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Formulation and In Vitro Evaluation of Sterically Stabilised Phospholipid Nanomicelles Loaded with Beclomethasone Dipropionate for Nebulisation

机译:雾化负载倍氯米松二丙酸酯的稳定稳定的磷脂纳米脂质体的配方和体外评估

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Purpose: The aim of this study was to formulate and evaluate the potential of sterically stabilised phospholipid nanomicelles (SSMs) loaded with beclomethasone dipropionate (BDP) for pulmonary delivery through nebulisation. Method: BDP-SSMs were prepared by the coprecipitation and reconstitution method and characterised for different physicochemical and aerodynamic properties. Results: Particle size of BDP-SSMs determined by photon correlation spectroscopy (PCS) was 19.89±0.67 nm with polydispersity index of approximately 0.22±0.02. At 5mM of PEG5000-DSPE, the maximum solubilisation efficiency of BDP was 209.65±7.74 ng/ml with a single-sized peak population. Zeta potential measurement of BDP-SSMs was -28.03±2.05 mV. The entrapment efficiency (%EE), yield (%Y) and drug loading (%DL) of the lyophilised formulations were 100.87±3.5, 95.11±0.38 and 0.72± 0.03%, respectively. TEM photograph of BDP-SSMs revealed spherical nanoparticles. BDP-SSMs exhibited a prolonged dissolution behaviour as compared to solubilised BDP powder (P <0.05). Aerodynamic characteristic values of BDP-SSMs using Pari LC or Omron nebulisers were equivalent and more superior than some marketed inhaler products. Conclusion: SSMs showed great potential as pulmonary delivery systems for BDP as they exhibited high pulmonary deposition and prolonged in vitro release.
机译:目的:本研究的目的是制定和评估装载有倍氯米松二丙酸酯(BDP)的空间稳定化磷脂纳米胶束(SSM)通过雾化肺部递送的潜力。方法:通过共沉淀和重构方法制备BDP-SSM,并针对其不同的理化和空气动力学特性进行表征。结果:通过光子相关光谱法(PCS)测定的BDP-SSM的粒径为19.89±0.67 nm,多分散指数约为0.22±0.02。在5mM的PEG5000-DSPE上,BDP的最大增溶效率为209.65±7.74 ng / ml,具有单一大小的峰人口。 BDP-SSM的Zeta电势测量值为-28.03±2.05 mV。冻干制剂的包封率(%EE),收率(%Y)和载药量(%DL)分别为100.87±3.5、95.11±0.38和0.72±0.03%。 BDP-SSM的TEM照片显示球形纳米颗粒。与溶解的BDP粉末相比,BDP-SSMs表现出延长的溶解行为(P <0.05)。使用Pari LC或Omron雾化器的BDP-SSM的空气动力学特性值相同,并且比某些市售吸入器产品优越。结论:SSMs具有较高的肺部沉积和体外释放时间,因此具有作为BDP肺部递送系统的巨大潜力。

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