Cubic phase nanoparticles for sustained release of ibuprofen: formulation, characterization, and enhanced bioavailability study

被引:86
作者
Dian, Linghui [1 ,2 ]
Yang, Zhiwen [3 ]
Li, Feng [1 ]
Wang, Zhouhua [1 ]
Pan, Xin [1 ]
Peng, Xinsheng [2 ]
Huang, Xintian [1 ]
Guo, Zhefei [1 ]
Quan, Guilan [1 ]
Shi, Xuan [1 ]
Chen, Bao [1 ]
Li, Ge [4 ]
Wu, Chuanbin [1 ,4 ]
机构
[1] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
[2] Guangdong Med Coll, Sch Pharmaceut Sci, Dongguan, Peoples R China
[3] Shanghai Jiao Tong Univ, Affiliated Peoples Hosp 1, Songjiang Branch, Dept Gastroenterol, Shanghai 200030, Peoples R China
[4] Guangdong Res Ctr Drug Delivery Syst, Guangzhou, Guangdong, Peoples R China
基金
中国国家自然科学基金;
关键词
ibuprofen; cubic nanoparticles; oral drug delivery; bioavailability; IN-VITRO; ORAL BIOAVAILABILITY; DRUG; DELIVERY; MICROPARTICLES; MATRIX; ESTER;
D O I
10.2147/IJN.S40547
中图分类号
TB3 [工程材料学];
学科分类号
0805 ; 080502 ;
摘要
In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner structure was verified by cryogenic transmission electron microscopy. With an encapsulation efficiency greater than 85%, the ibuprofen-loaded cubic nanoparticles had a narrow size distribution around a mean size of 238 nm. Differential scanning calorimetry and X-ray diffraction determined that ibuprofen was in an amorphous and molecular form within the lipid matrix. The in vitro release of ibuprofen from cubic nanoparticles was greater than 80% at 24 hours, showing sustained characteristics. The pharmacokinetic study in beagle dogs showed improved absorption of ibuprofen from cubic nanoparticles compared to that of pure ibuprofen, with evidence of a longer half-life and a relative oral bioavailability of 222% (P < 0.05). The ibuprofen-loaded cubic nanoparticles provide a promising carrier candidate with an efficient drug delivery for therapeutic treatment.
引用
收藏
页码:845 / 854
页数:10
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