本研究主要以 Poly(aminoadmine) dendrimers作為載體，並且以兩種功能性小分子L-Histidine和L-Cysteine作表面修飾，形成四種不同載體(G4.5、G-Cys、G-His、G-Cys-His)。抗癌藥物Doxorubicin以物理性方式包覆於載體中，藥物含量(LC%)為7.03%、7.22%、8.69%、8.99%；包覆效率(EE%)38%、39%、47.5%、49.9%，結果顯示修飾後G4.5提升藥物包覆能力。經由體外釋放模擬證實在37℃下四種載體皆具有酸鹼應答能力且成功將藥物釋，酸性環境中(pH5.0)藥物釋放量皆高於pH7.4，而且GHC/DOX和GH/DOX藥物釋放量高於GC/DOX、G/DOX，相對地毒性也較高；酸性環境中加入放射線(γ ray)後Dendrimer Dendrimer Dendrimer Dendrimer載體明顯 有所變化，而放射線下含有His的載體成功捕捉自由基，保護Dendrimer Dendrimer Dendrimer不受到影響和安全 不受到影響和安全 將藥物包覆於內； 將藥物包覆於內； 不管是否有加入放射線，pH7.4環境中穩定包覆藥物。由螢光顯微鏡和流式細胞儀觀察Hela cell吞噬能力，顯微鏡下藍色螢光來自於G4.5位置於細胞質，紅光(DOX)大多分於細胞核中；發現細胞暴露於γ ray，可觀察到部分細胞裡的胞器和細胞質皆破損，讓藥物和載體更容易進入細胞中，增加細胞死亡率。上述證實放射線能夠成功增加Dendrimer Dendrimer DendrimerDendrimer在酸性環境中 藥物釋放量，且證實Hela將樹狀高分子包覆DOX吞噬於內和將藥物釋放制細胞中，有效抑制細胞生長

Poly(aminoadmine) dendrimers was modified with two amine moieties, L-histidine and L-cysteine(G4.5, G-Cys, G-His,G-His-Cys), which is as carrier for drug delivery. There are four kind of carriers physically load Doxorubicin anticancer drug with the loading capacity of 7.03%、7.22%、8.69%、8.99% and encapsulation efficiency of 38%、39%、47.5%、49.9% respectively. In vitro, G4.5/DOX, GC/DOX, GH/DOX,
GHC/DOX are all pH response and successful drug release under 37℃ at pH5.0. Acid environment (pH 5.0) of drug released were higher than pH7.4. And then, GH/DOX and GHC/DOX drug release are higher than GC/DOX, G/DOX, relatively high toxicity. More specifically, Dendrimer vary significantly at acidic environment after γ radiation (5Gy). DOX was released relatively faster from G4.5 and GC after radiaiton. GH/DOX and GHC/DOX successfully capture free radicals, protecting Dendrimer to effect from free radical. Drug loaded inside carriers is stable at pH7.4 regardless of whether there was added radiation. Using microscopy and flow cytometry to observe Hela cell Intracellular uptake of DOX. Blue fluorescence from G4.5 located in the cytoplasm and red (DOX) most points in the nucleus. Under radiation some cells can be observed in the cytoplasm and organelles are damaged so the drug and the carrier more easily into cells, increasing cell death. It proved to Radiation has possibility to trigger more drug released from PAMAM dendrimer carrier in acidic condition. Doxorubicin loaded PAMAM dendrimer carrier can be successfully internalized into HeLa cells and the released Doxorubicin are located in nucleus

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