肿瘤预防与治疗
腫瘤預防與治療
종류예방여치료
JOURNAL OF CANCER CONTROL AND TREATMENT
2014年
5期
217-221
,共5页
整合素受体%R8%脂质体
整閤素受體%R8%脂質體
정합소수체%R8%지질체
Integrin Receptor%R8%Liposomes
目的：制备整合素受体RGD和细胞穿膜肽R8共修饰载紫杉醇( PTX)脂质体( RGD/R8-LP-PTX),对其理化性质进行表征,并观察脂质体与食管癌Ec9706细胞的亲和力和增殖抑制作用。方法：采用薄膜分散法制备RGD/R8-LP-PTX,观察脂质体的粒径,电位以及包封率；通过定量细胞摄取实验观察食管癌Ec9706细胞对RGD/R8-LP的摄取效率以及对脂质体摄取的影响因素。定性共聚焦实验观察肿瘤细胞对脂质体的摄取。 MTT实验观察RGD/R8-LP-PTX对食管癌Ec9706细胞的细胞毒性；构建食管癌Ec9706细胞肿瘤球模型,观察脂质体对肿瘤球的生长抑制能力。结果： RGD/R8-LP-PTX的粒径在124．8±9．4 nm,电位为21．35±3．55 mV。食管癌Ec9706细胞对RGD/R8-LP的摄取以及 RGD/R8-LP-PTX 对食管癌 Ec9706细胞的增殖抑制率具有时间依赖性；食管癌Ec9706细胞对RGD/R8-LP的摄取效率显著高于R8-LP、RGD-LP和LP,差异有统计学意义(P<0．01)；在给药48 h后,R8-LP-PTX、RGD-LP-PTX和LP-PTX的细胞存活率分别是RGD/R8-LP-PTX组的1．6倍、1．7倍和2．2倍,差异有统计学意义(P<0．01)。给药7天后,生理盐水组肿瘤球持续生长,体积增大1．48倍,LP-PTX组肿瘤球体积增大到原体积的1．12倍, RGD/R8-LP-PTX组、R8-LP-PTX组和 RGD-LP-PTX组肿瘤球体积减小到原体积的36%、59%和64%,差异具有统计学意义(P<0．01)。结论：整合素受体RGD和细胞穿膜肽R8共修饰载紫杉醇(PTX)脂质体能够有效穿透肿瘤细胞膜进入肿瘤细胞,是一种有效的食管癌化疗靶向给药系统。
目的：製備整閤素受體RGD和細胞穿膜肽R8共脩飾載紫杉醇( PTX)脂質體( RGD/R8-LP-PTX),對其理化性質進行錶徵,併觀察脂質體與食管癌Ec9706細胞的親和力和增殖抑製作用。方法：採用薄膜分散法製備RGD/R8-LP-PTX,觀察脂質體的粒徑,電位以及包封率；通過定量細胞攝取實驗觀察食管癌Ec9706細胞對RGD/R8-LP的攝取效率以及對脂質體攝取的影響因素。定性共聚焦實驗觀察腫瘤細胞對脂質體的攝取。 MTT實驗觀察RGD/R8-LP-PTX對食管癌Ec9706細胞的細胞毒性；構建食管癌Ec9706細胞腫瘤毬模型,觀察脂質體對腫瘤毬的生長抑製能力。結果： RGD/R8-LP-PTX的粒徑在124．8±9．4 nm,電位為21．35±3．55 mV。食管癌Ec9706細胞對RGD/R8-LP的攝取以及 RGD/R8-LP-PTX 對食管癌 Ec9706細胞的增殖抑製率具有時間依賴性；食管癌Ec9706細胞對RGD/R8-LP的攝取效率顯著高于R8-LP、RGD-LP和LP,差異有統計學意義(P<0．01)；在給藥48 h後,R8-LP-PTX、RGD-LP-PTX和LP-PTX的細胞存活率分彆是RGD/R8-LP-PTX組的1．6倍、1．7倍和2．2倍,差異有統計學意義(P<0．01)。給藥7天後,生理鹽水組腫瘤毬持續生長,體積增大1．48倍,LP-PTX組腫瘤毬體積增大到原體積的1．12倍, RGD/R8-LP-PTX組、R8-LP-PTX組和 RGD-LP-PTX組腫瘤毬體積減小到原體積的36%、59%和64%,差異具有統計學意義(P<0．01)。結論：整閤素受體RGD和細胞穿膜肽R8共脩飾載紫杉醇(PTX)脂質體能夠有效穿透腫瘤細胞膜進入腫瘤細胞,是一種有效的食管癌化療靶嚮給藥繫統。
목적：제비정합소수체RGD화세포천막태R8공수식재자삼순( PTX)지질체( RGD/R8-LP-PTX),대기이화성질진행표정,병관찰지질체여식관암Ec9706세포적친화력화증식억제작용。방법：채용박막분산법제비RGD/R8-LP-PTX,관찰지질체적립경,전위이급포봉솔；통과정량세포섭취실험관찰식관암Ec9706세포대RGD/R8-LP적섭취효솔이급대지질체섭취적영향인소。정성공취초실험관찰종류세포대지질체적섭취。 MTT실험관찰RGD/R8-LP-PTX대식관암Ec9706세포적세포독성；구건식관암Ec9706세포종류구모형,관찰지질체대종류구적생장억제능력。결과： RGD/R8-LP-PTX적립경재124．