Preparation and evaluation of 5, 9-dimethyl-2-cyclopropyl-2-decanol as a penetration enhancer for drugs through rat skin.
Summary of "Preparation and evaluation of 5, 9-dimethyl-2-cyclopropyl-2-decanol as a penetration enhancer for drugs through rat skin."
In the present study a new alcohol derivative of tetrahydrogeraniol (THG), an acyclic monoterpene, has been prepared by using Grignard reagent and methyl cyclopropyl ketone. Penetration enhancing effects of THG and the synthesized derivative 5,9-dimethyl-2-cyclopropyl-2-decanol (DICNOL) on the transdermal penetration of 5-fluorouracil (5-FU) and tramadol hydrochloride (tramadol HCl) across the excised rat skin were studied by an in vitro permeation technique using Franz diffusion cells. Azone was used as standard enhancer for comparison. DICNOL and THG significantly enhanced 5-FU and tramadol HCl penetration through rat skin compared with the control. DICNOL enhanced the permeability of 5-FU and tramadol HCl across full thickness skin by about 11 and 20 fold, respectively. Increased partition coefficient and diffusion coefficient values were obtained by these enhancers. The results suggest that the amount of DICNOL in the skin, especially in the stratum corneum, may be related to its penetration enhancing effects.
Affiliation
Drug Delivery Research Centre, Department of Pharmaceutics, Faculty of Pharmacy, Gomal University, Dera Ismail Khan (KP) Pakistan.
Journal Details
This article was published in the following journal.
Name: Pakistan journal of pharmaceutical sciences
ISSN: 1011-601X
Pages: 451-7
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/21959804
- DOI: http://dx.doi.org/
Medical and Biotech [MESH] Definitions
Evaluation Studies As Topic
Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.
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Ccaat-enhancer-binding Protein-alpha
A CCAAT-enhancer-binding protein found in LIVER; ADIPOSE TISSUE; INTESTINES; LUNG; ADRENAL GLANDS; PLACENTA; OVARY and peripheral blood mononuclear cells (LEUKOCYTES, MONONUCLEAR). Experiments with knock-out mice have demonstrated that CCAAT-enhancer binding protein-alpha is essential for the functioning and differentiation of HEPATOCYTES and ADIPOCYTES.
Transcription Factor Chop
A CCAAT-enhancer binding protein that is induced by DNA DAMAGE and growth arrest. It serves as a dominant negative inhibitor of other CCAAT-enhancer binding proteins.
Ccaat-enhancer-binding Proteins
A class of proteins that were originally identified by their ability to bind the DNA sequence CCAAT. The typical CCAAT-enhancer binding protein forms dimers and consists of an activation domain, a DNA-binding basic region, and a leucine-rich dimerization domain (LEUCINE ZIPPERS). CCAAT-BINDING FACTOR is structurally distinct type of CCAAT-enhancer binding protein consisting of a trimer of three different subunits.
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