What question did this study set out to answer?

To elucidate the mechanistic reasons why previously developed acetazolamide cocrystals fail to deliver expected improvements in drug solubility and permeability.

May 9, 2025Crystal Growth & Design

Elucidating the Mechanistic Shortcomings of Acetazolamide Cocrystals in Harnessing the Anticipated Solubility and Permeability Advantages

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Authors

NPNoopur PandeyBirla Institute of Technology, Mesra ATAastha TiwariBirla Institute of Technology, Mesra SKSudeshna KunduChiba University

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Implication

In vitro and computational analysis reveals acetazolamide cocrystals fail to improve drug solubility or permeability, highlighting the need for predictive models in cocrystal engineering.

Key Points

To elucidate the mechanistic reasons why previously developed acetazolamide cocrystals fail to deliver expected improvements in drug solubility and permeability.
Evaluated in vitro solubility, dissolution profiles, and Caco-2 cell monolayer permeability for acetazolamide cocrystals formulated with 4-hydroxybenzoic acid, salicylamide, and 4,4′-bipyridine.
Performed lattice energy calculations, solution-state 1H NMR spectroscopy, and in silico molecular dynamics simulations of the drug-efflux transporter complex.
Cocrystals demonstrated minimal to no solubility or dissolution advantage over pure acetazolamide or physical mixtures, driven by high lattice stability and identical solution-state molecular structures.
Caco-2 permeability assays showed no significant enhancement in drug absorption, consistent with molecular dynamics simulations demonstrating unchanged stability in the acetazolamide-efflux transporter complex.

Cite This Study

Pandey et al. (2025) studied this question.

synapsesocial.com/papers/69f4239377959d23c6206cd3 https://doi.org/10.1021/acs.cgd.5c00244

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Implication

In vitro and computational analysis reveals acetazolamide cocrystals fail to improve drug solubility or permeability, highlighting the need for predictive models in cocrystal engineering.

Elucidating the Mechanistic Shortcomings of Acetazolamide Cocrystals in Harnessing the Anticipated Solubility and Permeability Advantages

Discussion

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Implication

Key Points

Cite This Study

Elucidating the Mechanistic Shortcomings of Acetazolamide Cocrystals in Harnessing the Anticipated Solubility and Permeability Advantages

Discussion

Member takes

Implication

Key Points

Cite This Study

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