Evaluating a targeted Palbociclib-Trastuzumab loaded smart niosome platform for treating HER2 positive breast cancer cells

IF 5.2 2区医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics: X Pub Date : 2024-03-11 DOI:10.1016/j.ijpx.2024.100237

Shaghayegh Saharkhiz , Negar Nasri , Nazanin Naderi , Ghasem Dini , Saeid Shirzadi Ghalehshahi , Fateme Firoozbakht

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Abstract

In this study, we present a targeted and pH-sensitive niosomal (pHSN) formulation, incorporating quantum dot (QD)-labeled Trastuzumab (Trz) molecules for the specific delivery of Palbociclib (Pal) to cells overexpressing human epidermal growth factor receptor 2 (HER2). FTIR analyses confirmed the successful preparation of the pHSNs and their bioconjugation. The labeled Trz-conjugated Pal-pHSNs (Trz-Pal-pHSNs) exhibited a size of approximately 170 nm, displaying a spherical shape with a neutral surface charge of −1.2 mV. Pal encapsulation reached ∼86%, and the release pattern followed a two-phase pH-dependent mechanism. MTT assessments demonstrated enhanced apoptosis induction, particularly in HER2-positive cells, by Trz-Pal-pHSNs. Fluorescence imaging further validated the internalization of particles into cells. In conclusion, Trz-Pal-pHSNs emerge as a promising platform for personalized medicine in the treatment of HER2-positive breast cancer.

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评估用于治疗 HER2 阳性乳腺癌细胞的靶向 Palbociclib-Trastuzumab 负载智能 niosome 平台

在这项研究中，我们提出了一种具有靶向性和 pH 值敏感性的 niosomal（pHSN）制剂，其中加入了量子点（QD）标记的曲妥珠单抗（Trz）分子，用于将 Palbociclib（Pal）特异性地递送到过表达人表皮生长因子受体 2（HER2）的细胞中。傅立叶变换红外分析证实了 pHSNs 的成功制备及其生物共轭。标记的Trz-共轭Pal-pHSNs（Trz-Pal-pHSNs）大小约为170 nm，呈球形，表面中性电荷为-1.2 mV。Pal 的封装率达到了 ∼86%，释放模式遵循两相 pH 依赖性机制。MTT 评估表明，Trz-Pal-pHSNs 增强了细胞凋亡诱导作用，尤其是在 HER2 阳性细胞中。荧光成像进一步验证了颗粒在细胞内的内化。总之，Trz-Pal-pHSNs 是治疗 HER2 阳性乳腺癌的一种前景广阔的个性化医疗平台。

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来源期刊

International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

6.60

自引率

0.00%

发文量

审稿时长

24 days

期刊介绍： International Journal of Pharmaceutics: X offers authors with high-quality research who want to publish in a gold open access journal the opportunity to make their work immediately, permanently, and freely accessible. International Journal of Pharmaceutics: X authors will pay an article publishing charge (APC), have a choice of license options, and retain copyright. Please check the APC here. The journal is indexed in SCOPUS, PUBMED, PMC and DOAJ. The International Journal of Pharmaceutics is the second most cited journal in the "Pharmacy & Pharmacology" category out of 358 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.