P-glycoprotein targeted nanoscale drug carriers

Wengang Li, Dina Bashir Kamil Abu Samra, Jasmeen Merzaban, Niveen M. Khashab

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

Multi-drug resistance (MDR) is a trend whereby tumor cells exposed to one cytotoxic agent develop cross-resistance to a range of structurally and functionally unrelated compounds. P -glycoprotein (P -gp) efflux pump is one of the mostly studied drug carrying processes that shuttle the drugs out of tumor cells. Thus, P -gp inhibitors have attracted a lot of attention as they can stop cancer drugs from being pumped out of target cells with the consumption of ATP. Using quantitive structure activity relationship (QSAR), we have successfully synthesized a series of novel P -gp inhibitors. The obtained dihydropyrroloquinoxalines series were fully characterized and then tested against bacterial and tumor assays with over-expressed P -gps. All compounds were bioactive especially compound 1c that had enhanced antibacterial activity. Furthermore, these compounds were utilized as targeting vectors to direct drug delivery vehicles such as silica nanoparticles (SNPs) to cancerous Hela cells with over expressed P -gps. Cell uptake studies showed a successful accumulation of these decorated SNPs in tumor cells compared to undecorated SNPs. The results obtained show that dihydropyrroloquinoxalines constitute a promising drug candidate for targeting cancers with MDR. Copyright © 2013 American Scientific Publishers All rights reserved.
Original languageEnglish (US)
Pages (from-to)1399-1402
Number of pages4
JournalJournal of Nanoscience and Nanotechnology
Volume13
Issue number2
DOIs
StatePublished - Feb 1 2013

ASJC Scopus subject areas

  • Biomedical Engineering
  • Bioengineering
  • Materials Science(all)
  • Chemistry(all)
  • Condensed Matter Physics

Fingerprint

Dive into the research topics of 'P-glycoprotein targeted nanoscale drug carriers'. Together they form a unique fingerprint.

Cite this