Vitamin D3-based conjugates for topical treatment of psoriasis: synthesis, antiproliferative activity, and cutaneous penetration studies. Academic Article uri icon


  • No Heading Purpose. The goals of the experiments reported in this paper were to explore skin bioavailability and cell growth inhibitory activity of new vitamin D 3–based conjugates studied as a potential drug complex for psoriasis. Methods. Conjugation was made between polyunsaturated fatty acids (PUFAs), such as linolenic acid or γ-linolenic acid, and calcipotriol—a vitamin D 3 analogue clinically used for topical treatment of psoriasis. These complexes were prepared by coupling the corresponding fatty acid with calcipotriol in the presence of dicyclohexyl-carbodiimide (DCC) and 4-(dimethylamino)-pyridine (DMAP) to obtain an ester bond. Results. The 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 …

publication date

  • January 1, 2005