作者: Bong-Seop Lee , Takayuki Amano , Hong Qiang Wang , Joe L. Pantoja , Chi Woo Yoon
DOI: 10.1021/NN400347J
关键词: Pharmacology 、 Camptothecin 、 Endocytosis 、 Chemistry 、 Drug delivery 、 In vivo 、 Glioma 、 Tumor microenvironment 、 Prodrug 、 Blood–brain barrier
摘要: Chemotherapy for intracranial gliomas is hampered by limited delivery of therapeutic agents through the blood brain barrier (BBB). An optimal agent tumors would selectively cross BBB, accumulates in tumor tissue and be activated from an innocuous prodrug within tumor. Here we show tumor-targeted efficacy a nanometer-sized (nanoprodrug) camptothecin (CPT) to treat experimental glioblastoma multiforme (GBM). The CPT nanoprodrug was prepared using spontaneous nanoemulsification biodegradable, antioxidant α-tocopherol. oxidized more efficiently than nonoxidized nanoprodrug, suggesting enhanced oxidative microenvironment. vitro imaging U-87 MG glioma cells revealed efficient intracellular uptake via direct cell membrane penetration rather endocytosis. vivo study mice demonstrated that nanopr...