A cost-effective method to prepare curcumin nanosuspensions with enhanced oral bioavailability

被引:88
|
作者
Wang, Yutong [1 ]
Wang, Changyuan [1 ]
Zhao, Jing [1 ]
Ding, Yanfang [1 ]
Li, Lei [1 ]
机构
[1] Dalian Med Univ, Sch Pharm, 9 West Sect Lvshun South Rd, Dalian 116044, Peoples R China
关键词
Curcumin; Nanosuspension; CO2; Bioavailability; IN-VIVO EVALUATION; SOLID DISPERSION; DRUG-DELIVERY; NANOTECHNOLOGY; NANOPARTICLES; ABSORPTION;
D O I
10.1016/j.jcis.2016.09.003
中图分类号
O64 [物理化学(理论化学)、化学物理学];
学科分类号
070304 ; 081704 ;
摘要
Background: Nanosuspension is one of the most promising strategies to improve the oral bioavailability of insoluble drugs. The existing techniques applied to produce nanosuspensions are classified as "bottom up" or "top-down" methods, or a combination of both. Curcumin (CUR), a Biopharmaceutics Classification System (BCS) class IV substance, is a promising drug candidate in view of its good bioactivity, but its use is limited due to its poor solubility and permeability. In the present study, CUR nanosuspensions were developed to enhance CUR oral bioavailability using a cost-effective method different from conventional techniques. Results: The physicochemical properties of CUR nanosuspensions were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The crystalline state of CUR in different nanosuspensions analyzed using differential scanning calorimeter (DSC) and X-ray diffraction analysis (PXRD) confirmed its amorphous state. In vitro dissolution degree of the prepared CUR nanosuspensions using TPGS or Brij78 as stabilizer was greatly increased. Pharmacokinetic studies demonstrated that the oral bioavailability of CUR was increased 3.18 and 3.7 times after administration of CUR/TPGS nanosuspensions or CUR/Brij78 nanosuspensions, when compared with the administration of CUR suspension. Conclusions: CUR nanosuspensions produced by our cost-effective method could improve its oral bioavailability. In addition, the low-cost and time-saving method reported here is highly suitable for a fast and inexpensive preparation. (C) 2016 Elsevier Inc. All rights reserved.
引用
收藏
页码:91 / 98
页数:8
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