Issue 3, 2022

Polymorphism and distinct physicochemical properties of the phloretin–nicotinamide cocrystal

Abstract

The emergence of cocrystals as alternative solid forms for development of novel drug products signifies the relevance of polymorphism studies in cocrystals. We report two novel polymorphs of the cocrystal involving an anti-inflammatory and antioxidative active ingredient, phloretin (PHL), and a pharmaceutically acceptable coformer, nicotinamide (NA). The two polymorphs were structurally characterized. In addition, all the polymorphs and their polymorphic phase transformation were investigated by thermal, slurry and solubility measurements. Form I was identified as the most stable polymorph under ambient conditions. The three polymorphs showed distinct photoluminescence which was rationalized on the basis of π⋯π interactions in their crystal structures. Form I was found to show a higher apparent solubility and dissolution rate which was rationalized on the basis of parameters deduced from molecular dynamics (MD) simulations. The polymorphs of the PHL–NA cocrystal emphasized the impact of polymorphism on the physicochemical properties of cocrystals.

Graphical abstract: Polymorphism and distinct physicochemical properties of the phloretin–nicotinamide cocrystal

Supplementary files

Article information

Article type
Paper
Submitted
07 oct. 2021
Accepted
25 nov. 2021
First published
02 déc. 2021

CrystEngComm, 2022,24, 560-570

Polymorphism and distinct physicochemical properties of the phloretin–nicotinamide cocrystal

S. Aitipamula, L. P. Shan and K. M. Gupta, CrystEngComm, 2022, 24, 560 DOI: 10.1039/D1CE01352A

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