Bhavane Rohan, Karathanasis Efstathios, Annapragada Ananth V
School of Health Information Sciences, University of Texas-Houston Health Science Center, Houston, Texas, USA.
Int J Nanomedicine. 2007;2(3):407-18.
Nanostructured agglomerated vesicles encapsulating ciprofloxacin were evaluated for modulated delivery from the lungs in a healthy rabbit model. An aliphatic disulfide crosslinker, cleavable by cysteine was used to form cross-links between nanosized liposomes to form the agglomerates. The blood levels of drug after pulmonary instillation of free ciprofloxacin, liposomal ciprofloxacin, and the agglomerated liposomes encapsulating ciprofloxacin were evaluated. The liposomes and agglomerated vesicles showed extended release of drug into the blood over 24 hours, while the free ciprofloxacin did not. The agglomerates also allowed modulation of the drug release rate upon the introduction of cysteine into the lungs post-drug instillation; the cysteine-cleavable agglomerates accelerated their drug release rate, indicated by an increased level of drug in the blood. This technology holds promise for the post-administration modulation of antibiotic release, for the prevention and treatment of pulmonary and systemic infections.
在健康兔模型中评估了包裹环丙沙星的纳米结构团聚囊泡从肺部的调节递送情况。使用一种可被半胱氨酸裂解的脂肪族二硫键交联剂在纳米尺寸脂质体之间形成交联以形成团聚体。评估了肺部滴注游离环丙沙星、脂质体环丙沙星以及包裹环丙沙星的团聚脂质体后药物的血药浓度。脂质体和团聚囊泡在24小时内将药物持续释放到血液中,而游离环丙沙星则不然。在药物滴注后将半胱氨酸引入肺部时,团聚体还能调节药物释放速率;半胱氨酸可裂解的团聚体加速了药物释放速率,这表现为血液中药物水平的升高。这项技术有望用于抗生素释放的给药后调节,以预防和治疗肺部及全身感染。