State Key Laboratory of Component-Based Chinese Medicine, Research Center of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China; Guang'anmen Hospital, China Academy of Chinese Medical Sciences, Beijing, 100053, China.
State Key Laboratory of Component-Based Chinese Medicine, Research Center of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China.
Int J Pharm. 2024 Jan 5;649:123625. doi: 10.1016/j.ijpharm.2023.123625. Epub 2023 Nov 18.
Pulmonary fibrosis is a chronic and progressive disease, current systemic administration is not fully effective with many side effects, such as gastrointestinal and liver injury. The pulmonary delivery system for pulmonary fibrosis may contribute to maximize therapeutic benefit. Natural compounds might have prominence as potential drug candidates, but the low bioavailabilities affect their clinical use. Tetrandrine is a natural alkaloid with good anti-inflammatory, antifibrogenetic and antioxidant effects, and it is used as a clinical therapeutic drug for the treatment of silicosis in China. In the present study, we explore a new strategy of pulmonary delivery system to improve low solubility and pesticide effect of tetrandrine. Tetrandrine was loaded into alginate nanogels by reverse microemulsion method. The release behavior of tetrandrine reached zero-order kinetics release and the maximum free radical clearance rates reached up to 90%. The pulmonary fibrosis rats were treated with tetrandrine nanogels by using ultrasonic atomizing inhalation. Tetrandrine nanogels decreased the development and progression of fibrosis by reducing inflammation response and bating the deposition of extra cellular matrix. In conclusion, ultrasonic atomizing inhalation of tetrandrine nanogels provided a new therapeutic strategy for pulmonary fibrosis.
肺纤维化是一种慢性进行性疾病，目前的全身给药方法疗效不充分，且有许多副作用，如胃肠道和肝脏损伤。肺纤维化的肺部给药系统可能有助于最大限度地提高治疗效果。天然化合物可能具有作为潜在药物候选物的突出地位，但低生物利用度会影响其临床应用。汉防己甲素是一种具有良好抗炎、抗纤维化和抗氧化作用的天然生物碱，在中国被用作治疗矽肺的临床治疗药物。在本研究中，我们探索了一种新的肺部给药系统策略，以提高汉防己甲素的低溶解度和农药效果。汉防己甲素通过反相微乳液法被载入海藻酸钠纳米凝胶中。汉防己甲素的释放行为达到零级动力学释放，最大自由基清除率高达 90%。肺纤维化大鼠通过超声雾化吸入汉防己甲素纳米凝胶进行治疗。汉防己甲素纳米凝胶通过减少炎症反应和抑制细胞外基质的沉积，减轻纤维化的发展和进展。总之，汉防己甲素纳米凝胶的超声雾化吸入为肺纤维化提供了一种新的治疗策略。
