Xia Yujie, Pack Daniel W
Department of Chemical and Biomolecular Engineering, University of Illinois, 600 S. Mathews Avenue, Urbana, Illinois, 61801, USA.
Pharm Res. 2014 Nov;31(11):3201-10. doi: 10.1007/s11095-014-1412-5. Epub 2014 May 16.
Pulsatile delivery of proteins, in which release occurs over a short time after a period of little or no release, is desirable for many applications. This paper investigates the effect of biodegradable polymer shell thickness on pulsatile protein release from biodegradable polymer microcapsules.
Using precision particle fabrication (PPF) technology, monodisperse microcapsules were fabricated encapsulating bovine serum albumin (BSA) in a liquid core surrounded by a drug-free poly(lactide-co-glycolide) (PLG) shell of uniform, controlled thickness from 14 to 19 μm.
When using high molecular weight PLG (Mw 88 kDa), microparticles exhibited the desired core-shell structure with high BSA loading and encapsulation efficiency (55-65%). These particles exhibited very slow release of BSA for several weeks followed by rapid release of 80-90% of the encapsulated BSA within 7 days. Importantly, with increasing shell thickness the starting time of the pulsatile release could be controlled from 25 to 35 days.
Biodegradable polymer microcapsules with precisely controlled shell thickness provide pulsatile release with enhanced control of release profiles.
蛋白质的脉冲式释放,即在一段很少或没有释放的时间后在短时间内发生释放,在许多应用中是理想的。本文研究了可生物降解聚合物壳厚度对可生物降解聚合物微胶囊中蛋白质脉冲式释放的影响。
采用精密颗粒制造(PPF)技术,制备了单分散微胶囊,其液芯中包裹有牛血清白蛋白(BSA),周围是厚度均匀、可控的无药物聚(丙交酯-共-乙交酯)(PLG)壳,厚度为14至19μm。
当使用高分子量PLG(Mw 88 kDa)时,微粒呈现出所需的核壳结构,具有高BSA负载量和包封效率(55-65%)。这些颗粒在几周内显示出非常缓慢的BSA释放,随后在7天内迅速释放80-90%的包封BSA。重要的是,随着壳厚度的增加,脉冲式释放的起始时间可以从25天控制到35天。
壳厚度精确控制的可生物降解聚合物微胶囊提供了脉冲式释放,并增强了对释放曲线的控制。