薑黃素高分子粒子之物理化學性質及生物活性研究

Physicochemical Characterization and Biological Activities Evaluation of Curcumin Polymeric Particles

杜楚欣(Cho-Ian Tou)

指導教授 ： 顏峰霖

高雄醫學大學/藥學院/香粧品學系碩士班/碩士(2012年)

摘要

薑黃素 (CUR) 具備良好的抗氧化及抗發炎活性，然而其水溶解度不佳為其應用於臨床的最大阻礙。因此，本研究為改善CUR之水溶解度而選用Eudragit® E100 (EE100) 及聚乙烯醇 (PVA) 為賦形劑並以溶劑置換法製備薑黃素高分子粒子系統 (CPP)，然後對CPP進行多項物理化學性質分析，結果顯示CPP255 (CUR：EE100：PVA比例為1：2.5：2.5) 為本研究最理想之組成配方。CPP255的平均粒徑為130.96 ± 28.32 nm並呈單分散分佈 (多分佈指數為0.20 ± 0.02)，其包埋率高於90%。因此證實EE100及PVA能有效包覆CUR且粒子大小到逹次微米尺寸。另外，從CPP255之紫外線 / 可見光光譜、傅立葉紅外線光譜得知CUR與賦形劑形成分子間的氫鍵。再藉由Ｘ射線粉末繞射及示差熱分析之結果確認CUR從結晶態轉變成無定型態。由於溶解度試驗的結果說明CPP255可以明顯提升CUR之水溶解度逹200倍以上，從而證實細化藥物的粒子尺寸、藥物與載體的分子間氫鍵的形成和結晶態與無定型態的轉變皆為CPP提升CUR水溶解度的主要機制。另外，針對CPP之生物活性進行研究，證實CPP可以保留CUR的生物活性並具備良好的抗氧化及抗光傷害能力。最後以體外皮膚穿透試驗得知CPP能穿透角質層並存於皮膚。綜合上述結果，CPP255值得進一步發展成為化粧保養品或醫藥的高分子粒子。

關鍵字

薑黃素 ； 水溶解度 ； 抗氧化 ； 抗光傷害 ； 體外皮膚穿透實驗

並列摘要

Curcumin (CUR) is a well known antioxidant and anti-inflammation compound which was limited to clinical applications by its poor aqueous solubility. The aim of the present study was developed a curcumin polymeric particles system using Eudragit® E100 (EE100) and polyvinyl alcohol (PVA) as carrier by solvent displacement technique in order to increase water solubility of CUR. The results demonstrated that the weight ratio of CUR: EE100: PVA at 1:2.5:2.5 (CPP255) had a fine particle size (130.96 ± 28.32 nm) with monodispersion (Polydispersity index = 0.20 ± 0.02), which was considered as the best formulation at current study. In addition, encapsulation efficiency of CPP255 was exceeded 90% which elucidated EE100 and PVA could encapsulate CUR effectively. Moreover, the result of XRD and DSC demonstrated that the crystalline CUR was transformed to amorphous state in CPP255. FTIR and UV-Vis spectra were shown an intermolecular hydrogen bond between CUR and EE100-PVA. These findings may be due to CPP255 improved the water solubility of CUR and having over 200 folds increases compared with raw CUR. Furthermore, the activities of CPP255 were evaluated by the DPPH scavenging assay, lipid peroxidation assay and UVB-induced HaCaT cell damage model. The results indicated CPP255 had better antioxidant and anti-photodamage activity than raw CUR in water. CPP255 can help CUR penetrated horny layer and retained in epidermis and dermis. Consequently, we suggest that CPP255 could be developed as cosmetic and /or medicine in further study.

並列關鍵字

curcumin ； solubility ； antioxidant ； anti-photodamage ； in vitro penetration studies

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