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Open AccessArticle

Enhanced Anticancer Activity of 5’-DFUR-PCL-MPEG Polymeric Prodrug Micelles Encapsulating Chemotherapeutic Drugs

1
Department of Chemical Engineering, Michigan Technological University, Houghton, MI, 49931, USA
2
Department of Biological Engineering, University of Idaho, Moscow, ID 83844, USA
*
Author to whom correspondence should be addressed.
Nanomaterials 2018, 8(12), 1041; https://doi.org/10.3390/nano8121041
Received: 19 November 2018 / Revised: 10 December 2018 / Accepted: 11 December 2018 / Published: 13 December 2018
(This article belongs to the Special Issue Polymeric Micelles and Their Application in Nanomedicine)
The compound 5’-deoxy-5-fluorouridine (5’-DFUR) is a prodrug of the anti-tumor drug 5-fluorouracil (5-FU). Thymidine phosphorylase (TP) is an enzyme that can convert 5’-DFUR to its active form 5-FU and the expression of TP is upregulated in various cancer cells. In this study, 5’-DFUR associated with amphiphilic copolymer poly(ε-caprolactone)-methoxy poly(ethylene glycol) (5’-DFUR-PCL-MPEG) was synthesized, characterized, and self-assembled into functional polymeric micelles. To demonstrate that the prodrug 5’-DFUR could convert into cytotoxic 5-fluorouracil (5-FU) by endogenous TP, HT-29 colorectal cancer cells were treated with 5’-DFUR-PCL-MPEG polymeric micelles for various time periods. Chemotherapeutic drugs doxorubicin (DOX) and 7-ethyl-10-hydroxycamptothecin (SN-38) were also encapsulated separately into 5’-DFUR-PCL-MPEG polymeric micelles to create a dual drug-loaded system. HT-29 cells were treated with DOX or SN-38 encapsulated 5’-DFUR-PCL-MPEG polymeric micelles to examine the efficacy of dual drug-loaded micelles. As a result, HT-29 cells treated with 5’-DFUR-PCL-MPEG polymeric micelles showed up to 40% cell death rate after a 72-h treatment. In contrast, HT-29 cells challenged with DOX or SN-38 encapsulated 5’-DFUR-incorporated polymeric micelles showed 36% and 31% in cell viability after a 72-h treatment, respectively. View Full-Text
Keywords: 5’-DFUR; 5-fluorouracil; thymidine phosphorylase; prodrug; polymeric micelle; doxorubicin; SN-38 5’-DFUR; 5-fluorouracil; thymidine phosphorylase; prodrug; polymeric micelle; doxorubicin; SN-38
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Sawdon, A.J.; Zhang, J.; Wang, X.; Peng, C.-A. Enhanced Anticancer Activity of 5’-DFUR-PCL-MPEG Polymeric Prodrug Micelles Encapsulating Chemotherapeutic Drugs. Nanomaterials 2018, 8, 1041.

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