Division of Pharmaceutical Technology, Defence Research Laboratory, Tezpur, Assam, 784001, India.
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Guwahati, Assam, 781125, India.
Drug Deliv Transl Res. 2019 Oct;9(5):997-1007. doi: 10.1007/s13346-019-00642-1.
Resealed erythrocytes (RSE) are potential, site-specific carrier system for drug delivery with prolonged drug release activity. In this study, erythrocytes obtained from Wistar albino rats were loaded with ambroxol hydrochloride (AH) with the focus to convenience the lung targeting possibility of the carrier erythrocytes. AH loading in erythrocytes using preswell dilution technique with glutaraldehyde (GA) as a cross-linking agent was evaluated and validated. Drug-loaded erythrocyte was characterized in terms of in vitro drug release followed by osmotic fragility study which showed amplified drug entrapment efficiency (DEE) and hemoglobin content values as well. In vivo lung fibrosis study, rats were sensitized to egg albumin by intraperitoneal (i.p.) injection and then inhalation in a whole body inhalation chamber. A sign of inflammation, airway sub-mucosal fibrosis, hypertrophy, and hyperplasia was observed. A series of in vivo studies were carried out to describe the effect of AH-loaded RSE including measurement of cytokines in Bronchoalveolar Lavage (BAL) fluid and histopathology study. AH showed a stepwise reduced level of cytokines in BAL at a different time interval after being injected of AH-loaded RSE. Furthermore, in vivo lung distribution experiments were performed for optimized formulation, and degree of distribution of the drugs inside the targeted organ was found to be satisfactory.
重封的红细胞(RSE)是一种潜在的、具有特定部位的药物传递载体系统,具有延长的药物释放活性。在这项研究中,从 Wistar 白化大鼠中获得的红细胞被加载盐酸氨溴索(AH),重点是方便载体红细胞的肺部靶向可能性。使用戊二醛(GA)作为交联剂的预膨胀稀释技术评估和验证了红细胞中 AH 的负载。以体外药物释放为特征的载药红细胞随后进行渗透脆性研究,显示出放大的药物包封效率(DEE)和血红蛋白含量值。在体内肺纤维化研究中,大鼠通过腹腔(i.p.)注射致敏,然后在全身吸入室中吸入。观察到炎症、气道黏膜下纤维化、肥大和增生的迹象。进行了一系列体内研究来描述载有 AH 的 RSE 的作用,包括测量支气管肺泡灌洗液(BAL)中的细胞因子和组织病理学研究。在注射载有 AH 的 RSE 后不同时间间隔,BAL 中的细胞因子水平呈逐步降低。此外,还进行了体内肺分布实验,优化了制剂,发现药物在靶向器官内的分布程度令人满意。