Micro- and Nanoencapsulated Hybrid Delivery System (MNEHDS): A Novel Approach for Colon-Targeted Oral Delivery of Berberine

doi:10.1021/acs.molpharmaceut.0c00970

	Micro- and Nanoencapsulated Hybrid Delivery System (MNEHDS): A Novel Approach for Colon-Targeted Oral Delivery of Berberine
	Zhang, Lingzhi 1,4; Li, Mingyan 1,4; Zhang, Guiqiu 1,4; Gao, Changxing 1,4; Wang, Shengfang 2,3; Zhang, Tingting 1,4; Ma, Chen 1,4; Wang, Lianyan 3; Zhu, Qing 1,4
刊名	MOLECULAR PHARMACEUTICS
	2021-04-05
卷号	18 期号:4 页码:1573-1581
关键词	berberine microencapsulation nanoencapsulation nanoparticle controlled release Eudragit dextran sulfate sodium-induced colitis drug delivery system
ISSN号	1543-8384
DOI	10.1021/acs.molpharmaceut.0c00970
英文摘要	Berberine (BBR) is currently explored in the oral treatment of many disorders, especially in those involving inflammatory processes. Nanotechnology-based drug delivery systems are emerging as an effective approach for improving the poor oral absorption/bioavailability of BBR. To optimize the BBR immunoregulatory effects on a specific part of the gastrointestinal tract, here we describe a micro- and nanoencapsulated hybrid delivery system (MNEHDS) for colon-targeted oral delivery of BBR and test its therapeutic efficacy in a murine colitis model. The MNEHDS is formed by encapsulation of BBR-loaded poly(lactic-co-glycolic acid) nanoparticles into a pH-sensitive, BBR-pre-entrapped Eudragit FS30D matrix to form a hybrid microparticle composed of the BBR and BBR nanoparticles. Once in the colonic environment, the microencapsulated BBR is almost completely released for immediate action, while BBR nanoparticles can provide sustained release of BBR subsequent to their intestinal absorption. One dose of oral MNEHDS/BBR treatment results in significant attenuation of acute colitis induced by dextran sulfate sodium. The MNEHDS/BBR also proves to be effective during chronically induced colitis with two doses given 1 week apart. The improved efficacy is accompanied by decreased production of colon inflammation. Comparatively, oral treatment with one or two 7-day courses of free BBR has less effect on ameliorating either acute or chronic colitis. Thus, MNEHDS represents a novel delivery system for BBR, and potentially other therapeutic agents, to treat inflammatory bowel disease.
资助项目	National Natural Science Foundation of China, China[31370922] ; National Natural Science Foundation of China, China[81973262] ; Beijing Natural Science Foundation, China[5131002] ; CAMS Major Collaborative Innovation Project, China[2016-12M-1-011] ; National Science and Technology Major Project of China[2016ZX10004001-005]
WOS研究方向	Research & Experimental Medicine ; Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000637870700007
资助机构	National Natural Science Foundation of China, China ; Beijing Natural Science Foundation, China ; CAMS Major Collaborative Innovation Project, China ; National Science and Technology Major Project of China
内容类型	期刊论文
源URL	[http://ir.ipe.ac.cn/handle/122111/48517]
专题	中国科学院过程工程研究所
通讯作者	Wang, Lianyan; Zhu, Qing
作者单位	1.Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China 2.Northeast Forestry Univ, Coll Chem Chem Engn & Resource Utilizat, Harbin 150040, Peoples R China 3.Chinese Acad Sci, Inst Proc Engn, Key Lab Green Proc & Engn, State Key Lab Biochem Engn, Beijing 100190, Peoples R China 4.Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, Beijing Key Lab New Drug Mech & Pharmacol Evaluat, Beijing 100050, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Lingzhi,Li, Mingyan,Zhang, Guiqiu,et al. Micro- and Nanoencapsulated Hybrid Delivery System (MNEHDS): A Novel Approach for Colon-Targeted Oral Delivery of Berberine[J]. MOLECULAR PHARMACEUTICS,2021,18(4):1573-1581.
APA	Zhang, Lingzhi.,Li, Mingyan.,Zhang, Guiqiu.,Gao, Changxing.,Wang, Shengfang.,...&Zhu, Qing.(2021).Micro- and Nanoencapsulated Hybrid Delivery System (MNEHDS): A Novel Approach for Colon-Targeted Oral Delivery of Berberine.MOLECULAR PHARMACEUTICS,18(4),1573-1581.
MLA	Zhang, Lingzhi,et al."Micro- and Nanoencapsulated Hybrid Delivery System (MNEHDS): A Novel Approach for Colon-Targeted Oral Delivery of Berberine".MOLECULAR PHARMACEUTICS 18.4(2021):1573-1581.