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紫杉醇包封纳米粒经鼻腔给药治疗脑损伤。

Intranasal delivery of Paclitaxel encapsulated nanoparticles for brain injury due to Glioblastoma.

机构信息

Department of Pharmacy, Chongqing Emergency Medical Center, Chongqing University Central Hospital, Chongqing, China.

Department of Neurosurgery, Chongqing Emergency Medical Center, Chongqing University Central Hospital, Chongqing, China.

出版信息

J Appl Biomater Funct Mater. 2020 Jan-Dec;18:2280800020977170. doi: 10.1177/2280800020977170.

Abstract

Brain injury is a common cause for physical and emotional effects to the large number of populations. Moreover, glioblastoma is the tumor in brain with no possible treatment leading to death. The blood-brain barrier's makes the treatment more difficult by preventing the drugs to reach central nervous system. Paclitaxel (PTX) encapsulated Poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), PTX-PLGA-NPs were developed using emulsification method. The PTX-PLGA-NPs were characterized using Malvern Zetasizer and Scanning Electron Microscopy and were evaluated for their cytotoxicity in U87MG cells. PTX-PLGA-NPs were prepared using single emulsion method having size of 154 ± 22.19 nm with zeta potential of -23.7 mV. The PTX-PLGA-NPs were spherical in shape and have dose dependent cytotoxicity on U87MG cells. The PTX was released from the particles with initial burst release followed by sustained release pattern. The biodistribution was studied in mice with glioblastoma model using I radiolabeled PTX-PLGA-NPs and anti-glioblastoma was studied with PTX-PLGA-NPs. The biodistribution studies revealed PTX-PLGA-NPs after intranasal administration resulted in higher in vivo uptake with high anti-glioblastoma efficacy. The results suggest that PTX-PLGA-NPs administered through intranasal route have potential in the treatment of glioblastoma.

摘要

脑损伤是大量人群身体和情绪受到影响的常见原因。此外,胶质母细胞瘤是大脑中的肿瘤,没有可能的治疗方法导致死亡。血脑屏障通过阻止药物到达中枢神经系统,使治疗更加困难。紫杉醇(PTX)包封聚(乳酸-共-乙醇酸)(PLGA)纳米粒(NPs),PTX-PLGA-NPs 是通过乳化法开发的。使用马尔文 Zetasizer 和扫描电子显微镜对 PTX-PLGA-NPs 进行了表征,并在 U87MG 细胞中评估了它们的细胞毒性。PTX-PLGA-NPs 是通过单乳液法制备的,粒径为 154 ± 22.19nm,zeta 电位为-23.7mV。PTX-PLGA-NPs 呈球形,对 U87MG 细胞具有剂量依赖性细胞毒性。PTX 从粒子中释放出来,最初有突释,随后是持续释放模式。使用放射性标记的 PTX-PLGA-NPs 在患有胶质母细胞瘤模型的小鼠中进行了生物分布研究,并使用 PTX-PLGA-NPs 研究了抗胶质母细胞瘤。生物分布研究表明,经鼻内给药后,PTX-PLGA-NPs 体内摄取量增加,抗胶质母细胞瘤效果高。结果表明,经鼻内给予 PTX-PLGA-NPs 具有治疗胶质母细胞瘤的潜力。

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