Persaud Suzanne, Eid Sandra, Swiderski Natalia, Serris Ioannis, Cho Hyunah
School of Pharmacy and Health Sciences, Fairleigh Dickinson University, Florham Park, NJ 07932, USA.
Pharmaceutics. 2020 Mar 2;12(3):222. doi: 10.3390/pharmaceutics12030222.
Rectal artesunate suppositories are a useful option for pre-referral treatment of severe malaria, specifically in children under 6 years of age in remote malaria-endemic areas. The main challenges are to improve the solubility of drugs in the rectal fluids and prevent the product from turning rancid or melting in a tropical climate. In this short proof-of-concept study, three types of rectal suppositories of artesunate were prepared: (i) polyethylene glycol (PEG)-based suppositories carrying free artesunate (non-modified artesunate), (ii) PEG-based suppositories carrying artesunate-loaded micelles and (iii) 3D-printed suppositories carrying a PEG/artesunate mixture. Physical parameters of suppositories, release profiles of artesunate (the fastest to the slowest: ii≥i>iii) and thermostability (the most stable to the least stable: iii>ii>i) of suppositories at increased temperature were assessed to determine the advantages and disadvantages of each formulation.
直肠青蒿琥酯栓是严重疟疾转诊前治疗的一种有用选择,特别是在偏远疟疾流行地区的6岁以下儿童中。主要挑战是提高药物在直肠液中的溶解度,并防止产品在热带气候中变质或融化。在这项简短的概念验证研究中,制备了三种类型的青蒿琥酯直肠栓:(i)携带游离青蒿琥酯(未修饰青蒿琥酯)的聚乙二醇(PEG)基栓剂,(ii)携带载有青蒿琥酯的胶束的PEG基栓剂,以及(iii)携带PEG/青蒿琥酯混合物的3D打印栓剂。评估了栓剂的物理参数、青蒿琥酯的释放曲线(从最快到最慢:ii≥i>iii)以及在升高温度下栓剂的热稳定性(从最稳定到最不稳定:iii>ii>i),以确定每种制剂的优缺点。