Abstract：
:Oral delivery is the most fascinating route for interminable drug remedy. However, the intestinal absorption of alendronate (ALN), a bisphosphonate drug after oral administration is very poor. Absorption enhancers, which help to achieve the efficiency-safety balance, are considered one of the most promising agents for the improvement the intestinal absorption of drugs. In the current study, we focused on using sucrose fatty acid esters (SEs) as promising absorption enhancers to enhance the intestinal absorption of alendronate using an in situ closed-loop method in rats. The intestinal absorption of alendronate was significantly enhanced in the presence of SEs, especially L-1695. In addition, no considerable increase was observed in the activity of lactate dehydrogenase (LDH) or in protein release from the intestinal epithelium in the presence of sugar esters at concentrations equivalent to or lower than 1.0% (w/v), suggesting that these compounds are safe. Furthermore, mechanistic studies revealed increased membrane fluidity and loosening of the tight junctions (TJs) might be the underlying mechanism by which SEs improve the intestinal intake of alendronate, via transcellular and paracellular routes, respectively. These findings suggest that SEs are effective absorption enhancers for improving the intestinal absorption of alendronate, without causing serious damage to the enteric epithelium.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Alama T,Katayama H,Hirai S,Ono S,Kajiyama A,Kusamori K,Katsumi H,Sakane T,Yamamoto Adoi
10.1016/j.ijpharm.2016.10.046subject
Has Abstractpub_date
2016-12-30 00:00:00pages
476-489issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(16)31013-4journal_volume
515pub_type
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