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PEG-Fmoc-Ibuprofen Conjugate as a Dual Functional Nanomicellar Carrier for Paclitaxel.
Bioconjug Chem 2016; 27(9):2198-205BC

Abstract

Ibuprofen is a kind of nonsteroidal anti-inflammatory drug (NSAIDs), and it is considered to possess some antitumor effect. In this study, a novel nanomicellar carrier based on PEG-derivatized ibuprofen, PEG2K-Fmoc-Ibuprofen (PEG2K-FIbu), was developed for delivery of anticancer agents such as paclitaxel (PTX). This conjugate readily forms stable mixed micelles with PTX with a relatively high PTX loading capacity of 67%. The release of PTX from PTX-loaded PEG2K-FIbu micelles was significantly slower than that from Taxol formulation. PTX-loaded PEG2K-FIbu micelles and Taxol showed a comparable in vitro cytotoxicity. Importantly, PTX-loaded PEG2K-FIbu micelles demonstrated a much more pronounced in vivo therapeutic efficacy compared with Taxol with respect to both inhibition of tumor growth and animal survival. Our system may represent an attractive dual-functional delivery system to achieve synergistic activity with PTX while minimizing the carrier-associated toxicity.

Authors+Show Affiliations

School of Pharmacy, Shenyang Pharmaceutical University , Shenyang 110016, China.Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania 15261, United States.Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania 15261, United States.Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania 15261, United States.Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania 15261, United States.School of Pharmacy, Shenyang Pharmaceutical University , Shenyang 110016, China.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27532881

Citation

Zhao, Min, et al. "PEG-Fmoc-Ibuprofen Conjugate as a Dual Functional Nanomicellar Carrier for Paclitaxel." Bioconjugate Chemistry, vol. 27, no. 9, 2016, pp. 2198-205.
Zhao M, Huang Y, Chen Y, et al. PEG-Fmoc-Ibuprofen Conjugate as a Dual Functional Nanomicellar Carrier for Paclitaxel. Bioconjug Chem. 2016;27(9):2198-205.
Zhao, M., Huang, Y., Chen, Y., Xu, J., Li, S., & Guo, X. (2016). PEG-Fmoc-Ibuprofen Conjugate as a Dual Functional Nanomicellar Carrier for Paclitaxel. Bioconjugate Chemistry, 27(9), pp. 2198-205. doi:10.1021/acs.bioconjchem.6b00415.
Zhao M, et al. PEG-Fmoc-Ibuprofen Conjugate as a Dual Functional Nanomicellar Carrier for Paclitaxel. Bioconjug Chem. 2016 09 21;27(9):2198-205. PubMed PMID: 27532881.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - PEG-Fmoc-Ibuprofen Conjugate as a Dual Functional Nanomicellar Carrier for Paclitaxel. AU - Zhao,Min, AU - Huang,Yixian, AU - Chen,Yichao, AU - Xu,Jieni, AU - Li,Song, AU - Guo,Xingjie, Y1 - 2016/08/25/ PY - 2016/8/18/entrez PY - 2016/8/18/pubmed PY - 2017/6/22/medline SP - 2198 EP - 205 JF - Bioconjugate chemistry JO - Bioconjug. Chem. VL - 27 IS - 9 N2 - Ibuprofen is a kind of nonsteroidal anti-inflammatory drug (NSAIDs), and it is considered to possess some antitumor effect. In this study, a novel nanomicellar carrier based on PEG-derivatized ibuprofen, PEG2K-Fmoc-Ibuprofen (PEG2K-FIbu), was developed for delivery of anticancer agents such as paclitaxel (PTX). This conjugate readily forms stable mixed micelles with PTX with a relatively high PTX loading capacity of 67%. The release of PTX from PTX-loaded PEG2K-FIbu micelles was significantly slower than that from Taxol formulation. PTX-loaded PEG2K-FIbu micelles and Taxol showed a comparable in vitro cytotoxicity. Importantly, PTX-loaded PEG2K-FIbu micelles demonstrated a much more pronounced in vivo therapeutic efficacy compared with Taxol with respect to both inhibition of tumor growth and animal survival. Our system may represent an attractive dual-functional delivery system to achieve synergistic activity with PTX while minimizing the carrier-associated toxicity. SN - 1520-4812 UR - https://www.unboundmedicine.com/medline/citation/27532881/PEG_Fmoc_Ibuprofen_Conjugate_as_a_Dual_Functional_Nanomicellar_Carrier_for_Paclitaxel_ L2 - https://dx.doi.org/10.1021/acs.bioconjchem.6b00415 DB - PRIME DP - Unbound Medicine ER -