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Geetha Bolla, Bipul Sarma, Ashwini Kumar Nangia
The subject of crystal engineering started in the 1970s with the study of topochemical reactions in the solid state. A broad chemical definition of crystal engineering was published in 1989, and the supramolecular synthon concept was proposed in 1995 followed by heterosynthons and their potential applications for the design of pharmaceutical cocrystals in 2004. This review traces the development of supramolecular synthons as robust and recurring hydrogen bond patterns for the design and construction of supramolecular architectures, notably, pharmaceutical cocrystals beginning in the early 2000s to the present time. The ability of a cocrystal between an active pharmaceutical ingredient (API) and a pharmaceutically acceptable coformer to systematically tune the physicochemical properties of a drug (i.e., solubility, permeability, hydration, color, compaction, tableting, bioavailability) without changing its molecular structure is the hallmark of the pharmaceutical cocrystals platform, as a bridge between drug discovery and pharmaceutical development. With the design of cocrystals via heterosynthons and prototype case studies to improve drug solubility in place (2000-2015), the period between 2015 to the present time has witnessed the launch of several salt-cocrystal drugs with improved efficacy and high bioavailability. This review on the design, synthesis, and applications of pharmaceutical cocrystals to afford improved drug products and drug substances will interest researchers in crystal engineering, supramolecular chemistry, medicinal chemistry, process development, and pharmaceutical and materials sciences. The scale-up of drug cocrystals and salts using continuous manufacturing technologies provides high-value pharmaceuticals with economic and environmental benefits.
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Bolla, G., Sarma, B., & Nangia, A. K. (2022). Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs. Chemical Reviews, 122(13), 11514–11603. https://doi.org/10.1021/acs.chemrev.1c00987
Bolla, Geetha, et al. "Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs." Chemical Reviews, vol. 122, no. 13, 2022, pp. 11514–11603, https://doi.org/10.1021/acs.chemrev.1c00987.
Bolla, Geetha, Bipul Sarma, and Ashwini Kumar Nangia. "Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs." Chemical Reviews 122, no. 13 (2022): 11514–11603. https://doi.org/10.1021/acs.chemrev.1c00987.
Bolla G., Sarma B., Nangia A. K. Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs // Chemical Reviews. — 2022. — Vol. 122, № 13. — P. 11514–11603. — URL: https://doi.org/10.1021/acs.chemrev.1c00987
@article{bolla2022crystal,
title = {{Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs}},
author = {Geetha Bolla and Bipul Sarma and Ashwini Kumar Nangia},
journal = {Chemical Reviews},
year = {2022},
volume = {122},
number = {13},
pages = {11514--11603},
doi = {10.1021/acs.chemrev.1c00987},
url = {https://doi.org/10.1021/acs.chemrev.1c00987}
}TY - JOUR AU - Bolla, Geetha AU - Sarma, Bipul AU - Nangia, Ashwini Kumar TI - Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs JO - Chemical Reviews VL - 122 IS - 13 SP - 11514 EP - 11603 PY - 2022 DA - 2022/06/01 DO - 10.1021/acs.chemrev.1c00987 UR - https://doi.org/10.1021/acs.chemrev.1c00987 ER -
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