本論文以聚乳酸-甘醇酸共聚物(poly(lactide-co-glycolide) acid, PLGA）為包覆基材，利用電噴霧 (electrospray)技術製備出包覆癌症化療藥物順鉑(cisplatin)的載體粒子，同時利用共價鍵結法(縮合反應)或混摻合法兩種方式來修飾載體粒子表面使其帶有馬來醯亞胺-聚乙二醇-胺(maleimide-poly(ethylene glycol)-amine)，提供後續表面抗體嫁接的平台。經實驗證實，我們發現傳統生物嫁接法存在許多弊病，如maleimide在鹼性條件下容易水解產生順丁烯二酸(maleic acid)，進而無法嫁接抗體於其上，但我們成功的利用混摻合法並經由電噴霧技術製備出具有標靶能力之次微米級藥物載體粒子，其平均粒徑為525±99 nm，CD44抗體成功嫁接率約為12-15%。In vitro藥物釋放試驗顯示，cisplatin encapsulated PEG/PLGA粒子其中因摻合有mal-PEG-NH2一親水性物質，其累積釋放百分比在72小時即可達100％。我們最後以CD44受器過量表徵的卵巢癌細胞株(CP70及SKOV3)進行此一次微米藥物載體粒子的體外癌症細胞阻殺實驗，證實藥物濃度於最低濃度1.25 μM時仍能比現今癌症化療藥物cisplatin大部分以free form劑型的給藥方法提高約一成的療效，顯現更佳的細胞阻殺效果，其可能原因為此載體粒子受受體介導的內吞作用(receptor-mediated endocytosis)影響，能更有效的將藥物直接遞送至細胞內，進而阻斷癌症細胞的增殖。

In this research, we used electrospray system synthesized poly(lactide-co-glycolide) acid cicplatin encapsulated submicron drug carriers, and conjugated with traditional bioconjugation method or directly mixed with maleimide-poly(ethylene glycol)-amine, in order to modify the surface of these drug carriers, for the application of further antibody conjugation.
As a result, we found out that there are inefficiencies in the traditional bioconjugation method, which for example include dehydrogenation of maleimide to maleic acid, and ends up with unefficient antibody conjugating. In contrast, submicron particles prepared by electrospray containing blended maleimide showed efficient antibody conjugation, and active targeting property toward CD44 antigen, the average diameter of drug carriers prepared are 525±99 nm, and the conjugation rate is 12-15%. According to the In-vitro release profile, cisplatin encapsulated PEG/PLGA can reach 100% release in 72 hours because of hydrophilic mal-PEG-NH2 contained.
Finally, we used CD44 over expressed ovarian cancer cell line, CP70 and SKOV3 to do the In-vitro cancer inhibition test. The results came to 10 % more efficient that free form of cisplatin solution, the possible mechanism is receptor-mediated endocytosis, which promises better transfection efficiency.

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