title: Preparation, characterization and evaluation of breviscapine lipid emulsions coated with monooleate-PEG-COOH.
abstract: Series of monooleate-modified PEG with active carboxylic terminus on the other end (MO-PEG-COOH) were used to modify the lipid emulsions surface to prepare a sterically stabilized lipid emulsions for carrying Traditional Chinese Medicine - breviscapine. Based on the research of relationship between polymer structure and prolonged circulation activity, we developed an optimized formulation and a technological method to prepare the sterile and stable MO-PEG(10,000)-COOH (Bre-LE-PEG(10,000)) coated breviscapine lipid emulsions (Bre-LE) for intravenous administration. Follow the optimum preparation, the average particle size, polydispersity index, zeta potential, Ke value and content of final product were determined to be (207.1±8.5)nm, 0.197±0.005, (-33.6±2.0)mV, (21.1±2.3)% and (95.0±1.8)% respectively (n=3). The characteristics, stability and safety of Bre-LE-PEG(10,000) were also studied with Bre-LE as a control. Increased plasma concentration by surface modification of the lipid emulsions may enhance the pharmacological activity of breviscapine to promote blood circulation.
authors: State Key Laboratory of Bioelectronics, Jiangsu Laboratory for Biomaterials and Devices, School of Biological Science and Medical Engineering, Southeast University, Nanjing, 210096, China.
authors: Fei
authors: F
authors: Xiong
authors: Chen
authors: C
authors: Xiong
authors: Juan
authors: J
authors: Yao
authors: Xinmei
authors: X
authors: Chen
authors: Ning
authors: N
authors: Gu
mesh_terms: D000818:Animals; D047310:Apigenin / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D002264:Carboxylic Acids / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D002317:Cardiovascular Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D004355:Drug Stability; D004527:Egg Proteins / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D004655:Emulsions; D005419:Flavonoids / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D005965:Glucuronates / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D007668:Kidney / Q000033:anatomy & histology / Q000187:drug effects; D008099:Liver / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D008516:Medicine, Chinese Traditional; D051379:Mice; D009829:Oleic Acids / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D011817:Rabbits; D013024:Soybean Oil / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D013154:Spleen / Q000378:metabolism
chemical_list: D002264:Carboxylic Acids; D002317:Cardiovascular Agents; D004527:Egg Proteins; D004655:Emulsions; D005419:Flavonoids; D005965:Glucuronates; D009829:Oleic Acids; C061097:breviscapine; C484876:scutellarin; D011092:Polyethylene Glycols; D047310:Apigenin; D013024:Soybean Oil