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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.
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页码:845 / 854
页数:10
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