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Development of a novel nanotechnology-based ophthalmic drug delivery device.

机译：基于纳米技术的新型眼科药物输送装置的开发。

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摘要

Topical delivery by eye drops, which accounts for approximately 90% of all ophthalmic formulations, is extremely inefficient. Only approximately 5% of the drug applied as drops penetrates the outer layer of the eye and reaches the target, while the rest is lost due to tear drainage. A number of conditions like glaucoma, conjunctivitis, and proliferative retinopathy need a sustained release of drug inside the eye for drug to be therapeutically effective. In addition to eye drops, other ocular drug delivery systems include drug-loaded liposomes or nanoparticles and drug-loaded contact lenses (hydrogels). Particle drug delivery systems also have difficulty penetrating the outer layer of the eye and can be lost before the drug can be released. Contact lens delivery systems often show a burst release with poor release over long periods of time.;To improve sustain delivery of drugs to the eye, we have designed a novel system that includes drug-loaded nanoparticles suspended within a thin, membrane that can be attached to a standard commercial-grade contact lens for support. The lens system will provide constant contact with the eye's surface and the particles will supply a continuous release of medication, resulting in more drug reaching the target. First, PLGA nanoparticles, synthesized by the emulsion solvent evaporation technique, are loaded with the hydrophobic drug lidocaine. Next, the nanoparticles are loaded within a thin, collagen membrane that can be stored dried, and later rehydrated and attached to a contact lens for delivery to the eye.;Drug loading and drug release rates must be controlled within the novel delivery system in order to ensure that therapeutic levels of the drug are delivered safely to the eye. The PLGA nanoparticles were found to be irregular in shape, 247 nm in diameter, and contained 5.17 wt% of lidocaine. The nanoparticles loaded into the collagen membrane did not have a significant effect on light transmittance through the membrane, compared to a commercially available contact lens. For initial drug release in the first 48 hours, the complete lens system, nanoparticles only, and collagen membrane only released 21.8%, 53.0% and 7.6% of the initial drug loading, respectively. For the first 400 hours tested, the complete lens system, nanoparticles only, and collagen membrane only released 20.8%, 63.9 and 7.0% of the initial drug loading, respectively.
机译：滴眼剂的局部递送效率极低，而滴眼剂占所有眼科制剂的约90％。滴剂中仅约5％的药物穿过眼的外层并到达目标，而其余的则由于眼泪引流而丢失。青光眼，结膜炎和增生性视网膜病变等多种疾病需要眼内药物的持续释放才能使药物具有治疗效果。除滴眼剂外，其他眼用药物输送系统还包括载药脂质体或纳米颗粒以及载药隐形眼镜（水凝胶）。颗粒药物输送系统也难以穿透眼睛的外层，并且在释放药物之前可能会丢失。角膜接触镜给药系统通常会显示出突发性释放，长时间释放效果不佳。；为了改善药物向眼睛的持续递送，我们设计了一种新颖的系统，该系统包括将药物负载的纳米颗粒悬浮在薄膜中，附在标准的商用级隐形眼镜上以提供支持。镜片系统将提供与眼睛表面的持续接触，并且颗粒将提供药物的连续释放，从而导致更多的药物到达目标。首先，将通过乳液溶剂蒸发技术合成的PLGA纳米颗粒装载疏水性药物利多卡因。接下来，将纳米颗粒加载到胶原蛋白薄膜中，该胶原蛋白薄膜可以干燥保存，然后再水化并附着在隐形眼镜上以递送到眼睛。;必须在新型递送系统中控制药物的加载和药物释放速率以确保药物的治疗水平安全地传递到眼睛。发现PLGA纳米颗粒形状不规则，直径247nm，并且含有5.17wt％的利多卡因。与市售的隐形眼镜相比，加载到胶原膜中的纳米颗粒对穿过膜的透光率没有显着影响。对于最初的48小时内的初始药物释放，完整的镜片系统，仅纳米颗粒和胶原膜分别仅释放初始药物载量的21.8％，53.0％和7.6％。在测试的前400个小时中，完整的镜片系统，仅纳米颗粒和胶原膜分别仅释放初始药物载量的20.8％，63.9和7.0％。

著录项

  • 作者

    Sharma, Munish.;

  • 作者单位

    Oklahoma State University.;

  • 授予单位 Oklahoma State University.;
  • 学科 Chemistry Analytical.;Engineering Chemical.;Health Sciences Pharmacy.;Chemistry Pharmaceutical.
  • 学位 M.S.
  • 年度 2010
  • 页码 71 p.
  • 总页数 71
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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