负载多西他赛并涂有壳聚糖、羧甲基壳聚糖或乙二醇壳聚糖的聚乳酸-共-乙醇酸纳米粒子。

IF 2.2 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Nusaiba K Al-Nemrawi, Alaa Abu Dayah, Ruba Darweesh
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引用次数: 0

摘要

简介多西他赛(DTX)是一种具有高毒性和低生物利用度的化疗药物。为了解决这些问题,研究人员在 PLGA 纳米颗粒(NPs)中添加了 DTX,并在其表面包覆了粘附性聚合物:壳聚糖(CS)、羧甲基壳聚糖(CMCS)或乙二醇壳聚糖(GCS)。对 NPs 的尺寸、电荷和多分散性进行了表征:使用 SEM、FTIR、DSC 和 XRD 对颗粒进行了研究。进行了体外研究,以评估 NPs 的粘附性和药物释放情况。结果验证了球形和单分散 DTX NPs 的成功形成。包覆的 NPs 带有高正电荷,达到 +44.30±0.21 mV,而未包覆的 NPs 几乎呈中性:结果:这些配方表现出优异的封装效率(大于 98%)和负载能力(大于 45%)。包衣过程中使用的所有聚合物都增强了 PLGA NPs 的粘附性和 DTX 的持续释放。粘附性和释放都与所使用的包衣聚合物及其浓度有关。这些制剂在冰箱中可稳定保存三个月:总之,在 PLGA NPs 中加入 DTX 并用 CS、CMCS 或 GCS 包衣,是增加 NPs 在粘膜表面停留时间的有效方法,有望降低 DTX 的所需剂量并减少其副作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Poly(Lactic-co-Glycolic Acid Nanoparticles Loaded with Docetaxel and Coated with Chitosan, Carboxymethyl Chitosan, or Glycol Chitosan.

Introduction: Docetaxel (DTX) is a chemotherapeutic drug that has high toxicity and low bioavailability. To solve these problems, PLGA nanoparticles (NPs) were loaded with DTX and coated with mucoadhesive polymers; chitosan (CS), carboxymethyl chitosan (CMCS), or glycol chitosan(GCS). The NPs were characterized for size, charge, and polydispersity.

Method: The particles were explored using SEM, FTIR, DSC, and XRD. In vitro studies were performed to evaluate the mucoadhesive properties of the NPs and the drug release. The results validated the successful formation of spherical and monodispersed DTX NPs. The coated NPs exhibited highly positive charges, reaching +44.30±0.21 mV, whereas the uncoated NPs were almost neutral.

Result: The formulations demonstrated excellent encapsulation efficiency (>98%) and loading capacity (>45%). All polymers used in the coating process enhanced the mucoadhesive properties of PLGA NPs and sustained DTX release. Both the mucoadhesiveness and release were related to the used coating polymer and its concentration. The formulations were stable for up to three months in the refrigerator.

Conclusion: In conclusion, loading DTX in PLGA NPs and coating them with CS, CMCS, or GCS provides a promising strategy to increase the NPs' residence time on mucosal surfaces, which is expected to decrease the required dose of DTX and reduce its side effects.

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来源期刊
Current pharmaceutical biotechnology
Current pharmaceutical biotechnology 医学-生化与分子生物学
CiteScore
5.60
自引率
3.60%
发文量
203
审稿时长
6 months
期刊介绍: Current Pharmaceutical Biotechnology aims to cover all the latest and outstanding developments in Pharmaceutical Biotechnology. Each issue of the journal includes timely in-depth reviews, original research articles and letters written by leaders in the field, covering a range of current topics in scientific areas of Pharmaceutical Biotechnology. Invited and unsolicited review articles are welcome. The journal encourages contributions describing research at the interface of drug discovery and pharmacological applications, involving in vitro investigations and pre-clinical or clinical studies. Scientific areas within the scope of the journal include pharmaceutical chemistry, biochemistry and genetics, molecular and cellular biology, and polymer and materials sciences as they relate to pharmaceutical science and biotechnology. In addition, the journal also considers comprehensive studies and research advances pertaining food chemistry with pharmaceutical implication. Areas of interest include: DNA/protein engineering and processing Synthetic biotechnology Omics (genomics, proteomics, metabolomics and systems biology) Therapeutic biotechnology (gene therapy, peptide inhibitors, enzymes) Drug delivery and targeting Nanobiotechnology Molecular pharmaceutics and molecular pharmacology Analytical biotechnology (biosensing, advanced technology for detection of bioanalytes) Pharmacokinetics and pharmacodynamics Applied Microbiology Bioinformatics (computational biopharmaceutics and modeling) Environmental biotechnology Regenerative medicine (stem cells, tissue engineering and biomaterials) Translational immunology (cell therapies, antibody engineering, xenotransplantation) Industrial bioprocesses for drug production and development Biosafety Biotech ethics Special Issues devoted to crucial topics, providing the latest comprehensive information on cutting-edge areas of research and technological advances, are welcome. Current Pharmaceutical Biotechnology is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments.
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