Preparation and protective effects of 1,8-cineole-loaded self-microemulsifying drug delivery system on lipopolysaccharide-induced endothelial injury in mice

被引：26

作者：

Jiang, Feng ^{[1
,2
]}

Wu, Guoping ^{[1
,2
]}

Li, Wanrong ^{[1
,2
]}

Yang, Jiajia ^{[1
,2
]}

Yan, Junli ^{[1
,2
]}

Wang, Yi ^{[1
,2
]}

Yao, Wenli ^{[1
,2
]}

Zhou, Xue ^{[1
,2
]}

He, Zhiyong ^{[1
,2
]}

Wu, Linjing ^{[1
,2
]}

Xiao, Chaoda ^{[1
,2
]}

Xiao, Ting ^{[1
,2
]}

Zhang, Min ^{[3
]}

Shen, Xiangchun ^{[1
,2
]}

Tao, Ling ^{[1
,2
]}

机构：

[1] Guizhou Med Univ, High Educ Key Lab Guizhou Prov Nat Med Pharmacol, Key Lab Optimal Utilizat Nat Med Resources, Dept Pharmaceut TCM,Sch Pharmaceut Sci,Union Key, Guian New Dist 550025, Guizhou, Peoples R China

[2] Guizhou Med Univ, Sch Pharmaceut Sci, High Efficacy Applicat Nat Med Resources Engn Ctr, Guian New Dist 550025, Guizhou, Peoples R China

[3] Guizhou Med Univ, Sch Basic Med Sci, Guian New Dist 550025, Guizhou, Peoples R China

来源：

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2019年 / 127卷

关键词：

1,8-cineole; Self-microemulsifying drug delivery system; Vascular protection; Endothelial function; IN-VITRO; ATHEROSCLEROSIS; EUCALYPTOL; CYTOKINES; RATS;

D O I：

10.1016/j.ejps.2018.10.012

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

An optimised 1,8-cineole-loaded self-microemulsifying drug delivery system (CIN-SMEDDS) with a mean droplet size, polydispersity index, mean zeta potential and encapsulation efficiency of 38.14 +/- 1.47 nay, 0.208 +/- 0.036, -9.312 +/- 1.764 mV and 95.35% +/- 1.13%, respectively, successfully ameliorated the lipopolysaccharide (LPS)-induced endothelial injury in mice. Acute toxicity assay in mice through the oral administration of CIN-SMEDDS showed that the median lethal dose of CIN-SMEDDS was 2998.9 mg/kg. The results of 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide assay indicated that the cytotoxicity of CIN-SMEDDS to Caco-2 cells may be ascribed to the surfactant/co-surfactant mixture. In particular, CIN-SMEDDS remarkably inhibited inflammatory cytokines IL-1 beta IL-6 and IL-8 with a simultaneous increase in IL-10 in LPS-treated mice. Haematoxylin-eosin staining results showed that CIN-SMEDDS attenuated LPS-induced vascular endothelial injury. Western blot results showed that the vascular protective effects of CIN-SMEDDS were associated with the NF-kappa B and peroxisome proliferator-activated receptor gamma signalling pathways. These findings indicated that CIN-SMEDDS can attenuate LPS-induced endothelial injury and thus was proposed as a promising agent for the treatment of inflammatory cardiovascular disease.

引用

页码：14 / 23

页数：10

共 25 条

[1]

Assessment of cell viability and permeation enhancement in presence of lipid-based self-emulsifying drug delivery systems using Caco-2 cell model: Polysorbate 80 as the surfactant [J].