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Lopinavir-menthol co-crystals for enhanced dissolution rate and intestinal absorption
Noha D Fayed1, Mona F Arafa1, Ebtesam A Essa1
1Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Tanta, Tanta, Egypt.
Journal of Drug Delivery Science and Technology
|July 18, 2022
Summary
Menthol co-crystallization significantly improved lopinavir
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Materials Science
Background:
- Lopinavir, an antiretroviral, has poor oral bioavailability due to low dissolution and high P-glycoprotein efflux.
- Enhancing lopinavir's dissolution and absorption is crucial for effective therapeutic outcomes.
Purpose of the Study:
- To enhance the dissolution rate and intestinal absorption of lopinavir.
- To investigate menthol as a co-former for lopinavir co-crystals.
Main Methods:
- Lopinavir and menthol were co-processed using ethanol-assisted kneading at various molar ratios.
- Characterization involved FTIR, DSC, XRD, and dissolution studies.
- Intestinal permeability was assessed using an in situ rabbit intestinal perfusion model.
Main Results:
- Lopinavir-menthol co-crystals (1:2 molar ratio) were successfully formed, confirmed by FTIR, DSC, and XRD.
- Co-crystallization significantly increased lopinavir's dissolution efficiency from 24.96% to 91.43%.
- Menthol co-perfusion enhanced lopinavir's intestinal permeability, indicating reduced P-gp efflux.
Conclusions:
- Menthol is an effective co-former for enhancing lopinavir dissolution and intestinal absorption.
- Co-crystallization offers a promising strategy to overcome lopinavir's bioavailability challenges.
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