Liposome-encapsulated berberine treatment reduces adverse ventricle remodeling after myocardial infarction

J.W. Wang, I.E. Allijn, B.M.S. Czarny, X.Y. Wang, S.Y. Chong, G. Pastorin, D.P.V. De Kleijn, G. Storm, R.M. Schiffelers

Research output: Contribution to journalArticleAcademicpeer-review


Introduction: Adverse left ventricle remodeling can be measured as a reduction in ejection fraction after myocardial infarction. Left ventricle remodeling leads to congestive heart failure and is a main determinant of mortality and morbidity after myocardial infarction. Berberine is an isoquinoline alkaloid extracted from barberry that has anti-inflammatory and anti-oxidant activities. Pretreatment with long-term administration of high doses of berberine has shown beneficial effects in experimental diabetes and cardiac ischemia reperfusion injury. However, the poor solubility and the short half-life in the circulation have impeded the clinical use of berberine. Purpose: To examine whether encapsulation of berberine into long-circulating liposomes could improve its therapeutic availability and efficacy to protect cardiac function in vivo. Methods: Berberine was loaded into liposomes at a concentration of 0.3 mg/ml. Lipopolysaccharide (LPS) activated mouse macrophages RAW 264.7 were treated with free berberine or liposome-encapsulated berberine (Lipo-Berb) and analyzed for cell viability, reactive oxygen species production and cytokine secretion. C57BL/6J male mice (10-12 week old) subjected to myocardial infarction (MI) via permanent ligation of the left anterior descending artery were blindly selected for intravenous injection of empty liposomes, free berberine or lipo-Berb (1.5 mg/kg). Three doses were administered at the onset of MI, and at 3 and 6 days after MI. Ejection fraction was assessed by echocardiography at baseline, 7 and 28 days after MI. Results: Free berberine improved the viability of LPS-insulted macrophages, reduced production of reactive oxygen species and inhibited the secretion of inflammatory mediators including IL-6 and TNFα. As expected these protective effects of berberine in vitro were diminished upon encapsulation into liposomes. In vivo, however, the liposome-encapsulated berberine significantly preserved ejection fraction after 28 days of MI while free berberine did not show any preservation of ejection fraction (29.5±1.9 for lipo-Berb, 18.2±3.2 for free berberine and 18.0±3.1 for empty liposomes; n=6-10; p
Original languageEnglish
Article numberP4586
Pages (from-to)919
Number of pages1
JournalEuropean Heart Journal
Publication statusPublished - 24 Aug 2016


  • berberine
  • endogenous compound
  • interleukin 6
  • lipopolysaccharide
  • liposome
  • reactive oxygen metabolite
  • tumor necrosis factor
  • animal experiment
  • animal model
  • C57BL 6 mouse
  • cell viability
  • cytokine production
  • drug solubility
  • echocardiography
  • encapsulation
  • experimental diabetes mellitus
  • half life time
  • heart ejection fraction
  • heart muscle ischemia
  • heart ventricle remodeling
  • human versus animal comparison
  • in vitro study
  • intravenous drug administration
  • left anterior descending coronary artery
  • ligation
  • macrophage
  • male
  • mediator
  • mouse
  • nonhuman
  • RAW 264.7 cell line
  • reperfusion injury


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