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载泊沙康唑的大麻籽油纳米胶束治疗侵袭性真菌病。

Posaconazole-hemp seed oil loaded nanomicelles for invasive fungal disease.

机构信息

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, 110062, New Delhi, India.

Department of Pharmaceutics, Delhi Pharmaceutical Sciences and Research University (DPSRU), New Delhi, 110017, India.

出版信息

Sci Rep. 2024 Jul 18;14(1):16588. doi: 10.1038/s41598-024-66074-1.

Abstract

Invasive fungal infections (IFI) pose a significant health burden, leading to high morbidity, mortality, and treatment costs. This study aims to develop and characterize nanomicelles for the codelivery of posaconazole and hemp seed oil for IFI via the oral route. The nanomicelles were prepared using a nanoprecipitation method and optimized through the Box Behnken design. The optimized nanomicelles resulted in satisfactory results for zeta potential, size, PDI, entrapment efficiency, TEM, and stability studies. FTIR and DSC results confirm the compatibility and amorphous state of the prepared nanomicelles. Confocal laser scanning microscopy showed that the optimized nanomicelles penetrated the tissue more deeply (44.9µm) than the suspension (25µm). The drug-loaded nanomicelles exhibited sustained cumulative drug release of 95.48 ± 3.27% for 24 h. The nanomicelles showed significant inhibition against Aspergillus niger and Candida albicans (22.4 ± 0.21 and 32.2 ± 0.46 mm, respectively). The pharmacokinetic study on Wistar rats exhibited a 1.8-fold increase in relative bioavailability for the nanomicelles compared to the suspension. These results confirm their therapeutic efficacy and lay the groundwork for future research and clinical applications, providing a promising synergistic antifungal nanomicelles approach for treating IFIs.

摘要

侵袭性真菌感染(IFI)对健康造成重大负担,导致高发病率、死亡率和治疗费用。本研究旨在通过口服途径开发并表征米托蒽醌和大麻籽油的共递送纳米胶束,用于治疗 IFI。纳米胶束采用纳米沉淀法制备,并通过 Box-Behnken 设计进行优化。优化后的纳米胶束在zeta 电位、粒径、PDI、包封效率、TEM 和稳定性研究中均取得了满意的结果。FTIR 和 DSC 结果证实了制备的纳米胶束的相容性和非晶态。共聚焦激光扫描显微镜显示,与混悬剂(25µm)相比,优化后的纳米胶束能更深地穿透组织(44.9µm)。载药纳米胶束在 24 小时内表现出 95.48±3.27%的持续累积药物释放。纳米胶束对黑曲霉和白色念珠菌显示出显著的抑制作用(分别为 22.4±0.21 和 32.2±0.46mm)。在 Wistar 大鼠的药代动力学研究中,与混悬剂相比,纳米胶束的相对生物利用度增加了 1.8 倍。这些结果证实了它们的治疗效果,并为未来的研究和临床应用奠定了基础,为治疗 IFI 提供了一种有前途的协同抗真菌纳米胶束方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b733/11258229/0d28bce2bc41/41598_2024_66074_Fig1_HTML.jpg

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