中国生化药物杂志
中國生化藥物雜誌
중국생화약물잡지
CHINESE JOURNAL OF BIOCHEMICAL PHARMACEUTICS
2014年
4期
56-58,62
,共4页
可断裂PEG%脂质体%肿瘤靶向
可斷裂PEG%脂質體%腫瘤靶嚮
가단렬PEG%지질체%종류파향
cleavable PEG%liposomes%tumor targeting
目的：制备氧化-还原敏感的可断裂PEG（聚乙二醇，polyethylene glycol）与RGD（精氨酸-甘氨酸-天冬氨酸，Arg-Gly-Asp）共修饰脂质体（C/RGD-LP），并对其体外性质进行评价。方法采用薄膜分散法制备可断裂PEG与RGD共修饰脂质体，测定脂质体的粒径、电位以及血清稳定性。采用流式观察肝癌HepG2细胞在PEG断裂前后对脂质体摄取效率的变化。MTT法检测该脂质体对细胞的毒性。结果 C/RGD-LP的粒径为（104.8±5.5）nm，电位为（-4.45±1.75）mV，在血清中有良好的稳定性。加入还原剂半胱氨酸后，HepG2细胞对PEG断裂后的脂质体摄取效率为断裂前的2.8倍，差异有统计学意义（P＜0.01）；细胞摄取实验结果显示：加入还原剂半胱氨酸后，PEG断裂后细胞的荧光强度显著强于未加入Cys组和无RGD修饰普通脂质体组（P＜0.01）。MTT实验结果表明：C/RGD-LP无明显细胞毒性。结论可断裂PEG与RGD共修饰脂质体制备方法简单，具有良好的稳定性，PEG能够有效屏蔽RGD肽，是一种潜在的肿瘤靶向给药系统。
目的：製備氧化-還原敏感的可斷裂PEG（聚乙二醇，polyethylene glycol）與RGD（精氨痠-甘氨痠-天鼕氨痠，Arg-Gly-Asp）共脩飾脂質體（C/RGD-LP），併對其體外性質進行評價。方法採用薄膜分散法製備可斷裂PEG與RGD共脩飾脂質體，測定脂質體的粒徑、電位以及血清穩定性。採用流式觀察肝癌HepG2細胞在PEG斷裂前後對脂質體攝取效率的變化。MTT法檢測該脂質體對細胞的毒性。結果 C/RGD-LP的粒徑為（104.8±5.5）nm，電位為（-4.45±1.75）mV，在血清中有良好的穩定性。加入還原劑半胱氨痠後，HepG2細胞對PEG斷裂後的脂質體攝取效率為斷裂前的2.8倍，差異有統計學意義（P＜0.01）；細胞攝取實驗結果顯示：加入還原劑半胱氨痠後，PEG斷裂後細胞的熒光彊度顯著彊于未加入Cys組和無RGD脩飾普通脂質體組（P＜0.01）。MTT實驗結果錶明：C/RGD-LP無明顯細胞毒性。結論可斷裂PEG與RGD共脩飾脂質體製備方法簡單，具有良好的穩定性，PEG能夠有效屏蔽RGD肽，是一種潛在的腫瘤靶嚮給藥繫統。
목적：제비양화-환원민감적가단렬PEG（취을이순，polyethylene glycol）여RGD（정안산-감안산-천동안산，Arg-Gly-Asp）공수식지질체（C/RGD-LP），병대기체외성질진행평개。방법채용박막분산법제비가단렬PEG여RGD공수식지질체，측정지질체적립경、전위이급혈청은정성。채용류식관찰간암HepG2세포재PEG단렬전후대지질체섭취효솔적변화。MTT법검측해지질체대세포적독성。결과 C/RGD-LP적립경위（104.8±5.5）nm，전위위（-4.45±1.75）mV，재혈청중유량호적은정성。가입환원제반광안산후，HepG2세포대PEG단렬후적지질체섭취효솔위단렬전적2.8배，차이유통계학의의（P＜0.01）；세포섭취실험결과현시：가입환원제반광안산후，PEG단렬후세포적형광강도현저강우미가입Cys조화무RGD수식보통지질체조（P＜0.01）。MTT실험결과표명：C/RGD-LP무명현세포독성。결론가단렬PEG여RGD공수식지질체제비방법간단，구유량호적은정성，PEG능구유효병폐RGD태，시일충잠재적종류파향급약계통。
Objective To prepare the cleavable PEG and RGD co-modified liposome for tumor targeting.Methods Liposomes were prepared by film-ultrasonic method.The particle size,Zeta potential and stability in FBS were evaluated.Cellular uptake by HepG2 cell was explored.MTT assay was used to evaluate the cytotoxicity of blank liposomes. Results The particle diameter of C/RGD-LP was (104.8 ±5.5 )nm with the Zeta potential of (-4.45 ±1.75 )mV.The cellular uptake of C/RGD-LP increased 2.8 times after Cys was added.The C/RGD-LP showed little cytotoxicity to HepG2 cell.Conclusion Cleavable PEG and RGD co-modified liposomes were easy to prepare and has a special application value for targeting tumor.
