Effect of phosphatidylcholine on the stability and lipolysis of nanoemulsion drug delivery systems

doi:10.1016/j.ijpharm.2020.119354

	Effect of phosphatidylcholine on the stability and lipolysis of nanoemulsion drug delivery systems
	Zhang, Bo 1,2; Zhou, Xin 1,3; Miao, Yunqiu 1; Wang, Xiaoli 1; Yang, Yuting 1,3; Zhang, Xinxin 1; Gan, Yong 1
刊名	INTERNATIONAL JOURNAL OF PHARMACEUTICS
	2020-06-15
卷号	583 页码:9
关键词	Phosphatidylcholine Nanoemulsion Stability Lipolysis kinetics Curcumin
ISSN号	0378-5173
DOI	10.1016/j.ijpharm.2020.119354
通讯作者	Zhang, Xinxin(xinxinzhang@simm.ac.cn) ; Gan, Yong(ygan@simm.ac.cn)
英文摘要	Phosphatidylcholines (PCs) have been widely used in pharmaceutical research. Unfortunately, our understanding of how PCs influence the in vivo lipolysis process of drug delivery systems is still limited. In this study, PCs with fatty acid chains of varying lengths and saturability were used as emulsifiers to prepare curcumin-loaded nanoemulsions (Cur-NEs). The differences in particle size as well as drug and free fatty acid release during the lipolysis process were studied in a simulated blood environment. Furthermore, the pharmacokinetics and antitumor efficacy of Cur-NEs were evaluated in mice. The prepared 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) and 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC)-stabilized Cur-NEs showed similar particle size and stability during storage but exhibited different lipolysis behaviors in vitro and in vivo. Due to the gel state of DPPC in the physiological environment, DPPC-stabilized Cur-NEs had low binding affinity with proteins and maintained their integrity in plasma, leading to sustained drug release, prolonged circulation time and enhanced antitumor efficacy in 4T1 tumor-bearing mice. In contrast, DOPC and DSPC-stabilized Cur-NEs were prone to coalescence in the plasma, resulting in rapid drug release and elimination from circulation. Our findings demonstrated that proper use of PCs is beneficial for obtaining desired transport behavior and drug therapeutic effects, providing guiding principles for rational design of nanodelivery systems.
资助项目	National Natural Science Foundation of China, China[81571796] ; National Natural Science Foundation of China, China[81973250] ; National Science and Technology Major Project, China[2018ZX09721002-003] ; National Science and Technology Major Project, China[NBHY-2017-J1-3] ; Strategic Priority Research Program of Chinese Academy of Sciences, China[XDA15014200] ; K.C. Wong Education Foundation
WOS关键词	LIPID EMULSIONS ; PHARMACOKINETICS ; APOLIPOPROTEIN ; NANOPARTICLES ; ENCAPSULATION ; DEGRADATION ; LIPOSOMES ; TOXICITY ; COMPLEX ; OIL
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER
WOS记录号	WOS:000537121800006
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/291629]
专题	中国科学院上海药物研究所
通讯作者	Zhang, Xinxin; Gan, Yong
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Univ Sci & Technol China, Nano Sci & Technol Inst, Suzhou 215123, Peoples R China 3.Nanchang Univ, Dept Pharm, Nanchang 330031, Jiangxi, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Bo,Zhou, Xin,Miao, Yunqiu,et al. Effect of phosphatidylcholine on the stability and lipolysis of nanoemulsion drug delivery systems[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2020,583:9.
APA	Zhang, Bo.,Zhou, Xin.,Miao, Yunqiu.,Wang, Xiaoli.,Yang, Yuting.,...&Gan, Yong.(2020).Effect of phosphatidylcholine on the stability and lipolysis of nanoemulsion drug delivery systems.INTERNATIONAL JOURNAL OF PHARMACEUTICS,583,9.
MLA	Zhang, Bo,et al."Effect of phosphatidylcholine on the stability and lipolysis of nanoemulsion drug delivery systems".INTERNATIONAL JOURNAL OF PHARMACEUTICS 583(2020):9.