Preparation, Characterization, and In Vivo Evaluation of an Oral Multiple Nanoemulsive System for Co-Delivery of Pemetrexed and Quercetin

Pharmaceutics
Rudra PangeniJin Woo Park

Abstract

Co-administration of conventional and natural chemotherapeutics offers synergistic anticancer efficacy while minimizing adverse effects. In this study, an oral co-delivery system for pemetrexed (PMX) and quercetin (QCN) was designed based on water-in-oil-in-water nanoemulsion (NE), which is highly absorbable because it enhances the intestinal membrane permeability of PMX and aqueous solubility of QCN. To create this system, an ion-pairing complex of PMX with Nα-deoxycholyl-l-lysyl-methylester (DCK) was formed and further incorporated with QCN into the NE, yielding PMX/DCK-QCN-NE. The results revealed synergistic inhibitory effects on human lung carcinoma (A549) cell proliferation and migration after combined treatment with PMX/DCK and QCN. The intestinal membrane permeability and cellular uptake of PMX/DCK and QCN from the NE were significantly improved via facilitated transport of PMX by the interaction of DCK with bile acid transporters, as well as NE formulation-mediated alterations in the membrane structure and fluidity, which resulted in 4.51- and 23.9-fold greater oral bioavailability of PMX and QCN, respectively, than each free drug. Tumor growth in A549 cell-bearing mice was also maximally suppressed by 62.7% after dail...Continue Reading

References

Mar 30, 2004·Biochemical and Biophysical Research Communications·Hiran C CoorayMargery A Barrand
May 1, 2004·Clinical Lung Cancer·Alex A Adjei
Aug 19, 2004·Cancer Chemotherapy and Pharmacology·I E L M KuppensJ H M Schellens
Mar 24, 2005·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Xianyi ShaXiaoling Fang
Jun 6, 2006·Molecular Pharmaceutics·Anand Balakrishnan, James E Polli
Feb 2, 2008·American Journal of Physiology. Gastrointestinal and Liver Physiology·Francesco RaimondiRoberto Paludetto
Apr 21, 2009·Colloids and Surfaces. B, Biointerfaces·Yan GaoGuangxi Zhai
Jun 30, 2009·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·C Bobin-DubigeonJ M Bard
Apr 27, 2010·International Journal of Pharmaceutics·Wenjing XiaoLijuan Chen
Jul 20, 2010·Life Sciences·Chen ChenChunyan Ji
Aug 19, 2011·Molecular Pharmaceutics·Adam J SmithR Douglas Shytle
Dec 13, 2012·Journal of Pharmaceutical Sciences·Jin Woo ParkYoungro Byun
Jan 16, 2013·Chemotherapy Research and Practice·Katrin Sak
May 8, 2013·Journal of Controlled Release : Official Journal of the Controlled Release Society·Kaushik ThankiSanyog Jain
Jun 24, 2014·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·R A ForsgårdR Holma
Jun 19, 2015·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Amrita SaxenaJiaur R Gayen
Jun 20, 2015·Nanoscale Research Letters·Linghui DianChuanbin Wu
Nov 7, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Ok-Cheol JeonJin Woo Park
Jan 23, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ju-Suk NamSang-Soo Lee
Aug 16, 2016·BMC Complementary and Alternative Medicine·Asuman Demiroglu-ZergerogluHulya Sivas
Jul 6, 2017·Oncology Reports·Mahmoud HashemzaeiRamin Rezaee
Dec 27, 2017·Journal of Controlled Release : Official Journal of the Controlled Release Society·Kejun JiangZhirong Zhang

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BETA
transmission electron microscopy

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IncuCyte
WinNonlin
IncuCyte Zoom

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