کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8513280 | 1556492 | 2018 | 26 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Labrasol® and Salts of Medium-Chain Fatty Acids Can Be Combined in Low Concentrations to Increase the Permeability of a Macromolecule Marker Across Isolated Rat Intestinal Mucosae
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کلمات کلیدی
ΔIscMCFAC10CCHTEERC12FD4lbfSodium caprate - اسید سدیمmedium-chain fatty acid - اسید چرب متوسط زنجیره ایKrebs-Henseleit buffer - بافر Krebs-Henseleitepithelial delivery/permeability - تحویل / نفوذ پذیری اپیتلیالOral drug delivery - تحویل داروی خوراکیMacromolecular drug delivery - تحویل داروی مقوی مولکولیPeptide delivery - تحویل پپتیدPermeation enhancer - تقویت کننده نفوذBCs - روند BCsbiopharmaceutics classification system - سیستم طبقه بندی بیولوژیکی داروapparent permeability coefficient - ضریب نفوذپذیری ظاهریBioavailability - فراهم زیستیLipid-based formulation - فرمولاسیون مبتنی بر لیپیدSodium laurate - لاوراد سدیمTrans-epithelial electrical resistance - مقاومت الکتریکی Trans-epithelialPapp - پاپpolyethylene glycol - پلی اتیلن گلیکولPEG - پلیاتیلن گلیکول Carbachol - کارباکول
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Labrasol® and Salts of Medium-Chain Fatty Acids Can Be Combined in Low Concentrations to Increase the Permeability of a Macromolecule Marker Across Isolated Rat Intestinal Mucosae Labrasol® and Salts of Medium-Chain Fatty Acids Can Be Combined in Low Concentrations to Increase the Permeability of a Macromolecule Marker Across Isolated Rat Intestinal Mucosae](/preview/png/8513280.png)
چکیده انگلیسی
In addition to their solubilizing properties, excipients used in lipid-based formulations can improve intestinal permeability of macromolecules. We determined whether admixing of medium-chain fatty acid (MCFA) permeation enhancers with a lipoidal excipient (Labrasol®) could potentiate transepithelial flux of a poorly permeable macromolecule (fluorescein isothiocyanate dextran 4 kDa [FD4]) across rat intestinal mucosae mounted in Ussing chambers. Low concentrations of sodium caprate (C10), sodium undecylenate (C11:1), or sodium laurate (C12) combined with Labrasol® increased the apparent permeability coefficient (Papp) of FD4 to values typically seen with higher concentrations of MCFAs or Labrasol® alone. For example, combination of C11:1 (0.5 mg/mL) with Labrasol® (1 mg/mL) increased the Papp of FD4 by 10- and 11-fold over the respective individual agents at the same concentrations where no enhancement was evident. The increased enhancement ratios seen with the combinations were associated with some perturbation in intestinal histology and with attenuation of an epithelial functional measure, carbachol-stimulated inward short-circuit current. In conclusion, combining three MCFAs separately with Labrasol® increased the Papp of FD4 to values greater than those seen for MCFAs or Labrasol® alone. Ultimately, this may permit lower concentrations of MCFA to be used in combination with other excipients in oral formulations of poorly permeable molecules.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 107, Issue 6, June 2018, Pages 1648-1655
Journal: Journal of Pharmaceutical Sciences - Volume 107, Issue 6, June 2018, Pages 1648-1655
نویسندگان
Joanne Heade, Sam Maher, Sinead B. Bleiel, David J. Brayden,