Pharmaceutical Cocrystals for Drug Delivery

Author:
  • ANAshwini K. Nangia
    Ashwini K. Nangia
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Abstract
Pharmaceutical cocrystals offer the ability to tune solubility, permeability, tableting, and bioavailability of a solid, oral drug formulation without changing the chemical structure of the drug molecule. Crystal engineering of pharmaceutical cocrystals and salts via supramolecular heterosynthons with acceptable generally recognized as safe (GRAS) coformers provides a platform technology for improving drug efficacy and optimal delivery. With almost 90% of drugs in Biopharmaceutics Classification System (BCS) class II and IV suffering from low‐solubility and/or low‐permeability challenges, pharmaceutical cocrystals have provided an opportune intervention in populating the drugs pipeline over the past decade. From the prototype pharmaceutical cocrystal of itraconazole‐succinic acid to the first salt‐cocrystal drug complex Entresto containing valsartan‐sacubitril, this review covers the origins of the subject in the early 2000s to the peak growth curve of model cocrystal systems between 2005 and 2015, to the successful lab‐to‐market translation witnessed in the past decade. The combined application of cocrystal engineering with machine learning and neural network tools is bringing speed and accuracy to the research exercise for designing drug–coformer cocrystals with optimal therapeutic properties. This article provides a snapshot summary of the latest trends in drug cocrystals and salts research leading to drug discovery, pharmaceutical development, and continuous manufacturing.

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