Encapsulation for improved manufacturing and controlled-delivery of therapeutic compounds

在开发有效的治疗产品的过程中，药物的合成和纯化只是过程的一部分。考虑如何给药也很重要。脂质体或脂质囊泡是给药功能性化合物的一种有吸引力的递送系统。已知脂质体系统可以增加药物滞留时间并减少给药后的毒副作用。一个非常令人感兴趣的领域是脂质体在吸入给药系统中的使用，以靶向，持续和非侵入性的方式将药物输送到肺部。脂质体包裹化合物的微囊化在可生物降解的胶囊中，提供了一种可能的药物输送到肺部的方法，增加了药物的稳定性和保留率。这项研究有可能更有效地治疗结核病和糖尿病等疾病，而且不需要痛苦的注射。这些好处无疑将改善许多患有这类疾病的加拿大人的健康和生活质量。本研究的目的是开发一种结合乳化和喷雾干燥的新型工艺路线，以生产具有更好稳定性和控释性的吸入微囊化脂质体药物颗粒。这将通过首先建立脂质体形成和活性化合物包裹的配方和加工参数来实现。然后通过乳化和喷雾干燥脂质体溶液来生产可生物降解的颗粒。评估合适的制造技术的关键因素包括：加工后药物和脂质体的完整性，颗粒是否具有适合吸入的特性以及颗粒降解和药物释放的速度。

In the development of an effective therapeutic product, the synthesis and purification of the drug are only part of the process.  It is also important to consider how the drug will be delivered.  Liposomes or lipid vesicles are an attractive delivery system for administering functional compounds.  Liposomal systems are known to increase drug retention time and to reduce toxic side effects after administration.  One area of great interest is the use of liposomes in drug delivery systems administered by inhalation for a targeted, sustained and non-invasive means of delivering drugs to the lungs.  The microencapsulation of liposome-entrapped compounds in biodegradable capsules offers a possible means of drug delivery to the lungs with increased stability and drug retention. This research has the potential for treating diseases such as tuberculosis and diabetes more effectively and without painful injections.  Such benefits will undoubtedly improve the health and quality of life of the many Canadians who suffer from such diseases.       The goal of this research is to develop a novel processing route incorporating emulsification and spray-drying to produce microencapsulated liposomal drug particles with improved stability and controlled-release properties for inhalation.  This will be achieved by first establishing formulation and processing parameters for liposome formation and the entrapment of active compounds.  Biodegradable particles would then be produced by emulsification and spray-drying of liposomal solutions.  Key factors for assessing suitable manufacturing techniques include: the integrity of the drugs and liposomes after processing, whether the particles have characteristics suitable for inhalation and the rate of particle degradation and drug release.