Biochemistry Department, Faculty of Science, Ege University, 35040, Izmir, Turkey; Center for Drug Research, Development and Pharmacokinetic Applications (ARGEFAR), Ege University, 35100, Izmir, Turkey.
Biochemistry Department, Faculty of Science, Ege University, 35040, Izmir, Turkey.
Colloids Surf B Biointerfaces. 2021 Oct;206:111946. doi: 10.1016/j.colsurfb.2021.111946. Epub 2021 Jun 26.
The aim of this study was the preparation of solid lipid nanoparticles (SLN) formed from cetyl palmitate with having targeting molecules for monocarboxylate transporter-1 (MCT-1): β-hydroxybutyric acid and anticancer agents: carmustine (BCNU) and temozolomide (TMZ) for enhanced anti-proliferation against glioblastoma multiforme (GBM). Properties including size, morphology, chemical structure, zeta potential, drug encapsulation efficacy, drug release, biocompatibility, stability were determined, and in vitro studies were done. BCNU and TMZ loaded SLNs had a hydrodynamic size of 227 nm ± 46 a zeta potential of -25 mV ± 4 with biocompatible features. The data showed rapid drug release at first and then continuous release. Nanoparticles could be stored for nine months. BCNU and TMZ loaded SLNs exhibited a remarkable increment in the antitumor activity compared to the free-drugs and induced apoptosis on U87MG cells. In addition, targeted nanoparticles were more uptaken by MCT-1 expressing brain cells. This study indicated that BCNU and TMZ loaded SLNs could act as a useful anticancer system for targeted GBM therapy.
本研究旨在制备由十六酸十六酯形成的固体脂质纳米粒（SLN），并将其靶向单羧酸转运蛋白-1（MCT-1）：β-羟基丁酸和抗癌药物：卡莫司汀（BCNU）和替莫唑胺（TMZ），以增强对多形性胶质母细胞瘤（GBM）的抗增殖作用。对其包括粒径、形态、化学结构、Zeta 电位、药物包封效率、药物释放、生物相容性和稳定性在内的性质进行了测定，并进行了体外研究。载有 BCNU 和 TMZ 的 SLN 的水动力学粒径为 227nm±46，Zeta 电位为-25mV±4，具有生物相容性。数据显示，药物释放初期较快，随后持续释放。纳米粒可在 9 个月内储存。与游离药物相比，载有 BCNU 和 TMZ 的 SLN 显著提高了抗肿瘤活性，并诱导 U87MG 细胞发生细胞凋亡。此外，靶向纳米粒被表达 MCT-1 的脑细胞更多摄取。本研究表明，载有 BCNU 和 TMZ 的 SLN 可作为一种用于靶向 GBM 治疗的有用抗癌系统。
