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Drug structural features affect drug delivery from hyperbranched polyesteramide hot melt extrudates
Elena Raviña-Eirin1, Jhonny Azuaje2, Eddy Sotelo2
1Department of Pharmacy and Pharmaceutical Technology and Institute of Industrial Pharmacy, Faculty of Pharmacy, University of Santiago de Compostela, 15782, Spain.
Hybrane S1200 shows potential for hot melt extrusion (HME) of poorly soluble drugs, but interactions with nifedipine and ketoconazole impede drug release due to polymer vesicle formation.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Hot melt extrusion (HME) is a promising technique for formulating poorly soluble drugs.
- Hybrane S1200 is a potential carrier for HME, but its interactions with specific drugs need evaluation.
Purpose of the Study:
- To assess Hybrane S1200's utility as an HME carrier for instant-release systems.
- To investigate the drug release of ketoconazole and nifedipine formulated with Hybrane S1200.
Main Methods:
- Hot melt extrusion of drug-polymer mixtures (ketoconazole/nifedipine with Hybrane S1200).
- Drug dissolution rate testing of extrudates.
- Microscopic observation of dissolution medium for polymer-drug interactions.
Main Results:
- Extrusion with Hybrane S1200 was feasible at low temperatures (<90°C).
- Nifedipine extrudates showed no drug release; ketoconazole extrudates showed 60% release.
- Turbidity and vesicle formation in dissolution medium indicated polymer-drug interactions.
Conclusions:
- Hybrane S1200 can be extruded with ketoconazole and nifedipine, forming monophasic systems.
- Drug-polymer interactions, likely due to drug acid-base profiles, hinder drug release.
- Vesicle formation by the modified polymer may encapsulate drugs, impeding delivery.
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