二丙酸倍氯米松纳米微囊治疗豚鼠哮喘模型的实验研究

Experimental Study on BDP Nanocapsule in Treatment of Asthmatic Pulgea Pigs

目的 :研究二丙酸倍氯米松 (BDP)纳米缓释微囊对豚鼠哮喘的治疗作用 ,以研制哮喘长期吸入治疗的糖皮质激素新剂型。方法 :以聚乳酸 聚羟基乙酸共聚物 (PLGA )为基质材料 ,采用超声乳化法制备BDP纳米缓释微囊 ,经扫描电镜观察微囊形态 ,激光散射实验测定其粒径分布 ,并进行体内过敏实验及药效学研究。结果 :BDP PLGA纳米微囊为表面光滑的球形囊 ,粒径分布呈均值为126 4nm的正态分布 ;BDP PLGA纳米缓释微囊对豚鼠无过敏反应 ,能明显控制哮喘发作且呈剂量依赖性 ;纳米微囊治疗组血中白细胞总数和肺泡灌洗液中细胞总数及嗜酸性粒细胞明显低于模型组 (P<0 01) ,且嗜酸性粒细胞减少呈剂量依赖性 (P<0 05)。结论 :BDP PLGA纳米缓释微囊显著抑制气道内炎性细胞浸润并有良好的缓释性 。

To study the therapeutic action of a sustained releasing nanocapsule preparation of beclomethasone propionate(BDP)in asthmatic guinea pigs Methods:With polylactate polyethanol acid copolymer (PLGA) as matrix and ultrasound emulsification,the PLGA microencapsuled BDP of nanoparticals(NP) were prepared The morphology of NP was observed with scanning electron microscope and its diameter was measured by laser emission The allergy experiment in healthy guinea pigs and its pharmacodynamics in asthmatic guinea pigs model were performed Results:The features of PLGA BDP NP were described as smooth surface and 126 4 nm in average diameter with normal distribution It was demonstrated that there was no allergy in vivo It could effectively control asthma attack and seemed to be dose depended The total number of cells and esoinophil in asthmatic guinea pigs model blood as well as bronchoalveolar lavage fluid(BALF)were significantly higher thanthat of BDP therapy and BDP nanocapsule therapy groups(P<0 01) Moreover,esoinophil counts seemed to be dose depended(P<0 05) But there was no difference between BDP therapy group and BDP nanocapsule the_ rapy group Conclusion:PLGA BDP nanocapsule exerted its anti inflammatory action by significantly inhabiting the inflammatory cell recruitment It may be suitable for inhalation because of its effective slow controlled releasing