Department of Neurosurgery, Second Affiliated Hospital, Nanchang University, Nanchang, Jiangxi, China.
Int J Nanomedicine. 2018 May 22;13:3039-3051. doi: 10.2147/IJN.S161163. eCollection 2018.
Glioblastoma multiforme (GBM) is the most common malignant brain tumor originating in the central nervous system in adults. Based on nanotechnology such as liposomes, polymeric nanoparticles, and lipid nanoparticles, recent research efforts have been aimed to target drugs to the brain.
In this study, lactoferrin- and arginine-glycine-aspartic acid (RGD) dual- ligand-comodified, temozolomide and vincristine-coloaded nanostructured lipid carriers (L/RT/V-NLCs) were introduced for GBM combination therapy. The physicochemical properties of L/R-T/V-NLCs such as particle size, zeta potential, and encapsulated efficiency are measured. The drug release profile, cellular uptake, cytotoxicity, tissue distribution, and antitumor activity of L/R-T/V-NLCs are further investigated in vitro and in vivo.
L/R-T/V-NLCs were stable with nanosize and high drug encapsulation efficiency. L/R-T/V-NLCs exhibited sustained-release behavior, high cellular uptake, high cytotoxicity and synergy effects, increased drug accumulation in the tumor tissue, and obvious tumor inhibition efficiency with low systemic toxicity.
L/R-T/V-NLCs could be a promising drug delivery system for glioblastoma chemotherapy.
多形性胶质母细胞瘤（GBM）是成人中枢神经系统中最常见的恶性脑肿瘤。基于脂质体、聚合物纳米粒和脂质纳米粒等纳米技术，最近的研究工作旨在将药物靶向递送到大脑。
在这项研究中，引入了乳铁蛋白和精氨酸-甘氨酸-天冬氨酸（RGD）双重配体修饰、替莫唑胺和长春新碱共载纳米结构脂质载体（L/RT/V-NLCs），用于 GBM 联合治疗。测量了 L/R-T/V-NLCs 的物理化学性质，如粒径、Zeta 电位和包封效率。进一步在体外和体内研究了 L/R-T/V-NLCs 的药物释放特性、细胞摄取、细胞毒性、组织分布和抗肿瘤活性。
L/R-T/V-NLCs 具有纳米尺寸和高药物包封效率的稳定性。L/R-T/V-NLCs 表现出持续释放行为、高细胞摄取、高细胞毒性和协同作用、增加肿瘤组织中的药物积累以及明显的肿瘤抑制效率，同时具有低系统毒性。
L/R-T/V-NLCs 可能是胶质母细胞瘤化疗的一种有前途的药物递送系统。
