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Title of Journal: Pharm Res

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Abbravation: Pharmaceutical Research

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Kluwer Academic Publishers-Plenum Publishers

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DOI

10.1002/bjs.1800810920

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1573-904X

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Vitamin DSubscript3/Subscript–Based Conjugates

Authors: Shimon BenShabat Rachel Benisty Uri WoRMSEr Amnon C Sintov
Publish Date: 2005/01/01
Volume: 22, Issue: 1, Pages: 50-57
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Abstract

Conjugation was made between polyunsaturated fatty acids PUFAs such as linolenic acid or γlinolenic acid and calcipotriol—a vitamin D3 analogue clinically used for topical treatment of psoriasis These complexes were prepared by coupling the corresponding fatty acid with calcipotriol in the presence of dicyclohexylcarbodiimide DCC and 4dimethylaminopyridine DMAP to obtain an ester bondThe conjugates were capable of enhancing the penetration of the vitamin into the skin as well as inhibiting proliferation of keratinocytes in cultures The antiproliferative activity even increased after simulating the full hydrolysis of the conjugates In vitro skin penetration studies revealed that the conjugates penetrated into the skin at higher levels relative to calcipotriol alone It was also demonstrated that the conjugate containing n3 fatty acid penetrated into the skin at higher levels as compared to the conjugate containing n6 PUFA Highperformance liquid chromatography analysis has shown that after penetration a major portion of calcipotriolPUFA conjugate was first converted mainly into another isomer form presumably by transesterification and only then it was hydrolyzed to form apparently high local concentrations of both calcipotriol and PUFA

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