Atropine and Roscovitine Release from Model Silicone Hydrogels
Atropine and Roscovitine Release from Model Silicone Hydrogels
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DOI：
10.1097/opx.0000000000000807
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发表时间：
2016-04-01
影响因子：
1.4
通讯作者：
Sheardown, Heather
中科院分区：
文献类型：
--
作者：
Lasowski, Frances;Sheardown, Heather
目的眼球前部给药顺应性低，导致大量药物丢失。在儿科患者中，近视和视网膜母细胞瘤等眼病可能可以通过药物治疗，但与高药物浓度相关的风险，加上需要定期剂量，限制了它们的有效性。本研究探讨了阿托品和罗可维汀分别用于治疗近视和视网膜母细胞瘤的模型硅凝胶材料的可行性。研究了不同材料的性能，包括吸水率、水接触角和透光率。结果表明，在不影响材料吸水率、透光性和表面亲水性等关键性能的情况下，高达2wt%的药物可以被掺入硅胶模型水凝胶材料中。对于DMA含量至少为70%的材料，平衡含水率在15%到32%之间，透过率超过%。两种药物均可延长释放超过14天，材料释放的药物总量为16%至76%以上。虽然有爆裂效应，但这被认为是由于表面结合的药物，因此如果需要的话，可以使用适当的包装溶液来克服这种情况。结论硅酮水凝胶材料具有在不影响晶状体性能的情况下输送药物超过2周的潜力。这可能会克服定期滴注的需要，并允许在磨损期间保持泪膜中的药物浓度。这是一种治疗儿童眼科疾病的潜在选择，包括近视和视网膜母细胞瘤。
PurposeDrug delivery to the anterior eye has a low compliance and results in significant drug losses. In pediatric patients, eye diseases such as myopia and retinoblastoma can potentially be treated pharmacologically, but the risk associated with high drug concentrations coupled with the need for regular dosing limits their effectiveness. The current study examined the feasibility of atropine and roscovitine delivery from model silicone hydrogel materials which could potentially be used to treat myopia and retinoblastoma, respectively.MethodsModel silicone hydrogel materials that comprised TRIS and DMA were prepared with the drug incorporated during synthesis. Various materials properties, with and without incorporated drug, were investigated including water uptake, water contact angle, and light transmission. Drug release was evaluated under sink conditions into phosphate buffered saline.ResultsThe results demonstrate that up to 2 wt% of the drugs can be incorporated into model silicone hydrogel materials without adversely affecting critical materials properties such as water uptake, light transmission, and surface hydrophilicity. Equilibrium water content ranged from 15 to 32% and transmission exceeded 89% for materials with at least 70% DMA. Extended release exceeding 14 days was possible with both drugs, with the total amount of drug released from the materials ranging from 16% to over 76%. Although a burst effect was noted, this was thought to be due to surface-bound drug, and therefore storage in an appropriate packaging solution could be used to overcome this if desired.ConclusionsSilicone hydrogel materials have the potential to deliver drugs for over 2 weeks without compromising lens properties. This could potentially overcome the need for regular drop instillation and allow for the maintenance of drug concentration in the tear film over the period of wear. This represents a potential option for treating a host of ophthalmic disorders in children including myopia and retinoblastoma.