Urea co-inclusion compounds of 13 cis-Retinoic acid for simultaneous improvement of dissolution profile, photostability and safe handling characteristics

Seema Thakral, A. K. Madan

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

13-cis Retinoic acid (cis-RA), a synthetic retinoid used in the treatment of severe acne, is known to exhibit extremely low aqueous solubility and high photosensitivity. In this study, urea, a well-known adductor for linear compounds, was successfully employed for the adduction of cis-RA - a substituted cyclic organic compound. Formation of urea inclusion compounds was confirmed by FTIR, DSC and XRD. A modified Zimmerschied calorimetric method was employed for the estimation of the minimum amount of rapidly adductible endocyte (RAE) required for adduction of cis-RA in urea. Urea-cis-RA-RAE inclusion compounds containing varying proportions of guests were prepared and their thermal behaviour studied by DSC. The inclusion compounds were found to have an improved dissolution profile as demonstrated by an overall increase in the dissolution efficiency. An accelerated photostability study, conducted as per Q1B ICH guidelines, revealed that co-inclusion of cis-RA in urea delayed photo-degradation of the drug when compared with that of the pure drug. The results suggest the possibility of exploiting co-inclusion of the drug in a urea host lattice for improved solubility, stability and reduced handling problems for cis-RA.

Original languageEnglish (US)
Pages (from-to)823-832
Number of pages10
JournalJournal of Pharmacy and Pharmacology
Volume60
Issue number7
DOIs
StatePublished - Jul 2008

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