Rapid Delivery of Therapeutics Via Dissolution of Polymeric Films

通过聚合物薄膜的溶解快速递送治疗药物

• 批准号: 539432-2019
• 负责人: Adronov, Alex
• 金额: $ 8.74万
• 依托单位: McMaster University
• 依托单位国家: 加拿大
• 项目类别: Collaborative Research and Development Grants
• 财政年份: 2020
• 资助国家: 加拿大
• 起止时间: 2020-01-01 至 2021-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=699557
• 关键词: Rapid; Delivery; Therapeutics; Via; Dissolution

Oral delivery of pharmaceuticals is the most common form of drug administration, and is dominated by the use of tablets and capsules of various forms. However, there are a number of problems associated with tablets that diminish the utility of this form of dose administration. For instance, patients that have difficulty swallowing (children, the elderly, people with severe nausea, and patients suffering from dysphasia) are unable to tolerate solid tablets. In addition, tablets must pass through the gastrointestinal tract, with the therapeutic agents being absorbed through the gut. This takes significant amounts of time, delaying the onset of therapeutic action. Finally, drugs that are swallowed generally undergo metabolism, and can cause liver toxicity. As an alternative to tablets, thin polymer films that rapidly dissolve in the mouth have received significant attention. These films have been introduced in the market by Pfizer as Listerine PocketPaks, and have been a popular breath freshener since 2001. However, these films can also be loaded with pharmaceutical agents for oral drug delivery. This allows a therapeutic dose to be released in the mouth, and to be absorbed through the mucosal membranes directly into the bloodstream, bypassing the stomach and liver. This is advantageous as it results in rapid entry of drugs into circulation, bypasses gastrointestinal metabolism, decreases liver toxicity, and does not require swallowing. However, loading different drug compounds, especially those that are not water soluble, within a rapidly dissolving thin polymer film poses challenges, as different structures will impact film integrity and properties. This proposal aims to investigate new formulations for incorporation and encapsulation of a wide array of drugs within polymer films, and to help the industrial partner (Rapid Dose Therapeutics, Inc.) develop alternative delivery methods for the pharmaceutical industry.

口服给药是最常见的给药形式，主要是使用各种剂型的片剂和胶囊。 然而，存在与片剂相关的许多问题，这些问题削弱了这种剂量给药形式的效用。 例如，吞咽困难的患者（儿童、老人、严重恶心的患者以及患有吞咽困难的患者）无法耐受固体片剂。 此外，片剂必须通过胃肠道，治疗药物通过肠道吸收。 这需要大量的时间，从而延迟了治疗作用的开始。 最后，吞咽的药物通常会发生代谢，并可能引起肝毒性。 作为片剂的替代品，在口腔中快速溶解的聚合物薄膜受到了极大的关注。 这些薄膜由辉瑞公司以 Listerine PocketPaks 的名称推向市场，自 2001 年以来一直是流行的口气清新剂。然而，这些薄膜也可以装载用于口服药物输送的药剂。 这使得治疗剂量可以在口腔中释放，并通过粘膜直接吸收到血液中，绕过胃和肝脏。 这是有利的，因为它导致药物快速进入循环，绕过胃肠道代谢，降低肝毒性，并且不需要吞咽。 然而，在快速溶解的聚合物薄膜中负载不同的药物化合物，尤其是那些不溶于水的药物化合物，会带来挑战，因为不同的结构会影响薄膜的完整性和性能。 该提案旨在研究在聚合物薄膜中掺入和封装多种药物的新配方，并帮助工业合作伙伴（Rapid Dose Therapeutics, Inc.）为制药行业开发替代递送方法。