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从软性水凝胶隐形眼镜中控制柚皮苷的释放:对隐形眼镜关键性能和体外释放的研究。

Controlled release of naringenin from soft hydrogel contact lens: An investigation into lens critical properties and in vitro release.

机构信息

Ocular Therapeutics Research Group (OTRG), Pharmaceutical & Molecular Biotechnology Research Centre (PMBRC), South East Technological Univeristy (SETU), Waterford City, County Waterford X91 K0EK, Ireland.

Research and Development Department, Bausch + Lomb Ireland Ltd., Waterford City, County Waterford X91 V383, Ireland.

出版信息

Int J Pharm. 2022 Jun 10;621:121793. doi: 10.1016/j.ijpharm.2022.121793. Epub 2022 May 6.

Abstract

The naringenin (NAR)-impregnated hydrogel lenses (nesofilcon A material) were manufactured in this study with the feasibility to achieve controlled daily drug release. The lenses were fabricated using a comparable commercial-standard process, utilizing injection molding and thermal curing approaches. NAR-loaded lenses were prepared by both direct entrapment and 'soak and release' methods. Their critical properties were tested to ISO standards and comparable to the commercial lenses. NAR was fully characterized by studying its physical and chemical stability throughout the manufacturing processes using thermal analysis, high performance liquid chromatography and X-ray diffraction analysis. The NAR-loaded lenses showed > 97% light transmission, >75% water content, 0.50-0.53 ± 0.06 MPa tensile strength, with a lens diameter of 14.1 ± 0.1 mm. Lens polymerization kinetics were studied using differential scanning calorimetry. NAR released from the lens, prepared by a direct entrapment approach, followed a diffusion-controlled mechanism, and provided a controlled drug release of 72-82% for 24 h. A faster release rate was observed for NAR-loaded lenses prepared by a soak and release method, with over 90% of NAR was releasedin the first five hours.

摘要

本研究制造了载有柚皮素(NAR)的水凝胶隐形眼镜(nesofilcon A 材料),以实现控制每日药物释放的可行性。隐形眼镜是使用类似的商业标准工艺,通过注塑和热固化方法制造的。通过直接包埋和“浸泡和释放”方法制备载有 NAR 的隐形眼镜。它们的关键性能经过测试,符合 ISO 标准,与商业隐形眼镜相当。通过热分析、高效液相色谱和 X 射线衍射分析研究 NAR 在整个制造过程中的物理和化学稳定性,对 NAR 进行了全面的表征。载有 NAR 的隐形眼镜的透光率>97%,含水量>75%,拉伸强度为 0.50-0.53±0.06 MPa,镜片直径为 14.1±0.1 mm。通过差示扫描量热法研究了隐形眼镜的聚合动力学。通过直接包埋方法制备的载有 NAR 的隐形眼镜,其 NAR 释放遵循扩散控制机制,在 24 小时内提供了 72-82%的控释。通过浸泡和释放方法制备的载有 NAR 的隐形眼镜的释放速度更快,在前 5 小时内释放了超过 90%的 NAR。

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