Academic Journal

d-Polyarginine Lipopeptides as Intestinal Permeation Enhancers.

التفاصيل البيبلوغرافية
العنوان: d-Polyarginine Lipopeptides as Intestinal Permeation Enhancers.
المؤلفون: Garcia Garcia, Josep, Fernández Blanco, Álvaro, Teixidó Turà, Meritxell, Sánchez Navarro, Macarena, Giralt Lledó, Ernest
المصدر: Articles publicats en revistes (Química Inorgànica i Orgànica)
بيانات النشر: WILEY-VCH
سنة النشر: 2018
المجموعة: Dipòsit Digital de la Universitat de Barcelona
مصطلحات موضوعية: Transport biològic, Mucosa gastrointestinal, Insulina, Lipopèptids, Biological transport, Gastrointestinal mucosa, Insulin, Lipopeptides
الوصف: An estimated 285 million people were living with diabetes in 2010, and this number is expected to reach 440 million by 2030. Current treatment of this disease involves the intradermal injection of insulin analogues. Many alternative administration routes have been proposed, the oral route being the most widely studied. One of the most interesting approaches for insulin delivery is the use of permeation enhancers to increase its transport across the gastrointestinal tract (GIT). Cell‐penetrating peptides (CPPs) are a remarkable example of this family of compounds. Another alternative is the use of medium‐chain fatty acids (MCFAs) to temporally disrupt the tight junctions of the GIT, thereby allowing greater drug transport. A combination of both strategies can provide a synergistic way to increase drug transport through the GIT. In this study we evaluated the complexation of insulin glulisine, an insulin analogue administered subcutaneously or intravenously in clinical practice, with a well‐known CPP modified with the MCFA lauric acid. We prepared several formulations, examined their stability, and tested the best candidates in an intestinal cell‐based model. In particular, two compounds (C12‐r4 and C12‐r6) were found to significantly increase the transport of insulin, and therefore show promise as a new delivery system worthy of further evaluation.
نوع الوثيقة: article in journal/newspaper
وصف الملف: 9 p.; application/pdf
اللغة: English
Relation: Versió postprint del document publicat a: http://dx.doi.org/10.1002/cmdc.201800428; Chemmedchem, 2018; http://dx.doi.org/10.1002/cmdc.201800428; http://hdl.handle.net/2445/125041
الاتاحة: http://hdl.handle.net/2445/125041
Rights: (c) WILEY-VCH, 2018 ; info:eu-repo/semantics/openAccess
رقم الانضمام: edsbas.A0268207
قاعدة البيانات: BASE