Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex

Jinjie Zhang1, Qiang Peng1, Sanjun Shi1, Qiang Zhang2, Xun Sun1, Tao Gong1, Zhirong Zhang11Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, People&#39;s Republic of China; 2State Key Laboratory of Na...

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Autores principales:	Zhang J, Peng Q, Shi S, Zhang Q, Sun X, Gong T, Zhang Z
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/64dc7258c8fa4fb0af3198910fc22007
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spelling	oai:doaj.org-article:64dc7258c8fa4fb0af3198910fc220072021-12-02T01:11:25ZPreparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex1176-91141178-2013https://doaj.org/article/64dc7258c8fa4fb0af3198910fc220072011-12-01T00:00:00Zhttp://www.dovepress.com/preparation-characterization-and-in-vivo-evaluation-of-a-self-nanoemul-a8904https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Jinjie Zhang1, Qiang Peng1, Sanjun Shi1, Qiang Zhang2, Xun Sun1, Tao Gong1, Zhirong Zhang11Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, People&#39;s Republic of China; 2State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Peking, People&#39;s Republic of ChinaBackground: 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&reg; M 1944 CS, Cremophor&reg; RH 40, and Transcutol&reg; 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 Cmax (28.60 &micro;g/mL) than the morin suspension (5.53 &micro;g/mL) or MPC suspension (23.74 &micro;g/mL) (all P &lt; 0.05). Tmax 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 &lt; 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.Keywords: morin, phospholipid complex, self-nanoemulsifying drug delivery system, oral bioavailabilityZhang JPeng QShi SZhang QSun XGong TZhang ZDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 3405-3414 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Zhang J Peng Q Shi S Zhang Q Sun X Gong T Zhang Z Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex
description	Jinjie Zhang1, Qiang Peng1, Sanjun Shi1, Qiang Zhang2, Xun Sun1, Tao Gong1, Zhirong Zhang11Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, People&#39;s Republic of China; 2State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Peking, People&#39;s Republic of ChinaBackground: 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&reg; M 1944 CS, Cremophor&reg; RH 40, and Transcutol&reg; 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 Cmax (28.60 &micro;g/mL) than the morin suspension (5.53 &micro;g/mL) or MPC suspension (23.74 &micro;g/mL) (all P &lt; 0.05). Tmax 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 &lt; 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.Keywords: morin, phospholipid complex, self-nanoemulsifying drug delivery system, oral bioavailability
format	article
author	Zhang J Peng Q Shi S Zhang Q Sun X Gong T Zhang Z
author_facet	Zhang J Peng Q Shi S Zhang Q Sun X Gong T Zhang Z
author_sort	Zhang J
title	Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex
title_short	Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex
title_full	Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex
title_fullStr	Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex
title_full_unstemmed	Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex
title_sort	preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (snedds) loaded with morin-phospholipid complex
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/64dc7258c8fa4fb0af3198910fc22007
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Preparation, characterization, and in vivo evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) loaded with morin-phospholipid complex

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