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Novel Soluplus(®)-TPGS mixed micelles for encapsulation of paclitaxel with enhanced in vitro cytotoxicity on breast and ovarian cancer cell lines.
Colloids Surf B Biointerfaces. 2016 Apr 01; 140:403-411.CS

Abstract

The aim of this work was to develop mixed micelles based on two biocompatible copolymers of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus(®)) and D-α-tocopheryl polyethylene-glycol 1000 succinate (TPGS), to improve the aqueous solubility and the in vitro anti-tumor activity of paclitaxel (PTX). Pure and mixed nanomicelles were prepared by solvent evaporation method and characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). Solubility of PTX was increased 60,000 and 38,000 times, when it was formulated in pure Soluplus(®) micelles and in mixed micelles (Soluplus(®):TPGS; 4:1 ratio), respectively. The in vitro PTX release profile from micellar systems was characterized employing the dialysis membrane method where all drug-loaded formulations showed a sustained and slow release of PTX. In vitro assays were conducted on human cancer cell lines including ovarian cancer cells SKOV-3, breast cancer cells MCF-7 and triple negative breast cancer cells MDA-MB-231. Cytotoxicity studies showed that mixed micelles exhibited better antitumor activity compared to PTX solution against the three cell lines. Furthermore mixed micelles showed a significant increase on PTX cellular uptake in comparison with pure Soluplus(®) micelles and free drug in all cell lines assayed. More important, blank mixed micelles have shown cytotoxic activity due to the ability of TPGS to induce apoptosis in cancer cells. This effect was associated with the expression levels of cleaved-PARP, an apoptosis-related protein. On the basis of these results, the mixed micelles developed in this study might be a potential nano-drug delivery system for cancer chemotherapy.

Authors+Show Affiliations

Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina; National Science Research Council (CONICET), Buenos Aires, Argentina.Departamento de Farmacología, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina.Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina; National Science Research Council (CONICET), Buenos Aires, Argentina.Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina.Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina; National Science Research Council (CONICET), Buenos Aires, Argentina.Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina; National Science Research Council (CONICET), Buenos Aires, Argentina. Electronic address: diegochiappetta@yahoo.com.ar.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26780253

Citation

Bernabeu, Ezequiel, et al. "Novel Soluplus(®)-TPGS Mixed Micelles for Encapsulation of Paclitaxel With Enhanced in Vitro Cytotoxicity On Breast and Ovarian Cancer Cell Lines." Colloids and Surfaces. B, Biointerfaces, vol. 140, 2016, pp. 403-411.
Bernabeu E, Gonzalez L, Cagel M, et al. Novel Soluplus(®)-TPGS mixed micelles for encapsulation of paclitaxel with enhanced in vitro cytotoxicity on breast and ovarian cancer cell lines. Colloids Surf B Biointerfaces. 2016;140:403-411.
Bernabeu, E., Gonzalez, L., Cagel, M., Gergic, E. P., Moretton, M. A., & Chiappetta, D. A. (2016). Novel Soluplus(®)-TPGS mixed micelles for encapsulation of paclitaxel with enhanced in vitro cytotoxicity on breast and ovarian cancer cell lines. Colloids and Surfaces. B, Biointerfaces, 140, 403-411. https://doi.org/10.1016/j.colsurfb.2016.01.003
Bernabeu E, et al. Novel Soluplus(®)-TPGS Mixed Micelles for Encapsulation of Paclitaxel With Enhanced in Vitro Cytotoxicity On Breast and Ovarian Cancer Cell Lines. Colloids Surf B Biointerfaces. 2016 Apr 1;140:403-411. PubMed PMID: 26780253.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel Soluplus(®)-TPGS mixed micelles for encapsulation of paclitaxel with enhanced in vitro cytotoxicity on breast and ovarian cancer cell lines. AU - Bernabeu,Ezequiel, AU - Gonzalez,Lorena, AU - Cagel,Maximiliano, AU - Gergic,Esteban P, AU - Moretton,Marcela A, AU - Chiappetta,Diego A, Y1 - 2016/01/07/ PY - 2015/10/28/received PY - 2015/12/11/revised PY - 2016/01/01/accepted PY - 2016/1/19/entrez PY - 2016/1/19/pubmed PY - 2016/11/15/medline KW - Breast and ovarian cancer cell lines KW - In vitro anti-tumoral activity KW - Paclitaxel encapsulation KW - Soluplus(®)—TPGS mixed micelles SP - 403 EP - 411 JF - Colloids and surfaces. B, Biointerfaces JO - Colloids Surf B Biointerfaces VL - 140 N2 - The aim of this work was to develop mixed micelles based on two biocompatible copolymers of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus(®)) and D-α-tocopheryl polyethylene-glycol 1000 succinate (TPGS), to improve the aqueous solubility and the in vitro anti-tumor activity of paclitaxel (PTX). Pure and mixed nanomicelles were prepared by solvent evaporation method and characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). Solubility of PTX was increased 60,000 and 38,000 times, when it was formulated in pure Soluplus(®) micelles and in mixed micelles (Soluplus(®):TPGS; 4:1 ratio), respectively. The in vitro PTX release profile from micellar systems was characterized employing the dialysis membrane method where all drug-loaded formulations showed a sustained and slow release of PTX. In vitro assays were conducted on human cancer cell lines including ovarian cancer cells SKOV-3, breast cancer cells MCF-7 and triple negative breast cancer cells MDA-MB-231. Cytotoxicity studies showed that mixed micelles exhibited better antitumor activity compared to PTX solution against the three cell lines. Furthermore mixed micelles showed a significant increase on PTX cellular uptake in comparison with pure Soluplus(®) micelles and free drug in all cell lines assayed. More important, blank mixed micelles have shown cytotoxic activity due to the ability of TPGS to induce apoptosis in cancer cells. This effect was associated with the expression levels of cleaved-PARP, an apoptosis-related protein. On the basis of these results, the mixed micelles developed in this study might be a potential nano-drug delivery system for cancer chemotherapy. SN - 1873-4367 UR - https://www.unboundmedicine.com/medline/citation/26780253/Novel_Soluplus_®__TPGS_mixed_micelles_for_encapsulation_of_paclitaxel_with_enhanced_in_vitro_cytotoxicity_on_breast_and_ovarian_cancer_cell_lines_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0927-7765(16)30003-0 DB - PRIME DP - Unbound Medicine ER -