ارزیابی آزمایشگاهی آلکیل گلیکوزیدها برای افزایش نفوذپذیری
In Vitro Assessment of Alkyl Glycosides as Permeability Enhancers
نویسندگان |
این بخش تنها برای اعضا قابل مشاهده است ورودعضویت |
اطلاعات مجله |
AAPS PharmSciTech |
سال انتشار |
2001 |
فرمت فایل |
PDF |
کد مقاله |
18384 |
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چکیده (انگلیسی):
A series of alkylglycosides has been evaluated on
human cell lines to determine its ability to open cellular
tight junctions. Alkylglycosides were applied to cell
monolayers; the resulting change in resistance was
determined by transepithelial electrical resistance
measurements. Change in resistance across cell
monolayers is an indication of tight junction activation,
whereas subsequent increase in resistance signifies
monolayer recovery. Of the 13 alkylglycosides tested, 4
caused irreversible solubilization of cell membranes, 5
allowed a partial recovery of the monolayer after a
relatively rapid reduction in resistance, and 4 induced a
decrease in resistance with more complete cell
recovery. Alkylglycosides allowing extensive cell
recovery after removal may indicate tight junctions'
activity dominance over membrane fluidity. Repeated
application of alkylglycosides for 6 hours lowered
resistance across cells, which returned to near-normal
values after a recovery period of 48 hours. A model dye
was transported across the cell monolayer only in the
presence of an alkylglycoside, although recovery of
cells was incomplete. Activity of the alkylglycosides
was unrelated to either the carbon chain length or to the
carbohydrate moiety. A direct correlation was
established between the concentration of applied
alkylglycoside and reduction in resistance over a
constant time period. Dodecylmaltoside and
octylglucoside were found to be optimal in decreasing
resistance at low concentrations and allowing
significant recovery of cells. Therefore these 2
alkylglycosides may be useful in facilitating drug
transport across biological membranes.
کلمات کلیدی مقاله (فارسی):
نفوذپذیری / افزایش دهنده، گلیکوزیدهای آلکیل، اتصالات محکم.
کلمات کلیدی مقاله (انگلیسی):
permeability/enhancers, alkylglycosides, tight junctions.
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