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Positively-charged microemulsion for improving the oral bioavailability of alendronate: in-vitro and in-vivo assessment

文献类型：期刊论文

作者Meng, Jian2; Hu, Liandong1
刊名JOURNAL OF PHARMACY AND PHARMACOLOGY
出版日期2011-03
卷号63期号:3页码:400-408
关键词alendronate oral bioavailability paracellular route positively-charged microemulsion
ISSN号0022-3573
DOI10.1111/j.2042-7158.2010.01229.x
文献子类Article
英文摘要Objectives Alendronate is a poorly absorbed bisphosphonate with an oral bioavailability of 0.7%. In this study, a positively-charged microemulsion was prepared with the aim of improving the bioavailability of alendronate. Methods The positively-charged microemulsion was evaluated for physical stability, cellular uptake and permeability enhancement on Caco-2 monolayers. The bioavailability of alendronate from the microemulsion was compared with the commercially available tablet (Fosmax) for beagle dogs. Key findings The 2.0, 0.4 and 0.2% positively-charged microemulsion, stable for 4 h after preparation, promoted alendronate transport across the Caco-2 cells by a factor of 194, 146,and 45.1, respectively, compared with the alendronate solution, though no significant cellular uptake enhancement of alendronate was observed. The permeability enhancement was parallel to the reduction in transendothelial electrical resistance, which indicated the microemulsion modulated the tight junctions and widened the paracellular pathway. In-vivo results showed that the microemulsion gave the highest alendronate plasma concentration at 502 ng/ml (C-max) after 0.563 h (T-max), while tablets gave a C-max of 152 ng/ml after 0.750 h (T-max). Furthermore, the AUC(0-infinity) of alendronate from the microemulsion increased by 2.82-fold when compared with the tablets. Conclusions Based on the results, the oral bioavailability of alendronate could be significantly improved by the positively-charged microemulsion, which opened the tight junctions and thus increased absorption through the paracellular route.
WOS关键词CACO-2 CELLS ; ABSORPTION ENHANCEMENT ; LABRASOL ; MONOLAYERS ; TRANSPORT ; FORMULATIONS ; GENTAMICIN ; MECHANISM ; RATS ; OIL
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000287702500011
出版者WILEY-BLACKWELL
源URL[http://119.78.100.183/handle/2S10ELR8/278592]  
专题上海药物代谢研究中心
通讯作者Meng, Jian
作者单位1.Hebei Univ, Sch Pharm, Baoding, Hebei Province, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Meng, Jian,Hu, Liandong. Positively-charged microemulsion for improving the oral bioavailability of alendronate: in-vitro and in-vivo assessment[J]. JOURNAL OF PHARMACY AND PHARMACOLOGY,2011,63(3):400-408.
APA Meng, Jian,&Hu, Liandong.(2011).Positively-charged microemulsion for improving the oral bioavailability of alendronate: in-vitro and in-vivo assessment.JOURNAL OF PHARMACY AND PHARMACOLOGY,63(3),400-408.
MLA Meng, Jian,et al."Positively-charged microemulsion for improving the oral bioavailability of alendronate: in-vitro and in-vivo assessment".JOURNAL OF PHARMACY AND PHARMACOLOGY 63.3(2011):400-408.

入库方式： OAI收割

来源：上海药物研究所

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