|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|
|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|
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.
|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|
|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
|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.|