STTR Phase I: Design and development of novel oral drug formulations by leveraging the food effect

这项小型企业技术转移（STTR）第一阶段项目的更广泛影响/商业潜力是开发新型的基于食品的口服剂型药物，可能优于传统片剂，因为它们可以在不影响治疗效果的情况下以较低剂量施用。目前，片剂制剂需要高剂量给药才能达到预期的治疗效果，这促使口服给药系统得到改进。拟议的剂型可能有能力减轻药物标签上的食品限制，特别是对具有显著胃肠道毒性的口服药物有帮助。患者可以从不考虑食物而灵活服用药物中获益，从而减轻复杂的药物治疗方案，并最终提高依从性。近期的商业重点将是推进两种拟议测试药物的通用平台的开发。这项小型企业技术转让（STTR）第一阶段项目旨在通过利用食物促进药物吸收的作用来开发更多生物可利用的剂型。由于超过40%的已上市药物和约90%的正在开发的药物存在溶解度差和相关的生物利用度低的问题，因此拟议的技术将作为药物与食物一起服用时增强吸收的平台。该项目将有效地利用食品成分（如脂类、蛋白质）开发出更多生物利用度更高的上市口服药物剂型。活动包括使用计算建模工具定量估计特定膳食食品成分对提高药物吸收效率的影响。最终，这一过程将为理性、有效地设计基于先验的新型食品配方提供信息，而不是通过反复试验的过程。该奖项反映了美国国家科学基金会的法定使命，并通过使用基金会的知识价值和更广泛的影响审查标准进行评估，被认为值得支持。

The broader impact/commercial potential of this Small Business Technology Transfer (STTR) Phase I project is the development of novel food-based oral dosage forms of pharmaceutics potentially superior to traditional tablets as they can be administered at lower doses without compromising therapeutic benefits. Currently tablet form preparations require administration at high doses to achieve desired therapeutic effects, motivating improved oral delivery systems. The proposed dosage forms may have the ability to mitigate food restrictions in drug labels and particularly helping oral drugs with significant gastrointestinal toxicities. Patients could benefit from the flexibility of taking medications irrespective of food to ease complex drug regimens and ultimately improve compliance. The near-term commercial focus will be to advance development toward a general platform with two proposed test drugs. This Small Business Technology Transfer (STTR) Phase I project seeks to develop more bioavailable dosage forms by exploiting the effect of food in enhancing drug absorption. As more than 40% of marketed drugs and about 90% of drugs in development pipelines suffer from poor solubility and associated low bioavailability, the proposed technology will serve as a platform for drugs showing enhanced absorption when taken with food. This project will effectively enable the use of food ingredients (e.g., lipids, proteins) to develop more bioavailable dosage forms of marketed oral drugs. Activities include use of computational modeling tools to quantitatively estimate the effect of specific dietary food ingredients in increasing the efficiency of drug absorption. Ultimately this process will inform rational, efficient design of novel food-based formulations a priori rather than by a trial-and-error process.This award reflects NSF's statutory mission and has been deemed worthy of support through evaluation using the Foundation's intellectual merit and broader impacts review criteria.