Double flow focusing microfluidic-assisted based preparation of methotrexate-loaded liposomal nanoparticles: Encapsulation efficacy, drug release and stability

Double flow focusing microfluidic-assisted based preparation of methotrexate-loaded liposomal nanoparticles: Encapsulation efficacy, drug release and stability
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DOI:
10.1016/j.colsurfa.2021.126166
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发表时间:
2021-01-26
影响因子:
5.2
通讯作者:
Varshosaz, Jaleh
Varshosaz, Jaleh
中科院分区:
化学2区
文献类型:
--
作者:
Aghaei, Halimeh;Nazar, Ali Reza Solaimany;Varshosaz, Jaleh

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本研究提出了一种利用双流聚焦微流控(double- mhff)装置在单步工艺中制备载甲氨蝶呤(MTX)脂质体颗粒的新方法。双mhff设计通过增加两相的扩散表面积来增强质量扩散,可以作为制备载药聚乙二醇化脂质体的良好选择。通过调整流速比(FRR)、总流速(TFR)、总脂质浓度和MTX浓度等操作参数和配方参数,优化所制备的MTX-脂质体(MTX- l)和MTX-聚乙二醇化脂质体(MTX- pll)的粒径、多分散性(PDI)和包封效率等理化特性。同时,对MTX-L和MTX-PLL颗粒进行了释放研究。MTX-L和MTX-PLL纳米颗粒的平均粒径范围分别在90 ~ 230 nm和118 ~ 258 nm, PDI分别< 0.32和0.23。双mhff器件具有很高的封装效率(>= 60%),尤其适用于MTXPLL。此外,MTX-PLL纳米颗粒具有长达72小时的缓释和长效性(< 48%)。这意味着MTX的高封装效率和低释放是生产过程的结果。
This study presents a novel and facile route to produce the methotrexate (MTX) loaded liposomal particles using the double flow focusing microfluidic (double-MHFF) device in a single step process. The double-MHFF design, due to the intensification of the mass diffusion by increasing the diffusion surface area of both phases can be a good candidate to produce the drug-loaded PEGylated liposomes. The physicochemical characteristics of the prepared MTX-liposome (MTX-L) and MTX-PEGylated liposome (MTX-PLL) such as particle size, polydispersity (PDI), and encapsulation efficiency are optimized by adjusting the operational and formulation parameters, like flow rate ratio (FRR), total flow rate (TFR), total lipid concentration and MTX concentration. Also, the release study is performed for MTX-L and MTX-PLL particles. The range of average size of the MTX-L and MTX-PLL nanoparticles are within 90-230 nm and 118-258 nm with PDI < 0.32 and PDI < 0.23, respectively. The double-MHFF device has the ability for achieving high encapsulation efficiency (>= 60 %), especially for MTXPLL. Also, the MTX-PLL nanoparticles have a sustained release and long-term fashion up to 72 h (< 48 %). This means that the high encapsulation efficiency and low release of MTX result from the production process.