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 十月 2021
Accepted
25 十一月 2021
First published
02 十二月 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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements