1. Improving Solubility and Oral Bioavailability of Febuxostat by Polymer-Coated Nanomatrix.
- Author
-
Yin YF, Guo Y, Song WD, Duan XC, Zheng XC, Zhong T, Zhang S, Yao X, Xu MQ, Zhang Q, and Zhang X
- Subjects
- Administration, Oral, Animals, Biological Availability, Crystallization, Drug Delivery Systems methods, Febuxostat administration & dosage, Gout Suppressants administration & dosage, Gout Suppressants chemistry, Gout Suppressants metabolism, Hypromellose Derivatives administration & dosage, Hypromellose Derivatives chemistry, Hypromellose Derivatives metabolism, Male, Methylcellulose chemistry, Nanostructures administration & dosage, Polymers administration & dosage, Rats, Rats, Sprague-Dawley, Silicon Dioxide administration & dosage, Silicon Dioxide chemistry, Silicon Dioxide metabolism, Solubility, Febuxostat chemistry, Febuxostat metabolism, Nanostructures chemistry, Polymers chemistry, Polymers metabolism
- Abstract
Here, the mesoporous silica (Sylysia 350) was selected as mesoporous material, hydroxypropyl methylcellulose (HPMC) was selected as crystallization inhibitor, and febuxostat (FBT) was selected as model drug, respectively. The FBT-Sylysia-HPMC nanomatrix (FBT@SHN) was prepared. The characteristics of FBT@SHN were investigated in vitro and in vivo. Our results indicated that the FBT in FBT@SHN was in amorphous form. The solubility and dissolution of FBT in FBT@SHN were significantly increased. The oral bioavailability of FBT in FBT@SHN was greatly improved 5.8-fold compared with that in FBT suspension. This nanomatrix could be used as a drug delivery platform for improving the oral bioavailability.
- Published
- 2018
- Full Text
- View/download PDF