负载新型抗结核剂的褐藻糖胶涂层脂质体:制备、评估和细胞毒性研究。

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pharmaceutical Development and Technology Pub Date : 2024-04-01 Epub Date: 2024-03-28 DOI:10.1080/10837450.2024.2332454
Manar M Obiedallah, Vsevolod V Melekhin, Yaroslava A Menzorova, Emmanuella T Bulya, Artem S Minin, Maxim A Mironov
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引用次数: 0

摘要

在这篇文章中,我们介绍了一种新型抗结核咪唑四嗪衍生物,该衍生物被设计在褐藻糖胶包裹的脂质体中,以降低其细胞毒性并研究其粘附特性。首先,使用从 Ascophyllum nodosum 提取的褐藻糖胶进一步稳定脂质体悬浮液,并赋予其粘附性。PEG-600 和/或吐温-80 用于延长脂质体悬浮液的保质期。褐藻糖胶与脂质的比例为1:2,这是产生稳定的褐藻糖胶包裹脂质体的最佳比例。最佳配方的粒度为 336.3 ± 5.4,PDI 为 0.33,zeta 电位为 -39.6。原子力显微镜证实了颗粒的这一大小和实际球形。此外,未包衣脂质体和褐藻糖胶包衣脂质体的体外释放曲线显示,与游离抗结核剂相比,包衣脂质体的释放速度明显更快。通过 MTT 试验,褐藻糖胶包衣脂质体的细胞毒性(IC50 7.14 ± 0.91 µg/ml)比游离药物(IC50 0.49 ± 0.06)低 14 倍。此外,使用蜗牛粘蛋白也证实了这些脂质体制剂的粘附能力,这凸显了其作为抗结核治疗的有效给药系统的潜力,并显著改善了溶解速度和降低了细胞毒性。
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Fucoidan coated liposomes loaded with novel antituberculosis agent: preparation, evaluation, and cytotoxicity study.

In this article, we described a novel antituberculosis imidazotetrazine derivative designed in fucoidan-coated liposomes to reduce its cytotoxicity and investigate its mucoadhesive properties. Firstly, fucoidan extracted from Ascophyllum nodosum was used for additional stabilization of liposomal suspensions and to give it mucoadhesive properties. PEG-600 and/or Tween-80 were used to increase the shelf life of liposomal suspension. The ratio of the fucoidan: lipids 1:2 was found to be the optimum that produces stable fucoidan-coated liposomes. The particle size of the optimum formulation was 336.3 ± 5.4, the PDI was 0.33, and the zeta potential was -39.6. This size and the practical spherical shape of the particles were confirmed by atomic force microscopy. In addition, the in vitro release profiles from uncoated and fucoidan-coated liposomes revealed significant and faster release compared to free antituberculosis agent. Using the MTT assay test, the fucoidan-coated liposomes exhibited fourteen times lower cytotoxicity (IC50 7.14 ± 0.91 µg/ml) than the free drug (IC50 0.49 ± 0.06). Moreover, the mucoadhesive capabilities of these liposomal formulations were also confirmed using snail mucin, which highlighting their potential use as an effective delivery system for antituberculosis therapy, with notable improvements in dissolution rate and reduced cytotoxicity.

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来源期刊
CiteScore
5.90
自引率
2.90%
发文量
82
审稿时长
1 months
期刊介绍: Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology. Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as: -Preformulation and pharmaceutical formulation studies -Pharmaceutical materials selection and characterization -Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation -QbD in the form a risk assessment and DoE driven approaches -Design of dosage forms and drug delivery systems -Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies -Drug delivery systems research and quality improvement -Pharmaceutical regulatory affairs This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.
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