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Development and Characterization of Dapsone Cocrystal Prepared by Scalable Production Methods
Lilian Henriques do Amaral1,2, Flavia Almada do Carmo1, Maria Inês Amaro2
1Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, UFRJ, Rio de Janeiro, RJ, Brazil.
AAPS Pharmscitech
|July 4, 2018
Summary
Caffeine/dapsone cocrystals were successfully prepared using scalable methods like spray drying for pulmonary delivery. These cocrystals show enhanced solubility and are suitable for inhalation formulations.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Dapsone (DAP) is an antibiotic with limited solubility, hindering effective pulmonary delivery.
- Caffeine (CAF) can be used to form cocrystals to improve drug properties.
Purpose of the Study:
- To investigate the formation of caffeine/dapsone (CAF/DAP) cocrystals using scalable methods.
- To evaluate the suitability of CAF/DAP cocrystal powders for pulmonary delivery.
Main Methods:
- Cocrystal formation via liquid-assisted grinding (LAG) and spray drying.
- Characterization using X-ray diffractometry (XRD), DSC, TGA, and FTIR.
- Particle size analysis by laser diffraction and solubility testing in pH 7.4 buffer.
Main Results:
- CAF/DAP cocrystals were successfully prepared by LAG and spray drying.
- Spray-dried powders exhibited particle sizes suitable for dry powder inhalers (5.1–5.4 μm).
- CAF/DAP cocrystal solubility (506.5 μg/mL) was significantly higher than pure DAP (217.1 μg/mL).
- In vitro studies showed no cytotoxicity and suggested improved DAP permeability.
Conclusions:
- Spray-dried CAF/DAP cocrystals are a promising candidate for pulmonary delivery formulations.
- This approach offers enhanced solubility and potentially improved therapeutic efficacy for pulmonary pathologies.
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