This study aimed to design and evaluate enhanced permeation and retention (EPR)‐mediated anticancer effect of polymer‐modified and drug‐loaded magnetite nanocomposites. The preformulated bare (10 nm), chitosan‐superparamagnetic iron oxide (SPIO; 69 nm), heparin‐SPIO (42 nm), and (3‐aminopropyl)triethoxysilane‐polyethylene glycol‐SPIO (17 nm) nanocomposites were utilized to evaluate the EPR‐mediated localized cancer targeting and retention of doxorubicin (DOX) and paclitaxel (PTX) in human ovarian cancer cell lines, A2780 and OVCAR‐3 in vitro and in the tumor‐baring Balb/c mice in vivo. Fluorescence microscopy showed that DOX‐ and PTX‐loaded SPIO nanoparticles caused long‐term accumulation and cytoplasmic retention in A2780 and OVCAR‐3 cells, as compared to free drugs in vitro. In vivo antiproliferative effect of present formulations on immunodeficient female Balb/c mice showed a tremendous amount of ovarian tumor shrinkage within 6 weeks. The present nanocomposite systems of targeted drug delivery proved to be efficient drug carrier with sustained drug release and long‐term retention with enhanced cytotoxic properties in vitro and in vivo.

中文翻译：

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抗肿瘤药物负载聚合物改性磁铁矿纳米颗粒：EPR 介导的药物递送的比较分析。

本研究旨在设计和评估聚合物改性和载药磁铁矿纳米复合材料的增强渗透和保留 (EPR) 介导的抗癌作用。预先配制的裸露（10 nm）、壳聚糖-超顺磁性氧化铁（SPIO；69 nm）、肝素-SPIO（42 nm）和（3-氨基丙基）三乙氧基硅烷-聚乙二醇-SPIO（17 nm）纳米复合材料用于评估EPR 介导的局部癌症靶向和阿霉素 (DOX) 和紫杉​​醇 (PTX) 在人卵巢癌细胞系、A2780 和 OVCAR-3 体外和体内裸露肿瘤 Balb/c 小鼠中的保留。荧光显微镜显示，与体外游离药物相比，载有 DOX 和 PTX 的 SPIO 纳米颗粒在 A2780 和 OVCAR-3 细胞中引起长期积累和细胞质滞留。本制剂对免疫缺陷雌性 Balb/c 小鼠的体内抗增殖作用在 6 周内显示出大量的卵巢肿瘤缩小。目前的靶向药物递送纳米复合系统被证明是有效的药物载体，具有持续的药物释放和长期保留，并在体外和体内具有增强的细胞毒性。