Cauldbeck Helen, Le Hellaye Maude, McDonald Tom O, Long Mark, Williams Rachel L, Rannard Steve P, Kearns Victoria R
Department of Eye and Vision Science University of Liverpool Liverpool L7 8TX United Kingdom.
Department of Chemistry University of Liverpool, Crown Street Liverpool L69 7ZD United Kingdom.
J Polym Sci A Polym Chem. 2018 Apr 15;56(8):938-946. doi: 10.1002/pola.28973. Epub 2018 Feb 9.
Complicated cases of retinal detachment can be treated with silicone oil tamponades. There is the potential for silicone oil tamponades to have adjunctive drug releasing behaviour within the eye, however the lipophilic nature of silicone oil limits the number of drugs that are suitable, and drug release from the hydrophobic reservoir is uncontrolled. Here, a radiometric technique was developed to accurately measure drug solubility in silicone oil and measure release into culture media. All-trans retinoic acid (atRA), a lipophilic drug known to act as an anti-proliferative within the eye, was used throughout this work. Chain-end modification of polydimethylsiloxane with atRA produced a polydimethylsiloxane retinoate (PDMS-atRA), which was used as an additive to silicone oil to modify the solvent environment within the silicone oil and the distribution coefficient. Blends of PDMS-atRA and silicone oil containing different concentrations of free atRA were produced. The presence of PDMS-atRA in silicone oil had a positive effect on atRA solubility and the longevity of release . The drug release period was independent of atRA starting concentration and dependent on the PDMS-atRA concentration in the blend. A clinically relevant release period of atRA over 7 weeks from a silicone oil blend with PDMS-atRA was observed. © 2018 The Authors. Journal of Polymer Science Part A: Polymer Chemistry Published by Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. , , 938-946.
复杂性视网膜脱离病例可用硅油填充治疗。硅油填充在眼内具有辅助药物释放的潜力，然而，硅油的亲脂性限制了适用药物的数量，并且疏水性储库中的药物释放不受控制。在此，开发了一种放射测量技术，以准确测量药物在硅油中的溶解度并测量其向培养基中的释放量。全反式维甲酸（atRA）是一种已知在眼内具有抗增殖作用的亲脂性药物，在整个研究中均被使用。用atRA对聚二甲基硅氧烷进行链端改性，得到聚二甲基硅氧烷视黄酸酯（PDMS-atRA），将其用作硅油添加剂，以改变硅油内的溶剂环境和分配系数。制备了含有不同浓度游离atRA的PDMS-atRA与硅油的混合物。硅油中PDMS-atRA的存在对atRA的溶解度和释放寿命有积极影响。药物释放期与atRA起始浓度无关，而取决于混合物中PDMS-atRA的浓度。观察到从含有PDMS-atRA的硅油混合物中atRA在7周以上的临床相关释放期。© 2018作者。《聚合物科学杂志》A辑：聚合物化学由Wiley Periodicals, Inc.出版。J. Polym. Sci., Part A: Polym. Chem.,, 938 - 946。
