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载环糊精水凝胶隐形眼镜作为药物包载和释放的平台。

Cyclodextrin-containing hydrogels for contact lenses as a platform for drug incorporation and release.

机构信息

Biomaterials and Drug Delivery Laboratories, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, China.

出版信息

Acta Biomater. 2010 Feb;6(2):486-93. doi: 10.1016/j.actbio.2009.07.021. Epub 2009 Jul 18.

Abstract

Poly(2-hydroxyethyl methacrylate) hydrogels containing beta-cyclodextrin (pHEMA/beta-CD) have been investigated as a platform for sustained release of ophthalmic drugs. First of all, pHEMA/beta-CD hydrogel membranes and contact lenses were prepared by photopolymerization of HEMA, mono-methacrylated beta-CD (mono-MA-beta-CD) and trimethylolpropane trimethacrylate using a cast molding process. The hydrogels were characterized by Fourier transform infrared spectroscopy, equilibrium swelling ratio (ESR) and tensile tester. The results showed that the incorporation of beta-CD in the hydrogels increased the ESR and tensile strength. Then, puerarin was used as a model to evaluate drug loading and in vitro and in vivo release behavior of the pHEMA/beta-CD hydrogels. It was revealed that puerarin loading and in vitro release rate were dependent on beta-CD content in the pHEMA/beta-CD hydrogels. In rabbit eyes the pHEMA/beta-CD hydrogel contact lenses exhibited longer mean residence times (MRT(F)) of puerarin in tear fluid than that of pHEMA contact lenses and 1% puerarin eye drops. The puerarin concentration in the aqueous humor of rabbit reached a maximum of 0.81microg ml(-1) after wearing the pHEMA/beta-CD contact lens, which had been presoaked in 0.802mg ml(-1) puerarin solution for 4.81h. Also, the pHEMA/beta-CD contact lenses had a higher drug bioavailability in aqueous humor than puerarin eye drops. The data demonstrate that pHEMA/beta-CD hydrogel contact lenses can effectively deliver puerarin through the cornea.

摘要

聚(2-羟乙基甲基丙烯酸酯)水凝胶中含有β-环糊精(pHEMA/β-CD),已被研究作为眼科药物缓释的平台。首先,通过 HEMA、单甲基丙烯酰化 β-环糊精(mono-MA-β-CD)和三羟甲基丙烷三甲基丙烯酸酯的光聚合作用,采用浇铸成型工艺制备了 pHEMA/β-CD 水凝胶膜和隐形眼镜。通过傅里叶变换红外光谱、平衡溶胀比(ESR)和拉伸试验机对水凝胶进行了表征。结果表明,β-CD 的掺入增加了水凝胶的 ESR 和拉伸强度。然后,以葛根素为模型,评价了 pHEMA/β-CD 水凝胶的载药量和体外及体内释放行为。结果表明,葛根素的载药量和体外释放速率取决于 pHEMA/β-CD 水凝胶中β-CD 的含量。在兔眼中,pHEMA/β-CD 水凝胶隐形眼镜在泪液中的葛根素平均驻留时间(MRT(F))长于 pHEMA 隐形眼镜和 1%葛根素滴眼液。佩戴 pHEMA/β-CD 隐形眼镜后,兔眼房水中的葛根素浓度达到 0.81μg ml(-1)的最大值,该隐形眼镜预先浸泡在 0.802mg ml(-1)的葛根素溶液中 4.81h。此外,pHEMA/β-CD 隐形眼镜在房水中的药物生物利用度高于葛根素滴眼液。数据表明,pHEMA/β-CD 水凝胶隐形眼镜可通过角膜有效传递葛根素。

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