矽邊活化劑對包覆咖啡因傳遞體製備之影響

Effects of Silicone Edge Activators on the Preparation of Caffeine Transfersome

徐照程(Jaw-Cherng Hsu) ； 吳盈萱(Ying-Hsuan Wu)

《長庚科技學刊》 35期 (2021/12) Pp. 23-29

https://doi.org/10.6192/CGUST.202112_(35).3

摘要

本研究以高壓均質法搭配三種不同HLB值之含矽邊活化劑開發新式傳遞體，P-12D所製成的傳遞體粒徑最小的，平均粒徑為166.0 nm。相同矽邊活化劑條件下，不同脂質比例對粒徑大小的影響不大。在包覆率部分，LP-18M傳遞體表現較不佳，推測是疏水性邊活化劑不利相對較親水性之咖啡因包覆。P-15D-3的變形速度最快，比Liposome（18.70 s），高出37.59%。結果發現邊活化劑添加的比例越少，相對變形能力也較差。經皮傳輸試驗中，P-15D-3表現最佳，穿透通量0.43 mg/cm^2．hr，比Tw80-1高出22.22%。最佳配方條件以PEG/PPG-15/15 Dimethicone作為邊活化劑，添加助溶劑1,3-BG，脂質比例為80：20，脂質濃度為2%。

關鍵字

傳遞體 ； 矽邊活化劑 ； 咖啡因 ； 粒徑 ； 包覆率 ； 相對變形 ； 經皮吸收

並列摘要

In this study, a high-pressure homogenization method was used to develop a new type of Transfersome with three kind of silicon edge activators. The Transfersome made of P-12D has the smallest particle size, with an average particle size of 166.0 nm. Under the same silicon edge activator conditions, different lipid ratios have little effect on the particle size. In terms of the entrapment efficiency, the poor performance of the LP-18M Transfersome is presumed to be that the hydrophobic edge activator is not good for the relatively hydrophilic caffeine entrapment. P-15D-3 has the fastest relative deformability, 37.59% higher than Liposome (18.70 s). As a result, it was found that the smaller the proportion of edge activator added, the poorer the relative deformability. In the in vitro transdermal delivery test, P-15D-3 performed best, with a penetration flux of 0.43 mg/cm^2．hr, which was 22.22% higher than Tw80-1. The best formulation conditions is use PEG/PPG-15/15 Dimethicone as edge activator, add co-solvent 1, 3-BG, lipid ratio is 80:20, lipid concentration is 2%.

並列關鍵字

Transfersome ； Silicone Edge Activators ； Caffeine ； Particle size ； Entrapment efficiency ； Relative deformability ； In vitro transdermal delivery

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