Development of novel spray dried dispersion formulations to improve oral and pulmonary delivery

虽然口服给药途径一直是药物输送的首选途径，但吸入途径对全身和局部作用的活性药物成分(API)都很有吸引力。然而，这两条路线都存在制定方面的挑战。例如，由于难以提供更大剂量，通过吸入途径的剂量通常被限制在几毫克以内，而对于口服途径，药物吸收和全身生物利用度的限制因素往往是原料药的水溶解性。这些限制可以通过设计能够改善水溶解度的载体来克服，并且可以装载更大量的原料药。为提供原料药的载体的准备工作将基于雷丁大学建立的新技术，并与商商科学公司合作。该方法的关键是使用共晶(API和载体分子的结晶固体)来改变原料药的物理化学性质。对于肺部给药，这将有可能改善气雾剂的性质，从而最大限度地增加原料药在肺部的沉积。对于口服给药，我们将寻求探索提高药物溶解度的潜力。这种方法的一个优点是消除了对原料药的任何化学修饰，这意味着这种技术有可能在相对较短的时间内投放市场。它有可能对许多紧迫的健康问题产生重大影响，如细菌耐药性、癌症和其他肺部疾病。共晶体将使用简单到复杂的工艺(例如喷雾干燥)来生产，随后将进行广泛的物理化学表征。成功的候选人将拥有一套与学术界和工业界高度相关的技能。

Whilst the oral route has always been the preferred option for drug delivery, the inhaled route is attractive both for systemically and locally acting active pharmaceutical ingredients (APIs). Formulation challenges present for both routes however. For example, doses via the inhaled route are often limited to few milligrams due to difficulties in delivering larger doses, whilst for the oral route, the limiting factor for drug absorption and systemic bioavailability is often the API's water solubility.These limitations can potentially be overcome by designing carriers that can improve water solubility, and which can be loaded with larger amounts of API. Preparation of carriers for API delivery will be based on novel technologies established at the University of Reading and by working in collaboration with Quotient Sciences. Key to the approach is the use of co-crystals (crystalline solids of API and carrier molecules) to modify the API's physicochemical properties. For pulmonary delivery this will have the potential to improve the aerosol properties that subsequently maximise API deposition in the lung. For oral delivery we will look to explore the potential to improve drug solubility. One advantage of this approach is the elimination of any chemical modification of the API meaning this technology can potentially be delivered to market in a relatively short period. It has the potential to have a significant impact on many urgent health issues, such as bacterial resistance, cancers and other lung conditions. Co-crystals will be produced using simple-to-complex processes (e.g. spray drying) and will be followed by extensive physicochemical characterisation. The successful candidate will emerge with a set of skills highly relevant to academia and industry.