近年來5-氟尿嘧啶﹙5-fluorouracil, 5-FU﹚被利用為癌症治療關鍵的化療藥物，但由於5-FU藥物常見的缺點，諸如極短的半衰期﹙10-15分鐘﹚、腎毒性等副作用，因此臨床上主要使用靜脈連續注射作為主要治療手段，這樣也增加了副作用的風險。本論文第一部分量測包覆5-FU的生物分布於白蛋白微氣泡對比劑﹙Microbubbles, MBs﹚結合超音波﹙Ultrasound, US﹚增加目標腫瘤區域之5-FU濃度，延長5-FU的半衰期，降低其餘代謝器官之5-FU濃度。實驗使用人類血清白蛋白﹙Human Serum Albumin, HSA﹚和0.32 mg / ml 5-FU溶液製備5-FU-MBs。結果證實，5-FU於MBs中最大藥物負載效率為18.04 ± 0.24%，電位為 - 0.57 ± 0.58 mV。於動物實驗中，治療時間31天，5-FU-MBs+US組別治療效果比5-FU組更加顯著，而在生物分布結果中， 5-FU-MBs+US組別於腫瘤中的藥物濃度也比5-FU組更高，代謝器官中的5-FU濃度則與其他組別相近，因此可以證明，包覆5-FU之MBs結合超音波可有效增加腫瘤中局部藥物傳遞效率及時間更為延長，對臨床投藥的劑量能有效的降低。
第二部分中，則開發穩定的包覆氧氣的新型MBs﹙OMB﹚解決許多病症需要使用高壓氧局部進行治療的瓶頸，本論文使用人體血清白蛋白﹙Human Serum Albumin, HSA﹚包覆氧氣製備OMBs；結果表明，MBs與OMBs平均粒徑分別為1.86 ± 0.82 μm和3.46 ± 0.48 μm，OMBs經超音波打破後的溶氧濃度為9.66 ± 0.494 mg/L，打破效率為92.38 ± 0.99%，證實此新型微氣泡在凍乾前後同時具有包覆氧氣的特殊性，也很好的保留了原先MBs的基本性質以及特性，可以穩定保存並用於各種缺氧性疾病治療。

Recently, 5-fluorouracil (5-FU) has been used as a chemotherapeutical drug in cancer treatment. However, 5-FU has several limitations such as extremely short half-life (10- 15 minutes) and renal toxicity etc. Hence, continuous intravenous injection is mainly used clinically, which may increase the risk of adverse effects. In this study, 5-FU is loaded in albumin microbubbles (MBs) to produce 5-FU-loaded microbubbles (5-FU-MBs). 5-FU-MBs combine with ultrasound which can increase the 5-FU concentration in the target tumor area, prolong the half-life of 5-FU, and reduce the 5-FU concentration in metabolic organs. 5-FU-MBs is produced by human serum albumin (HSA) and 0.32 mg/ml 5-FU solution. The drug encapsulation efficiency of 5-FU in MBs is 18.04 ± 0.24% and its zeta potential is -0.57 ± 0.58 mV. In the in vivo studies, after 31 days treatments, the results show that the therapeutic effect in 5-FU-MBs+US group is more significant than 5-FU group. The drug concentration within tumor in 5-FU-MBs+US group is significant higher than other groups. In biodistribution study, the concentration of 5-FU in metabolic organ in 5-FU-MBs+US group is close to other groups. Therefore, it can be proved that 5-FU-MBs combined with ultrasound can obviously increase the efficiency of local drug delivery in tumors. The dosage of drug can be reduced clinically.
The second part in this thesis is to investigate oxygen-loaded MBs (OMB) used to treat hypoxic tissues. In previous studies, a successful cancer therapy is significantly affected by hypoxia in tissue, then, the dosage of drugs is increased or hyperbaric oxygen treatment is used clinically in order to achieve the therapeutic effect. In our thesis, OMB is produced as an oxygen loaded the human serum albumin (HSA) shell microbubbles. The experimental results show that the average particle size of MBs and OMBs are 1.86 ± 0.82 μm and 3.46 ± 0.48 μm, respectively. After application of ultrasound energy, the dissolved oxygen concentration of OMBs is 9.66 ± 0.494 mg/L, and the destruction efficiency is 92.38 ± 0.99%.The thesis also demonstrated the lyophilized microbubble which is easy for long term serving, still stable, and the property of lyophilized microbubble after rehydration is similar to non-lyophilized microbubble.

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