کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
11011550 | 1802865 | 2019 | 32 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Nintedanib-cyclodextrin complex to improve bio-activity and intestinal permeability
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Cyclodextrin complex of nintedanib was prepared aiming for increased bio-activity and improved transport across intestinal membrane with reduced p-glycoprotein (p-gp) efflux. Based on preliminary phase solubility studies and molecular modeling, sulfobutyl ether derivative of β-cyclodextrin (SBE-β-CD, Captisol®) was selected to prepare inclusion complex. Complexation was confirmed using FTIR, 1H NMR, DSC, and XRD. Bioactivity of the formed complex was tested using lung fibroblast cells, WI-38 for anti-proliferative activity and effect on collagen deposition and cells migration. In-vitro permeability studies were performed using epiIntestinal tissue model to assess the effect of complexation on transport and p-gp efflux. Results of the study demonstrated that cyclodextrin complexation increased stability of nintedanib in PBS (pH 7.4) and simulated intestinal fluid (SIF). Further, bioactivity of nintedanib also improved. Interestingly, complexation has increased transport of nintedanib across intestinal membrane and reduced efflux ratio, suggesting the role of cyclodextrin complexation in modulating p-gp efflux.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Carbohydrate Polymers - Volume 204, 15 January 2019, Pages 68-77
Journal: Carbohydrate Polymers - Volume 204, 15 January 2019, Pages 68-77
نویسندگان
Bhuvaneshwar Vaidya, Snehal K. Shukla, Srikanth Kolluru, Melanie Huen, Nihal Mulla, Neelesh Mehra, Dipti Kanabar, Srinath Palakurthi, Seyoum Ayehunie, Aaron Muth, Vivek Gupta,