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Issue 67, 2016, Issue in Progress
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Folate-decorated redox/pH dual-responsive degradable prodrug micelles for tumor triggered targeted drug delivery

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Abstract

To address the obstacles facing the clinical use of paclitaxel, including poor water solubility, side effects and lack of tumor selectivity, a novel folate-decorated and redox and pH dual-responsive micellar drug delivery system was developed based on folate-poly(ethylene glycol)-b-poly((α-paclitaxel-SS-caprolactone)-co-caprolactone) (i.e., FA-PEG-b-P((PTX-SS-CL)-co-CL)) conjugates with thiol and acid-cleavable linkages. The paclitaxel (PTX) conjugated amphiphilic block copolymer prodrug was self-assembled in phosphate buffer (pH 7.4, 0.1 M) into nanosized spherical micelles (∼96.5 nm). In vitro release studies demonstrated that the prodrug micelles are relatively stable at normal physiologic conditions but susceptible to tumor-relevant reductive and acidic conditions which would trigger the release of chemically loaded drugs. Notably, folate-decorated PTX prodrug micelles based on FA-PEG-b-P((PTX-SS-CL)-co-CL) conjugates displayed apparent targetability to folate receptor-overexpressing HeLa cells. MTT assays showed that the therapeutic efficacy of these micelles against HeLa cancer cells (IC50 = 0.75 μg mL−1) was enhanced compared with free PTX (IC50 = 0.87 μg mL−1). These results suggest that FA-PEG-b-P((PTX-SS-CL)-co-CL) conjugates may offer a promising strategy for PTX delivery in the treatment of various tumors, with enhanced efficacy and fewer adverse effects.

Graphical abstract: Folate-decorated redox/pH dual-responsive degradable prodrug micelles for tumor triggered targeted drug delivery

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Publication details

The article was received on 06 May 2016, accepted on 22 Jun 2016 and first published on 24 Jun 2016


Article type: Paper
DOI: 10.1039/C6RA11824K
Citation: RSC Adv., 2016,6, 62630-62639

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    Folate-decorated redox/pH dual-responsive degradable prodrug micelles for tumor triggered targeted drug delivery

    S. J. Tabatabaei Rezaei, L. Sarbaz and H. Niknejad, RSC Adv., 2016, 6, 62630
    DOI: 10.1039/C6RA11824K

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