摘要
目的制备柚皮素脂质体冻干粉,并观察其对急性肺损伤(ALI)大鼠模型的治疗效果。方法乙醇注入法制备柚皮素脂质体并进行质量评价,加入冻干保护剂甘露醇(5%,W/V),冻干并进行相关粉体学评价。大鼠气管喷注脂多糖(LPS)(5 mg/kg)制备急性肺损伤模型,将48只SD雌性大鼠随机分成6组(n=8),分别为空白对照组(A组)、模型组(B组)、柚皮素原料药+LPS组(C组)、脂质体冻干粉+LPS组(D组)、地塞米松+LPS组(E组)和空白脂质体冻干粉+LPS组(F组),光学显微镜观察给药后各组大鼠肺组织形态学改变,并测定肺组织湿/干重比。结果最佳处方制得的柚皮素脂质体包封率为(82.44±0.98)%,平均粒径为(133±11)nm,Zeta电位为(-35.9±5)m V。冻干粉的休止角为36°,堆密度为0.3 g/ml。光镜观察结果显示,与A组空白对照比较,B^F组肺组织均出现不同程度炎性细胞的浸润、毛细血管充血、出血和肺泡壁增厚,其中以B组和F组改变最为显著,C组次之,D组和E组最轻。LPS诱导后B^F组肺组织湿/干重比均有不同程度增加,但D组和E组湿/干重比的增加量明显低于B组(P=0.0012,P=0.0018)。结论乙醇注入法制备柚皮素脂质体工艺简单可行,其冻干粉对大鼠急性肺损伤疗效显著。
Objective To prepare the lyophilized powder of naringenin liposome and investigate its pharmacodynamics in rat models of acute lung injury（ ALI）. Methods Naringenin liposome was prepared by ethanol injection method and then its quality was evaluated. Also,the related characteristics was evaluated by adding mannitol（ 5%,W / V） as lyoprotectant to be freeze-dried. The rat ALI models were established by inhaling lipopolysaccharide（ LPS）（ 5 mg / kg）. Totally 48 female Sprague-Dawley rats were randomly divided into six groups： control group（ A）,LPS group（ B）,LPS ＋ naringenin group（ C）,LPS ＋ lyophilized liposome group（ D）,LPS ＋ dexamethasone group（ E）,and LPS ＋ blank liposome group（ F）,with 8 rats in each group. Lung wet / dry weight ratio was calculated,and the histopathological morphologies were observed under the light microscope. Results The encapsulation efficiency of the prepared liposome was（ 82. 44 ± 0. 98） %,the average particle size was（ 133 ± 11） nm,and the Zeta potential was（- 35. 9 ± 5） m V. The angle of repose of lyophilized powder was 36° and the bulk density was 0. 3 g / ml. Compared with the group A,the lung tissues from groups B to F showed different remarkable histopathological changes under a light microscope,including infiltration of inflammatory cells, capillary congestion, hemorrhage, and marked thickening of the alveolar wall,among which group B and F changed the most significant,followed by group C,whereas groups D and E were the lightest. The wet / dry weight ratios increased in groups B to F compared with group A in some degree,and the increase of the lung wet / dry weight ratio in group D and E was significantly lower than in group B（ P = 0. 0012,P = 0. 0018）. Conclusion The technology of preparing naringenin liposome by ethanol injection is simple and feasible,and lyophilized powder has an obvious therapeutic effect on ALI.
出处
《中国医学科学院学报》
CAS
CSCD
北大核心
2015年第2期208-214,共7页
Acta Academiae Medicinae Sinicae
