Hariyadi Dewi Melani, Purwanti Tutiek, Maulydia Dinda, Estherline Cindy Alicia, Hendradi Esti, Rahmadi Mahardian
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga, Surabaya, Indonesia.
Department of Pharmacy Practice, Faculty of Pharmacy, Universitas Airlangga, Surabaya, Indonesia.
J Adv Pharm Technol Res. 2021 Jul-Sep;12(3):242-249. doi: 10.4103/japtr.JAPTR_197_21. Epub 2021 Jul 16.
It has been known that in respiratory disease, antibiotic is selected for respiratory diseases or lung infections and this research focused on ciprofloxacin HCl as a model. The aim was to evaluate the effect of kappa-carrageenan polymer concentrations on characteristics, release, and drug deposition in the lung. Ciprofloxacin HCl-carrageenan microspheres were produced with kappa carrageenan (0.75%, 0.50%, and 0.25%) as polymer and KCl (1.5%) as crosslinker. Physical characteristics were included morphology, size, moisture content, swelling index, mucoadhesivity, drug loading, entrapment efficiency, and yield. Freeze-dried microspheres were inhaled by animal, and drug deposition was observed. Results showed that dried, smooth, and spherical microspheres of size of 1.34 to 1.70 μm and loading of 15.63% to 38.72%. Entrapment efficiency and yield were 25.38%-51.61% and 52.53%-63.19%, respectively. Mucoadhesivity was 0.0059-0.0096 kg force, and release in 24 h was 74.38%-81.02%. Release kinetics demonstrated Higuchi mechanism. Increasing carrageenan concentration affected size, loading, and efficiency but did not influence adhesivity, yield, and release. Higher amount of polymer caused the lower deposit on the lungs. Respirable size of ciprofloxacin HCl-kappa carrageenan microspheres was successfully achieved target site and prolonged residence time in lungs.
众所周知，在呼吸系统疾病中，会选择抗生素来治疗呼吸系统疾病或肺部感染，本研究聚焦于盐酸环丙沙星作为模型。目的是评估κ-卡拉胶聚合物浓度对肺部特性、释放及药物沉积的影响。以κ-卡拉胶（0.75%、0.50%和0.25%）为聚合物、氯化钾（1.5%）为交联剂制备盐酸环丙沙星-卡拉胶微球。物理特性包括形态、大小、水分含量、溶胀指数、粘膜粘附性、载药量、包封率和产率。将冻干微球吸入动物体内，并观察药物沉积情况。结果显示，干燥、光滑且呈球形的微球大小为1.34至1.70μm，载药量为15.63%至38.72%。包封率和产率分别为25.38%-51.61%和52.53%-63.19%。粘膜粘附性为0.0059-0.0096千克力，24小时释放率为74.38%-81.02%。释放动力学符合 Higuchi 机制。增加卡拉胶浓度会影响微球大小、载药量和包封率，但不影响粘附性、产率和释放。聚合物用量增加会导致肺部沉积量降低。盐酸环丙沙星-κ-卡拉胶微球的可吸入粒径成功达到目标部位，并延长了在肺部的停留时间。
