Chemical Engineering, University of Florida, Gainesville, FL 32611, United States.
J Control Release. 2012 Aug 20;162(1):152-8. doi: 10.1016/j.jconrel.2012.06.017. Epub 2012 Jun 18.
We combine laboratory-based timolol release studies and in vivo pharmacodynamics studies in beagle dogs to evaluate the efficacy of glaucoma therapy through extended wear contact lenses. Commercial contact lenses cannot provide extended delivery of ophthalmic drugs and so the studies here focused on increasing the release duration of timolol from ACUVUE TruEye contact lenses by incorporating vitamin E diffusion barriers. The efficacy of timolol delivered via extended wear contact lenses was then compared to eye drops in beagle dogs that suffer from spontaneous glaucoma. The lenses were either replaced every 24h or continuously worn for 4 days, and the pharmacodynamics effect of changes in the intraocular pressure (IOP) of timolol from the ACUVUE TruEye contact lenses can be significantly increased by incorporation of vitamin E. The in vivo studies showed that IOP reduction from baseline by pure contact lens on daily basis was comparable with that by eye drops but with only 20% of drug dose, which suggested higher drug bioavailability for contact lenses. In addition, by inclusion of vitamin E into the lenses, the IOP was reduced significantly during the 4-day treatment with continuous wear of lens.
我们将基于实验室的噻吗洛尔释放研究和体内药效学研究与在患有自发性青光眼的比格犬中进行的研究相结合,通过长戴接触镜评估青光眼治疗的效果。商业接触镜不能提供眼科药物的延长释放,因此本研究的重点是通过加入维生素 E 扩散屏障来增加 ACUVUE TruEye 接触镜中噻吗洛尔的释放持续时间。然后将通过长戴接触镜递送的噻吗洛尔的功效与患有自发性青光眼的比格犬的眼药水进行比较。镜片要么每 24 小时更换一次,要么连续佩戴 4 天,通过加入维生素 E,可以显著增加 ACUVUE TruEye 接触镜中噻吗洛尔的眼压 (IOP) 变化的药效学作用。体内研究表明,每天仅通过纯接触镜从基线降低 IOP 的效果与眼药水相当,但药物剂量仅为 20%,这表明接触镜具有更高的药物生物利用度。此外,通过在镜片中加入维生素 E,在连续佩戴镜片的 4 天治疗期间,IOP 显著降低。