d-Gluconic acid–based methotrexate prodrug–loaded mixed micelles composed of MDR reversing copolymer: in vitro and in vivo results

2018 ◽  
Vol 296 (12) ◽  
pp. 1971-1981 ◽  
Author(s):  
Popat S. Kumbhar ◽  
Swapnil Birange ◽  
Mahesh Atavale ◽  
John I. Disouza ◽  
Arehalli S. Manjappa
Keyword(s):  
2018 ◽  
Vol 15 (4) ◽  
pp. 564-575 ◽  
Author(s):  
Arehalli S. Manjappa ◽  
Popat S. Kumbhar ◽  
Prajakta S. Khopade ◽  
Ajit B. Patil ◽  
John I. Disouza

2018 ◽  
Vol 44 (9) ◽  
pp. 1409-1416 ◽  
Author(s):  
Yingying Ding ◽  
Changyuan Wang ◽  
Yutong Wang ◽  
Youwei Xu ◽  
Jing Zhao ◽  
...  

2018 ◽  
Vol 82 (2) ◽  
pp. 238-246 ◽  
Author(s):  
Zhen Lu ◽  
Cuiping Bu ◽  
Weicheng Hu ◽  
Hui Zhang ◽  
Mengrui Liu ◽  
...  

2013 ◽  
pp. 1463 ◽  
Author(s):  
Xiaoling Fang ◽  
Chen ◽  
Xianyi Sha ◽  
Zhang ◽  
Zhong ◽  
...  

1979 ◽  
Vol 236 (1) ◽  
pp. E10
Author(s):  
S Binet ◽  
Y Delage ◽  
S Erlinger

To test the hypothesis that incorporation of sulfobromophthalein (BSP) into mixed micelles could account for the increase in its biliary transport maximum (Tmax) by bile salts, we have compared in hamsters the influence on BSP Tmax of taurocholate and taurochenodeoxycholate (two micelle-forming physiological bile salts) to that of taurodehydrocholate, a bile salt which, in vitro, does not form micelles. In a first series of experiments, it was observed that taurocholate and taurochenodeoxycholate increased the secretion of phospholipid (40 and 53%, respectively), and cholesterol (50 and 110%, respectively), whereas taurodehydrocholate decreased the secretion of phospholipid (-31%) and cholesterol (-43%). This result suggests that, in vivo, taurodehydrocholate or its metabolites do not form mixed micelles. In a second series of experiments, it was seen that the three bile salts induced a similar increase in BSP Tmax (63% with taurocholate, 52% with taurochenodeoxycholate, and 51% with taurodehydrocholate). These results provide circumstantial evidence for the hypothesis that mixed micelle formation is not an important determinant of maximal BSP secretion into bile.


Drug Delivery ◽  
2020 ◽  
Vol 27 (1) ◽  
pp. 1369-1377
Author(s):  
Xiaojing Xia ◽  
Jin Tao ◽  
Zhuwa Ji ◽  
Chencheng Long ◽  
Ying Hu ◽  
...  

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 546 ◽  
Author(s):  
Shuichi Setoguchi ◽  
Ryoji Hidaka ◽  
Nami Nagata-Akaho ◽  
Daisuke Watase ◽  
Mitsuhisa Koga ◽  
...  

The aim of this study was to develop a prodrug of ubiquinol-10 (UqH-10), the active form of ubiquinone-10 (Uq-10), for oral delivery. Bioavailability of UqH-10 is hampered by its high susceptibility to oxidation and water-insolubility. We prepared three novel N,N-dimethylglycine ester derivatives of UqH-10, including a 1-monoester (UqH-1-DMG), 4-monoester (UqH-4-DMG), and 1,4-bis-ester (UqH-DMG), and assessed their physicochemical properties in vitro and in vivo. UqH-DMG spontaneously formed an aqueous micelle solution comprising 20 nm particles at 36.5 °C. Cationic UqH-DMG formed nano-sized (5 nm) mixed-micelles with taurocholic acid. Reconversion of the derivatives to UqH-10 was accelerated in human liver microsomes. The oral bioavailability of UqH-10 after administration of UqH-derivatives or Uq-10 was determined in fasted and postprandial rats secreting normal and high levels of bile, respectively. In fasted rats, plasma UqH-10 after UqH-derivatives administration reached Cmax at 2–3 h and after Uq-10 administration, it remained low. The AUC0-24h of UqH-10 after UqH-derivatives administration was 2–3-fold higher than that after Uq-10 administration. In postprandial rats, the Tmax of UqH-10 after UqH-derivatives administration was an hour earlier than after Uq-10 administration. In conclusion, cationic UqH-derivatives are convenient prodrugs that enhance UqH-10 bioavailability by forming nanosized mixed-micelles with intestinal bile acids.


2017 ◽  
Vol 50 (7) ◽  
pp. 577-582 ◽  
Author(s):  
Takayuki Takei ◽  
Kohei Fukumoto ◽  
So Danjo ◽  
Takuma Yoshinaga ◽  
Hiroto Nishimata ◽  
...  
Keyword(s):  

Author(s):  
Kıvılcım Öztürk ◽  
Fatma Betül Arslan ◽  
Süleyman Can Öztürk ◽  
Sema Çalış

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