Das Shyamal, Tucker Ian, Stewart Peter
New Zealand's National School of Pharmacy, University of Otago, Adams Building, 18 Frederick Street, P.O. Box 56, Dunedin 9054, New Zealand.
Curr Drug Deliv. 2015;12(1):26-39. doi: 10.2174/1567201811666140716123050.
Tuberculosis is the second leading cause of death from infectious diseases. Although antitubercular drugs have been traditionally administered orally, there is a growing interest in delivering drugs via the pulmonary route using nebulisers or dry powder inhalers. Drugs in dry powder inhalers (DPI) are stable and DPI are user-friendly compared to nebulisation which is time consuming, inconvenient and inefficient and requires special equipment. For tuberculosis treatment, drugs should target alveolar macrophages that harbour microorganisms and/or maintain high drug concentration at the infection site in the lung. Drug particles include micro-particles or nanoparticles. Powders can be engineered by micronisation, crystallisation, spray drying, freeze drying and particle coating approaches. The formulation may contain single or combination drugs. This paper will provide an update on current status of TB, its pathogenesis, current treatment strategies, shortcomings of current oral or parenteral delivery strategies, pulmonary delivery devices, advantages of pulmonary delivery of powder formulations, formulation approaches and pharmacokinetic studies of pulmonary delivery of powders for inhalation.
结核病是传染病致死的第二大主要原因。尽管传统上抗结核药物是口服给药,但越来越多的人对通过雾化器或干粉吸入器经肺部途径给药产生兴趣。干粉吸入器(DPI)中的药物稳定,与雾化相比,干粉吸入器对用户友好,雾化耗时、不便且效率低下,还需要特殊设备。对于结核病治疗,药物应靶向携带微生物的肺泡巨噬细胞和/或在肺部感染部位维持高药物浓度。药物颗粒包括微粒或纳米颗粒。粉末可通过微粉化、结晶、喷雾干燥、冷冻干燥和颗粒包衣方法进行加工。该制剂可包含单一药物或联合药物。本文将提供结核病的现状、发病机制、当前治疗策略、当前口服或肠胃外给药策略的缺点、肺部给药装置、粉末制剂肺部给药的优势、制剂方法以及吸入用粉末肺部给药的药代动力学研究的最新情况。