采用新型超临界流体法制备负载 PEG 的盐酸伊立替康脂质体,并通过 Box-Behnken 设计对条件进行优化。

IF 5.5 3区 材料科学 Q2 MATERIALS SCIENCE, MULTIDISCIPLINARY
Misagh Mohammadi, Mehrnaz Karimi, Farhad Raofie
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引用次数: 0

摘要

一种名为盐酸伊立替康的半合成喜树碱衍生物常用于治疗结直肠癌,包括结直肠腺癌和涉及小细胞的肺癌。伊立替康的半衰期很短,因此需要持续输注才能使血液中的药物浓度保持在治疗水平,这可能会产生累积毒性。目前已开发出包括脂质体在内的有效给药技术来解决这些缺陷。本研究提出了一种被称为 "向水溶液中注入超临界流体(Expansion Supercritical Fluid)"的连续超临界流体方法,在这种方法中,压力迅速降低,但仍保持在临界压力以上,从而制造出携带盐酸伊立替康的聚乙二醇化(PEG)脂质体。为了实现这一目标,我们采用盒-贝肯设计法制造了 PEG 化脂质体,并对操作参数(流速、温度和压降)进行了优化。在理想情况下,封装效率、平均尺寸和制备的脂质体数量分别为 94.6%、55 nm 和 758。此外,还对 PEG 化脂质体在 8 周内的稳定性进行了研究,并将 PEG 化脂质体负载的伊立替康的释放曲线与传统脂质体和游离伊立替康进行了比较,结果表明,在脂质体第一次猝灭释放后,药物会持续释放。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Preparation irinotecan hydrochloride loaded PEGylated liposomes using novel method supercritical fluid and condition optimized by Box–Behnken design

Preparation irinotecan hydrochloride loaded PEGylated liposomes using novel method supercritical fluid and condition optimized by Box–Behnken design

A semi-synthetic camptothecin derivative known as irinotecan hydrochloride is frequently used to treat colorectal cancer, including colorectal adenocarcinoma and lung cancers involving small cells. Irinotecan has a very short half-life; therefore, continuous infusions are required to keep the drug’s blood levels at therapeutic levels, which could produce cumulative toxicities. Effective delivery techniques, including liposomes, have been developed to address these shortcomings. In this study, a continuous supercritical fluid approach dubbed Expansion Supercritical Fluid into an aqueous solution, in which the pressure decreases rapidly but remains over the critical pressure, is proposed to manufacture polyethylene glycolylated (PEGylated) liposomes carrying irinotecan hydrochloride. To accomplish this, PEGylated liposomes were created using a Box–Behnken design, and the operating parameters (flow rate, temperature, and pressure drop) were optimized. Encapsulation efficiency, mean size, and prepared liposome count were 94.6%, 55 nm, and 758 under ideal circumstances. Additionally, the stability of the PEGylated liposome was investigated during 8 weeks, and also PEGylated liposome-loaded irinotecan release profile was compared to conventional liposomes and free irinotecan, and a constant drug release was seen after the first burst release from liposomes.

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来源期刊
Nanoscale Research Letters
Nanoscale Research Letters 工程技术-材料科学:综合
CiteScore
11.30
自引率
0.00%
发文量
110
审稿时长
48 days
期刊介绍: Nanoscale Research Letters (NRL) provides an interdisciplinary forum for communication of scientific and technological advances in the creation and use of objects at the nanometer scale. NRL is the first nanotechnology journal from a major publisher to be published with Open Access.
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