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

这一小型企业技术转让(STTR)第一阶段项目的更广泛的影响/商业潜力是开发以食品为基础的新型口服药物剂型，可能优于传统片剂，因为它们可以在不影响治疗效益的情况下以较低的剂量给予。目前，片剂制剂需要高剂量给药才能达到预期的治疗效果，从而促进口服给药系统的改进。拟议的剂型可能有能力减轻药物标签上的食品限制，特别是有助于具有显著胃肠道毒性的口服药物。患者可以从不考虑食物的灵活用药中受益，以简化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动开发一个通用平台，提出两种试验药物。这个小型企业技术转让(STTR)第一阶段项目寻求通过利用食品在促进药物吸收方面的作用来开发更多的生物可用剂型。由于超过40%的上市药物和开发流程中约90%的药物存在溶解性差和相关的低生物利用度问题，拟议的技术将成为药物与食物一起服用时表现出更强吸收的平台。该项目将有效地利用食品成分(例如，脂质、蛋白质)来开发更多生物可利用的口服药物剂型。活动包括使用计算建模工具来定量估计特定饮食食品成分在提高药物吸收效率方面的效果。最终，这一过程将先验地指导合理、高效的新型食品配方的设计，而不是通过反复试验的过程。这一奖项反映了NSF的法定使命，并通过使用基金会的智力优势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.