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Anandamide-loaded nanoparticles: Preparation and characterization

机译:载有anandamide的纳米颗粒:制备与表征

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Objective: Preparation and characterization of anandamide (N-arachidonoyl-ethanolamine, AEA) loaded polycaprolactone nanoparticles (PCL NP) as a research tool to clarify the presence of an AEA transporter in cell membranes and to avoid AEA plastic adsorption and instability. Materials and methods: High performance liquid chromatography and light scattering were used to determine encapsulation efficiency, particle size, drug release, permeability and stability. Results: A high encapsulation efficiency 96.05 ±1.77% and a particle size of 83.52 ± 21.38 nm were obtained. Nearly 40% of AEA remained in the NP after a 99.9% dilution and only 50% was released after 24 h at 37°C with a 99% dilution. PCL NP prevented the adsorption of the drug to polypropylene or polystyrene, but not to acrylic multiwell plates. Drug permeability through artificial membranes was low (10~(-7) to 10~(-8)cm/s) and was affected by the presence of NP. NP increased AEA stability in suspension (drug half-life 431 h vs. 12h) and freeze-dried with 5% sucrose. Conclusion: This article presents the first study where stable AEA-loaded NP with high encapsulation efficiencies have been obtained.
机译:目的:制备和表征载有甲酰胺(N-花生四烯酸乙醇胺,AEA)的聚己内酯纳米颗粒(PCL NP),作为澄清细胞膜中AEA转运蛋白的存在以及避免AEA塑料吸附和不稳定性的研究工具。材料和方法:高效液相色谱法和光散射法用于测定包封效率,粒径,药物释放,通透性和稳定性。结果:获得了高的包封效率96.05±1.77%和粒径83.52±21.38 nm。在99.9%稀释后,近40%的AEA保留在NP中,而在37°C 24小时后,以99%稀释仅释放了50%的AEA。 PCL NP阻止了药物吸附到聚丙烯或聚苯乙烯上,但不能吸附到丙烯酸多孔板上。通过人造膜的药物渗透率低(10〜(-7)至10〜(-8)cm / s),并受NP的影响。 NP增加了悬浮液中AEA的稳定性(药物半衰期为431小时vs. 12小时),并用5%蔗糖冷冻干燥。结论:本文提出了第一项研究,获得了具有高包封效率的稳定的AEA负载NP。

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