Optimization of solid self-dispersing micelle for enhancing dissolution and oral bioavailability of valsartan using Box-Behnken design

被引:15
作者
Goo, Yoon Tae [1 ]
Park, Sun Young [1 ]
Chae, Bo Ram [1 ]
Yoon, Ho Yub [1 ]
Kim, Chang Hyun [1 ]
Choi, Ji Yeh [2 ]
Song, Seh Hyon [3 ]
Choi, Young Wook [1 ]
机构
[1] Chung Ang Univ, Coll Pharm, 84 Heuksuk Ro Dongjak Gu, Seoul 06974, South Korea
[2] York Univ, Dept Psychol, 4700 Keele St, Toronto, ON, Canada
[3] Kyungsung Univ, Coll Pharm, 309 Suyeong Ro Nam Gu, Busan 48434, South Korea
基金
新加坡国家研究基金会;
关键词
Valsartan; Solid self-dispersing micelle; Box-Behnken design; Dissolution; Oral bioavailability; Reduced quantity; DRUG-DELIVERY-SYSTEM; INTESTINAL PERMEABILITY; ATORVASTATIN CALCIUM; ABSORPTION; SMEDDS; TOOL; SOLIDIFICATION; FLUORESCENCE; SPECTROSCOPY; ENHANCEMENT;
D O I
10.1016/j.ijpharm.2020.119483
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A novel solid self-dispersing micelle (S-SDM) was developed to enhance the oral bioavailability of valsartan (VST) and to reduce the total mass of solidified supersaturable self-microemulsifying drug delivery system (S-SuSMEDDS), composed of Capmul MCM, Tween 80 (T80), Gelucire 44/14 (G44), Poloxamer 407, Florite PS-10 (FLO), and low-substituted hydroxypropyl cellulose B1 (HPC). Excluding oil component from S-SuSMEDDS, SSDM was optimized using a Box-Behnken design with three independent variables: X-1 (T80/G44, 0.63), X-2 (FLO/HPC, 0.41), and X-3 (solid carrier, 177.6 mg); and three response factors: Y-1 (droplet size, 191.9 nm), Y-2 (dissolution efficiency at 15 min, 55.0%), and Y-3 (angle of repose, 32.4'). The desirability function was 0.636, showing an excellent agreement between the predicted and experimental values. With approximately 75% weight of S-SuSMEDDS, no distinct crystallinity of VST was observed in S-SDM, resulting in critical micelle concentration value of 32 mu g/mL. Optimized S-SDM showed an approximate 4-fold improved dissolution (pH 1.2, 500 mL) compared with raw VST. Following oral administration in rats, optimized S-SDM improved relative bioavailability by approximately 235%, 216%, and 127% versus raw VST, Diovan (R) (commercial reference), and S-SuSMEDDS, respectively. Thus, optimized S-SDM could be a selectable candidate for developing water-insoluble drugs in reduced quantity.
引用
收藏
页数:11
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