Department of Pharmaceutical Sciences, College of Pharmacy, Chicago State University, Chicago, IL 60628, USA.
Int J Nanomedicine. 2013;8:1393-402. doi: 10.2147/IJN.S43479. Epub 2013 Apr 10.
Enhanced and targeted drug delivery using biodegradable microspheres is emerging as a promising approach for cancer therapy. The main objective of the present research was to formulate, characterize, and evaluate iron oxide (magnetic) containing a bovine serum albumin-based microsphere drug delivery system, capable of efficiently delivering sulforaphane, a histone deacetylase inhibitor, for an extended period of time in vivo. Magnetic microspheres were prepared by spray-drying and characterized for their physicochemical properties and dissolution profile. Further, they were evaluated for therapeutic efficacy in in vitro and in vivo systems. In vitro studies in B16 melanoma cells revealed that there was about 13%-16% more inhibition of cell viability when either 30 μM or 50 μM of sulforaphane was used with iron oxide in the polymeric carrier. Data from in vivo studies in C57BL/6 mice revealed that the magnetic microspheres (localized to the tumor site with the help of a strong magnet) inhibited 18% more tumor growth as compared with sulforaphane in solution. In addition, there was a 40% reduction in histone deacetylation levels in mice treated with iron oxide microspheres containing sulforaphane. Thus, magnetic microspheres are shown to be an effective drug delivery system for anticancer drugs.
使用可生物降解的微球增强和靶向药物递送，正在成为癌症治疗的一种有前途的方法。本研究的主要目的是制备、表征和评估含有牛血清白蛋白的氧化铁（磁性）基微球药物递送系统，该系统能够在体内有效地长时间递送电磺胺，一种组蛋白去乙酰化酶抑制剂。通过喷雾干燥法制备磁性微球，并对其物理化学性质和溶解特性进行了表征。进一步，在体外和体内系统中评估了其治疗效果。在 B16 黑色素瘤细胞中的体外研究表明，当 30 μM 或 50 μM 的电磺胺与聚合物载体中的氧化铁一起使用时，细胞活力的抑制率约增加 13%-16%。在 C57BL/6 小鼠的体内研究中，数据表明与溶液中的电磺胺相比，磁性微球（在强磁铁的帮助下定位于肿瘤部位）抑制肿瘤生长的效果提高了 18%。此外，用含有电磺胺的氧化铁微球治疗的小鼠中组蛋白去乙酰化水平降低了 40%。因此，磁性微球被证明是一种有效的抗癌药物的药物递送系统。
