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首页> 外文期刊>Polymers for advanced technologies >Hyperbranched poly (ester) s for delivery of small molecule therapeutics
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Hyperbranched poly (ester) s for delivery of small molecule therapeutics

机译：用于递送小分子治疗剂的超支化聚（酯）S.

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>The development of molecular platforms for sustained release of actives is important for both veterinary and personal care applications. A time release platform composed of hyperbranched poly (ester) s (HBPEs) derived from glycerol, a trifunctional bio‐alcohol, and adipic acid, a difunctional bio‐acid, can be readily generated and conjugated with active agents for sustained delivery. The HBPE delivery platform is composed of very inexpensive building blocks that are on the FDA's Generally Regarded As Safe list. Two such active agents, 2‐undecanone and salicylic acid, have been covalently bonded to the HBPE and evaluated for sustained release. 2‐Undecanone is an effective, naturally occurring mosquito repellent, but due to its volatility, it must be reapplied every 15 to 30?minutes. The duration of the effectiveness of 2‐undecanone is enhanced by a sustained release formulation. Salicylic acid and derivatives are widely used for treatment of acne and inflammation, but it causes irritation if dosed at too high a level. A time‐release formulation of salicylic acid would reduce irritation as well as lengthen the duration of its effectiveness. Both actives were covalently bonded to the HBPE and shown to release over time by hydrolysis, either chemically or enzymatically. Moreover, their time release profiles were shown to be a function of composition, catalyst and catalyst level, and physical form.
机译： >持续释放活性物质的分子平台的开发对于兽医和个人护理应用是重要的。可以容易地产生由衍生自甘油，三官能生物醇和己二酸，双官能生物酸的超支化聚（酯）S（HBPES）组成的时间释放平台，并与活性剂缀合，以持续递送。 HBPE交付平台由FDA的非常便宜的构建块组成，通常被视为安全列表。两种这样的活性剂，2-未甲烷酮和水杨酸，已与HBPE共价键合并评估持续释放。 2 - 未鳕鱼是一种有效的，天然存在的蚊子驱蚊剂，但由于其波动性，必须每15到30分钟重新删除一次。通过持续释放制剂增强了2-未甲烷酮的有效性的持续时间。水杨酸和衍生物广泛用于治疗痤疮和炎症，但如果在过高的水平下给药导致刺激。水杨酸的时间释放制剂会降低刺激，并且延长其有效性的持续时间。两种活性物质与HBPE共价键合并显示通过化学或酶促通过水解释放。此外，它们的时间释放型材被证明是组合物，催化剂和催化剂水平和物理形式的函数。

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