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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Preparation and characterization of PLGA nanospheres for the targeted delivery of NR2B-specific antisense oligonucleotides to the NMDA receptors in the brain
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Preparation and characterization of PLGA nanospheres for the targeted delivery of NR2B-specific antisense oligonucleotides to the NMDA receptors in the brain

机译：PLGA纳米球的制备和表征，用于将NR2B特异性反义寡核苷酸靶向递送至大脑中的NMDA受体

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Treatment of central nervous system (CNS) diseases with potentially useful Pharmaceuticals is prevented by the blood-brain barrier (BBB).The BBB is a unique protective barrier in the body.It is formed by epithelial-like tight junctions,which are expressed by the brain capillary endothelial cells.Although most molecules are potentially active in the CNS,they cannot readily enter the brain because of their properties.Antisense oligonucleotides (ODNs) have a great potential as neuropharmaceuticals;however,the large size and polar nature of nucleic acid drugs prevent these molecules from bypassing the BBB and readily entering the CNS following systemic administration.One approach to improve both the pharmacokinetics and the pharmacodynamics of ODNs involves the use of sustained-release polymer formulations,such as poly(lactide-co-glycolide) (PLGA) nanoparticulate systems.In this study,nanospheres were prepared by the emulsification diffusion technique and characterized in terms of particle size,surface morphology,encapsulation efficiency,in vitro release profiles and ODN stability.The nanospheres produced were spherical with homogenous size distribution.Nanospheres were prepared with different encapsulation efficiency.Release profiles of formulations were also evaluated.The results show that formulations with different ODN content exhibited different release profiles.Moreover,the chemical integrity of ODN during the processes was conserved.These results demonstrate that a stable ODN formulation could be prepared utilizing PLGA nanospheres as a potential delivery system for the treatment of CNS diseases.
机译：血脑屏障（BBB）可以防止使用可能有用的药物治疗中枢神经系统（CNS）疾病.BBB是机体内独特的保护屏障，由上皮样紧密连接形成，其表达方式为尽管大多数分子在中枢神经系统中都具有潜在的活性，但由于其特性，它们无法轻易进入大脑。反义寡核苷酸（ODN）作为神经药物具有巨大的潜力;然而，核酸的大尺寸和极性性质药物可防止这些分子绕过BBB并在全身给药后容易进入CNS。一种改善ODN药代动力学和药效学的方法包括使用缓释聚合物制剂，例如聚丙交酯-乙交酯（ PLGA）纳米颗粒体系。在这项研究中，纳米颗粒通过乳化扩散技术制备并通过颗粒表征尺寸，表面形态，包封效率，体外释放曲线和ODN稳定性。产生的纳米球呈球形，具有均匀的粒径分布。制备具有不同包封效率的纳米球。还评估了制剂的释放曲线。结果表明，具有不同ODN的制剂结果表明，利用PLGA纳米球作为中枢神经系统疾病的潜在释放系统，可以制备出稳定的ODN制剂。

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