Abstract
Penetration and distribution of thiocolchicoside from a commercially available foam (Miotens® 0.25%, w/v) through human excised full-thickness skin were evaluated using two different in vitro apparatus: a Franz diffusion cell and a Saarbruecken penetration model-based cell. In order to evaluate the intrinsic capability of the drug to penetrate into the skin, a simple drug aqueous solution prepared at the same drug concentration as Miotens® was also tested. Results showed that both apparatus were suitable to study thiocolchicoside penetration into human skin. Penetrated drug amounts were comparable using the two apparatus, probably because skin acts as “sink” for the drug. Miotens® was found to significantly promote thiocolchicoside accumulation into full human skin thickness in comparison with the simple drug solution. The mixture of propylene glycol and propylene glycol diperlargonate contained into Miotens® foam has been proven to be effective to promote penetration of thiocolchicoside into human skin.
Similar content being viewed by others
References
M. Carta, L. Murru, P. Botta, G. Talani, G. P. Sechi, P.-L. De Riu, E. Sanna, and G. Biggio. The muscle relaxant thiocolchicoside is an antagonist of GABA receptor function in the central nervous system. Neuropharmacology. 51:805–815 (2006).
M. Artusi, P. Santi, P. Colombo, and H. E. Junginger. Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies. Int. J. Pharm. 250:203–213 (2003).
M. Artusi, S. Nicoli, P. Colombo, R. Bettini, S. Sacchi, and P. Santi. Effect of chemical enhancers and iontophoresis on thiocolchicoside permeation across rabbit and human skin in vitro. J. Pharm Sci. 93:2431–2438 (2004).
G. C. Ceschel, P. Maffei, S. Porzio, G. Melillo, G. F. Caselli, M. C. Dragani, M. M. Gentile, and G. Clavenna. In vitro permeation screening of a new formulation of thiocolchicoside containing various enhancers. Drug Deliv. 9:259–263 (2002).
F. Bonina, C. Puglia, D. Trombetta, M. C. Dragani, M. M. Gentile, and G. Clavenna. Vehicle effects on in vitro skin permeation of thiocolchicoside. Pharmazie. 57:750–752 (2002).
H. Wagner, K. H. Kostka, C. M. Lehr, and U. F. Schaefer. Drug distribution in human skin using two different in vitro test systems: comparison with in vivo data. Pharm. Res. 17:1475–1481 (2000).
J. Luengo, B. Weiss, M. Schneider, A. Ehlers, F. Strake, K. Konig, K. H. Kostka, C. M. Lehr, and U. F. Schaefer. Influence of nanoencapsulation on human skin transport of flufenamic acid. Skin Pharmacol. Physiol. 19:190–197 (2006).
H. Wagner, K. H. Kostka, C. M. Lehr, and U. F. Schaefer. Human skin penetration of flufenamic acid: in vivo/in vitro correlation (deeper skin layers) for skin samples from the same subject. J. Invest. Dermatol. 118:540–544 (2002).
S. M. Harrison, B. W. Barry, and P. H. Dugard. Effects of freezing on human skin permeability. J. Pharm. Pharmacol. 36:261–262 (1984).
R. L. Bronaugh. Diffusion cell design. In V. P. Shah, and H. I. Maibach (eds.), Topical Drug Bioavailability, Bioequivalence and Penetration, Plenum Press, New York, 1993, pp. 117–125.
N. M. Volpato, P. Santi, C. Laureri, and P. Colombo. Assay of acyclovir in human skin by high-performance liquid chromatography. J. Pharm. Biomed. Anal. 16:515–520 (1997).
A. Rosso, and S. Zuccaro. Determination of alkaloids from the colchicines family by reversed-phase high-performance liquid chromatography. J. Chromatogr. A. 825:96–101 (1998).
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Aguzzi, C., Rossi, S., Bagnasco, M. et al. Penetration and Distribution of Thiocolchicoside through Human Skin: Comparison Between a Commercial Foam (Miotens® ) and a Drug Solution . AAPS PharmSciTech 9, 1185–1190 (2008). https://doi.org/10.1208/s12249-008-9162-5
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1208/s12249-008-9162-5