负载姜黄素二氟类似物的叶酸共轭聚合物胶束用于靶向宫颈癌和卵巢癌。
Folic acid conjugated polymeric micelles loaded with a curcumin difluorinated analog for targeting cervical and ovarian cancers.
作者信息
Luong Duy, Kesharwani Prashant, Alsaab Hashem O, Sau Samaresh, Padhye Subhash, Sarkar Fazlul H, Iyer Arun K
机构信息
Use-inspired Biomaterials & Integrated Nano Delivery (U-BiND) Systems Laboratory Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, 259 Mack Ave, Wayne State University, Detroit, MI 48201, USA.
Use-inspired Biomaterials & Integrated Nano Delivery (U-BiND) Systems Laboratory Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, 259 Mack Ave, Wayne State University, Detroit, MI 48201, USA; Pharmaceutics Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
出版信息
Colloids Surf B Biointerfaces. 2017 Sep 1;157:490-502. doi: 10.1016/j.colsurfb.2017.06.025. Epub 2017 Jun 21.
Abstract
The current study utilizes folic acid conjugated poly(styrene-co-maleic anhydride) block copolymer (FA-SMA) to enhance the solubility of a hydrophobic but very potent synthetic curcumin-difluorinated (CDF) analog and its targeted delivery to folate receptor-alpha overexpressing cancers. The nanomicelles showed high aqueous solubility. Importantly, the encapsulation of CDF in nanomicelles resulted in high photo-stability of the otherwise photo-labile drug. When the nanomicelles were tested in folate-receptor overexpressing ovarian and cervical cancer cells they exhibited high anticancer activity causing significant cell population to undergo apoptosis due to upregulation of tumor suppressor phosphatase and tensin homolog (PTEN) and inhibition of nuclear factor kappa-B (NFκB), which further confirmed the targeting ability and anticancer potentials of folate-targeted formulations.
摘要
当前的研究利用叶酸共轭聚（苯乙烯 - 马来酸酐）嵌段共聚物（FA - SMA）来提高一种疏水性但非常有效的合成姜黄素二氟化（CDF）类似物的溶解度，并将其靶向递送至叶酸受体α过度表达的癌症细胞。纳米胶束显示出高水溶性。重要的是，将CDF包裹在纳米胶束中使原本对光不稳定的药物具有高光稳定性。当在叶酸受体过度表达的卵巢癌和子宫颈癌细胞中测试纳米胶束时，它们表现出高抗癌活性，由于肿瘤抑制因子磷酸酶和张力蛋白同源物（PTEN）的上调以及核因子κB（NFκB）的抑制，导致大量细胞群体发生凋亡，这进一步证实了叶酸靶向制剂的靶向能力和抗癌潜力。
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