Related Experiment Video

Updated: May 5, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
07:32

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Published on: August 28, 2015

11.0K

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

Connie M Remsberg1, Yunqi Zhao, Jody K Takemoto

  • 1College of Pharmacy, Department of Pharmaceutical Sciences, Washington State University, Pullman, WA 99163, USA. mforrest@ku.edu.

Pharmaceutics
|December 5, 2013
PubMed

Insights

Polymeric micelles significantly enhance ridaforolimus solubility and plasma half-life, improving its potential as an anti-cancer drug. This formulation aids drug delivery for better cancer treatment outcomes.

Area of Science:

  • Pharmaceutical Sciences
  • Nanotechnology
  • Oncology

Background:

  • Ridaforolimus, a rapamycin analog, shows potent anti-cancer effects but suffers from poor aqueous solubility.
  • Lipophilic drugs often require advanced formulations for effective cancer therapy.
  • Polymeric micelles offer a promising nanocarrier system for improving drug solubility and delivery.

Purpose of the Study:

  • To encapsulate ridaforolimus within DSPE-PEG2000 polymeric micelles.
  • To evaluate the impact of micelle formulation on ridaforolimus solubility and pharmacokinetic properties.
  • To assess the potential of micellar ridaforolimus for enhanced cancer treatment via the EPR effect.

Main Methods:

  • Ridaforolimus was encapsulated into DSPE-PEG2000 micelles using a solvent extraction technique.
  • Solubility of ridaforolimus in micelle formulation was quantified.
  • Micelle size was determined using dynamic light scattering.
  • Pharmacokinetic studies were performed in rats comparing micellar ridaforolimus to a control formulation.

Main Results:

  • Micelle encapsulation increased ridaforolimus solubility by approximately 40-fold (from 200 μg/mL to 8.9 mg/mL).
  • The resulting drug-loaded micelles exhibited a size of 33 ± 15 nm, suitable for tumor accumulation via the EPR effect.
  • Intravenous administration of micellar ridaforolimus in rats resulted in a 170% increase in half-life and a 58% decrease in clearance compared to the control.

Conclusions:

  • DSPE-PEG2000 micelles effectively enhance the aqueous solubility of ridaforolimus.
  • The micelle formulation significantly improves the pharmacokinetic profile of ridaforolimus, prolonging its circulation time.
  • This nanomicelle formulation holds promise for improving the efficacy of ridaforolimus in cancer therapy.

More Related Videos

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles09:56

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

Published on: August 2, 2016

14.2K
A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles09:57

A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles

Published on: December 23, 2016

8.3K

Related Concept Videos

Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions01:15

Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions

PK–PD modeling has significantly influenced FDA regulatory decisions, particularly drug approval, dosage optimization, and labeling. These models integrate pharmacokinetics (PK) and pharmacodynamics (PD) to predict drug behavior and effects, aiding in optimizing dosing regimens and enhancing the probability of clinical trial success.One notable example is Nesiritide (Natrecor®), a recombinant human brain natriuretic peptide for treating acute decompensated congestive heart failure...
97
Pharmacokinetic–Pharmacodynamic Relationship: Duration of Dose-Effect Relationship01:14

Pharmacokinetic–Pharmacodynamic Relationship: Duration of Dose-Effect Relationship

For drugs producing a quantal response, onset occurs when plasma concentration reaches a minimum effective level (Cmin). The drug's action duration depends on how long the plasma concentration remains above Cmin.Two primary factors influence this duration: dose size and the rate of drug removal from the action site. Both depend on the drug's redistribution to poorly perfused tissues and elimination processes. A larger dose promotes rapid onset and prolongs the effect's duration.Consider a...
124
Methods for Studying Drug Absorption: In situ01:09

Methods for Studying Drug Absorption: In situ

In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
887
Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
170