Controllable preparation of SB-3CT loaded PLGA microcapsules for traumatic-brain-injury pharmaco-therapy
Controllable preparation of SB-3CT loaded PLGA microcapsules for traumatic-brain-injury pharmaco-therapy
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SB-3CT负载PLGA微胶囊的可控制备用于创伤性脑损伤药物治疗
DOI：
10.1016/j.cej.2018.01.140
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发表时间：
2018-05-01
影响因子：
15.1
通讯作者：
Cen, Lian
中科院分区：
文献类型：
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作者：
Chen, Hong;Jia, Feng;Cen, Lian
本研究旨在探索可控制备载药2-[[（4-苯氧基苯基）磺酰基]甲基]硫杂环丙烷（SB-3CT）的聚乳酸-羟基乙酸共聚物（PLGA）微囊，用于创伤性脑损伤（TBI）的药物治疗。采用毛细管微流控技术制备了SB-3CT PLGA微囊。评价了相应PLGA微囊的载药和释放行为，并与其降解曲线相关联。所得PLGA微胶囊具有高尔夫球特征的形貌和高度的单分散性。可以通过改变毛细管装置的几何形状和操作参数来实现对微胶囊的尺寸和尺寸分布的精确控制，以产生在35-65 μ m范围内的均匀且可再现的PLGA微胶囊。药物包封率为99%，释放时间约为50 d。通过在TBI后的大鼠创伤部位局部注射PLGA-SB-3CT混悬液来尝试TBI的药物治疗。通过加速行为恢复（平衡木和平衡木行走能力，以及空间记忆能力）和减少CA 2和海马门以及损伤皮质区的神经元细胞凋亡，证明了给药后对脑组织的保护作用。因此，PLGA-SB-3CT可以作为TBI治疗的有希望的药物治疗选择。
This study is to explore controllable preparation of poly (lactic-co-glycolic acid) (PLGA) microcapsules to load 2-[[(4-phenoxyphenyl)sulfonyl]methyl]-thiirane (SB-3CT) for traumatic brain injury (TBI) pharmacological therapy. Capillary-based microfluidic method was proposed to prepare SB-3CT loaded PLGA microcapsules. Drug loading and release behavior of the corresponding PLGA microcapsules were evaluated and correlated with their degradation profile. The obtained PLGA microcapsules had a golf-featured morphology and high monodispersion. Precise control on the size and size distribution of the microcapsules could be achieved by varying the geometry of the capillary device and operation parameters to yield uniform and reproducible PLGA microcapsules in the range of 35-65 mu m. A high drug encapsulation efficiency of 99% within the obtained PLGA microcapsules with a releasing duration of around 50 d was ensured. Pharmacological therapy of TBI was tried by local injection of PLGA-SB-3CT suspension in rats at the trauma site after TBI. The protection on brain tissue upon administration was demonstrated by accelerated behavioral recovery (beam balance and beam walk latencies, and spatial memory ability) and reduction in the neuronal cell apoptosis in CA2 and hilus hippocampus as well as the injury cortical region. Hence, PLGA-SB-3CT could serve as a promising pharmaco-therapeutic option for TBI treatment.