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Miniaturized High-Throughput Amorphous Solid Dispersion Screening via Picoliter Volume 2D-Inkjet Printing of
Georgios Papakostas1, Philip A Corner1, Andrew L Hook2
1Early Product Development & Manufacturing, Pharmaceutical Sciences, BioPharmaceuticals R&D, AstraZeneca, Charter Way, Macclesfield SK10 2NA, United Kingdom.
Molecular Pharmaceutics
|March 7, 2025
Summary
Inkjet printing enables rapid screening of drug formulations using microgram quantities of material. This innovative approach accelerates the development of amorphous solid dispersions (ASDs) by efficiently evaluating drug-polymer interactions.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Developing new drugs with poor physicochemical properties requires extensive resources.
- Early-stage drug development often lacks sufficient material for traditional formulation screening.
- Existing scaled-down methods still demand milligram to gram quantities of drug substance.
Purpose of the Study:
- To introduce a novel, material-efficient method for screening amorphous solid dispersion (ASD) formulations.
- To demonstrate the utility of picoliter inkjet printing for creating drug-polymer microarrays.
- To enable rapid evaluation of drug-polymer compositions using minimal drug material.
Main Methods:
- Utilized picoliter inkjet printing to create addressable formulation microarrays.
- Screened eight model drug compounds against seven matrix polymers at 5% w/w intervals (5-80% w/w).
- Dispensed only 1 μg of material per spot, with five replicates for each composition.
Main Results:
- Successfully screened numerous drug-polymer compositions using microgram quantities of drug substance.
- Ranked polymers based on their efficacy in preventing drug recrystallization.
- Identified unique crystallization kinetics and moisture resolubilization behaviors for different ASD formulations.
Conclusions:
- Picoliter inkjet printing offers a highly efficient method for early-stage formulation development.
- This technique significantly reduces the time and material required for screening ASDs.
- The approach is expected to accelerate the industrial development of new amorphous solid dispersion formulations.
