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Solid lipid nanoparticles with and without hydroxypropyl β-cyclodextrin: A comparative study of nanoparticles designed for colonic drug delivery

机译:有和没有羟丙基β-环糊精的固体脂质纳米颗粒:用于结肠给药的纳米颗粒的比较研究

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摘要

New solid lipid nanoparticles (SLN), composed of Compritol ATO888 (C) and hydroxypropyl - cyclodextrin (HP), were developed in order to study a new colon-specific formulation for diclofenac sodium (D) delivery. The prepared batches differ from each other by the molecular ratio between HP and D and by the composition of the matrix. Nanoparticles composed of an exclusively lipid matrix and nanoparticles with an oligomeric and lipid matrix were compared in order to establish the effect of both components on the drug delivery tests performed. The SLN preparation method was based on the oil/water hot homogenization process. Emulsions produced were cooled at room temperature and lyophilized in order to obtain dried nanoparticles; possible damage to nanoparticle shape and size was avoided by the addition of cryoprotectants to the aqueous dispersion of nanoparticles before exsiccation. An invitro toxicity study was performed using CaCo _2 cells to establish the safety of the prepared SLN. Data obtained showed that production method studied guarantees emulsions composed of nanosized drops which can be dried by lyophilization into SLN with a size range of 300600nm. Invitro and exvivo tests demonstrated that dried SLN can be considered as colon delivery systems; however, the matrix composition as well as the presence of cryoprotectant on their surface influences the release and permeation rate of D. The invitro toxicity studies indicated that the SLN are well tolerated.
机译:为了研究一种新的结肠特异性制剂用于双氯芬酸钠(D)的输送,开发了由Compritol ATO888(C)和羟丙基-环糊精(HP)组成的新型固体脂质纳米颗粒(SLN)。所制备的批次之间的区别在于HP和D之间的分子比以及基质的组成。比较仅由脂质基质组成的纳米颗粒以及具有寡聚和脂质基质的纳米颗粒,以便确定两种组分对所进行的药物递送测试的影响。 SLN的制备方法基于油/水热均质过程。将产生的乳液在室温下冷却并冻干,以获得干燥的纳米颗粒。通过在干燥前向纳米颗粒的水分散体中添加冷冻保护剂,避免了对纳米颗粒形状和尺寸的可能损害。使用CaCo _2细胞进行了体外毒性研究,以确定所制备的SLN的安全性。获得的数据表明,所研究的生产方法可保证由纳米滴组成的乳液,可通过冻干干燥成尺寸为300600nm的SLN进行干燥。体外和离体试验表明,干燥的SLN可被视为结肠递送系统。但是,基质成分以及表面上防冻剂的存在会影响D的释放和渗透速率。体外毒性研究表明SLN具有良好的耐受性。

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