کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8994202 | 1114267 | 2005 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and comparative skin permeability of atenolol and propranolol esters
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موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
The prodrug approach is one of the methods which have been evaluated for improving the systemic delivery of pharmacologically active compounds. ln the present study, we have synthesized ester prodrugs of atenolol and propranolol by adding alkyl side chains to the β-hydroxy function of the drug with the objective of enhancing their lipophilicity. In vitro skin permeability study in excised mice skin showed that the prodrugs permeate freely through the skin than the respective drug moieties and significant flux enhancement (6.2-fold) was observed in both cases. In the case of atenolol, the highest permeability coefficient was shown by capriate (C10 side chain) where as in propranolol the highest permeability was recorded with caproate ester (C6 side chain). The difference in permeability may be attributed to their difference in the intrinsic lipophilicities.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Drug Delivery Science and Technology - Volume 15, Issue 2, 2005, Pages 187-190
Journal: Journal of Drug Delivery Science and Technology - Volume 15, Issue 2, 2005, Pages 187-190
نویسندگان
B. Anroop, B. Ghosh, V. Parcha, A. Kumar, J. Khanam,