SBIR Phase I: Engineering Platform for the Nanoformulations of Water Insoluble Drugs Using Supercritical Antisolvent Process with Enhanced Mass Transfer

这个小型企业创新研究（SBIR）第一阶段项目建议开发一个水不溶性药物纳米配方的灵活平台。随着医学实践向“彻底治愈疾病”的方向发展，将新药输送到特定区域，靶向特定组织，成为整个药学研究的重要目标。不幸的是，许多新药的水溶性较差，从而降低了它们的生物利用度。据报道，精心配制的纳米颗粒和纳米球具有治疗优势，如生物利用度，避免网状内皮系统（RES）去除的能力，以及直接靶向肿瘤。该项目将开发超临界抗溶剂增强传质（SAS-EM）工艺，用于生产水不溶性药物的纳米颗粒，并将其封装在可生物降解的聚合物中作为纳米球。第一阶段研究的三个关键步骤包括：(1)相行为研究，以确定合适的溶剂和实验条件；(2)颗粒形成研究，其中使用超临界抗溶剂工艺增强传质生产所述药物的纳米颗粒；(3)纳米颗粒/纳米球的粒径、粒径分布和结晶度表征。光散射技术将用于测量尺寸分布，并辅以扫描电镜可视化。x射线衍射测量将用于描述结晶度。该项目的商业应用是在药物输送领域。

This Small Business Innovation Research (SBIR) Phase I project proposes to develop a flexible platform for nano-formulations of water insoluble drugs. As the practice of medicine progresses towards "complete cure for diseases", delivering new drugs to specific areas to target specific tissues becomes an important objective of overall pharmaceutical research. Unfortunately many new drugs have poor water solubility that reduces their bioavailability. Carefully formulated nanoparticles and nanospheres are reported to have therapeutic advantages such as bioavailability, ability to avoid reticuloendothelial system (RES) removal, and direct tumor targeting. This project will develop the Supercritical Anti-Solvent with Enhanced Mass Transfer (SAS-EM) Process for producing nanoparticles of water insoluble drugs and encapsulatingthem in biodegradable polymers as nanospheres. The three key steps in the Phase I study include : (1) Phase behavior studies to identify the suitable solvent and experimental conditions, (2) Particle formation studies where nanoparticles of said drugs are produced using supercritical antisolvent process with enhanced mass transfer, and (3) Characterization of the nanoparticles/nanospheres for particle size, size distribution, and crystallinity. Light scattering techniques will be used to measure the size distribution complemented with Scanning electron microscopic visualization. X-ray diffraction measurements will be used to describe the crystallinity.The commercial applications of this project are in the area of pharmaceutical drug delivery.