SBIR Phase I: Preparation and Characterization of Polymer based Biodegradable Nanoparticles of Novel Inhibitors of Cell Proliferation

这个小企业创新研究（SBIR）第一阶段项目将研究基于聚合物的可生物降解纳米颗粒的制备和表征，这些纳米颗粒是新型细胞增殖抑制剂。基于聚合物的可生物降解纳米颗粒的发展是为了通过增加药物在疾病部位的生物利用度、包含对癌组织的递送、增加药物溶解度和最小化全身副作用来改善总体生存和生活质量。我们最近发现了新的抗细胞增殖化合物，这些化合物具有特异性和独特的特性，使它们成为治疗实体瘤的理想方法。本研究的主要目的是制备和表征我们的化合物的纳米颗粒配方。本项目所研究的化合物在临床开发过程中获得成功的机会很大，因为药物是局部给药，产生毒性的变化很小，而且化合物的分子靶点被证明是安全的治疗靶点。这种新型制剂的开发将允许在肿瘤部位持续递送新的细胞增殖抑制剂。该项目的更广泛影响/商业潜力：多种类型的人类恶性肿瘤迫切需要开发能够局部进入肿瘤部位的新型治疗方法。如果这个项目中所研究的化合物的纳米颗粒配方的成功开发，将通过降低癌症治疗的成本和提高许多癌症化疗患者的生存和生活质量来降低医疗成本。在提议的研究下开发的纳米颗粒制剂可以取代几种联合化疗方案，这些方案除了非常昂贵之外还有许多副作用。

This Small Business Innovation Research (SBIR) Phase I project will study the preparation and characterization of polymer based biodegradable nanoparticles of novel inhibitors of cell proliferation. The development of polymer-based biodegradable nanoparticles is guided by the desire to improve overall survival and quality of life by increasing the bioavailability of drug to the site of disease, containing delivery to the cancerous tissues, increasing drug solubility, and minimizing systemic side effects. We have recently discovered novel anti-cell proliferative compounds with specific and unique properties that make them an ideal treatment for solid tumors. The main aim of this study is preparation and characterization of nanoparticle formulations of our compounds. The compounds studied in this project have a high chance of success during clinical development because of the drugs are administered locally, which has very little change of producing toxicity, but also the molecular targets of the compound are proven to be safe therapeutic targets. Development of such novel formulations will allow sustained delivery of novel inhibitors of cell proliferation in the tumor site. The broader impact/commercial potential of this project: Development of novel therapeutics that could be delivered locally into tumor site is critically needed for several types of human malignancies. Successful development of nanoparticle formulations of the compounds studies in this project will, if successful, reduce healthcare costs by reducing the cost of cancer therapy and by improving the survival and quality of life for many patients under cancer chemotherapy. The nanoparticle formulations developed under the proposed studies could replace several combination chemotherapy regimens that have numerous side effects in addition to being very expensive.