Preparation, characterization and evaluation of breviscapine lipid emulsions coated with monooleate–PEG–COOH

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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–PEG10,000–COOH (Bre–LE–PEG10,000) 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–PEG10,000 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.

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