8±9．4 nm,전위위21．35±3．55 mV。식관암Ec9706세포대RGD/R8-LP적섭취이급 RGD/R8-LP-PTX 대식관암 Ec9706세포적증식억제솔구유시간의뢰성；식관암Ec9706세포대RGD/R8-LP적섭취효솔현저고우R8-LP、RGD-LP화LP,차이유통계학의의(P<0．01)；재급약48 h후,R8-LP-PTX、RGD-LP-PTX화LP-PTX적세포존활솔분별시RGD/R8-LP-PTX조적1．6배、1．7배화2．2배,차이유통계학의의(P<0．01)。급약7천후,생리염수조종류구지속생장,체적증대1．48배,LP-PTX조종류구체적증대도원체적적1．12배, RGD/R8-LP-PTX조、R8-LP-PTX조화 RGD-LP-PTX조종류구체적감소도원체적적36%、59%화64%,차이구유통계학의의(P<0．01)。결론：정합소수체RGD화세포천막태R8공수식재자삼순(PTX)지질체능구유효천투종류세포막진입종류세포,시일충유효적식관암화료파향급약계통。
Objective: To prepare RGD and R8 co-modified paclitaxel loaded liposome(RGD/R8-LP-PTX)for EC9706 cells’ treatment. Methods: The co-modified liposome was prepared by film-ultrasonic method. The appearance, particle size,Zeta potential were evaluated. The cellular uptake by EC9706 cells in vitro was used to evaluate the targeting efficiency. The anti-proliferation efficiency of RGD/R8-LP-PTX was evaluated by MTT assay. Tumor spheroids were used to evaluate anti-tumor ability of RGD/R8-LP-PTX in vitro. Results:The particle diameter of the co-modified liposome was 124. 8 ± 9. 4 nm with the Zeta potential of 21. 35 ± 3. 55mV. The uptake of the RGD/R8-LP by Ec9706 cells and the prolif-eration inhibition rate of RGD/R8-LP-PTX to Ec9706 cells were both found in a time-dependent manner. The result demon-strated that the co-modified liposome uptaken by EC9706 were 2. 1, 2. 6 times higher than that of R8-LP and RGD-LP, re-spectively. The MTT assay demonstrated the cell viability of R8-LP-PTX,RGD-LP-PTX and LP-PTX were 1. 6, 1. 7 and 2. 2 times higher than that of RGD/R8-LP-PTX respectively. Tumor spheroids continued to grow in size and volume in saline 148% of the primary volume while the tumor spheroid volumes changed into nearly 36%, 59% and 64% of the original volumes when treated with R8-LP-PTX,RGD-LP-PTX and LP-PTX respectively(P<0. 01). Conclusion: The RGD/R8-LP-PTX can penetrate the tumor cell membrane effectively ,it might serve as a promising delivery system of antitumor drugs against esophagus carcinoma.
