FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1969872783> ?p ?o ?g. }

• W1969872783 endingPage "853" @default.
• W1969872783 startingPage "844" @default.
• W1969872783 abstract "The development of HIV protease inhibitors (PIs) has been one of the most significant advances of the past decade in controlling HIV infection. Unfortunately, the benefits of HIV PIs are compromised by serious side effects. One of the most frequent and deleterious side effects of HIV PIs is severe gastrointestinal (GI) disorders including mucosal erosions, epithelial barrier dysfunction, and leak-flux diarrhea, which occurs in 16−62% of patients on HIV PIs. Although the underlying mechanisms behind HIV PI-associated serious adverse side effects remain to be identified, our recent studies have shown that activation of endoplasmic reticulum (ER) stress response plays a critical role in HIV PI-induced GI complications. The objective of this study was to develop a novel self-microemulsifying drug delivery system (SMEDDS) using various antioxidants as surfactants and cosurfactants to reduce the GI side effects of the most commonly used HIV PI, ritonavir. The biological activities of this SMSDDS of ritonavir were compared with that of Norvir, which is currently used in the clinic. Rat normal intestinal epithelial cells (IEC-6) and mouse Raw 264.7 macrophages were used to examine the effect of new SMEDDS of ritonavir on activation of ER stress and oxidative stress. Sprague−Dawley rats and C57/BL6 mice were used for pharmacokinetic studies and in vivo studies. The intracellular and plasma drug concentrations were determined by HPLC analysis. Activation of ER stress was detected by Western blot analysis and secreted alkaline phosphatase (SEAP) reporter assay. Reactive oxygen species (ROS) was measured using dichlorodihydrofluorescein diacetate as a probe. Cell viability was determined by Roche’s cell proliferation reagent WST-1. Protein levels of inflammatory cytokines (TNF-α and IL-6) were determined by enzyme-linked immunosorbent assays (ELISA). The intestinal permeability was assessed by luminal enteral administration of fluorescein isothiocyanate conjugated dextran (FITC−dextran, 4 kDa). The pathologic changes in intestine were determined by histological examination. The results indicated that incorporation of antioxidants in this new SMEDDS not only significantly reduced ritonavir-induced ER stress activation, ROS production and apoptosis in intestinal epithelial cells and macrophages, but also improved the solubility, stability and bioavailability of ritonavir, and significantly reduced ritonavir-induced disruption of intestinal barrier function in vivo. In conclusion, this new SMEDDS of ritonavir has less GI side effects compared to Norvir. This new SMEDDS can be used for other HIV PIs and any insoluble antiviral drug with serious GI side effects." @default.
• W1969872783 created "2016-06-24" @default.
• W1969872783 creator A5003128598 @default.
• W1969872783 creator A5007348590 @default.
• W1969872783 creator A5011573172 @default.
• W1969872783 creator A5037015805 @default.
• W1969872783 creator A5042318723 @default.
• W1969872783 creator A5045169479 @default.
• W1969872783 creator A5064436603 @default.
• W1969872783 creator A5066792315 @default.
• W1969872783 creator A5078832861 @default.
• W1969872783 creator A5080528601 @default.
• W1969872783 date "2010-04-07" @default.
• W1969872783 modified "2023-10-01" @default.
• W1969872783 title "Development of a Novel Self-Microemulsifying Drug Delivery System for Reducing HIV Protease Inhibitor-Induced Intestinal Epithelial Barrier Dysfunction" @default.
• W1969872783 cites W1589436694 @default.
• W1969872783 cites W1974635989 @default.
• W1969872783 cites W1979192842 @default.
• W1969872783 cites W1979791843 @default.
• W1969872783 cites W1983789568 @default.
• W1969872783 cites W1984423498 @default.
• W1969872783 cites W1993263198 @default.
• W1969872783 cites W1997384329 @default.
• W1969872783 cites W2004777338 @default.
• W1969872783 cites W2017506602 @default.
• W1969872783 cites W2020188047 @default.
