順鉑(Cisplatin)為現今最具有潛力的抗癌藥物之一，最常應用於膀胱癌，睾丸癌，卵巢癌，在1978年時，成為鉑化合物中第一個被FDA認證的抗癌藥物。但治療後會產生的抗藥性及些許的副作用，且順鉑的微親水及微親油特性，使得順鉑不管在任何溶液中的溶解度都極低，也造成藥物包覆率偏低的現象。因此結合其他藥物的合併治療對於順鉑尤為重要，故將順鉑與厚朴酚(Magnolol)做結合。厚朴酚由厚朴樹皮萃取出之化合物，具有抗氧化、抗發炎、抗神經退化、保護肝臟及抗癌症等等不同的功效。但因具有懸浮性及分散性不佳之特性，故本研究將厚朴酚包覆於PEI-PLGA及PEI-PCADK奈米顆粒，順鉑包覆於海藻酸鈉微米顆粒，將兩顆粒利用電性使其相互結合後，探討高分子載體改質之結果對於藥物之包覆性、穩定釋放性，以及對於人類牙齦上皮癌細胞株(OECM-1)和子宮頸癌細胞(HELA)之抑制效果，並做載體間之比較。
研究結果顯示PEI成功接於PLGA及PCADK兩高分子之表面，並且維持顆粒之圓球狀奈米型態，Mag-PEI-PCADK-Alg-Cis能包覆較多之厚朴酚，Mag-PEI-PLGA-Alg-Cis具有包覆較多之順鉑之能力，兩者皆為使藥物穩定釋放之載體，Mag-PEI-PCADK-Alg-Cis對於抑制OECM-1及HELA效果不僅比Mag-PEI-PCADK佳，更優於另一載體Mag-PEI-PLGA-Alg-Cis，此結果顯示出對癌症的治療，Mag-PEI-PCADK-Alg-Cis比起市售之高分子所改良之載體更具有潛力的。

Cisplatin is one of the most potent anticancer agents used in the treatment of various solid tumors including bladder cancer, testicular cancer and ovarian cancer. It was the first FDA-approved platinum compound for cancer treatment in 1978. However, its use is mainly limited due to the drug resistance and considerable side effects. Also, precence drug is practically insoluble in organic solvent and slightly soluble in water makes the drug difficult to encapsulate into polymeric drug delivery system that can maintain optimum concentration for longer period of time. In order to improve the anti-cancer effects, combination therapy of cisplatin with other cancer drugs has been applied as novel therapeutic strategy for several human cancers. In this research, we combined it with magnolol. Magnolol, the major bioactive ingredient of Magnolia officinalis is known to have antioxidant, anti-inflammatory, anti-neurodegenerative, liver protecting and anti-cancer effects. However, the poor solubility and suspension capacity under physiological conditions have hindered its bioavailability and clinical efficacy. Based on this concept, we prepared the magnolol-loaded nanoparticles by using PEI-PLGA and PEI-PCADK, and cisplatin-loaded micro particles by alginate as drug carrier respectively. After preparing ionic complex of both alginate and PEI-PLGA/PCADK particles, we investigated their encapsulation efficiency, drug release, and the antitumor effect of drug carrier by PLGA or PCADK on oral epidermoid carcinoma cells (OECM-1) and cervical cancer (HELA).
The result showed that the surface of PLGA and PCADK is successfully modified by PEI, and maintained the particle morphology and size. Mag-PEI-PCADK-Alg-Cis particle and Mag-PEI-PLGA-Alg-Cis particle can load more magnolol and cisplatin respectively. Both of them showed stable release of both magnolol and cisplatin. The inhibitory effect to OECM-1 and HELA of Mag-PEI-PCADK-Alg-Cis particle is not only better than Mag-PEI-PCADK also than Mag-PEI-PLGA-Alg-Cis particle. These findings reveal a potential therapeutic strategy of oral and cervical cancer.

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