Next Article in Journal
Safety Monitoring in Clinical Trials
Next Article in Special Issue
Exploring Polymeric Micelles for Improved Delivery of Anticancer Agents: Recent Developments in Preclinical Studies
Previous Article in Journal
Correlating Physicochemical Properties of Boronic Acid-Chitosan Conjugates to Glucose Adsorption Sensitivity
Article Menu

Export Article

Open AccessArticle
Pharmaceutics 2013, 5(1), 81-93;

Pharmacokinetic Evaluation of a DSPE-PEG2000 Micellar Formulation of Ridaforolimus in Rat

College of Pharmacy, Department of Pharmaceutical Sciences, Washington State University, Pullman, WA 99163, USA
Department of Pharmaceutical Chemistry, University of Kansas, Lawrence, Kansas 66047, USA
Faculty of Pharmacy, University of Manitoba, Winnipeg R3T 2N2, Canada
Author to whom correspondence should be addressed.
Received: 13 November 2012 / Revised: 20 December 2012 / Accepted: 21 December 2012 / Published: 27 December 2012
(This article belongs to the Special Issue Micellar Drug Delivery)
Full-Text   |   PDF [470 KB, uploaded 27 December 2012]   |  


The rapamycin analog, ridaforolimus, has demonstrated potent anti-proliferative effects in cancer treatment, and it currently is being evaluated in a range of clinical cancer studies. Ridaforolimus is an extremely lipophilic compound with limited aqueous solubility, which may benefit from formulation with polymeric micelles. Herein, we report the encapsulation of ridaforolimus in 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000) (DSPE-PEG2000) via a solvent extraction technique. Micelle loading greatly improved the solubility of ridaforolimus by approximately 40 times from 200 μg/mL to 8.9 mg/mL. The diameters of the drug-loaded micelles were 33 ± 15 nm indicating they are of appropriate size to accumulate within the tumor site via the enhanced permeability and retention (EPR) effect. The DSPE-PEG2000 micelle formulation was dosed intravenously to rats at 10 mg/kg and compared to a control of ridaforolimus in ethanol/PEG 400. The micelle significantly increased the half-life of ridaforolimus by 170% and decreased the clearance by 58%, which is consistent with improved retention of the drug in the plasma by the micelle formulation. View Full-Text
Keywords: ridaforolimus; preclinical pharmacokinetics; polymeric micelle; DSPE-PEG2000 ridaforolimus; preclinical pharmacokinetics; polymeric micelle; DSPE-PEG2000

Figure 1

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Share & Cite This Article

MDPI and ACS Style

Remsberg, C.M.; Zhao, Y.; Takemoto, J.K.; Bertram, R.M.; Davies, N.M.; Forrest, M.L. Pharmacokinetic Evaluation of a DSPE-PEG2000 Micellar Formulation of Ridaforolimus in Rat. Pharmaceutics 2013, 5, 81-93.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Pharmaceutics EISSN 1999-4923 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top