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Designing Lenalidomide Cocrystals with Reduced Solubility for Improved Pulmonary Drug Delivery [dataset] Open Access

Lenalidomide is a poorly soluble immunomodulatory drug that has been the subject of several cocrystal studies aiming to improve oral bioavailability by enhancing solubility. In this article, we present a cocrystal of lenalidomide and melamine with reduced solubility which may improve its bioavailability for inhalable formulations for treating pulmonary fibrosis. The structure of the hydrated cocrystal was determined by single crystal X-ray diffraction and revealed a 3-dimensional hydrogen-bonding network between lenalidomide, melamine and channel-included solvent. The cocrystal has a lower maximum solubility and a flatter dissolution profile than pure lenalidomide, making it more suitable for inhalable formulation approaches. A preliminary study shows that the cocrystal can be micronised with lactose as a model excipient with particle sizes in the appropriate order of magnitude for use in an inhalable formulation.

Descriptions

Resource type

Dataset

Contributors

Creator: Steed, Jonathan ¹
Contact person: Steed, Jonathan ¹
Data curator: Steed, Jonathan ¹
Data collector: Screen, Martin ¹
Editor: Screen, Martin ¹

¹ Durham University, UK

Funder

Engineering and Physical Sciences Research Council
AstraZeneca

Research methods

Dissolution measurements, X-ray crystallography, DSC, TGA, IR spectroscopy

Other description

Keyword

cocrystal
pulmonary
inhalation
pharmaceutical
lenalidomide

Subject

Chemistry

Location

Durham, England, United Kingdom

Language

English

Cited in

Identifier

ark:/32150/r2zp38wc706
doi:10.15128/r2zp38wc706

Rights

Creative Commons Attribution 4.0 International (CC BY)

Publisher

Durham University

Date Created

2/12/2024

File Details

Depositor

J.W. Steed

Date Uploaded

2 December 2024, 14:12:02

Date Modified

30 January 2025, 15:01:21

Audit Status

Audits have not yet been run on this file.

Characterization

File format: zip (ZIP Format)

Mime type: application/zip

File size: 22435242

Last modified: 2025:01:30 15:56:36+00:00

Filename: Research data for Designing Lenalidomide Cocrystals with Reduced Solubility for Improved Pulmonary Drug Delivery.zip

Original checksum: 4ae99567709d339086e5690f9cddcc75