Debnath Sujit Kumar, Saisivam Srinivasan, Debanth Monalisha, Omri Abdelwahab
Department of Pharmacy, Bengal College of Pharmaceutical Sciences and Research, Durgapur, West Bengal, India.
Department of Pharmacy, N. R. Vekaria Institute of Pharmacy, Junagadh, Gujarat, India.
PLoS One. 2018 Jan 25;13(1):e0190976. doi: 10.1371/journal.pone.0190976. eCollection 2018.
Prothionamide (PTH), a second line antitubercular drug is used to administer in conventional oral route. However, its unpredictable absorption and frequent administration limit its use. An alternate approach was thought of administering PTH through pulmonary route in a form of nanoparticles, which can sustain the release for several hours in lungs. Chitosan, a bio-degradable polymer was used to coat PTH and further freeze dried to prepare dry powder inhaler (DPI) with aerodynamic particle size of 1.76μm. In vitro release study showed initial burst release followed by sustained release up to 96.91% in 24h. In vitro release further correlated with in vivo study. Prepared DPI maintained the PTH concentration above MIC for more than 12h after single dose administration and increased the PTH residency in the lungs tissue more than 24h. Animal study also revealed the reduction of dose in pulmonary administration, which will improve the management of tuberculosis.
丙硫异烟胺(PTH)是一种二线抗结核药物,通常通过口服途径给药。然而,其吸收不可预测且给药频繁,限制了其使用。人们想到了一种替代方法,即以纳米颗粒的形式通过肺部途径给药PTH,纳米颗粒可以在肺部持续释放数小时。壳聚糖是一种可生物降解的聚合物,用于包裹PTH,然后进一步冷冻干燥以制备干粉吸入器(DPI),其空气动力学粒径为1.76μm。体外释放研究表明,最初有突释现象,随后在24小时内持续释放,释放率高达96.91%。体外释放进一步与体内研究相关。制备的DPI在单剂量给药后12小时以上将PTH浓度维持在最低抑菌浓度以上,并使PTH在肺组织中的驻留时间增加超过24小时。动物研究还表明,肺部给药时剂量减少,这将改善结核病的治疗。