Document Detail

Effects of lipid vehicle and P-glycoprotein inhibition on the mesenteric lymphatic transport of paclitaxel in unconscious, lymph duct-cannulated rats.
MedLine Citation:
PMID:  24786483     Owner:  NLM     Status:  Publisher    
Abstract The present study examined the effects of lipid vehicle and intestinally based efflux processes on intestinal lymphatic transport of paclitaxel (PTX) in the mesenteric lymph duct-cannulated anesthetized rat model. PTX solution alone, PTX solution pretreated with the P-glycoprotein (P-gp) inhibitor verapamil and/or PTX and a 2:1 (w/w) mixture of linoleic acid:glycerol monooleate were administered intraduodenally to anesthetized rats. Coadministration of a mixture of linoleic acid-monoolein significantly increased the extent of intestinal lymphatic transport of PTX, but it had little impact on the absolute oral bioavailability of PTX. In contrast, pretreatment with verapamil increased both the extent of lymphatic transport (3.5-fold) and absolute oral bioavailability (1.8-fold). Further increase in the lymphatic transport (6.5-fold) and absolute oral bioavailability (1.8-fold) was achieved by the combination of pretreatment with verapamil and coadministration with the linoleic acid-monoolein mixture. These data indicate that the application of lipid vehicle holds promise for selectively targeted lymphatic delivery of PTX. P-gp inhibition can result in both increased intestinal lymphatic levels and absolute oral bioavailability of PTX.
Qingqing Cai; Xinxian Deng; Zhongdong Li; Dianyun An; Teng Shen; Mingkang Zhong
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-4-30
Journal Detail:
Title:  Drug delivery     Volume:  -     ISSN:  1521-0464     ISO Abbreviation:  Drug Deliv     Publication Date:  2014 Apr 
Date Detail:
Created Date:  2014-5-2     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9417471     Medline TA:  Drug Deliv     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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