Chana Jasminder, Forbes Ben, Jones Stuart A
Institute of Pharmaceutical Science, King's College London, London, SE19NH, UK.
Institute of Pharmaceutical Science, King's College London, London, SE19NH, UK.
Nanomedicine. 2015 Jan;11(1):89-97. doi: 10.1016/j.nano.2014.07.012. Epub 2014 Aug 5.
This study demonstrated the feasibility of trigger-responsive inhaled delivery of medicines using soft solid shelled nanocapsules. The delivery system was a 50nm sized lipid rich capsule carrier that distended rapidly when mixed with an exogenous non-ionic surfactant trigger, Pluronic® L62D. Capsule distension was accompanied by solid shell permeabilisation which resulted in payload release from the carrier; 63.9±16.3% within 1h. In electrolyte rich aqueous fluids Pluronic® L62D was loosely aggregated, which we suggest to be the cause of its potency in lipid nanocapsule permeabilisation compared to other structurally similar molecules. The specificity of the interaction between L62D and the nanocapsule resulted in carrier payload delivery into human epithelial cells without any adverse effects on metabolic activity or barrier function. This effective, biocompatible, trigger-responsive delivery system provides a versatile platform technology for inhaled medicines.
本研究证明了使用软壳纳米胶囊进行触发响应式吸入给药的可行性。该给药系统是一种50纳米大小、富含脂质的胶囊载体，当与外源性非离子表面活性剂触发剂普朗尼克®L62D混合时会迅速膨胀。胶囊膨胀伴随着固体外壳通透性增加，导致载体内的药物释放；1小时内释放率为63.9±16.3%。在富含电解质的水性流体中，普朗尼克®L62D呈松散聚集状态，我们认为这是其与其他结构相似分子相比，在脂质纳米胶囊通透性方面具有效力的原因。L62D与纳米胶囊之间相互作用的特异性导致载体药物输送到人类上皮细胞中，而对代谢活性或屏障功能没有任何不良影响。这种有效、生物相容、触发响应式给药系统为吸入药物提供了一种通用的平台技术。
