Dual drug delivery of tamoxifen and quercetin: Regulated metabolism for anticancer treatment with nanosponges

Journal of Controlled Release : Official Journal of the Controlled Release Society
Jacob N LockhartEva Harth

Abstract

We report the synthesis and encapsulation of polyester nanosponge particles (NPs) co-loaded with tamoxifen (TAM) and quercetin (QT) to investigate the loading, release and in vitro metabolism of a dual drug formulation. The NPs are made in two variations, 4% and 8% crosslinking densities, to evaluate the effects on metabolism and release kinetics. The NP-4% formulation with a particle size of 89.3 ± 14.8 nm was found to have loading percentages of 6.91 ± 0.13% TAM and 7.72 ± 0.15% QT after targeting 10% (w/w) each. The NP-8% formulation with a particle size of 91.5 ± 9.8 nm was found to have loading percentages of 7.26 ± 0.10% TAM and 7.80 ± 0.12% QT. The stability of the formulation was established in simulated gastrointestinal fluids, and the metabolism of TAM was shown to be reduced 2-fold and 3-fold for NP-4%s and NP-8%s, respectively, while QT metabolism was reduced 3 and 4-fold. The implications for improved bioavailability of the NP formulations were supported by cytotoxicity results that showed a similar efficacy to free dual drug formulations and even enhanced anti-cancer effects in the recovery condition. This work demonstrates the suitability of the nanosponges not only as a dual release drug delivery system but also...Continue Reading

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Citations

Mar 26, 2016·Artificial Cells, Nanomedicine, and Biotechnology·Mostafa Heidari MajdAzam Sargazi
Oct 17, 2019·Experimental Biology and Medicine·Jennifer S WinklerMaria S Tomassone
Feb 23, 2020·Nanomedicine·Maria TannousRoberta Cavalli
Jan 13, 2018·Bioscience, Biotechnology, and Biochemistry·Zhen LuGuangxi Zhai
Jul 10, 2019·Anti-cancer Agents in Medicinal Chemistry·Manjula Vinayak, Akhilendra K Maurya
Jun 15, 2019·Journal of Materials Science. Materials in Medicine·Atul P SherjePravin Shende
Sep 6, 2020·Journal of Controlled Release : Official Journal of the Controlled Release Society·Xueqing ZhangBo Xiao
Aug 14, 2020·Biomacromolecules·Liwen ZhangCyrille Boyer

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