Enhancing hepatoprotective action: oxyberberine amorphous solid dispersion system targeting TLR4

Chen, Tingting1,7; Li, Qingguo2; Ai, Gaoxiang8; Huang, Ziwei2; Liu, Jun5,6; Zeng, Lingfeng3,4,6; Su, Ziren2; Dou, Yaoxing1,3,4,6

2024-06-28

10.1038/s41598-024-65190-2

SCIENTIFIC REPORTS   影响因子和分区

2045-2322

Oxyberberine (OBB) is a significant natural compound, with excellent hepatoprotective properties. However, the poor water solubility of OBB hinders its release and absorption thus resulting in low bioavailability. To overcome these drawbacks of OBB, amorphous spray-dried powders (ASDs) of OBB were formulated. The dissolution, characterizations, and pharmacokinetics of OBB-ASDs formulation were investigated, and its hepatoprotective action was disquisitive in the D-GalN/LPS-induced acute liver injury (ALI) mouse model. The characterizations of OBB-ASDs indicated that the crystalline form of OBB active pharmaceutical ingredients (API) was changed into an amorphous form in OBB-ASDs. More importantly, OBB-ASDs showed a higher bioavailability than OBB API. In addition, OBB-ASDs treatment restored abnormal histopathological changes, improved liver functions, and relieved hepatic inflammatory mediators and oxidative stress in ALI mice. The spray drying techniques produced an amorphous form of OBB, which could significantly enhance the bioavailability and exhibit excellent hepatoprotective effects, indicating that the OBB-ASDs can exhibit further potential in hepatoprotective drug delivery systems. Our results provide guidance for improving the bioavailability and pharmacological activities of other compounds, especially insoluble natural compounds. Meanwhile, the successful development of OBB-ASDs could shed new light on the research process of poorly soluble medicine.

Acute liver injury Oxyberberine Amorphous solid dispersions Bioavailability

SCI

英语

其他

National Natural Science Foundation of China[82074082] ; China Postdoctoral Science Foundation[2022M710910] ; Youth fund project of national natural science foundation of China[82305270] ; Modern Agricultural Scientific Research Collaborative Innovation Project of Jiangxi[JXSNKYJCRC202441] ; Research Project on Traditional Chinese Medicine by Guangdong Provincial Administration of Traditional Chinese Medicine[20241124]

Science & Technology - Other Topics

Multidisciplinary Sciences

WOS:001258865400007

NATURE PORTFOLIO

Web of Science

1.Guangzhou Univ Chinese Med, Meizhou Hosp Tradit Chinese Med, Meizhou Hosp, 3 Huanan Ave, Meizhou, Guangdong, Peoples R China
2.Guangzhou Univ Chinese Med, Sch Pharmaceut Sci, Guangzhou, Peoples R China
3.Guangzhou Univ Chinese Med, Coll Clin Med 2, Guangzhou, Peoples R China
4.Guangzhou Univ Chinese Med, Guangdong Prov Hosp Chinese Med, Affiliated Hosp 2, Guangzhou, Peoples R China
5.Guangdong Prov Enginering Technol Res Inst Tradit, Guangdong Second Tradit Chinese Med Hosp, Guangzhou, Peoples R China
6.Guangdong Prov Acad Chinese Med Sci, Bone & Joint Res Team Degenerat & Injury, Guangzhou, Peoples R China
7.Southern Univ Sci & Technol, Sch Med, Shenzhen, Peoples R China
8.Jiangxi Acad Agr Sci, Inst Anim Husb & Vet Sci, Nanchang, Peoples R China

Chen, Tingting,Li, Qingguo,Ai, Gaoxiang,et al. Enhancing hepatoprotective action: oxyberberine amorphous solid dispersion system targeting TLR4[J]. SCIENTIFIC REPORTS,2024,14(1).

Chen, Tingting.,Li, Qingguo.,Ai, Gaoxiang.,Huang, Ziwei.,Liu, Jun.,...&Dou, Yaoxing.(2024).Enhancing hepatoprotective action: oxyberberine amorphous solid dispersion system targeting TLR4.SCIENTIFIC REPORTS,14(1).

Chen, Tingting,et al."Enhancing hepatoprotective action: oxyberberine amorphous solid dispersion system targeting TLR4".SCIENTIFIC REPORTS 14.1(2024).