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目的:建立泡球蚴体外培养模型,初步观察ABZ自微乳(ABZ-S)体外抗泡球蚴作用。方法:以阿苯达唑片剂(ABZ-T)为阳性对照,泡球蚴体外培养6周后,分为5组:ABZ自微乳(ABZ-S)、ABZ-T组,各分为含ABZ高、中、低剂量(1,0.1,0.01)mg.L-1;空白培养液组、二甲基亚砜(DMSO)组和空白乳组溶剂均等于高剂量组不含药溶剂。用药48,120 h和14 d后,分别取样观察超微结构。实验期间对囊泡进行计数,并监测囊液中阿苯达唑亚砜(ABZSX)的浓度。结果:ABZ-S和ABZ-T均可抑制泡球蚴的生长。超微结构观察:与同等质量浓度(1,0.1 mg.L-1)片剂比,ABZ自微乳对泡球蚴的损害强于片剂;但在低质量浓度(0.01 mg.L-1),2种剂型在用药5 d后,囊泡数均不再改变,泡球蚴对药物浓度有依赖性。连续14 d测定囊液中药物浓度,10 d后囊液药物浓度趋于平衡,且同剂量下ABZ-S囊液中药物(ABZSX)浓度高于ABZ-T。结论:自微乳能够促进药物穿过囊壁细胞,提高囊液药物浓度,增强ABZ抗包虫病的疗效。
OBJECTIVE: To establish an in vitro culture model of metacercariae, and to observe the effect of ABZ-S on the anti-metacercariae in vitro. Methods: ABZ-T was used as a positive control. After cultured for 6 weeks in vitro, BALB / c mice were divided into 5 groups: ABZ-S and ABZ-T, Including ABZ high, medium and low dose (1, 0.1, 0.01) mg.L-1. The solvent of blank medium, dimethyl sulfoxide (DMSO) group and blank milk group were equal to the high dose group. After 48,120 h and 14 d of administration, the ultrastructures were observed by sampling. Vesicles were counted during the experiment and the concentration of albendazole sulfoxide (ABZSX) in the cyst fluid was monitored. Results: Both ABZ-S and ABZ-T inhibited the growth of metacercariae. Ultrastructural observation: compared with the same mass concentration (1, 0.1 mg.L-1) tablets, ABZ self-microemulsions harbored more damage to metacercariae than tablets; however, at low concentrations (0.01 mg.L-1 ). After two days of treatment, the number of vesicles did not change in the two dosage forms, and the hydatid cyst was dependent on the drug concentration. The concentration of drug in cyst fluid was measured continuously for 14 days. After 10 days, the drug concentration in cyst fluid became more balanced. The concentration of ABZ-S in ABZ-S cyst fluid was higher than that of ABZ-T at the same dose. Conclusion: Self-microemulsion can promote drug penetration through the cytoplasm, increase cystic fluid drug concentration and enhance the efficacy of anti-echinococcosis ABZ.