Effect of nerodilol and carvone on in vitro permeation of nicorandil across rat epidermal membrane

Autor:	S.M. Al-Saidan, Dantam V. Chandrasekhar, Yellela S.R. Krishnaiah, B. Rama
Rok vydání:	2006
Předmět:	Stereochemistry Skin Absorption Vasodilator Agents Pharmaceutical Science Cyclohexane Monoterpenes In Vitro Techniques Methylcellulose Administration Cutaneous Models Biological Permeability chemistry.chemical_compound Hypromellose Derivatives Pharmaceutical technology Drug Discovery Spectroscopy Fourier Transform Infrared medicine Animals Nicorandil Transdermal Pharmacology Carvone Terpenes Organic Chemistry Permeation Rats Membrane In vitro permeation chemistry Drug reservoir Monoterpenes Epidermis Gels Nuclear chemistry medicine.drug
Zdroj:	Drug development and industrial pharmacy. 32(4)
ISSN:	0363-9045
Popis:	The objective of the study was to investigate the effect of nerodilol and carvone on the in vitro transdermal delivery of nicorandil so as to fabricate a membrane-moderated transdermal therapeutic system. The in vitro permeation studies were carried across the rat epidermal membrane from the hydroxypropyl methylcellulose (HPMC) gels (prepared with 70:30 v/v ethanol-water) containing selected concentrations of a terpene such as nerodilol (0%w/w, 4%w/w, 8%w/w, 10%w/w, or 12%w/w) or carvone (0%w/w, 4%w/w, 8%w/w, 12%w/w, or 16%w/w). The amount of nicorandil permeated (Q(24)) from HPMC gel drug reservoir without a terpene was 3424.6+/-51.4 microg/cm(2), and the corresponding flux of the drug was 145.5+/-2.2 microg/cm(2). h. The flux of nicorandil increased with an increase in terpene concentration in HPMC gel. It was increased ranging from 254.9+/-3.1 to 375.7+/-3.2 microg/cm(2).h or 207.6+/-4.7 to 356.7+/-15.3 microg/cm(2). h from HPMC gels containing nerodilol (4%w/w to 12%w/w) or carvone (4%w/w to 16%w/w), respectively. Nerodilol increased the flux of nicorandil by about 2.62-folds whereas carvone increased the flux of the drug by about 2.49-folds across the rat epidermal membrane. The results of the Fourier Transform Infrared (FT-IR) study indicated that the enhanced in vitro transdermal delivery of nicorandil might be due to the partial extraction of stratum corneum lipids by nerodilol or carvone. It was concluded that the terpenes, nerodilol and carvone, produced a marked penetration enhancing effect on the transdermal delivery of nicorandil that could be used in the fabrication of membrane-moderated transdermal therapeutic systems.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd375645513c8dc27983d1ffb6e40f9e https://pubmed.ncbi.nlm.nih.gov/16638680 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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