ABSTRACT
PUE@PEG-PLGA micelles has excellent characteristics such as small particle size, high drug loading and slow drug release. The results of TEM electron microscopy showed that PUE@PEG-PLGA micelles had obvious core-shell structure. The critical micelle concentration(CMC) of PEG-PLGA micelles determined by pyrene assay was about 4.8 mg·L~(-1). Laser confocal experiments showed that PEG-PLGA micelles can enhance the cellular uptake of coumarin-6 and aggregate around the mitochondria; quantitative results of extracellular drug residues also indirectly confirmed that PEG-PLGA micelles can promote cellular uptake of the drug. Acute ischemic myocardial model rats were prepared by coronary artery ligation, and then the model rats were randomly divided into six groups: Sham operation group, model group, puerarin(PUE) group, as well as low-, mid-, and high-dose PUE@PEG-PLGA micelles groups. Drugs were given by iv administration 5 min after the ligation. The ST segment changes in the electrocardiogram were monitored; serum creatine kinase(CK), lactate dehydrogenase(LDH), aspartate aminotransferase(AST), and malondialdehyde(MDA) levels were detected and myocardial infarct size was also measured. Both PUE and PUE@PEG-PLGA micelles can reduce the elevated ST segment, reduce serum CK, LDH, AST and MDA levels, and reduce myocardial infarct size. The efficacy of PUE@PEG-PLGA medium and high dose groups was significantly better than that in the PUE group, and the efficacy in PUE@PEG-PLGA low dose group was basically equivalent to that in the PUE group. PUE@PEG-PLGA micelles can greatly improve the cardiomyocytes uptake of PUE, enhance the anti-acute myocardial ischemia effect of drugs, and reduce its dosage.
Subject(s)
Animals , Rats , Isoflavones , Pharmacology , Micelles , Myocardial Ischemia , Drug Therapy , Polyesters , Polyethylene Glycols , Random AllocationABSTRACT
<p><b>OBJECTIVE</b>To observe the protective effect of Yixinshu capsule on myocardial ischemia reperfusion injury (MIRI) in SD rats.</p><p><b>METHOD</b>Sixty healthy SD rats were randomized into six groups: sham group, MIRI model group, Xinsuning capsule group, low, middle or high dose Yixinshu capsule. Acute MIRI rat models were created by reperfusion for 120 min after anterior interventricular branch of the left coronary artery for 30 min. The serum creatine kinase (CK), lactic dehydrogenase (LDH), aspartate aminotransferase (AST) and malondialdehyde(MDA), blood viscosity, and infarction area of myocardium were determined.</p><p><b>RESULT</b>Yixinshu capsule could reduce serum CK, LDH, AST and LDH activity, improve the blood viscosity, and reduced the myocardial infarct size.</p><p><b>CONCLUSION</b>Yixinshu capsule can protect against MIRI in rats.</p>
Subject(s)
Animals , Male , Rats , Blood Viscosity , Capsules , Drugs, Chinese Herbal , Therapeutic Uses , Lipid Peroxidation , Myocardial Infarction , Drug Therapy , Metabolism , Pathology , Myocardial Reperfusion Injury , Rats, Sprague-DawleyABSTRACT
<p><b>OBJECTIVE</b>To detect the stability of PEGylated puerarin (PEG-PUE), in order to provide experimental basis for storage conditions of PEGylated puerarin.</p><p><b>METHOD</b>First, a method for determining the content of PEG-PUE was established. Next, a system study was conducted for the stability of PEG-PUE affected by different factors such as temperature, humidity, light and light avoidance.</p><p><b>RESULT</b>PEG-PUE was severely degraded under the conditions of high temperature, high humidity and light. It was also seriously degraded under high temperature.</p><p><b>CONCLUSION</b>PEG-PUE shall be stored under low temperature and in a dark and dry environment.</p>