PFI-RP: Innovation of Materials Based on Sustainable Resources to Enhance Performance of Challenging Drugs and Drug Candidates.

PFI-RP：基于可持续资源的材料创新，以提高挑战性药物和候选药物的性能。

• 批准号: 1827493
• 负责人: Kevin Edgar
• 金额: $ 74.94万
• 依托单位: Virginia Polytechnic Institute and State University
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2018
• 资助国家: 美国
• 起止时间: 2018-09-15 至 2023-02-28
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=1827493&HistoricalAwards=false
• 关键词: PFI; RP; Innovation; Materials; Based

The broader impact/commercial potential of this PFI project is to enhance performance of the drugs that patients currently find on the pharmacist?s shelf, and to increase the number of effective new drugs that reach patients to treat critical medical issues. Currently up to 90% of drug candidates don?t fully dissolve in water, contributing to failure of otherwise effective candidates; all humans are roughly 70% water. We will design new materials, made from renewable resources and thus benign and environmentally sound, that solve key problems in drug delivery to patients. These currently unsolved problems include the inability to create patient-friendly formulations (pills) from drugs that require high doses (creating hard to swallow "horse pills"). Another important unsolved problem is failures of many drug candidates that tend to quickly form crystals from a water solution. When these drugs fail, cost of drug development goes up, which is ultimately passed along to patients. Drugs that would otherwise effectively treat diseases and are sorely needed by patients, never reach them. Our work will bring more drugs to patients, faster and more cheaply, and will reduce cost, side effects, dose, and variation in performance from patient to patient for drugs currently on the pharmacy shelf.The proposed project targets the design, preparation, and evaluation of two new families of materials prepared from natural cellulose, which is incredibly abundant, renewable, benign, and harvested in large quantities already from trees. These materials will be carefully designed so as to be easily made by current manufacturers of cellulose derivatives, and to work exceptionally well at enhancing the performance of drugs. They will be designed to help create solutions of current drugs, or drug candidates that are under development, that have far more dissolved drug per volume than is possible using current technologies. The ability to create these more concentrated solutions of drug or drug candidates in the human body will permit patients to get enough drug/drug candidate into their bloodstream to have the desired therapeutic effect, but at much lower drug dose. We will design, make, and characterize these materials, show that they work to create more concentrated solutions of key drugs, and figure out what features enhance their performance, so we can design even better materials. With our industrial partners, we will advance the best candidate materials towards commercialization so that they can benefit patients.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.

该PFI项目更广泛的影响/商业潜力是提高患者目前在药剂师那里找到的药物的性能？的货架上，并增加有效的新药的数量，达到病人治疗关键的医疗问题。目前高达90%的候选药物不？由于水不能完全溶解在水中，导致其他有效的候选物失效;所有人大约70%是水。我们将设计新材料，由可再生资源制成，因此是良性和环保的，解决了向患者输送药物的关键问题。这些目前尚未解决的问题包括无法从需要高剂量的药物中创造出对患者友好的制剂（药丸）（创造出难以吞咽的“马药丸”）。另一个重要的未解决的问题是许多候选药物的失败，这些候选药物倾向于从水溶液中快速形成晶体。当这些药物失败时，药物开发的成本就会上升，最终沿着转嫁给患者。本来可以有效治疗疾病的药物和病人迫切需要的药物，从来没有到达他们手中。我们的工作将为患者带来更多的药物，更快，更便宜，并将降低成本，副作用，剂量，并从患者的性能差异，目前在药店货架上的药物。拟议中的项目的目标是设计，制备和评估两个新的家庭材料制备的天然纤维素，这是令人难以置信的丰富，可再生，良性，并已大量收获的树木。这些材料将被精心设计，以便易于由目前的纤维素衍生物制造商制造，并在提高药物性能方面发挥出色的作用。它们将被设计用于帮助创建当前药物或正在开发中的候选药物的解决方案，这些药物的单位体积溶解的药物远远超过使用当前技术的可能性。在人体中产生这些更浓缩的药物或药物候选物溶液的能力将允许患者将足够的药物/药物候选物进入他们的血流中以具有期望的治疗效果，但是以低得多的药物剂量。我们将设计、制造和表征这些材料，展示它们能为关键药物创造更浓缩的溶液，并找出哪些特性能提高它们的性能，这样我们就能设计出更好的材料。我们将与我们的工业合作伙伴一起，推动最佳候选材料的商业化，使其造福于患者。该奖项反映了NSF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。

项目成果

Improved dissolution of an enteric polymer and its amorphous solid dispersions by polymer salt formation

• DOI: 10.1016/j.ijpharm.2022.121886
• 发表时间: 2022-06-12
• 期刊: INTERNATIONAL JOURNAL OF PHARMACEUTICS
• 影响因子: 5.8
• 作者: Qi, Qingqing;Taylor, Lynne S.
• 通讯作者: Taylor, Lynne S.

Designing synergistic crystallization inhibitors: Bile salt derivatives of cellulose with enhanced hydrophilicity

设计协同结晶抑制剂：亲水性增强的纤维素胆盐衍生物

• DOI: 10.1016/j.carbpol.2022.119680
• 发表时间: 2022
• 期刊: Carbohydrate Polymers
• 影响因子: 11.2
• 作者: Novo, Diana C.;Gao, Chengzhe;Qi, Qingqing;Mosquera-Giraldo, Laura I.;Spiering, Glenn A.;Moore, Robert B.;Taylor, Lynne S.;Edgar, Kevin J.
• 通讯作者: Edgar, Kevin J.