Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM's NMIMS, Mumbai, Maharashtra, India.
Biotechnol J. 2021 Dec;16(12):e2100271. doi: 10.1002/biot.202100271. Epub 2021 Oct 12.
Over the globe, the incidence of glioblastoma multiforme (GM) is very low, that is, 1-4 cases per 100,000, but it is fatal and cancer grows very fast inside the brain tissues, namely astrocytes and oligodendrocytes. Because of the rapid growth, it is difficult to halt the dissemination of tumor in adjacent tissues. Although temozolomide (TMZ) is a currently approved standard of care, it develops resistance over the period. Therefore, there is a need to develop a novel drug delivery system. In this work, authors have developed platelets as drug delivery carriers-loaded with quercetin (QCT) for targeting GM. The effect of QCT and QCT-platelet was assessed on the U373-MG cell line. Natural human platelets were used as carriers for drug loading and drug delivery. Platelets possess an open canalicular system that allows the uptake of drug molecules in the platelet cytoplasm. The study showed that the maximum encapsulation efficiency of QCT-platelet was 93.96 ± 0.12% and the maximum drug release in 24 h was 76.26 ± 0.13% in-vitro at pH 5.5 that mimics the tumor microenvironment. In this work, there is a three-fold enhancement of solubility of QCT. The cytotoxic activity of QCT-platelets was studied in the U373-MG human astrocytoma glioblastoma cell line and the cell viability was 14.52 ± 1.53% after 48 h. Thus, platelets were proved as good carriers for therapeutic moieties and can be effectively used to target the glioblastoma tumor in the near future.
在全球范围内,多形性胶质母细胞瘤(GBM)的发病率非常低,即每 10 万人中有 1-4 例,但它是致命的,而且癌细胞在脑组织内生长非常快,即星形胶质细胞和少突胶质细胞。由于生长迅速,很难阻止肿瘤在邻近组织中的扩散。尽管替莫唑胺(TMZ)是目前批准的标准治疗方法,但它在一段时间后会产生耐药性。因此,需要开发一种新的药物输送系统。在这项工作中,作者开发了血小板作为药物输送载体-负载槲皮素(QCT),用于靶向 GBM。评估了 QCT 和 QCT-血小板对 U373-MG 细胞系的作用。天然人血小板被用作药物加载和药物输送的载体。血小板具有开放的腔道系统,允许药物分子在血小板细胞质中被摄取。研究表明,QCT-血小板的最大包封效率为 93.96±0.12%,在 pH5.5 下 24 小时内的最大药物释放量为 76.26±0.13%,体外模拟肿瘤微环境。在这项工作中,QCT 的溶解度提高了三倍。研究了 QCT-血小板对 U373-MG 人星形胶质细胞瘤胶质母细胞瘤细胞系的细胞毒性活性,48 小时后细胞活力为 14.52±1.53%。因此,血小板被证明是治疗有效成分的良好载体,并且可以在不久的将来有效地用于靶向神经胶质瘤肿瘤。