Folic acid conjugated polymeric micelles loaded with a curcumin difluorinated analog for targeting cervical and ovarian cancers

被引:83
作者
Luong, Duy [1 ]
Kesharwani, Prashant [1 ,2 ]
Alsaab, Hashem O. [1 ,3 ]
Sau, Samaresh [1 ]
Padhye, Subhash [4 ]
Sarkar, Fazlul H. [5 ]
Iyer, Arun K. [1 ,6 ]
机构
[1] Wayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharmaceut Sci, Use Inspired Biomat & Integrated Nanodelivery U B, 259 Mack Ave, Detroit, MI 48201 USA
[2] CSIR, Cent Drug Res Inst, Pharmaceut Div, Lucknow 226031, Uttar Pradesh, India
[3] Taff Univ, Dept Pharmaceut & Pharmaceut Technol, At Taif 26571, Saudi Arabia
[4] Univ Pune, Interdisciplinary Sci & Technol Res Acad, Abeda Inamdar Coll, Dept Chem, Pune 411001, Maharashtra, India
[5] Wayne State Univ, Sch Med, Barbara Ann Karmanos Canc Inst, Dept Pathol, Detroit, MI 48201 USA
[6] Wayne State Univ, Sch Med, Barbara Ann Karmanos Canc, Mol Therapeut Program, Detroit, MI 48201 USA
关键词
Ovarian cancer; Cervical cancer; Folk acid; Folate receptor-alpha targeting; Polymeric micelles; Curcumin difluorinated (CDF); Flavonoid analog; Targeted drug delivery; NF-KAPPA-B; 3,4-DIFLUOROBENZYLIDENE CURCUMIN; IN-VITRO; CELLULAR UPTAKE; DELIVERY; NANOPARTICLES; SIRNA; NANOCARRIERS; EXPRESSION; PROTEIN;
D O I
10.1016/j.colsurfb.2017.06.025
中图分类号
Q6 [生物物理学];
学科分类号
071011 ;
摘要
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 (NF kappa B), which further confirmed the targeting ability and anticancer potentials of folate-targeted formulations. (C) 2017 Elsevier B.V. All rights reserved.
引用
收藏
页码:490 / 502
页数:13
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