A combined approach of chemical enhancers and sonophoresis for the transdermal delivery of tizanidine hydrochloride

Autor:	Harendra S. Parekh, Srinivas Mutalik, Nigel M. Davies, Nayanabhirama Udupa
Rok vydání:	2009
Předmět:	Drug Acyclic Monoterpenes Skin Absorption media_common.quotation_subject Pharmaceutical Science Buffers In Vitro Techniques Pharmacology Administration Cutaneous Clonidine Mice Cyclohexenes medicine Animals Mineral Oil Ultrasonics Solubility Adjuvants Pharmaceutic Skin Transdermal media_common Eucalyptol Chromatography Ethanol Myristates Terpenes Chemistry General Medicine 1-Octanol Permeation Cyclohexanols Sonophoresis Tizanidine Drug delivery Monoterpenes Tizanidine Hydrochloride Limonene Oleic Acid medicine.drug
Zdroj:	Drug Delivery. 16:82-91
ISSN:	1521-0464 1071-7544
DOI:	10.1080/10717540802605053
Popis:	The effects of chemical enhancers and sonophoresis on the transdermal permeation of tizanidine hydrochloride (TIZ) across mouse skin were investigated. Parameters including drug solubility, apparent partition coefficient (APC), drug permeation, and degradation in skin were determined. Low frequency ultrasound was also applied in the presence and absence of chemical enhancers to assess whether drug permeation improved. APC values indicated that TIZ preferentially partitions into intercellular spaces and does not form a reservoir, with the drug also exhibiting good enzymatic stability in skin. Most of the enhancers studied significantly increased the permeation rate of TIZ through full thickness mouse skin in comparison with TIZ formulated in phosphate buffer. Maximum enhancement was observed for TIZ formulated as a suspension in 50% v/v aqueous ethanol containing 5% v/v citral. Sonophoresis significantly (p < 0.05) increased the cumulative amount of TIZ permeating through the skin at 15 and 30 min in comparison to passive diffusion. A synergistic effect was noted when sonophoresis was applied in the presence of chemical enhancers. The results suggest that the formulation of TIZ with an appropriate penetration enhancer may be useful in the development of a therapeutic system to deliver TIZ across the skin for a prolonged period, i.e. 24 hr. The application of ultrasound in association with chemical enhancers, such as the combination of 5% v/v citral in 50% v/v aqueous ethanol, could further serve as a non-oral and non-invasive drug delivery modality for the immediate therapeutic effect of muscle relaxants such as TIZ.
Databáze:	OpenAIRE
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