Abstract
Psoriasis is a relatively common, chronic, inflammatory disease that affects the skin, scalp, and joints. Calcipotriol is one of the most commonly used topical agents for the treatment of psoriasis. However, it is a water-insoluble active substance and frequently leads to skin irritation in patients. Cyclodextrins (CDs) are cyclic oligosaccharides consisting of (α-1,4-)-linked d-glucopyranose units. CD molecules have a hydrophilic outer surface and a lipophilic central cavity, and they are able to form inclusion complexes in aqueous solutions with many drugs. They can increase bioavailability, aqueous solubility, and stability and also reduce the side effects of the drugs. The aim of this study was to develop a new topical drug delivery system of calcipotriol in order to improve the solubility and dissolution characteristics of the drug and reduce the undesirable side effects. For this purpose, an inclusion complex of calcipotriol with Captisol® was prepared, and complex formation was confirmed. The inclusion complex and pure drug were formulated separately in an emulgel base. Dissolution profiles of calcipotriol from emulgel formulations were compared with a commercial product of the drug. The drug release was significantly increased with the emulgel formulations compared to the commercial cream product.
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References
Lebwohl, M.: A clinician’s paradigm in the treatment of psoriasis. J. Am. Acad. Dermatol. 53, S59–S69 (2005)
Nelson, A.A., Pearce, D.J., Fleischer, A.B., Balkrishnan, R., Feldman, S.R.: New treatments for psoriasis: which biologic is best? J. Dermatol. Treat. 17, 96–107 (2006)
Laws, P.M., Young, H.S.: Topical treatment of psoriasis. Expert Opin. Pharmacother. 11(12), 1999–2009 (2010)
Basavaraj, K.H., Navya, M.A., Rashmi, R.: Stress and quality of life in psoriasis: an update. Int. J. Dermatol. 50, 783–792 (2011)
Mendonça, C.O., Burden, A.D.: Current concepts in psoriasis and its treatment. Pharmacol. Ther. 99, 133–147 (2003)
Tiberio, R., Bozzo, C., Pertusi, G., Graziola, F., Gattoni, M., Griffanti, P., Boggio, P., Colombo, E., Leigheb, G.: Calcipotriol induces apoptosis in psoriatic keratinocytes. Clin. Exp. Dermatol. 34, e972–e974 (2009)
Reich, K., Bewley, A.: What is new in topical therapy for psoriasis? J. Eur. Acad. Dermatol. Venereol. 25(Suppl 4), 15–20 (2011)
Knudsen, N.Ø., Jorgensen, L., Hansen, J., Vermehren, C., Frokjaer, S., Foged, C.: Targeting of liposome-associated calcipotriol to the skin: effect of liposomal membrane fluidity and skin barrier integrity. Int. J. Pharm. 416(2), 478–485 (2011)
Knudsen, N.Ø., Rønholt, S., Salte, R.D., Jorgensen, L., Thormann, T., Basse, L.H., Hansen, J., Frokjaer, S., Foged, C.: Calcipotriol delivery into the skin with PEGylated liposomes. Eur. J. Pharm. Biopharm. 81, 532–539 (2012)
Knudsen, N.Ø., Schiffelers, R.M., Jorgensen, L., Hansen, J., Frokjaer, S., Foged, C.: Design of cyclic RKKH peptide conjugated PEG liposomes targeting the integrin α2β1 receptor. Int. J. Pharm. 428, 171–177 (2012)
Lin, Y.-K., Huang, Z.-R., Zhuo, R.-Z., Fang, J.-Y.: Combination of calcipotriol and methotrexate in nanostructured lipid carriers for topical delivery. Int. J. Nanomed. 5, 117–128 (2010)
Loftsson, T., Jarho, P., Másson, M., Järvinen, T.: Cyclodextrins in drug delivery. Expert Opin. Drug Deliv. 2(2), 335–351 (2005)
Laza-Knoerr, A.L., Gref, R., Couvreur, P.: Cyclodextrins for drug delivery. J. Drug Target. 18(9), 645–656 (2010)
Loftsson, T., Brewster, M.E.: Pharmaceutical applications of cyclodextrins: basic science and product development. J. Pharm. Pharmacol. 62, 1607–1621 (2010)
Loftsson, T., Petersen, D.S.: Cyclodextrin solubilization of water-insoluble drugs: calcipotriol and EB-1089. Pharmazie 52(10), 783–785 (1997)
Demirel, M., Yurtdaş, G., Genç, L.: Inclusion complexes of ketoconazole with beta-cyclodextrin: physicochemical characterization and in vitro dissolution behaviour of its vaginal suppositories. J. Incl. Phenom. Macrocycl. Chem. 70, 437–445 (2011)
Bandarkar, F.S., Vavia, P.R.: An optimized commercially feasible milling technique for molecular encapsulation of meloxicam in β-cyclodextrin. Drug Dev. Ind. Pharm. 37(11), 1318–1328 (2011)
Kakran, M., Sahoo, N.G., Li, L., Judeh, Z.: Dissolution enhancement of artemisinin with β-cyclodextrin. Chem. Pharm. Bull. 59(5), 646–652 (2011)
Yan, Z., Xu, W., Sun, J., Liu, X., Zhao, Y., Sun, Y., Zhang, T., He, Z.: Characterization and in vivo evaluation of an inclusion complex of oridonin and 2-hydroxypropyl-β-cyclodextrin. Drug Dev. Ind. Pharm. 34, 632–641 (2008)
Wang, L., Zeng, F., Zong, L.: Development of orally disintegrating tablets of perphenazine/hydroxypropyl-β-cyclodextrin inclusion complex. Pharm. Dev. Technol. (2012). doi:10.3109/10837450.2012.700932
Dandawate, P.R., Vyas, A., Ahmad, A., Banerjee, S., Deshpande, J., Swamy, K.V., Jamadar, A., Dumhe-Klaire, A.C., Padhye, S., Sarkar, F.H.: Inclusion complex of novel curcumin analogue CDF and β-cyclodextrin (1:2) and its enhanced in vivo anticancer activity against pancreatic cancer. Pharm. Res. 29, 1775–1786 (2012)
Kutner, A., Chodynski, M., Leszczynska, K., Szelejewski, W., Fıtak, H.: Process for the preparation of calcipotriol. Patent number: US 20100222614 (2010)
Acknowledgments
This study was supported by Management of Scientific Research Projects of Ankara University (Project Number: 07B3336002). The authors would like to thank Embil Drug Company (Turkey) for their support in supplying calcipotriol.
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Badilli, U., Amasya, G., Şen, T. et al. Topical emulgel formulation containing inclusion complex of calcipotriol with cyclodextrin. J Incl Phenom Macrocycl Chem 78, 249–255 (2014). https://doi.org/10.1007/s10847-013-0293-2
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DOI: https://doi.org/10.1007/s10847-013-0293-2