[1-12] Pharmaceutical particle engineering via spray drying: Understanding of and possibilities to control the formation of polymeric particles at molecular level

报告题目:Pharmaceutical particle engineering via spray drying: Understanding of and possibilities to control the formation of polymeric particles at molecular level 

报 告 人 :Dr. Feng Wan, Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen

报告时间:2018年1月12日(星期五)下午14:00

报告地点:独墅湖校区二期云轩楼2301室

 

Abstract 
Spray drying, well known as a one-step, continuous production process, has attracted lots of pharmaceutical scientists’ interests due to its advantages for solid-dose processing. However, understanding and controlling of particle formation in the spray drying process at a molecular level has not been reached, though the efforts were intensified in the last decade. In this study, we attempted to understand the formation and the nanoscale network of spray dried PLGA microparticles at a molecular level by using solid state NMR (ss-NMR) and neutron scattering. The 1H NMR transverse magnetization relaxation (T2 relaxation) method is used to analyze the molecular mobility and heterogeneity of the spray-dried PLGA microparticles. The T2 relaxation decay can be described by the short relaxation time (T2, r) component and the long relaxation time (T2, m) component.  The spray-dried PLGA microparticles from good solvents displayed the increased amount of T2, r component, indicating that more polymeric chain entanglements formed in the spray drying process using good solvents, which is further proved by the spin lattice relaxation time in the rotating frame of protons (1H T1ρ) measurement using 1H→13C cross-polarization magic-angle spinning (CP/MAS) NMR experiments. Furthermore, the domain size of the PLGA molecules network in the spray-dried PLGA microparticles from good solvent was higher than those of the spray-dried PLGA microparticles from poor solvent. Neutron scattering results indicated that the less crosslinked network of spray-dried PLGA microparticles from poor solvent resulted from the more rigid conformational structure due to the pronounced intramolecular interaction. Principal component analysis (PCA) of the spectral evolution of spray-dried PLGA microparticles upon incubation with water demonstrated that different original nanoscale networks responded differently. In conclusion, the organic solvents used in the spray drying play an important role in controlling the particle formation and the nanoscale network of the spraydried PLGA microparticles. 

报告人简介

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万锋,于 2011 年进入哥本哈根大学药学院攻读博士学位,开始从事应用喷雾干燥技术设计固体药物颗粒(微粒)传递系统的研究,并致力在长效注射和肺部吸入方面的应用。在设计和评价药物颗粒传递系统方面积累了丰富的经验并发表了多篇有影响力的论文。博士期间曾获得国家留学基金委授予的“优秀海外留学生”奖。博士毕业后申请并主持了丹麦科技署的独立研究基金(Danish Council for Independent Research,项目编号: DFF–4093-00062, 283 万丹麦克朗)和丹麦灵北基金(Lundbeck Foundation,丹麦最大的私立研究基金之一,项目编号:  R171-2014-1013,140万丹麦克朗) 。进一步从事可吸入的抗生素纳米制剂治疗呼吸道耐药菌感染的研究。这期间专注于研究和理解可吸入性纳米颗粒和生物系统的相互作用,从而达到合理地设计可吸入的抗生素纳米制剂,以及有效控制粒子在肺部沉积以后的行为。目前已经建立起一套科学有效的技术平台来评价可吸入性纳米颗粒和生物系统的相互作用,积累了宝贵的经验。在此基础上开展了相关的处方研究,并取得了具有前景的研究结果。