Racoviceanu Roxana, Trandafirescu Cristina, Voicu Mirela, Ghiulai Roxana, Borcan Florin, Dehelean Cristina, Watz Claudia, Aigner Zoltán, Ambrus Rita, Coricovac Dorina Elena, Cîrcioban Denisa, Mioc Alexandra, Szuhanek Camelia Alexandrina, Şoica Codruţa
Department of Pharmaceutical Chemistry, Victor Babeș University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041 Timisoara, Romania.
Department of Pharmacology and Clinical Pharmacy, Victor Babeș University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041 Timisoara, Romania.
Molecules. 2020 Nov 4;25(21):5130. doi: 10.3390/molecules25215130.
Albendazole is a benzimidazole derivative with documented antitumor activity and low toxicity to healthy cells. The major disadvantage in terms of clinical use is its low aqueous solubility which limits its bioavailability. Albendazole was incorporated into stable and homogeneous polyurethane structures with the aim of obtaining an improved drug delivery system model. Spectral and thermal analysis was used to investigate the encapsulation process and confirmed the presence of albendazole inside the nanoparticles. The in vitro anticancer properties of albendazole encapsulated in polyurethane structures versus the un-encapsulated compound were tested on two breast cancer cell lines, MCF-7 and MDA-MB-231, in terms of cellular viability and apoptosis induction. The study showed that the encapsulation process enhanced the antitumor activity of albendazole on the MCF-7 and MDA-MB-23 breast cancer lines. The cytotoxic activity manifested in a concentration-dependent manner and was accompanied by changes in cell morphology and nuclear fragmentation.
阿苯达唑是一种苯并咪唑衍生物，具有已被证实的抗肿瘤活性，且对健康细胞毒性较低。就临床应用而言，其主要缺点是水溶性低，这限制了其生物利用度。为了获得一种改进的药物递送系统模型，阿苯达唑被纳入稳定且均匀的聚氨酯结构中。采用光谱和热分析来研究包封过程，并证实了纳米颗粒中存在阿苯达唑。就细胞活力和凋亡诱导方面，对两种乳腺癌细胞系MCF-7和MDA-MB-231测试了包封在聚氨酯结构中的阿苯达唑与未包封化合物相比的体外抗癌特性。研究表明，包封过程增强了阿苯达唑对MCF-7和MDA-MB-23乳腺癌细胞系的抗肿瘤活性。细胞毒性活性呈浓度依赖性表现，并伴有细胞形态变化和核碎片化。
