Gulsen Derya, Chauhan Anuj
Chemical Engineering Department, University of Florida, Room 237, CHE PO Box 116005, Gainesville, FL 32611-6005, USA.
Int J Pharm. 2005 Mar 23;292(1-2):95-117. doi: 10.1016/j.ijpharm.2004.11.033. Epub 2005 Jan 22.
Approximately 90% of all ophthalmic drug formulations are now applied as eye-drops. While eye-drops are convenient and well accepted by patients, about 95% of the drug contained in the drops is lost due to absorption through the conjunctiva or through the tear drainage. A major fraction of the drug eventually enters the blood stream and may cause side effects. The drug loss and the side effects can be minimized by using disposable soft contact lenses for ophthalmic drug delivery. The essential idea is to encapsulate the ophthalmic drug formulations in nanoparticles, and disperse these drug-laden particles in the lens material. Upon insertion into the eye, the lens will slowly release the drug into the pre lens (the film between the air and the lens) and the post-lens (the film between the cornea and the lens) tear films, and thus provide drug delivery for extended periods of time. This paper focuses on dispersing stabilized microemulsion drops in poly-2-hydroxyethyl methacrylate (p-HEMA) hydrogels. The results of this study show that the p-HEMA gels loaded with a microemulsion that is stabilized with a silica shell are transparent and that these gels release drugs for a period of over 8 days. Contact lenses made of microemulsion-laden gels are expected to deliver drugs at therapeutic levels for a few days. The delivery rates can be tailored by controlling the particle and the drug loading. It may be possible to use this system for both therapeutic drug delivery to eyes and the provision of lubricants to alleviate eye problems prevalent in extended lens wear.
目前,约90%的眼科药物制剂是以眼药水的形式应用。虽然眼药水使用方便且患者易于接受,但其中约95%的药物会因通过结膜或泪液引流吸收而损失。大部分药物最终进入血液循环,可能会引起副作用。通过使用一次性软性隐形眼镜进行眼科药物递送,可以将药物损失和副作用降至最低。其基本理念是将眼科药物制剂包裹在纳米颗粒中,并将这些载药颗粒分散在镜片材料中。将隐形眼镜插入眼睛后,镜片会将药物缓慢释放到晶状体前(空气与晶状体之间的薄膜)和晶状体后(角膜与晶状体之间的薄膜)泪膜中,从而实现长时间的药物递送。本文重点研究将稳定化微乳液滴分散在聚甲基丙烯酸2-羟乙酯(p-HEMA)水凝胶中。这项研究的结果表明,负载有经二氧化硅壳稳定化微乳液的p-HEMA凝胶是透明的,并且这些凝胶能够在超过8天的时间内释放药物。由载有微乳液的凝胶制成的隐形眼镜有望在几天内以治疗水平递送药物。通过控制颗粒和药物负载量可以调整递送速率。利用该系统既可以向眼睛进行治疗性药物递送,又可以提供润滑剂以缓解长时间佩戴隐形眼镜时常见的眼部问题。