Department of Applied Physics, University of Eastern Finland, Kuopio, Finland.
School of Pharmacy, The Neotia University, Sarisa, West Bengal, India.
PLoS Negl Trop Dis. 2021 Jun 29;15(6):e0009533. doi: 10.1371/journal.pntd.0009533. eCollection 2021 Jun.
Visceral leishmaniasis is a vector-borne protozoan infection that is fatal if untreated. There is no vaccination against the disease, and the current chemotherapeutic agents are ineffective due to increased resistance and severe side effects. Buparvaquone is a potential drug against the leishmaniases, but it is highly hydrophobic resulting in poor bioavailability and low therapeutic efficacy. Herein, we loaded the drug into silicon nanoparticles produced from barley husk, which is an agricultural residue and widely available. The buparvaquone-loaded nanoparticles were several times more selective to kill the intracellular parasites being non-toxic to macrophages compared to the pure buparvaquone and other conventionally used anti-leishmanial agents. Furthermore, the in vivo results revealed that the intraperitoneally injected buparvaquone-loaded nanoparticles suppressed the parasite burden close to 100%. By contrast, pure buparvaquone suppressed the burden only by 50% with corresponding doses. As the conclusion, the biogenic silicon nanoparticles are promising carriers to significantly improve the therapeutic efficacy and selectivity of buparvaquone against resistant visceral leishmaniasis opening a new avenue for low-cost treatment against this neglected tropical disease threatening especially the poor people in developing nations.
内脏利什曼病是一种由媒介传播的原生动物感染，如果不治疗是致命的。目前还没有针对这种疾病的疫苗，而且由于耐药性和严重的副作用增加，现有的化学治疗药物已经无效。布帕喹酮是一种治疗利什曼病的潜在药物，但由于其高度疏水性，导致生物利用度低，治疗效果差。在此，我们将药物负载到由大麦壳制成的硅纳米颗粒中，大麦壳是一种农业废弃物，广泛存在。与纯布帕喹酮和其他常用的抗利什曼原虫药物相比，负载布帕喹酮的纳米颗粒对杀死细胞内寄生虫具有更高的选择性，而对巨噬细胞无毒。此外，体内结果表明，腹膜内注射的负载布帕喹酮的纳米颗粒将寄生虫负荷抑制接近 100%。相比之下，纯布帕喹酮以相应剂量仅抑制负担 50%。总之，生物硅纳米颗粒是一种很有前途的载体，可以显著提高布帕喹酮对耐药性内脏利什曼病的治疗效果和选择性，为这种威胁发展中国家贫困人口的被忽视热带病提供了一种低成本的治疗方法。
