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目的:制备阿克拉霉素A的长循环微乳(aclacinomycin A long circulation micoremulsions,ALM)用于肿瘤的小剂量化疗。方法:以聚乙二醇-二硬脂酰基磷脂酰乙醇胺为表面活性剂,制备了ALM,并测定了其理化性质。通过比较ALM与阿克拉霉素A(ACA)的血药浓度和急性毒性,评价了ALM的长循环及其降低ACA毒性的作用。采用小剂量化疗方案给药,评价了ALM的抗肿瘤作用。结果:ALM的粒径为(118.4±8.2)nm,Zeta电位为(-32.6±7.2)mV,载药率为(98.2±1.6)%(n=3)。与ACA相比,ALM的血药浓度显著提高,急性毒性较低,抗肿瘤作用较强,且更适用于肿瘤的小剂量化疗(P<0.01)。结论:ALM有可能成为一种适用于肿瘤小剂量化疗的药物。
OBJECTIVE: To prepare aclacinomycin A long-circulating microemulsions (ALM) for low-dose chemotherapy of tumors. Methods: ALM was prepared by using polyethylene glycol-distearoylphosphatidylethanolamine as surfactant, and its physicochemical properties were determined. The long cycle of ALM and its role in reducing ACA toxicity were evaluated by comparing plasma concentrations and acute toxicity of ALM with aclacinomycin A (ACA). A small dose chemotherapy regimen was administered to evaluate the anti-tumor effect of ALM. RESULTS: The particle size of ALM was (118.4 ± 8.2) nm, the Zeta potential was (-32.6 ± 7.2) mV and the drug loading rate was (98.2 ± 1.6)% (n = 3). Compared with ACA, ALM significantly increased blood concentration, acute toxicity, anti-tumor effect is stronger, and more suitable for low-dose chemotherapy chemotherapy (P <0.01). Conclusion: ALM may become a suitable low-dose chemotherapy for cancer drugs.