| Summary: | 碩士 === 長庚大學 === 生化與生醫工程研究所 === 101 === Lutein is a hydrophobic drug with low oral bioavailability. How to develop topical delivery carriers for lutein is an important issue for the ocular delivery. Topical ocular delivery has the advantages of user-friendliness and the cost efficiency. The aim of this study is to develop the lipid nanoparticles combined with cyclodextrin (CD) for corneal lutein delivery. The lipid formulations is first screened in order to quickly obtain the maximum cumulative amount of lutein in cornea, and to overcome the barriers caused by corneal structure. Different types of CD could significantly enhance the accumulative amount of lutein in porcine cornea. Our studies indicated that different type cyclodextrin such as α-CD, β-CD, Hydroxypropyl-β-CD and Hydroxyethyl-β-CD could increase lutein accumulation in the porcine cornea. Finally, 2% HP-β-CD in combined with lipid nanoparticles could enhance accumulation up to 209.2±18 (μg/g) wich was 4.91-fold higher than that of the lutein-loaded lipid nanoparticles. The hybrid nanoaprticles had 68% of drug loading efficiency, and had lower cytotoxicoty in both corneal cells and retinal cells. These results showed that different enhancer could not only improve the stability of lutein but also enhance the accumulation in the ocular tissue including cornea. Our finding demonstrates that the lipid nanoparticles can be a potent carrier for ocular lutein delivery.
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