利用表面经半乳糖修饰的新型电荷转换介孔二氧化硅纳米粒子输送鳄梨籽提取物，以抗索拉非尼的肝细胞癌为靶标。

IF 6.6 2区医学 Q1 NANOSCIENCE & NANOTECHNOLOGY

International Journal of Nanomedicine Pub Date : 2024-10-14 eCollection Date: 2024-01-01 DOI:10.2147/IJN.S478574

Aalok Basu, Arunsajee Sae-Be, Thanaphon Namporn, Orasa Suriyaphan, Pongtip Sithisarn, Jiraporn Leanpolchareanchai, Piyaporn Plommaithong, Apichat Chatsukit, Khanit Sa-Ngiamsuntorn, Parichart Naruphontjirakul, Pakatip Ruenraroengsak

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引用次数: 0

摘要

背景：索拉非尼耐药（SR）肝细胞癌（HCC）是当前肝癌治疗中的一个严重问题。从植物中提取的大量植物化学物质具有抗癌活性，但从未针对耐药细胞进行过测试：方法：分析了通过浸渍法分离的鳄梨籽提取物（APE）的植物化学成分和抗癌活性。方法：分析了浸渍分离出的鳄梨籽提取物（APE）的植物化学成分和抗癌活性。合成了用于递送 APE 的新型设计电荷开关式 pH 响应纳米载体--带有共轭半乳糖的胺化介孔二氧化硅纳米颗粒（GMSN），并对其理化性质进行了表征。评估了药物负载效率（%LE）和夹带效率（%EE）。测量了负载 APE 的 GMSN 对 HCC（HepG2、Huh-7）和 SR-HCC （SR-HepG2）的抗癌活性：结果：APE 对非耐药性 HepG2（IC50 50.9 ± 0.83 μg mL-1）、Huh-7（IC50 42.41 ± 1.88 μg mL-1）和 SR-HepG2 （IC50 62.58 ± 2.29 μg mL-1）细胞的抗癌活性得到证实。负载 APE 的 GMSN 直径为 131.41 ± 14.41 nm，LE 为 41.08 ± 2.09%，EE 为 44.96 ± 2.26%。半乳糖官能化（55%）没有扰乱原有的介孔结构。在酸性介质 pH 值为 5.5 时，GMSN 可产生 10.3 ± 0.61mV 的正表面电荷，并在 2 小时内快速释放 45% 的 APE。它们在非耐药性 HCC 和 SR-HCC 细胞中的抗癌活性得到了证实，与对照组和非包囊 APE 相比，IC50 值分别为 30.73 ± 3.14（HepG2）、21.86 ± 0.83（Huh-7）、35.64 ± 1.34（SR-HepG2） μg mL-1：结论：负载 APE 的 GMSN 对非耐药 HCC 和 SR-HCC 都非常有效，值得进一步进行体内研究。

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Delivery of Avocado Seed Extract Using Novel Charge-Switchable Mesoporous Silica Nanoparticles with Galactose Surface Modified to Target Sorafenib-Resistant Hepatocellular Carcinoma.

Background: Sorafenib-resistant (SR) hepatocellular carcinoma (HCC) is a current serious problem in liver cancer treatment. Numerous phytochemicals derived from plants exhibit anticancer activity but have never been tested against drug-resistant cells.

Methods: Avocado seed extract (APE) isolated by maceration was analysed for its phytochemical composition and anticancer activity. Novel design charge-switchable pH-responsive nanocarriers of aminated mesoporous silica nanoparticles with conjugated galactose (GMSN) were synthesised for delivering APE and their physicochemical properties were characterized. The drug loading efficiency (%LE) and entrapment efficiency (%EE) were evaluated. Anticancer activity of APE loaded GMSN was measured against HCC (HepG2, Huh-7) and SR-HCC (SR-HepG2).

Results: Anticancer activity of APE against non-resistant HepG2 (IC₅₀ 50.9 ± 0.83 μg mL^-1), Huh-7 (IC₅₀ 42.41 ± 1.88 μg mL^-1), and SR-HepG2 (IC₅₀ 62.58 ± 2.29 μg mL^-1) cells was confirmed. The APE loaded GMSN had a diameter of 131.41 ± 14.41 nm with 41.08 ± 2.09%LE and 44.96 ± 2.26%EE. Galactose functionalization (55%) did not perturb the original mesoporous structure. The GMSN imparted positive surface charges, 10.3 ± 0.61mV at acidic medium pH 5.5 along with rapid release of APE 45% in 2 h. The GMSN boosted cellular uptake by HepG2 and SR-HepG2 cells, whereas the amine functionalized facilitated their endosomal escape. Their anticancer activity was demonstrated in non-resistant HCC and SR-HCC cells with IC₅₀ values at 30.73 ± 3.14 (HepG2), 21.86 ± 0.83 (Huh-7), 35.64 ± 1.34 (SR-HepG2) μg mL^-1, respectively, in comparison to the control and non-encapsulated APE.

Conclusion: APE loaded GMSN is highly effective against both non-resistant HCC and SR-HCC and warrants further in vivo investigation.

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来源期刊

International Journal of Nanomedicine NANOSCIENCE & NANOTECHNOLOGY-PHARMACOLOGY & PHARMACY

CiteScore

14.40

自引率

3.80%

发文量

511

审稿时长

1.4 months

期刊介绍： The International Journal of Nanomedicine is a globally recognized journal that focuses on the applications of nanotechnology in the biomedical field. It is a peer-reviewed and open-access publication that covers diverse aspects of this rapidly evolving research area. With its strong emphasis on the clinical potential of nanoparticles in disease diagnostics, prevention, and treatment, the journal aims to showcase cutting-edge research and development in the field. Starting from now, the International Journal of Nanomedicine will not accept meta-analyses for publication.