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A folate receptor-targeted liposomal formulation for paclitaxel
Jun Wu1, Qing Liu, Robert J Lee
1Division of Pharmaceutics, College of Pharmacy, NCI Comprehensive Cancer Center, NSF Nanoscale Science and Engineering Center, The Ohio State University, 542 LM Parks Hall, 500 W. 12th Ave., Columbus, OH 43210, United States.
International Journal of Pharmaceutics
|March 28, 2006
Summary
A new folate receptor-targeted liposomal paclitaxel formulation shows improved stability and longer circulation time compared to traditional formulations, offering potential for FR+ cancer treatment.
Area of Science:
- Nanomedicine and Drug Delivery
- Cancer Therapeutics
- Pharmacokinetics
Background:
- Traditional paclitaxel formulations (Cremophor EL) exhibit significant vehicle toxicity.
- Folate receptor (FR) is overexpressed on many epithelial cancers, making it a viable therapeutic target.
- Liposomal drug delivery systems can enhance drug stability and circulation time.
Purpose of the Study:
- To synthesize and characterize a novel liposomal paclitaxel formulation targeting the folate receptor (FR).
- To evaluate the in vitro cytotoxicity and in vivo pharmacokinetic properties of the FR-targeted liposomes.
- To compare the novel formulation against a non-targeted liposome and the conventional Cremophor EL formulation.
Main Methods:
- Liposomes composed of DPPC/DMPG/mPEG-DSPE/folate-PEG-DSPE were prepared via polycarbonate membrane extrusion.
- Particle size and stability were assessed.
- In vitro cytotoxicity was evaluated in FR+ KB oral carcinoma cells.
- In vivo plasma clearance was studied in comparison to Cremophor EL paclitaxel.
Main Results:
- Liposomes exhibited a mean particle size of 97.1 nm and stability for at least 72 hours.
- FR-targeted liposomes demonstrated efficient uptake by FR+ KB cells.
- Paclitaxel-loaded FR-targeted liposomes showed 3.8-fold greater cytotoxicity than non-targeted liposomes.
- Liposomal formulations displayed significantly prolonged terminal half-lives (12.33-14.23 h) compared to Cremophor EL (1.78 h).
Conclusions:
- The novel FR-targeted liposomal paclitaxel formulation is stable and possesses favorable pharmacokinetic properties.
- This formulation offers a potential therapeutic strategy for FR-positive tumors, warranting further investigation.
- Targeted liposomes may reduce systemic toxicity and improve treatment efficacy for FR-expressing cancers.