کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8513138 | 1556490 | 2018 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Retina Compatible Interactions and Effective Modulation of Blood Ocular Barrier P-gp Activity by Third-Generation Inhibitors Improve the Ocular Penetration of Loperamide
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کلمات کلیدی
BRBBOBP-gp inhibitorsElacridarDVHTariquidarP-gpDAHABCQ-TOFi.p.LoPERGUHPLCLOQP-glycoprotein - P-گلیکوپروتئینSprague Dawley - اسپراگ داولیelectroretinography - الکتروترینگرافیiris-ciliary body - بدن ارگاسم زنانهExtraction efficiency - بهره وری استخراجLOD یا Limit of detection - حد تشخیصintraperitoneal - داخل صفاقیIntravenous - داخل وریدیQuadrupole time of flight - زمان پرواز چهار روزهaqueous humor - طنز آبیVitreous humor - طنز شیشه ایBruch's membrane - غشای بروشBAB - فصلLoperamide - لورامیدblood retinal barrier - مانع خون شبکیهlimit of quantification - محدودیت اندازه گیریlimit of detection - محدودیت تشخیصi.c. - مدار مجتمع.Ultra High Performance Liquid Chromatography - کروماتوگرافی مایع با کارایی فوق العاده بالا
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Effective drug delivery to the deeper ocular tissues remains an unresolved conundrum mainly due to the expression of multidrug resistance efflux proteins, besides tight junction proteins, in the blood ocular barriers (BOBs). Hence, the purpose of the current research was to investigate the ability of the third-generation efflux protein inhibitors, elacridar (EQ), and tariquidar (TQ), to diminish P-glycoprotein (P-gp) mediated efflux transport of loperamide (LOP), a P-gp substrate, across the BOB in Sprague Dawley rats. Initially, Western blot analysis confirmed the expression of P-gp in the iris-ciliary bodies and the retina choroid in the wild type rats. Next, the ocular distribution of LOP, in the presence and absence of EQ/TQ (at 2 doses), was evaluated. The significantly higher aqueous humor/plasma (DAH) and vitreous humor (VH)/plasma (DVH) distribution ratios of LOP in the rats pretreated with EQ or TQ demonstrated effective inhibition of P-gp activity in the BOB. Interestingly, the modulation of P-gp activity by EQ/TQ was more pronounced at the lower dose. The normal functioning and architecture of the retina, as indicated by electroretinography studies, confirmed the cytocompatibility of LOP and EQ/TQ interactions at the doses tested.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 107, Issue 8, August 2018, Pages 2128-2135
Journal: Journal of Pharmaceutical Sciences - Volume 107, Issue 8, August 2018, Pages 2128-2135
نویسندگان
Karthik Yadav Janga, Akshaya Tatke, Surabhi Shukla, Surya P. Lamichhane, Bharathi Avula, XiangDi Wang, Monica M. Jablonski, Ikhlas A. Khan, Soumyajit Majumdar,