Abstract
In this paper, we report on a potential cancer drug delivery system that utilizes the ligand targeting of the folate receptor. Our drug delivery system consists of Pluronic-P105 micelles, targeted with folic acid moieties. A melanoma folate positive (FR+) (B16-F10), and a fibroblast folate negative (FR-) (NIH-3T3) cell lines are used to compare the cellular accumulation of a chemotherapeutic drug (Doxorubicin) when the delivery is mediated by folated Pluronic P105 micelles. In order to obtain a proper comparison, we corrected for the quenching of Doxorubicin by folic acid molecules and illustrated the significant effect of quenching on the analysis of similar systems. Results show an 80% increase in the accumulation of the antineoplastic agent in the FR+ cell line, when compared to the FR- cell line, thus providing evidence that the efficacy of Pluronic micelles, as drug delivery vehicles, can be enhanced via folic acid targeting.
Keywords: Doxorubicin, micelles, folate, active targeting, quenching, B16-F10, melanoma.
Graphical Abstract
Anti-Cancer Agents in Medicinal Chemistry
Title:Targeting the Folate Receptor: Effects of Conjugating Folic Acid to DOX Loaded Polymeric Micelles
Volume: 16 Issue: 10
Author(s): Mohamed A. Elkhodiry, Ghaleb A. Husseini and Diana Velluto
Affiliation:
Keywords: Doxorubicin, micelles, folate, active targeting, quenching, B16-F10, melanoma.
Abstract: In this paper, we report on a potential cancer drug delivery system that utilizes the ligand targeting of the folate receptor. Our drug delivery system consists of Pluronic-P105 micelles, targeted with folic acid moieties. A melanoma folate positive (FR+) (B16-F10), and a fibroblast folate negative (FR-) (NIH-3T3) cell lines are used to compare the cellular accumulation of a chemotherapeutic drug (Doxorubicin) when the delivery is mediated by folated Pluronic P105 micelles. In order to obtain a proper comparison, we corrected for the quenching of Doxorubicin by folic acid molecules and illustrated the significant effect of quenching on the analysis of similar systems. Results show an 80% increase in the accumulation of the antineoplastic agent in the FR+ cell line, when compared to the FR- cell line, thus providing evidence that the efficacy of Pluronic micelles, as drug delivery vehicles, can be enhanced via folic acid targeting.
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Elkhodiry A. Mohamed, Husseini A. Ghaleb and Velluto Diana, Targeting the Folate Receptor: Effects of Conjugating Folic Acid to DOX Loaded Polymeric Micelles, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (10) . https://dx.doi.org/10.2174/1871520616666160219161600
DOI https://dx.doi.org/10.2174/1871520616666160219161600 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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