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首页> 外文期刊>Journal of pharmaceutical sciences. >Development of a respirable, sustained release microcarrier for 5-fluorouracil I: In vitro assessment of liposomes, microspheres, and lipid coated nanoparticles.
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Development of a respirable, sustained release microcarrier for 5-fluorouracil I: In vitro assessment of liposomes, microspheres, and lipid coated nanoparticles.

机译:开发用于5-氟尿嘧啶I的可呼吸,持续释放的微载体:脂质体,微球和脂质包裹的纳米颗粒的体外评估。

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The release rate of 5-fluorouracil (5-FU) from liposomes, microspheres, and lipid-coated nanoparticles (LNPs) was determined by microdialysis to investigate their use as a respirable delivery system for adjuvant (postsurgery) therapy of lung cancer. 5-FU was incorporated into liposomes using thin film hydration and into microspheres and LNPs by spray drying. Primary particle size distributions were measured by dynamic light scattering. Liposomes released 5-FU in 4-10 h (k(1) = 0.44-2.31/h, first-order release model). Extruded vesicles with diameters less than one micron released 5-FU more quickly than nonextruded vesicles. With poly-(lactide) (PLA) and Poly-(lactide-co-glycolide) (PLGA) microspheres, slower release rates were observed (k(1) = 0.067-0.202/h). Increasing the lactide:glycolide ratio (50:50-100:0) resulted in a progressive decrease in the release rate of 5-FU. poly-(lactide-co-caprolactone) (PLCL) microspheres released 5-FU more rapidly compared to PLGA systems (k(1) = 0.254-0.259/h). LNPs formulated with polymeric core excipients had lower release rates compared to monomeric excipients (k(1) = 0.043-0.105/h vs. k(1) = 0.192-0.345/h). Changing the lipid chain length of the shell lipid components had a relatively minor effect (k(1) = 0.043-0.129/h). Overall, these systems yielded a wide range of delivery durations that may be suitable for use as an inhalation delivery system for adjuvant therapy of lung cancer.
机译:通过微透析测定5-氟尿嘧啶(5-FU)从脂质体,微球和脂质包裹的纳米颗粒(LNP)的释放速率,以研究其作为可呼吸性递送系统在肺癌辅助治疗(手术后)中的用途。使用薄膜水合将5-FU掺入脂质体中,并通过喷雾干燥将5-FU掺入微球和LNP中。通过动态光散射来测量初级粒度分布。脂质体在4-10小时内释放了5-FU(k(1)= 0.44-2.31 / h,一阶释放模型)。直径小于1微米的挤压囊泡比未挤压囊泡释放5-FU的速度更快。使用聚(丙交酯)(PLA)和聚(丙交酯-共-乙交酯)(PLGA)微球,观察到较慢的释放速率(k(1)= 0.067-0.202 / h)。丙交酯:乙交酯的比例增加(50:50-100:0)导致5-FU释放速率逐渐降低。与PLGA系统相比,聚(丙交酯-己内酯)(PLCL)微球释放5-FU的速度更快(k(1)= 0.254-0.259 / h)。与单体赋形剂相比,用聚合物核心赋形剂配制的LNP具有更低的释放速率(k(1)= 0.043-0.105 / h vs. k(1)= 0.192-0.345 / h)。改变壳脂质成分的脂质链长度具有相对较小的影响(k(1)= 0.043-0.129 / h)。总体而言,这些系统产生的输送持续时间范围很广,可能适合用作肺癌辅助治疗的吸入输送系统。

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