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Folate receptor targeted delivery of liposomal daunorubicin into tumor cells

Sandy Ni1, Stacy M Stephenson, Robert J Lee

  • 1Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus 43210, USA.

Anticancer Research
|August 15, 2002
PubMed
Abstract

Insights

Targeting cancer cells with folate receptor (FR)-expressing tumors using FR-targeted liposomal daunorubicin (f-L-DNR) significantly enhances drug uptake and cytotoxicity compared to non-targeted liposomes. Further animal studies are recommended for this promising chemotherapy strategy.

Area of Science:

  • Oncology
  • Drug Delivery
  • Biochemistry

Background:

  • The folate receptor (FR) is overexpressed in various human cancers, presenting a therapeutic target.
  • Targeting FR offers a strategy to selectively deliver cytotoxic agents to tumor cells.

Purpose of the Study:

  • To evaluate the efficacy of FR-targeted liposomal daunorubicin (f-L-DNR) compared to non-targeted liposomal daunorubicin (L-DNR).
  • To assess cellular uptake and cytotoxicity of f-L-DNR in FR-expressing cancer cells.

Main Methods:

  • Liposomal daunorubicin retention was optimized using ammonium sulfate as a trapping agent.
  • Cellular uptake was quantified via flow cytometry and fluorometry.
  • Cytotoxicity was assessed using the MTT assay in FR-positive cell lines.

Main Results:

  • Liposomes with ammonium sulfate showed superior daunorubicin retention.
  • f-L-DNR demonstrated significantly higher cellular uptake (4.6- to 40-fold) in tested cell lines compared to L-DNR.
  • f-L-DNR exhibited markedly increased cytotoxicity (18- to 49-fold) against FR-expressing cells.
  • Folic acid effectively inhibited f-L-DNR uptake and cytotoxicity, confirming FR-mediated delivery.

Conclusions:

  • FR-mediated delivery of liposomal daunorubicin enhances drug uptake and efficacy in FR-expressing tumors.
  • These findings support further investigation of f-L-DNR in preclinical animal models for cancer therapy.

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