Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Instituto de Ortopedia y Banco de Tejidos Musculoesqueléticos, Universidade de Santiago de Compostela, 15872 Santiago de Compostela, Spain.
Acta Biomater. 2016 Sep 1;41:302-11. doi: 10.1016/j.actbio.2016.05.032. Epub 2016 May 21.
Combination of the ability of contact lenses (CLs) to act as a physical barrier against airborne antigen and to serve as a sustained depot of antihistaminic drugs may improve the efficiency of treatments of some ocular allergic diseases. The aim of this work was to develop CLs that exhibit affinity to olopatadine by mimicking the composition of the natural H1-receptor for which olopatadine behaves as a selective antagonist. Functional monomers that match the chemical groups of the receptor and application of the molecular imprinting technology led to hydrogels able to load high amounts of olopatadine and to sustain the release once in contact with lachrymal fluid. Optimized hydrogels prepared with acrylic acid, 2-acrylamido-2-methyl-1-propanesulfonic acid and benzylmethacrylate as functional monomers provided in few hours olopatadine concentrations similar to those of commercially available eye drops but the levels could be sustained for a whole day, demonstrating their efficacy. Olopatadine-loaded CLs successfully passed the HET-CAM test of ocular irritancy and showed good compatibility with mast cells. They were able to inhibit the release of histamine and TNF-α from sensitized mast cells, proving their potential application in preventing and treating allergic conjunctivitis.
Contact lenses (CLs) with affinity for antiallergic drugs may constitute an advantageous alternative to eye drops in management of ocular allergies for both contact lens wearers and patients who eventually use neutral CLs as therapeutic platforms. The present work represents a step forward in the state of the art of drug-CL combo products by (i) mimicking the composition of the human receptor of the drug, (ii) exploring combinations of functional monomers that include a monomer (2-acrylamido-2-methyl-1-propanesulfonic acid; AMPSA) with a strong acid group (pKa<4) able to enhance the interaction of the network with olopatadine in the saline environment of the lachrymal fluid, and (iii) analysing in detail the antihistamic effects provided by olopatadine released from the CLs on sensitized mast cells.
隐形眼镜（CL）具有作为空气传播抗原的物理屏障的能力，并作为抗组胺药物的持续储存库，这可能会提高某些眼部过敏性疾病治疗的效率。本工作的目的是通过模拟天然 H1 受体的组成来开发对奥洛他定具有亲和力的 CL，奥洛他定对其表现为选择性拮抗剂。与受体的化学基团匹配的功能单体和应用分子印迹技术导致水凝胶能够负载大量的奥洛他定，并在与泪液接触后持续释放。用丙烯酸、2-丙烯酰胺基-2-甲基-1-丙磺酸和苯甲基甲基丙烯酸酯作为功能单体制备的优化水凝胶在数小时内提供了与市售滴眼剂相似的奥洛他定浓度，但水平可维持一整天，证明了其功效。载有奥洛他定的隐形眼镜成功通过了眼刺激性 HET-CAM 测试，并且与肥大细胞具有良好的相容性。它们能够抑制致敏肥大细胞释放组胺和 TNF-α，证明了它们在预防和治疗过敏性结膜炎中的潜在应用。
具有抗过敏药物亲和力的隐形眼镜（CL）可能构成了管理眼部过敏的优势替代滴眼剂，无论是对隐形眼镜佩戴者还是最终将中性 CL 用作治疗平台的患者。本工作通过（i）模拟药物的人类受体的组成，（ii）探索包括具有强酸性基团（pKa<4）的单体（2-丙烯酰胺基-2-甲基-1-丙磺酸；AMPSA）的功能单体的组合，以增强网络与泪液盐环境中的奥洛他定的相互作用，以及（iii）详细分析从 CL 释放的奥洛他定对致敏肥大细胞提供的抗组胺作用，在药物-CL 组合产品的现有技术方面迈出了一步。
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