近年來，高分子奈米粒子已被廣泛用作藥物傳遞之載體，然而，有效提升癌症的藥物治療之奈米顆粒，目前發展仍舊是個挑戰。因此，製備合適粒徑和表面電荷的藥物載體是提升治療效率之重要關鍵。本研究主要以聚乙烯亞胺（PEI），藻酸（ALG）和聚縮酮（PCADK）作為載體，透過透析法製備了聚合物奈米粒子。其中陽離子聚乙烯亞胺和陰離子藻酸透過聚電解質藉由相互靜電吸引而形成奈米粒子，同時疏水性聚縮酮則被複合體包圍並形成奈米顆粒。由動態光散射儀量測所製備之奈米顆粒的粒徑大小約為11 nm，進一步也從掃瞄電子顯微鏡（SEM）證實此奈米顆粒之形狀及大小。界面電位顯示此奈米粒子的外層被PEI覆蓋著，PEI的存在有助於奈米顆粒的螢光性質。此外，奈米顆粒的形成以核磁共振氫譜（1H-NMR）和傅里葉轉換紅外光譜（FTIR）分析鑒定且證實了聚乙烯亞胺，藻酸和聚縮酮之間的相互作用以形成奈米顆粒。且包覆5-FU的奈米藥物載體的粒徑大於未包覆藥的奈米粒子。此載體之藥物包覆率和藥物含量分別為28.46% 和4.43%。此藥物載體分别在三個不同的pH值下進行約104小時的體外藥物釋放評估，結果顯示載體在酸性環境（pH 5和pH 6.8）和中性環境（pH 7.4）的釋放曲線呈現緩慢之藥物釋放方式，且5-FU的釋放量在104小時後分別為82%，77% 和 52%。體外細胞毒性測定結果顯示包覆5-FU的顆粒相對可以更好地被癌細胞吞噬，因此對WiDr結腸直腸腺癌細胞系的抗癌活性比5-FU具有更好的細胞毒性作用。目前的研究表明此載體深具潛力，並且可以幫助提高5-FU對癌症之治療效果。

Recent year, nanoparticles have been widely employed as carriers for drug delivery applications. However, the development of nanoparticles that can enhance effective therapeutic efficacy against cancer is always a challenge. The formulation of nanoparticle with suitable size and surface charge as an efficient drug carrier need to be implemented. In this study, the polymeric nanoparticles consisting of branched polyethylenime (PEI), alginic acid (ALG) and poly(cyclohexane-1,4-diyl acetone dimethylene ketal) (PCADK) were prepared via dialysis method. The cationic PEI and anionic ALG were electrostatically attracted to each other through polyelectrolyte complexation. Meanwhile, the hydrophobic PCADK was surrounded by the complex forming nanoparticles with examined size around 11 nm by DLS which were further verified by SEM. The positive zeta potential indicated the outer layer of nanoparticle was covered by PEI and the presence of PEI contributed to the fluorescence property of nanoparticle. Besides that, 1H-NMR and FTIR analysis confirmed the interaction among the PEI, ALG and PCADK for the formation of nanoparticles. The 5-FU encapsulated nanoparticles were prepared with particle size examined slightly larger than the blank nanoparticle. Both the encapsulation efficiency and drug loading of the 5-FU loaded nanoparticles were 28.46% and 4.43% respectively. The drug release profiles at pH 5, 6.8 and 7.4 for 104 h were composed of burst release and sustained release that resulted in the 5-FU release of 82%, 77% and 52% respectively. Moreover, cytotoxicity assay was carried out to analyze the anticancer activities in vitro against WiDr colorectal adenocarcinoma cell lines and the results showed that 5-FU nanoparticles had more cytotoxicity effect than free 5-FU due to better adsorption onto the cancer cells. Current study showed that the nanoparticles are potential drug carriers to enhance the therapeutic efficacy of 5-FU against the cancer.

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