• W1969872783 cites W2024508489 @default.
• W1969872783 cites W2025296211 @default.
• W1969872783 cites W2034025358 @default.
• W1969872783 cites W2066927092 @default.
• W1969872783 cites W2067036095 @default.
• W1969872783 cites W2068889976 @default.
• W1969872783 cites W2072616080 @default.
• W1969872783 cites W2083278580 @default.
• W1969872783 cites W2089271435 @default.
• W1969872783 cites W2094941678 @default.
• W1969872783 cites W2104884408 @default.
• W1969872783 cites W2120264503 @default.
• W1969872783 cites W2121346305 @default.
• W1969872783 cites W2122483069 @default.
• W1969872783 cites W2130326770 @default.
• W1969872783 cites W2137662702 @default.
• W1969872783 cites W2146229058 @default.
• W1969872783 cites W2150202137 @default.
• W1969872783 cites W2153335144 @default.
• W1969872783 cites W2155275692 @default.
• W1969872783 cites W2162723667 @default.
• W1969872783 cites W2169062009 @default.
• W1969872783 cites W2335043759 @default.
• W1969872783 cites W3026032990 @default.
• W1969872783 cites W4234796100 @default.
• W1969872783 cites W44088785 @default.
• W1969872783 cites W6767451 @default.
• W1969872783 doi "https://doi.org/10.1021/mp100003r" @default.
• W1969872783 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2882528" @default.
• W1969872783 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20349948" @default.
• W1969872783 hasPublicationYear "2010" @default.
• W1969872783 type Work @default.
• W1969872783 sameAs 1969872783 @default.
• W1969872783 citedByCount "15" @default.
• W1969872783 countsByYear W19698727832012 @default.
• W1969872783 countsByYear W19698727832013 @default.
• W1969872783 countsByYear W19698727832014 @default.
• W1969872783 countsByYear W19698727832017 @default.
• W1969872783 countsByYear W19698727832019 @default.
• W1969872783 countsByYear W19698727832020 @default.
• W1969872783 countsByYear W19698727832021 @default.
• W1969872783 countsByYear W19698727832022 @default.
• W1969872783 countsByYear W19698727832023 @default.
• W1969872783 crossrefType "journal-article" @default.
• W1969872783 hasAuthorship W1969872783A5003128598 @default.
• W1969872783 hasAuthorship W1969872783A5007348590 @default.
• W1969872783 hasAuthorship W1969872783A5011573172 @default.
• W1969872783 hasAuthorship W1969872783A5037015805 @default.
• W1969872783 hasAuthorship W1969872783A5042318723 @default.
• W1969872783 hasAuthorship W1969872783A5045169479 @default.
• W1969872783 hasAuthorship W1969872783A5064436603 @default.
• W1969872783 hasAuthorship W1969872783A5066792315 @default.
• W1969872783 hasAuthorship W1969872783A5078832861 @default.
• W1969872783 hasAuthorship W1969872783A5080528601 @default.
• W1969872783 hasBestOaLocation W19698727832 @default.
• W1969872783 hasConcept C104317684 @default.
• W1969872783 hasConcept C139447449 @default.
• W1969872783 hasConcept C142462285 @default.
• W1969872783 hasConcept C158617107 @default.
• W1969872783 hasConcept C178790620 @default.
• W1969872783 hasConcept C185592680 @default.
• W1969872783 hasConcept C203014093 @default.
• W1969872783 hasConcept C2776151105 @default.
• W1969872783 hasConcept C2776415932 @default.
• W1969872783 hasConcept C2779298103 @default.
• W1969872783 hasConcept C2779820397 @default.
• W1969872783 hasConcept C2993143319 @default.
• W1969872783 hasConcept C3013748606 @default.
• W1969872783 hasConcept C55493867 @default.
• W1969872783 hasConcept C71924100 @default.
• W1969872783 hasConcept C98274493 @default.
• W1969872783 hasConceptScore W1969872783C104317684 @default.

• next