Ingallina C, Rinaldi F, Bogni A, Ponti J, Passeri D, Reggente M, Rossi M, Kinsner-Ovaskainen A, Mehn D, Rossi F, Botta B, Carafa M, Marianecci C
Center for Life Nano Science@Sapienza, Istituto Italiano di Tecnologia (ITT), Viale Regina Elena 291, 00161 Rome, Italy; Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, P.zzle A. Moro 5, 00185 Roma, Italy.
Center for Life Nano Science@Sapienza, Istituto Italiano di Tecnologia (ITT), Viale Regina Elena 291, 00161 Rome, Italy.
Int J Pharm. 2016 Sep 25;511(2):969-82. doi: 10.1016/j.ijpharm.2016.08.002. Epub 2016 Aug 3.
The majority of active agents do not readily permeate into brain due to the presence of the blood-brain barrier and blood-cerebrospinal fluid barrier. Currently, the most innovative and promising non-invasive strategy in brain delivery is the design and preparation of nanocarriers, which can move through the brain endothelium. Niosomes can perform brain delivery, in fact polysorbates, can act as an anchor for apolipoprotein E from blood plasma. The particles mimic LDL and interact with the LDL receptor leading to the endothelial cells uptake. The efficacy of niosomes for anticancer therapeutic applications was correlated to their physicochemical and drug delivery properties. Dimensions and ζ-potential were characterized using dynamic light scattering and asymmetric flow-field fractionation system. Lipid bilayer was characterized measuring the fluidity, polarity and microviscosity by fluorescent probe spectra evaluation. Morphology and homogeneity were characterized using atomic force microscopy. Physicochemical stability and serum stability (45% v/v fetal bovine and human serum) were evaluated as a function of time using dynamic light scattering. U87-MG human glioblastoma cells were used to evaluate vesicle cytotoxicity and internalisation efficiency. From the obtained data, the systems appear useful to perform a prolonged (modified) release of biological active substances to the central nervous system.
由于血脑屏障和血脑脊液屏障的存在，大多数活性剂不易渗透到大脑中。目前，脑递送中最具创新性和前景的非侵入性策略是设计和制备能够穿过脑内皮的纳米载体。脂质体可以实现脑递送，事实上，聚山梨酯可以作为血浆中载脂蛋白E的锚定物。这些颗粒模拟低密度脂蛋白（LDL）并与LDL受体相互作用，导致内皮细胞摄取。脂质体在抗癌治疗应用中的功效与其物理化学和药物递送特性相关。使用动态光散射和不对称流场分级系统对尺寸和ζ电位进行表征。通过荧光探针光谱评估测量流动性、极性和微粘度来表征脂质双层。使用原子力显微镜表征形态和均匀性。使用动态光散射评估物理化学稳定性和血清稳定性（45% v/v胎牛血清和人血清）随时间的变化。使用U87-MG人胶质母细胞瘤细胞评估囊泡的细胞毒性和内化效率。从获得的数据来看，这些系统似乎有助于向中枢神经系统进行生物活性物质的长效（改良）释放。
