Inês M Reis, Philip J Dixon, Poorvajan Sekar, Anuj Chauhan
{"title":"维生素 E 负载型隐形眼镜对奥洛他定的持续输送。","authors":"Inês M Reis, Philip J Dixon, Poorvajan Sekar, Anuj Chauhan","doi":"10.1089/jop.2023.0111","DOIUrl":null,"url":null,"abstract":"<p><p><b><i>Purpose:</i></b> Topical antihistamines, such as olopatadine hydrochloride, an H1 receptor antagonist, are commonly prescribed for treating allergic conjunctivitis. Drug delivery via eye drops has many deficiencies including a short residence time due to tear drainage via the nasolacrimal duct, which results in a low bioavailability and potential for side effects. These deficiencies could be mitigated by a drug-eluting contact lens such as the recently approved ACUVUE<sup>®</sup> THERAVISION™ WITH KETOTIFEN which is a daily disposable etafilcon, a drug-eluting contact lens with ketotifen (19 μg per lens). Here, we investigate the feasibility of designing a drug-eluting lens with sustained release of olopatadine for treating allergies using an extended wear lens. <b><i>Methods:</i></b> Nanobarrier depots composed of vitamin-E (VE) are formed through direct entrapment by ethanol-driven swelling. The drug-loaded lenses are characterized for transparency and water content. <i>In vitro</i> release is measured under sink conditions and fitted to a diffusion control release model to determine diffusivity and partition coefficient. <b><i>Results:</i></b> <i>In vitro</i> studies indicate that ACUVUE OASYS<sup>®</sup> and ACUVUE TruEye™ lenses loaded with ∼0.3 g of VE/g of hydrogel effectively prolong olopatadine dynamics by 7-fold and 375-fold, respectively. Incorporation of VE into the lenses retains visible light transmission and other properties. <b><i>Conclusion:</i></b> The VE incorporation in commercial lenses significantly increases the release duration offering the possibility of antiallergy extended wear lenses.</p>","PeriodicalId":16689,"journal":{"name":"Journal of Ocular Pharmacology and Therapeutics","volume":"40 2","pages":"126-135"},"PeriodicalIF":1.9000,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11265619/pdf/","citationCount":"0","resultStr":"{\"title\":\"Sustained Delivery of Olopatadine from Vitamin-E Loaded Contact Lenses.\",\"authors\":\"Inês M Reis, Philip J Dixon, Poorvajan Sekar, Anuj Chauhan\",\"doi\":\"10.1089/jop.2023.0111\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p><b><i>Purpose:</i></b> Topical antihistamines, such as olopatadine hydrochloride, an H1 receptor antagonist, are commonly prescribed for treating allergic conjunctivitis. Drug delivery via eye drops has many deficiencies including a short residence time due to tear drainage via the nasolacrimal duct, which results in a low bioavailability and potential for side effects. These deficiencies could be mitigated by a drug-eluting contact lens such as the recently approved ACUVUE<sup>®</sup> THERAVISION™ WITH KETOTIFEN which is a daily disposable etafilcon, a drug-eluting contact lens with ketotifen (19 μg per lens). Here, we investigate the feasibility of designing a drug-eluting lens with sustained release of olopatadine for treating allergies using an extended wear lens. <b><i>Methods:</i></b> Nanobarrier depots composed of vitamin-E (VE) are formed through direct entrapment by ethanol-driven swelling. The drug-loaded lenses are characterized for transparency and water content. <i>In vitro</i> release is measured under sink conditions and fitted to a diffusion control release model to determine diffusivity and partition coefficient. <b><i>Results:</i></b> <i>In vitro</i> studies indicate that ACUVUE OASYS<sup>®</sup> and ACUVUE TruEye™ lenses loaded with ∼0.3 g of VE/g of hydrogel effectively prolong olopatadine dynamics by 7-fold and 375-fold, respectively. Incorporation of VE into the lenses retains visible light transmission and other properties. <b><i>Conclusion:</i></b> The VE incorporation in commercial lenses significantly increases the release duration offering the possibility of antiallergy extended wear lenses.