Modulated release from implantable ocular silicone oil tamponade drug reservoirs.
Modulated release from implantable ocular silicone oil tamponade drug reservoirs.
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DOI：
10.1002/pola.28973
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发表时间：
2018-04-15
期刊：
影响因子：
--
通讯作者：
Kearns VR
中科院分区：
文献类型：
--
作者：
Cauldbeck H;Le Hellaye M;McDonald TO;Long M;Williams RL;Rannard SP;Kearns VR
复杂的视网膜脱离病例可以用硅油填充治疗。硅油填塞物有可能在眼内具有连续的药物释放行为，然而，硅油的亲脂性限制了合适的药物数量，并且药物从疏水储库中的释放是不受控制的。在此，开发了一种辐射测量技术，以准确测量药物在硅油中的溶解度并测量释放到培养基中。全反式维甲酸（atRA）是一种已知在眼内起抗增殖作用的亲脂性药物，在整个研究中使用。用atRA对聚二甲基硅氧烷进行链端改性，生成聚二甲基硅氧烷视黄酸酯（PDMS-atRA），其用作硅油的添加剂，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和硅油的共混物。硅油中存在PDMS‐atRA对atRA溶解度和体外释放寿命有积极影响。药物释放期与atRA起始浓度无关，并取决于共混物中的PDMS-atRA浓度。观察到硅油与PDMS-atRA混合物中atRA的临床相关释放期超过7周。版权所有© 2018作者. Journal of Polymer Science Part A：Polymer Chemistry出版社：Wiley Periodicals，Inc. J.波利姆科学，A部分：聚合物Chem. 2018，56，938-946
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 in vitro. 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. 2018, 56, 938–946
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DOI：
10.1097/00006982-199313040-00002
发表时间：
1993-01-01
影响因子：
3.3
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