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
相关论文
共 41 条
[1]   Design and study of ibuprofen disintegrating sustained-release tablets comprising coated pellets [J].
Abbaspour, M. R. ;
Sadeghi, F. ;
Garekani, H. Afrasiabi .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2008, 68 (03) :747-759
[2]   In vitro permeation and in vivo anti-inflammatory and analgesic properties of nanoscaled emulsions containing ibuprofen for topical delivery [J].
Abdullah, Ghassan Z. ;
Abdulkarim, Muthanna F. ;
Salman, Ibrahim M. ;
Ameer, Omar Z. ;
Yam, Mun F. ;
Mutee, Ahmed F. ;
Chitneni, Mallikarjun ;
Mahdi, Elrashid S. ;
Basri, Mahiran ;
Sattar, Munavvar A. ;
Noor, Azmin M. .
INTERNATIONAL JOURNAL OF NANOMEDICINE, 2011, 6 :387-396
[3]   Nitro-arginine methyl ester, a non-selective inhibitor of nitric oxide synthase reduces ibuprofen-induced gastric mucosal injury in the rat [J].
Abraham, P ;
K, I ;
K, D .
DIGESTIVE DISEASES AND SCIENCES, 2005, 50 (09) :1632-1640
[4]   Development and in vitro evaluation of mesalamine delayed release pellets and tableted reservoir-type pellets [J].
Bendas, Ehab R. ;
Christensen, J. Mark ;
Ayres, James W. .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2010, 36 (04) :393-404
[5]   A lipid-based liquid crystalline matrix that provides sustained release and enhanced oral bioavailability for a model poorly water soluble drug in rats [J].
Boyd, Ben J. ;
Khoo, Shui-Mei ;
Whittaker, Darryl V. ;
Davey, Greg ;
Porter, Christopher J. H. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2007, 340 (1-2) :52-60
[6]   How important is the role of the physician in the correct use of a drug? An observational cohort study in general practice [J].
Bradbury, F .
INTERNATIONAL JOURNAL OF CLINICAL PRACTICE, 2004, 58 :27-32
[7]   Vaidecoxib: A review [J].
Chavez, ML ;
DeKorte, CJ .
CLINICAL THERAPEUTICS, 2003, 25 (03) :817-851
[8]   Self-assembled "nanocubicle" as a carrier for peroral insulin delivery [J].
Chung, H ;
Kim, J ;
Um, JY ;
Kwon, IC ;
Jeong, SY .
DIABETOLOGIA, 2002, 45 (03) :448-451
[9]   Nanoparticle agglutination: Acceleration of aggregation rates and broadening of the analyte concentration range using mixtures of various-sized nanoparticles [J].
Costanzo, PJ ;
Patten, TE ;
Seery, TAP .
LANGMUIR, 2006, 22 (06) :2788-2794
[10]   Gastrointestinal uptake of biodegradable microparticles: Effect of particle size [J].
Desai, MP ;
Labhasetwar, V ;
Amidon, GL ;
Levy, RJ .
PHARMACEUTICAL RESEARCH, 1996, 13 (12) :1838-1845