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Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex
Zhang, Jinjie1; Peng, Qiang1; Shi, Sanjun1; Zhang, Qiang2; Sun, Xun1; Gong, Tao1; Zhang, Zhirong1
关键词morin phospholipid complex self-nanoemulsifying drug delivery system oral bioavailability
刊名INTERNATIONAL JOURNAL OF NANOMEDICINE
2011
DOI10.2147/IJN.S25824
6页:3405-3414
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Nanoscience & Nanotechnology ; Pharmacology & Pharmacy
研究领域[WOS]Science & Technology - Other Topics ; Pharmacology & Pharmacy
关键词[WOS]ORAL DELIVERY ; RATS ; FORMULATIONS ; ABSORPTION ; QUERCETIN ; DESIGN
英文摘要

Background: As a poorly water-soluble drug, the oral application of morin is limited by its low oral bioavailability. In this study, a new self-nanoemulsifying drug delivery system (SNEDDS), based on the phospholipid complex technique, was developed to improve the oral bioavailability of morin.

Methods: Morin-phospholipid complex (MPC) was prepared by a solvent evaporation method and characterized by infrared spectroscopy and X-ray diffraction. After formation of MPC, it was found that the liposolubility of morin was significantly increased, as verified through solubility studies. An orthogonal design was employed to screen the blank SNEDDS, using emulsifying rate and particle size as evaluation indices. Ternary phase diagrams were then constructed to investigate the effects of drug loading on the self-emulsifying performance of the optimized blank SNEDDS. Subsequently, in vivo pharmacokinetic parameters of the morin-phospholipid complex self-nanoemulsifying drug delivery system (MPC-SNEDDS) were investigated in Wistar rats (200 mg/kg of morin by oral administration).

Results: The optimum formulation was composed of Labrafil (R) M 1944 CS, Cremophor (R) RH 40, and Transcutol (R) P (3: 5: 3, w/w), which gave a mean particle size of approximately 140 nm. Oral delivery of the MPC-SNEDDS exhibited a significantly greater C(max) (28.60 mu g/mL) than the morin suspension (5.53 mu g/mL) or MPC suspension (23.74 mu g/mL) (all P < 0.05). T(max) was prolonged from 0.48 to 0.77 hours and to 1 hour for MPC and MPC-SNEDDS, respectively. In addition, the relative oral bioavailability of morin formulated in the MPC-SNEDDS was 6.23-fold higher than that of the morin suspension, and was significantly higher than that of the MPC suspension (P < 0.05).

Conclusion: The study demonstrated that a SNEDDS combined with the phospholipid complex technique was a promising strategy to enhance the oral bioavailability of morin.

语种英语
WOS记录号WOS:000298166900001
项目编号2009CB930300 ; 2009ZX09310-002
资助机构National Basic Research Program of China (973 program) ; National Science and Technology Major Project of China
引用统计
被引频次:47[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/68100
专题北京大学药学院
作者单位1.Sichuan Univ, W China Sch Pharm, Minist Educ, Key Lab Drug Targeting & Drug Delivery Syst, Chengdu 610041, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing, Peoples R China
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GB/T 7714
Zhang, Jinjie,Peng, Qiang,Shi, Sanjun,et al. Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex[J]. INTERNATIONAL JOURNAL OF NANOMEDICINE,2011,6:3405-3414.
APA Zhang, Jinjie.,Peng, Qiang.,Shi, Sanjun.,Zhang, Qiang.,Sun, Xun.,...&Zhang, Zhirong.(2011).Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex.INTERNATIONAL JOURNAL OF NANOMEDICINE,6,3405-3414.
MLA Zhang, Jinjie,et al."Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex".INTERNATIONAL JOURNAL OF NANOMEDICINE 6(2011):3405-3414.
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