کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2485020 | 1114343 | 2013 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Determination of the Optimal Cell-Penetrating Peptide Sequence for Intestinal Insulin Delivery Based on Molecular Orbital Analysis with Self-Organizing Maps
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کلمات کلیدی
Penetratininsulin - انسولینMolecular orbital analysis - تجزیه و تحلیل مولکولی مداریMultivariate analysis - تحلیل چندمتغیرهAbsorption enhancer - تقویت جذبIntestinal absorption - جذب رودهSimulations - شبیهسازی یا سیمولاسیونBioavailability - فراهم زیستیSelf-organizing map - نقشه خودسازماندهCell-penetrating peptide - پپتید نفوذ سلولی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Our recent work has shown that the intestinal absorption of insulin can be improved significantly by coadministration of cell-penetrating peptides (CPPs), especially penetratin. However, a relatively high dose of penetratin is required to adequately stimulate the intestinal absorption of insulin. Therefore, in this study, we sought to determine the CPP that most effectively enhanced intestinal insulin absorption. An in situ loop absorption study using 26 penetratin analogues suggested that the chain length, hydrophobicity, and amphipathicity of the CPPs, as well as their basicity, contribute to their absorption-enhancing efficiency. Moreover, a molecular orbital method with self-organizing maps (SOMs) classification suggested that multiple factors, including the molecular weight, basicity, the lowest unoccupied molecular orbital energy, absolute hardness, and chemical potential of CPPs, are associated with their effects on intestinal insulin absorption. Furthermore, the new CPPs proposed by SOM clustering had a marked capacity to interact with insulin, and their ability to enhance insulin absorption was much stronger than that of the original penetratin. Therefore, the peptide sequence that optimally enhances intestinal insulin absorption could be defined by SOM with the molecular orbital method, and our present work emphasizes the utility of such methodologies in the development of effective drug delivery systems. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:469-479, 2013
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 2, February 2013, Pages 469-479
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 2, February 2013, Pages 469-479
نویسندگان
Noriyasu Kamei, Shingo Kikuchi, Mariko Takeda-Morishita, Yoshiaki Terasawa, Akihito Yasuda, Shuichi Yamamoto, Nobuo Ida, Reiji Nishio, Kozo Takayama,