Biomaterials and Drug Delivery Laboratories, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, P.R. China.
J Biomater Sci Polym Ed. 2010;21(3):271-88. doi: 10.1163/156856209X415774.
The purpose of this study is to develop a soft contact lens vehicle for puerarin delivery to alleviate glaucoma. Poly(2-hydroxy-ethyl methacrylate-co-N-vinylpyrrolidone-co-methyl acrylate) (pHEMA-NVP-MA) contact lenses were prepared by UV irradiation of HEMA, NVP and MA, to which the cross-linker, a mixture of trimethylolpropane trimethacrylate (TMPTMA) and allyl methacrylate (AMA) (1:1, w/w) was added previously. The contact lenses were characterized by equilibrium swelling ratio (ESR) and tensile tester. The results showed that incorporation of poly-N-vinylpyrrolidone (PVP) component in the hydrogels caused increase of ESR and decrease of tensile strength. Co-polymerization of MA monomer in the hydrogel led to a slight drop of ESR and improved tensile strength of hydrogel. Four kinds of hydrated contact lenses with different PVP content were presoaked in PBS solution of puerarin and the in vitro drug release was measured. The contact lenses matrix incorporated with PVP had a remarkable loading capacity of puerarin. In rabbit eyes, the presoaked contact lenses extended the mean resident time of puerarin to 77.45 min from 12.88 min of 1% puerarin eye drops. Moreover, contact lens presoaked in puerarin solution at the concentration of 0.802 mg/ml showed about the same bioavailability (AUC(0-t)) in tear fluid as that of the puerarin eye drops. This kind of presoaked contact lens has potential application as vehicle of puerarin to alleviate glaucoma.
本研究旨在开发一种用于葛根素传递的软性隐形眼镜载体，以缓解青光眼。通过 UV 辐照 HEMA、NVP 和 MA 制备了聚（2-羟乙基甲基丙烯酸酯-co-N-乙烯基吡咯烷酮-co-甲基丙烯酸酯）（pHEMA-NVP-MA）隐形眼镜，先前向其中加入了交联剂，即三羟甲基丙烷三甲基丙烯酸酯（TMPTMA）和烯丙基甲基丙烯酸酯（AMA）（1:1，w/w）的混合物。隐形眼镜通过平衡溶胀比（ESR）和拉伸试验机进行表征。结果表明，水凝胶中聚 N-乙烯基吡咯烷酮（PVP）成分的掺入导致 ESR 增加，拉伸强度降低。MA 单体在水凝胶中的共聚导致 ESR 略有下降，水凝胶的拉伸强度提高。将四种不同 PVP 含量的水合隐形眼镜浸泡在葛根素 PBS 溶液中，并测量体外药物释放。掺入 PVP 的隐形眼镜基质对葛根素有显著的载药能力。在兔眼内，浸泡过的隐形眼镜将葛根素的平均驻留时间从 1%葛根素滴眼液的 12.88 分钟延长至 77.45 分钟。此外，浸泡在 0.802mg/ml 葛根素溶液中的隐形眼镜在泪液中的生物利用度（AUC（0-t））与葛根素滴眼液大致相同。这种浸泡过的隐形眼镜作为葛根素缓解青光眼的载体具有潜在的应用前景。
