Effect of crystal habit on intrinsic dissolution behavior of celecoxib due to differential wettability

Sameer R. Modi, Ajay K.R. Dantuluri, Sathyanarayana R. Perumalla, Changquan Calvin Sun, Arvind K. Bansal

Research output: Contribution to journalArticlepeer-review

32 Scopus citations

Abstract

Intrinsic dissolution rate (IDR) is a useful technique to differentiate the solid forms of a drug. In the present study, the impact of crystal habit and crystal size on IDR of celecoxib (CEL) in different media was assessed. The IDR of plate-shaped CEL crystals (CEL-P) (53.4 ± 6.7 μg/min/cm2) was 46.3% higher than that of acicular crystals (CEL-A) (36.5 ± 1.7 μg/min/cm2) in pH 12 phosphate buffer. Contact angle experiments and values of dispersive and polar components of surface free energy indicated better wettability of CEL-P compacts than CEL-A. Higher IDR and better wettability of CEL-P were attributed to favorable exposure of hydrophilic crystal facets on compact surface, due to preferred orientation during compaction. In contrast to native samples, milled CEL-A (MCEL-A) and milled CEL-P (MCEL-P) showed similar IDR. Interestingly, IDR of CEL-A (36.5 ± 1.7 μg/min/cm2) and MCEL-A (35.64 ± 5.09 μg/min/cm2) did not show any significant difference (p > 0.05). However, IDR of CEL-P (53.4 ± 6.7 μg/min/cm2) was significantly higher (p < 0.05) than that of MCEL-P (39.15 ± 2.48 μg/min/cm2). This was ascribed to (i) differential cleavage behavior of CEL-A and CEL-P during milling and (ii) reduced degree of preferred orientation of hydrophilic facets in MCEL-P compacts. This work provides an interesting case study of the impact of particle level properties and surface molecular environment on IDR.

Original languageEnglish (US)
Pages (from-to)5283-5292
Number of pages10
JournalCrystal Growth and Design
Volume14
Issue number10
DOIs
StatePublished - Oct 1 2014

Fingerprint Dive into the research topics of 'Effect of crystal habit on intrinsic dissolution behavior of celecoxib due to differential wettability'. Together they form a unique fingerprint.

Cite this