کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2486544 | 1114386 | 2009 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis, hydrolysis, and skin retention of amino acid esters of α-tocopherol
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis, hydrolysis, and skin retention of amino acid esters of α-tocopherol Synthesis, hydrolysis, and skin retention of amino acid esters of α-tocopherol](/preview/png/2486544.png)
چکیده انگلیسی
The aim of this work was to synthesize new pro-vitamins of α-tocopherol (VE) able to release another moiety such as an amino acid, in order to obtain a combined antioxidant and moisturizing effect upon topical application. The new derivatives were characterized and tested for sensitivity to chemical and enzymatic hydrolysis. Lipophilicity was estimated using Log capacity factor and skin retention was determined in vitro, using rabbit ear skin as barrier. Five molecules were synthesized using L-proline, L-serine, L-tyrosine, L-asparagine, and L-citrulline as amino acidic moiety. All pro-vitamins showed similar or lower lipophilicity than α-tocopheryl acetate (VEAc), taken as reference, and similar stability in aqueous solutions. All pro-vitamins showed to be sensitive to enzymatic hydrolysis. None of the pro-vitamins crossed the skin in significant amounts, whereas they accumulated into the skin, in both the dermis and the epidermis. They are more hydrophilic and more water-soluble than the currently used acetate. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 98, Issue 7, July 2009, Pages 2364-2376
Journal: Journal of Pharmaceutical Sciences - Volume 98, Issue 7, July 2009, Pages 2364-2376
نویسندگان
Fabio Marra, Carmine Ostacolo, Sonia Laneri, Antonietta Bernardi, Antonia Sacchi, Cristina Padula, Sara Nicoli, Patrizia Santi,