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利用叶酸功能化的载有多西他赛-厄洛替尼的生物聚合物纳米颗粒经鼻腔给药进行癌症治疗：研发、优化、表征及生物分布分析

Harnessing Folate-Functionalized Nasal Delivery of Dox-Erlo-Loaded Biopolymeric Nanoparticles in Cancer Treatment: Development, Optimization, Characterization, and Biodistribution Analysis.

作者信息

Farheen Ms, Akhter Md Habban, Chitme Havagiray, Akhter Md Sayeed, Tabassum Fauzia, Jaremko Mariusz, Emwas Abdul-Hamid

机构信息

School of Pharmaceutical and Population Health Informatics (SoPPHI), DIT University, Dehradun 248009, India.

Department of Clinical Pharmacy, College of Pharmacy, King Khalid University, Abha 62529, Saudi Arabia.

出版信息

Pharmaceuticals (Basel). 2023 Jan 30;16(2):207. doi: 10.3390/ph16020207.

DOI:10.3390/ph16020207
PMID:37259356
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9959140/
Abstract

The aim of the present study is to develop Doxorubicin-Erlotinib nanoparticles (Dox-Erlo NPs) and folate-armored Dox-Erlo-NP conjugates for targeting glioma cancer. Glioma is one of the most common progressive cancerous growths originating from brain glial cells. However, the blood-brain barrier (BBB) is only semi-permeable and is highly selective as to which compounds are let through; designing compounds that overcome this constraint is therefore a major challenge in the development of pharmaceutical agents. We demonstrate that the NP conjugates studied in this paper may ameliorate the BBB penetration and enrich the drug concentration in the target bypassing the BBB. NPs were prepared using a biopolymer with a double-emulsion solvent evaporation technique and functionalized with folic acid for site-specific targeting. Dox-Erlo NPs and Dox-Erlo-NP conjugates were extensively characterized in vitro for various parameters. Dox-Erlo NPs and Dox-Erlo-NP conjugates incurred a z-average of 95.35 ± 10.25 nm and 110.12 ± 9.2 nm, respectively. The zeta potentials of the Dox-Erlo NPs and Dox-Erlo-NP conjugates were observed at -18.1 mV and -25.1 mV, respectively. A TEM image has shown that the NPs were well-dispersed, uniform, de-aggregated, and consistent. A hemolytic assay confirmed hemocompatibility with the developed formulation and that it can be safely administered. Dox-Erlo-NP conjugates significantly reduced the number of viable cells to 24.66 ± 2.08% and 32.33 ± 2.51% in U87 and C6 cells, respectively, and IC50 values of 3.064 µM and 3.350 µM in U87 and C6 cells were reported after 24 h, respectively. A biodistribution study revealed that a significant concentration of Dox and Erlo were estimated in the brain relative to drug suspension. Dox-Erlo-NP conjugates were also stable for three months. The findings suggest that the developed Dox-Erlo-NP conjugates may be a promising agent for administration in glioma therapy.

摘要

本研究的目的是开发用于靶向胶质瘤的阿霉素 - 厄洛替尼纳米颗粒（Dox - Erlo NPs）和叶酸修饰的Dox - Erlo - NP缀合物。胶质瘤是起源于脑胶质细胞的最常见的进行性癌性生长之一。然而，血脑屏障（BBB）只是半透性的，并且对哪些化合物能通过具有高度选择性；因此，设计能够克服这一限制的化合物是药物开发中的一项重大挑战。我们证明，本文研究的NP缀合物可以改善血脑屏障的穿透性，并绕过血脑屏障在靶部位富集药物浓度。使用生物聚合物通过双乳液溶剂蒸发技术制备纳米颗粒，并用叶酸进行功能化以实现位点特异性靶向。对Dox - Erlo NPs和Dox - Erlo - NP缀合物的各种参数进行了广泛的体外表征。Dox - Erlo NPs和Dox - Erlo - NP缀合物的z平均直径分别为95.35±10.25 nm和110.12±9.2 nm。观察到Dox - Erlo NPs和Dox - Erlo - NP缀合物的zeta电位分别为 - 18.1 mV和 - 25.1 mV。透射电子显微镜（TEM）图像显示纳米颗粒分散良好、均匀、未聚集且形态一致。溶血试验证实了所开发制剂的血液相容性，并且可以安全给药。Dox - Erlo - NP缀合物在U87和C6细胞中分别将活细胞数量显著降低至24.66±2.08％和32.33±2.51％，并且在24小时后，U87和C6细胞中的IC50值分别报告为3.064 μM和3.350 μM。生物分布研究表明，相对于药物悬浮液，在脑中估计有显著浓度的阿霉素和厄洛替尼。Dox - Erlo - NP缀合物也稳定了三个月。研究结果表明，所开发的Dox - Erlo - NP缀合物可能是胶质瘤治疗中有前景的给药制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/e0010c48c916/pharmaceuticals-16-00207-g013.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/170ec394f9ed/pharmaceuticals-16-00207-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/17b1616e8cc8/pharmaceuticals-16-00207-g009.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/e0010c48c916/pharmaceuticals-16-00207-g013.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/e104ec1f2762/pharmaceuticals-16-00207-g004.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/3c34285ce216/pharmaceuticals-16-00207-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/b841cfc4a095/pharmaceuticals-16-00207-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/170ec394f9ed/pharmaceuticals-16-00207-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/17b1616e8cc8/pharmaceuticals-16-00207-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/486ac11b4661/pharmaceuticals-16-00207-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/77c198bf3727/pharmaceuticals-16-00207-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/b2602a6b28e3/pharmaceuticals-16-00207-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79b3/9959140/e0010c48c916/pharmaceuticals-16-00207-g013.jpg

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本文引用的文献

[1]
Phytosterol-Loaded Surface-Tailored Bioactive-Polymer Nanoparticles for Cancer Treatment: Optimization, In Vitro Cell Viability, Antioxidant Activity, and Stability Studies.

Gels. 2022-4-2

[2]
Impact of Protein Corona on the Biological Identity of Nanomedicine: Understanding the Fate of Nanomaterials in the Biological Milieu.

Biomedicines. 2021-10-19

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Doxorubicin-loaded nanoparticle coated with endothelial cells-derived exosomes for immunogenic chemotherapy of glioblastoma.

Bioeng Transl Med. 2020-12-3

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Targeting Cancer Cells Overexpressing Folate Receptors with New Terpolymer-Based Nanocapsules: Toward a Novel Targeted DNA Delivery System for Cancer Therapy.

Biomedicines. 2021-9-21

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CA Cancer J Clin. 2021-9

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Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy.

Polymers (Basel). 2021-3-17

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Int J Mol Sci. 2021-1-18

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SPION and doxorubicin-loaded polymeric nanocarriers for glioblastoma theranostics.

Drug Deliv Transl Res. 2021-4

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Molecular Targets and Nanoparticulate Systems Designed for the Improved Therapeutic Intervention in Glioblastoma Multiforme.

Drug Res (Stuttg). 2021-3

[10]
Receptor-based targeting of engineered nanocarrier against solid tumors: Recent progress and challenges ahead.

Biochim Biophys Acta Gen Subj. 2021-2

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