a School of Life Sciences , The Nelson Mandela African Institution of Science and Technology , Tengeru , Arusha , Tanzania.
b Tanzania Veterinary Laboratory Agency , Temeke , Dar es Salaam , Tanzania.
Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):1428-1436. doi: 10.1080/21691401.2019.1596923.
Nanoparticles (NPs) have gained importance in addressing drug delivery challenges across biological barriers. Here, we reformulated pentamidine, a drug used to treat Human African Trypanosomiasis (HAT) in polymer based nanoparticles and liposomes and compared their capability to enhance pentamidine penetration across blood brain barrier (BBB). Size, polydispersity index, zeta potential, morphology, pentamidine loading and drug release profiles were determined by various methods. Cytotoxicity was tested against the immortalized mouse brain endothelioma cells over 96 h. Moreover, cells monolayer integrity and transportation ability were examined for 24 h. Pentamidine-loaded polycaprolactone (PCL) nanoparticles had a mean size of 267.58, PDI of 0.25 and zeta potential of -28.1 mV and pentamidine-loaded liposomes had a mean size of 119.61 nm, PDI of 0.25 and zeta potential 11.78. Pentamidine loading was 0.16 µg/mg (w/w) and 0.17 µg/mg (w/w) in PCL NPs and liposomes respectively. PCL nanoparticles and liposomes released 12.13% and 22.21% of pentamidine respectively after 24 h. Liposomes transported 87% of the dose, PCL NPs 66% of the dose and free pentamidine penetration was 63% of the dose. These results suggest that liposomes are comparatively promising nanocarriers for transportation of pentamidine across BBB.
纳米颗粒（NPs）在解决跨生物屏障的药物输送挑战方面具有重要意义。在这里，我们将戊二脒（一种用于治疗非洲人类锥虫病（HAT）的药物）重新配方为聚合物纳米颗粒和脂质体，并比较它们增强戊二脒穿透血脑屏障（BBB）的能力。通过各种方法确定了粒径、多分散指数、Zeta 电位、形态、戊二脒载药量和药物释放曲线。用戊二脒测定了对永生化的小鼠脑内皮瘤细胞的细胞毒性超过 96 小时。此外，还检查了细胞单层完整性和运输能力 24 小时。载戊二脒的聚己内酯（PCL）纳米颗粒的平均粒径为 267.58nm，PDI 为 0.25，Zeta 电位为-28.1mV，载戊二脒的脂质体平均粒径为 119.61nm，PDI 为 0.25，Zeta 电位为 11.78。PCL 纳米颗粒和脂质体中戊二脒的载药量分别为 0.16µg/mg（w/w）和 0.17µg/mg（w/w）。载药 24 小时后，PCL 纳米颗粒和脂质体分别释放了 12.13%和 22.21%的戊二脒。脂质体转运 87%的剂量，PCL 纳米颗粒转运 66%的剂量，游离戊二脒渗透 63%的剂量。这些结果表明，脂质体是比较有前途的纳米载体，可用于将戊二脒跨 BBB 转运。
