-targeted prostate cancer cells in vitro and in vivo. This formulation method may contribute to the development of highly selective and effective cancer therapeutic and diagnostic devices.

靶向癌症治疗能够将治疗药物递送至癌细胞，而不会对邻近的健康组织产生不良副作用。在过去十年中，人们对利用靶向纳米粒子开发先进的癌症治疗方法的兴趣日益增加。在此，我们描述了用生物相容性和可生物降解的聚（D,L - 乳酸 - 共 - 乙醇酸） - 嵌段 - 聚（乙二醇）（PLGA - b - PEG）共聚物配制且表面用A10 2 - 氟嘧啶核糖核酸适体进行功能化的载药纳米粒子的制备过程，该适体能够识别前列腺特异性膜抗原（PSMA）的细胞外结构域，PSMA是一种在前列腺癌细胞表面表达的特征明确的抗原。我们表明，自组装纳米粒子在体外和体内都能选择性地与以PSMA为靶点的前列腺癌细胞结合。这种配制方法可能有助于开发高度选择性和有效的癌症治疗及诊断设备。