CAJ | 학술논문

目的以聚己内酯-聚乙二醇-聚己内酯(PCL-PEG-PCL)为载体材料,制备载紫杉醇聚合物胶束,并评价其对EMT-6乳腺癌的抗肿瘤效果.方法采用薄膜-超声法制备载紫杉醇聚合物胶束并对其进行表征;采用差示扫描热分析法(DSC)分析紫杉醇在载药聚合物胶束中的分散状态;采用MTT法研究紫杉醇聚合物胶束对EMT-6乳腺癌细胞的细胞毒性;建立荷EMT-6乳腺癌小鼠模型,以市售紫杉醇注射液为对照,研究紫杉醇聚合物胶束的体内抗肿瘤活性.结果紫杉醇聚合物胶束为表面粗糙的球形,具有明显核壳结构,平均粒径为93nm;DSC研究结果表明,将紫杉醇制成缓释纳米粒后其结晶状态发生了变化,以无定型状态存在于聚合物胶束中;MTT研究表明,在相同紫杉醇含量下,紫杉醇聚合物胶束的细胞毒性低于市售紫杉醇／聚氧乙烯蓖麻油注射剂;体内抗肿瘤活性研究表明,紫杉醇聚合物胶束对小鼠EMT-6乳腺癌具有明显抑制作用,相同给药剂量下其抑瘤效果优于紫杉醇注射剂(肿瘤抑制率:85.79％ vs 63.37％,P＜0.05).结论制备的载紫杉醇聚合物胶束高效低毒,是一种有潜力的可用于肿瘤治疗的纳米载药体系.
목적 이취기내지-취을이순-취기내지(PCL-PEG-PCL)위재체재료,제비재자삼순취합물효속,병평개기대EMT-6유선암적항종류효과.방법 채용박막-초성법제비재자삼순취합물효속병대기진행표정;채용차시소묘열분석법(DSC)분석자삼순재재약취합물효속중적분산상태;채용MTT법연구자삼순취합물효속대EMT-6유선암세포적세포독성;건립하EMT-6유선암소서모형,이시수자삼순주사액위대조,연구자삼순취합물효속적체내항종류활성.결과 자삼순취합물효속위표면조조적구형,구유명현핵각결구,평균립경위93nm;DSC연구결과표명,장자삼순제성완석납미립후기결정상태발생료변화,이무정형상태존재우취합물효속중;MTT연구표명,재상동자삼순함량하,자삼순취합물효속적세포독성저우시수자삼순／취양을희비마유주사제;체내항종류활성연구표명,자삼순취합물효속대소서EMT-6유선암구유명현억제작용,상동급약제량하기억류효과우우자삼순주사제(종류억제솔:85.79％ vs 63.37％,P＜0.05).결론 제비적재자삼순취합물효속고효저독,시일충유잠력적가용우종류치료적납미재약체계.
Objective To develop paclitaxel-loaded polymeric micelles from poly (ε-caprolactone)-poly (ethylene glycol)-poly(ε-caprolactone) (PCL-PEG-PCL),and to evaluate in vitro cytotoxicity as well as in vivo antitumor activity against EMT-6 tumor breast cell.Methods Paclitaxel-loaded polymeric micelles were prepared by thin-film hydration and ultrasonic method.The physical status of paclitaxel inside the polymeric micelles was investigated by differential scanning calorimetry (DSC).In vitro cytotoxicity of paclitaxel-loaded polymeric micelles against EMT-6 cell line was assessed by MTT assay.In vivo anticancer activity was evaluated against EMT-6 tumorbearing mice,with commercially available Taxol injection as control.Results Paclitaxel-loaded polymeric micelles exhibited homogeneous spherical shapes with apparent core-shell morphology.The average diameter of paclitaxelloaded polymeric micelles was 93 nm.DSC study indicated that paclitaxel was in solid amorphous state after being encapsulated in the polymeric micelles.In vitro cytotoxicity demonstrated that the cytotoxic effect of paclitaxelloaded polymeric micelles was lower than that of Taxol injection at the same paclitaxel content.Paclitaxel-loaded polymeric micelles showed greater tumor growth-inhibition effect in vivo on EMT-6 breast tumor in comparison with that of Taxol injection,with tumor growth inhibition of 85.79％ and 63.37％,respectively (P＜0.05).Conculsions The prepared paclitaxel-loaded polymeric micelles showed high anti-tumoral efficacy and low toxicity,and might have the potential to be developed as an effective anticancer drug-delivery system for cancer chemotherapy.