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Lipoamino acid-based cerasomes for doxorubicin delivery: Preparation and in vitro evaluation

机译:基于脂质体的阿霉素递质的陶瓷体:制备和体外评价

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Cerasomes are hybrid organic-inorganic nanoparticles (NPs) that could be considered as liposomes with rather durable silicon shell. In this study, several cerasome-forming lipoamino acids (CFLA) were synthesized and used as structural blocks for cerasome preparation. Pure cerasomes which contained only CFLA, and mixed cerasomes based on a mixture of CFLA with a disintegrating dipalmitoylphosphatidylcholine (DPPC) lipid were fabricated and characterized in terms of morphology, mean size, zeta-potential, stability at storage. All obtained cerasome samples were found to be much more stable at storage than conventional liposomes (120 and 10 days, respectively). The cerasomes were loaded with doxorubicin (DOX) and tested in vitro using human breast adenocarcinoma MCF-7. Effects of the lipid composition on the physical-chemical properties and cellular uptake of the cerasomes both in 2D (monolayer culture) and 3D (multicellular tumor spheroids) were studied. The biggest accumulation efficiencies as well as the highest cytotoxicity level were found for the mixed cationic cerasomes. These cerasomes could be proposed as promising drug delivery system for cancer treatment.
机译:陶瓷小体是有机-无机杂化纳米颗粒(NPs),可以认为是具有相当耐用的硅壳的脂质体。在这项研究中,合成了几种形成陶瓷小体的脂氨基酸(CFLA),并将其用作制备陶瓷小体的结构单元。制备仅包含CFLA的纯陶瓷体,以及基于CFLA与崩解的二棕榈酰磷脂酰胆碱(DPPC)脂质的混合物的混合陶瓷体,并根据形态,平均大小,ζ电位,储存稳定性进行表征。发现所有获得的陶瓷体样品在储存时都比常规脂质体稳定得多(分别为120天和10天)。将阿霉素(DOX)加载到陶瓷小体上,并使用人乳腺癌MCF-7在体外进行测试。研究了脂质成分对2D(单层培养)和3D(多细胞肿瘤球体)中的脂质体的物理化学性质和细胞摄取的影响。对于混合的阳离子陶瓷体,发现最大的积累效率以及最高的细胞毒性水平。可以将这些陶瓷体作为有望用于癌症治疗的药物递送系统。

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