</p>\",\"PeriodicalId\":16689,\"journal\":{\"name\":\"Journal of Ocular Pharmacology and Therapeutics\",\"volume\":\"40 2\",\"pages\":\"126-135\"},\"PeriodicalIF\":1.9000,\"publicationDate\":\"2024-03-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11265619/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Ocular Pharmacology and Therapeutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1089/jop.2023.0111\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"OPHTHALMOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Ocular Pharmacology and Therapeutics","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1089/jop.2023.0111","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"OPHTHALMOLOGY","Score":null,"Total":0}
引用次数: 0
摘要
目的:外用抗组胺药(如盐酸奥洛他定,一种 H1 受体拮抗剂)是治疗过敏性结膜炎的常用处方药。通过滴眼液给药有许多不足之处,包括由于泪液通过鼻泪管排出,药物停留时间较短,导致生物利用度较低,并可能产生副作用。药物洗脱型隐形眼镜(如最近获批的 ACUVUE® THERAVISION™ WITH KETOTIFEN)可以缓解这些不足,该隐形眼镜是一种日抛型 etafilcon,是一种含有酮替芬(每片 19 微克)的药物洗脱型隐形眼镜。在此,我们研究了设计一种可持续释放奥洛他定的药物洗脱镜片的可行性,这种镜片可用于治疗过敏症。研究方法通过乙醇驱动的溶胀作用直接夹带维生素-E(VE)形成纳米载体。对载药镜片的透明度和含水量进行表征。在水槽条件下测量体外释放,并与扩散控制释放模型进行拟合,以确定扩散率和分配系数。结果:体外研究表明,ACUVUE OASYS® 和 ACUVUE TruEye™ 镜片每克水凝胶中含有 0.3 克 VE,可有效延长奥洛他定的释放时间,分别延长 7 倍和 375 倍。在镜片中加入 VE 还能保持可见光透射率和其他特性。结论:在商用镜片中加入 VE 可显著延长释放时间,为抗过敏延时镜片提供了可能。
Sustained Delivery of Olopatadine from Vitamin-E Loaded Contact Lenses.
Purpose: Topical antihistamines, such as olopatadine hydrochloride, an H1 receptor antagonist, are commonly prescribed for treating allergic conjunctivitis. Drug delivery via eye drops has many deficiencies including a short residence time due to tear drainage via the nasolacrimal duct, which results in a low bioavailability and potential for side effects. These deficiencies could be mitigated by a drug-eluting contact lens such as the recently approved ACUVUE® THERAVISION™ WITH KETOTIFEN which is a daily disposable etafilcon, a drug-eluting contact lens with ketotifen (19 μg per lens). Here, we investigate the feasibility of designing a drug-eluting lens with sustained release of olopatadine for treating allergies using an extended wear lens. Methods: Nanobarrier depots composed of vitamin-E (VE) are formed through direct entrapment by ethanol-driven swelling. The drug-loaded lenses are characterized for transparency and water content. In vitro release is measured under sink conditions and fitted to a diffusion control release model to determine diffusivity and partition coefficient. Results:In vitro studies indicate that ACUVUE OASYS® and ACUVUE TruEye™ lenses loaded with ∼0.3 g of VE/g of hydrogel effectively prolong olopatadine dynamics by 7-fold and 375-fold, respectively. Incorporation of VE into the lenses retains visible light transmission and other properties. Conclusion: The VE incorporation in commercial lenses significantly increases the release duration offering the possibility of antiallergy extended wear lenses.
期刊介绍:
Journal of Ocular Pharmacology and Therapeutics is the only peer-reviewed journal that combines the fields of ophthalmology and pharmacology to enable optimal treatment and prevention of ocular diseases and disorders. The Journal delivers the latest discoveries in the pharmacokinetics and pharmacodynamics of therapeutics for the treatment of ophthalmic disorders.
Journal of Ocular Pharmacology and Therapeutics coverage includes:
Glaucoma
Cataracts
Retinal degeneration
Ocular infection, trauma, and toxicology
Ocular drug delivery and biotransformation
Ocular pharmacotherapy/clinical trials
Ocular inflammatory and immune disorders
Gene and cell-based therapies
Ocular metabolic disorders
Ocular ischemia and blood flow
Proliferative disorders of the eye
Eyes on Drug Discovery - written by Gary D. Novack, PhD, featuring the latest updates on drug and device pipeline developments as well as policy/regulatory changes by the FDA.