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A Rapid and Quantitative Fluorimetric Method for Protein-Targeting Small Molecule Drug Screening
Published on: October 16, 2015
New high throughput screening method for drug release measurements
Aleksandra Pelczarska1, Florence Delie, Urszula Domańska
1Faculty of Chemistry, Physical Chemistry Division, Warsaw University of Technology, Warsaw, Poland.
Summary
A new high throughput screening (HTS) method enables rapid, automated analysis of drug release kinetics from polymeric microparticles. This reliable HTS method reduces sample consumption and provides comparable results to traditional methods for formulation development.
Area of Science:
- Drug delivery systems
- Polymeric microparticles
- Pharmaceutical formulation
Background:
- In vitro release kinetic profiles are critical for developing and validating new particulate drug delivery systems.
- Existing methods for assessing drug release kinetics are often time-consuming and require significant sample amounts, hindering early-stage formulation screening.
- Piroxicam-loaded polylactic acid (PLA) and polylactic-co-glycolic acid (PLGA) microparticles are relevant models for drug delivery research.
Purpose of the Study:
- To develop and validate a microscale high throughput screening (HTS) method for investigating drug release kinetics from microparticles.
- To compare the performance of the developed HTS method against a standard dialysis method.
- To assess the influence of various parameters on drug release profiles using the HTS technique.
Main Methods:
- Development of a microscale HTS method utilizing 96-well micro filter plates for automated sample separation by filtration.
- Investigation of drug release kinetics from piroxicam-loaded PLA and PLGA microparticles.
- Comparison of release profiles obtained from the HTS method with those from a standard dialysis method.
Main Results:
- The HTS method allows for 96 experiments to be conducted simultaneously in a fully automated manner with minimal sample and particle consumption.
- The drug release profiles generated by the HTS method were consistent with those obtained using the standard dialysis method.
- Parameters such as shaking, particle concentration, and release medium composition were identified as influential factors affecting release profiles.
Conclusions:
- The developed microscale HTS method is a reliable and efficient tool for evaluating drug release kinetics from microparticles.
- This HTS approach offers reduced standard deviation and lower material consumption compared to conventional methods.
- The method is suitable for formulation screening requirements in early drug development stages, facilitating faster preclinical investigations.
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