AIR Option 1: Technology Translation Development of a Prototype Solubility Enhancing Formulation for Improved drug Delivery using novel Cellulose Derivatives.

这个PFI: AIR技术翻译项目的重点是翻译我们最近发现的基于新型纤维素omega-羧基烷酸酯的药物结晶抑制剂，通过配制具有增强加工和药物传递特性的无定形固体分散体来改善水溶性差药物的传递。翻译的新型聚合物材料具有以下独特的特征：定制的两亲性和与羧酸基团的高度取代，与市场上用于非晶态固体分散体配方的主要竞争聚合物羟丙基甲基纤维素乙酸琥珀酸盐相比，具有典型的疏水药物过饱和溶液的结晶抑制作用。该项目通过合成纤维素的新型衍生物来实现这一目标，该衍生物设计用于与水溶性差的药物相互作用，这些药物将用于原型无定形固体分散体配方，预计将导致药物浓度升高，并最终改善治疗药物对患者的输送。使用普通加工技术成功生产原型配方的示范将导致与特种化学品和制药公司的伙伴关系和许可协议。潜在的经济影响预计将是在未来十年提高药物开发过程的效率，这将有助于美国在药物开发领域的竞争力。长期的社会影响将是新的和改进的药物的可用性，否则这些药物可能永远不会向公众提供，因为它们的水溶性很差。

This PFI: AIR Technology Translation project focuses on translating our recent discovery of pharmaceutical crystallization inhibitors based on novel cellulose omega-carboxyalkanoates to improve the delivery of poorly water soluble drugs by formulating amorphous solid dispersions with enhanced processing and drug delivery characteristics. The translated novel polymeric materials have the following unique features: tailored amphiphilicity and high degree of substitution with carboxylic acid groups that provides exemplary crystallization inhibition of supersaturated solutions of hydrophobic drugs when compared to the leading competing polymer, hydroxypropyl methylcellulose acetate succinate, used in the formulation of amorphous solid dispersions in this market space. The project accomplishes this goal by synthesis of novel derivatives of cellulose designed to interact with poorly water soluble drugs which will be used in prototype amorphous solid dispersions formulations which are expected to lead to elevated concentrations of the drug and ultimately improved delivery of the therapeutic agent to the patient. Demonstration of the successful production of prototype formulations using common processing techniques will lead to partnerships and licensing agreements with specialty chemical and pharmaceutical companies. The potential economic impact is expected to be improved efficiency of the drug development process in the next decade, which will contribute to the U.S. competitiveness in the area of drug development. The societal impact, long term, will be the availability of new and improved medicines that might otherwise have never been made available to the public because of their poor aqueous solubility.