지원사업
학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
커뮤니티
연구자들이 자신의 연구와 전문성을 널리 알리고, 새로운 협력의 기회를 만들 수 있는 네트워킹 공간이에요.
초록· 키워드
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To enhance the in vitro permeation of lovastatin through excised hairless mouse and human cadaver skins, solubility was determined in various hydrophilic and lipophilic vehicles, and the effects of vehicles and penetration enhancers on the skin permeation from solution formulations were investigated. Solubility of lovastatin was highest in N-methyl-2-pyrrolidone (NMP) ($278.2{\pm}10.1$ mg/ml) and dimethyl sulfoxide (DMSO) ($162.2{\pm}9.7$ mg/ml). Among different pure vehicles used, NMP, DMSO, propylene glycol and isopropyl myristate provided some drug permeation ($6.9{\pm}1.1$, $5.9{\pm}1.6$, $3.0{\pm}0.5$ and $2.2{\pm}0.3{\mu}g/cm^2$ at 24 hr, respectively) through hairless mouse skin. The addition of oleic acid, linoleic acid and oleyl alcohol to DMSO showed the maximum permeation at around 5 v/v%, however, capric acid and caprylic acid had no enhancing effect. The increase of enhancer concentrations showed bell-shaped permeation rate, suggesting the presence of optimal concentration in lovastatin penetration. Increasing donor concentration from 10 mg/ml to 80 mg/ml in DMSO and a cosolvent of DMSO, NMP and DGME (3 : 3 : 4 v/v) did not show significant dose dependent permeation in both hairless mouse and human cadaver skins. The maximum lovastatin flux through human cadaver skin was found to be $0.87{\pm}0.46{\mu}g/cm^2$/hr with 5 v/v% linoleic acid and donor dose of 4 mg/0.64 $cm^2$ in the cosolvent. These results suggest that transdermal delivery of lovastatin would be feasible by establishing the optimal concentrations of donor dose and unsaturated fatty acids in appropriate vehicles.
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참고문헌 (44)
참고문헌 신청
Alverts, A. W. / 1998 / Discovery, biochemistry and biology of lovastatin / Am. J. Cardiol 62:J10
Manzoni, M. / 2002 / Biosynthesis and biotechnological production of statins by filamentous fungi and application of these cholesterol-lowering drugs / Appl. Microbiol. Biotechnol 58:555
Corsini, A. / 1999 / New insights into the pharmacodynamic and pharmacokinetic properties of statins / Pharmacol. Ther 84:413
Shitara, Y. / 2006 / Pharmacokinetic and pharmacodynamic alterations of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors: drug-drug interactions and interindividual differences in transporter and metabolic enzyme functions / Pharmacol. Ther 112:71
Chuengsamarn, S. / 2010 / Effects of statins vs. non-statin lipid-lowering therapy on bone formation and bone mineral density biomarkers in patients with hyperlipidemia / Bone 46:1011
Manzoni, M. / 2002 / Biosynthesis and biotechnological production of statins by filamentous fungi and application of these cholesterol-lowering drugs / Appl. Microbiol. Biotechnol 58:555
Corsini, A. / 1999 / New insights into the pharmacodynamic and pharmacokinetic properties of statins / Pharmacol. Ther 84:413
Shitara, Y. / 2006 / Pharmacokinetic and pharmacodynamic alterations of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors: drug-drug interactions and interindividual differences in transporter and metabolic enzyme functions / Pharmacol. Ther 112:71
Chuengsamarn, S. / 2010 / Effects of statins vs. non-statin lipid-lowering therapy on bone formation and bone mineral density biomarkers in patients with hyperlipidemia / Bone 46:1011
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