Department of Chemical Engineering, University of Florida, Gainesville, FL 32611, USA.
Curr Eye Res. 2012 Mar;37(3):204-11. doi: 10.3109/02713683.2011.630154.
The efficacy of ophthalmic drug delivery through contact lenses in animal model was explored to evaluate its potential for serving as an alternative to eye drops, which are inefficient vehicles for delivering ophthalmic drugs.
The efficacy of timolol delivered via contact lenses was compared to eye drops in beagle dogs that suffer from spontaneous glaucoma. Experiments were conducted with NIGHT & DAY™ silicone hydrogel contact lenses and NIGHT & DAY™ loaded with vitamin E, which was included in the lens to extend the release duration of the drug. Timolol was loaded into contact lenses by soaking in drug/phosphate buffered saline solution, and the drug-loaded lenses were subsequently inserted in one of the eyes, with the other eye serving as control. The lenses were replaced every 24 hours, and the pharmacodynamics of intraocular pressure (IOP) and pupil size were monitored in both eyes.
The IOP reduction from baseline by NIGHT & DAY™ (5.02 ± 0.83 mmHg) was comparable with that by eye drops with similar drug dosing (4.64 ± 0.41 mmHg). In addition, lenses with one-third of the drug loading as eye drops resulted in the similar IOP reduction, suggesting higher bioavailability for contact lenses compared to eye drops. Inclusion of vitamin E into the lenses did not improve the IOP reduction. The IOP in the untreated eye also decreased from baseline for eye drops (3.17 ± 0.42 mmHg) but it remained relatively unchanged with treatments based on lenses, suggesting reduction in systemic absorption for delivery of drugs by contact lenses.
Ophthalmic drug delivery through contact lenses increases bioavailability and reduces systemic drug uptake.
通过接触镜将眼科药物递送至动物模型中,以评估其作为眼药水替代物的潜力,因为眼药水在递送眼科药物方面效率低下。
通过将噻吗洛尔递送至患有自发性青光眼的比格犬的接触镜中来比较其与眼药水的疗效。实验采用 NIGHT & DAY™硅水凝胶接触镜和 NIGHT & DAY™负载维生素 E,将维生素 E 包含在镜片中以延长药物释放时间。噻吗洛尔通过浸泡在药物/磷酸盐缓冲盐溶液中被加载到接触镜中,然后将载药的镜片插入一只眼睛中,另一只眼睛作为对照。每 24 小时更换一次镜片,并监测两只眼睛的眼内压 (IOP) 和瞳孔大小的药效学变化。
NIGHT & DAY™(5.02±0.83mmHg)的 IOP 降低与具有类似药物剂量的眼药水(4.64±0.41mmHg)相当。此外,药物负载量为眼药水的三分之一的镜片也能导致类似的 IOP 降低,这表明与眼药水相比,接触镜具有更高的生物利用度。将维生素 E 纳入镜片中并不能改善 IOP 降低。未经治疗的眼睛在使用眼药水时也会从基线下降(3.17±0.42mmHg),但在基于镜片的治疗中保持相对不变,这表明接触镜递送药物的全身吸收减少。
通过接触镜进行眼科药物递送可提高生物利用度并减少全身药物摄取。