Elhissi Abdelbary M A, Ahmed Waqar, Taylor Kevin M G
Drug Delivery Research Group, Institute of Nanotechnology and Bioengineering, School of Pharmacy and Biomedical Sciences, School of Computing, Engineering and Physical Sciences, University of Central Lancashire, Preston PR1 2HE, United Kingdom.
J Nanosci Nanotechnol. 2012 Aug;12(8):6693-9. doi: 10.1166/jnn.2012.4566.
Particulate-based proliposomes were made by coating sucrose carrier particles with egg phosphatidylcholine (EPC), soya phosphatidylcholine (SPC) or soya phosphatidylcholine with an equimole ratio of cholesterol (SPC:Chol, 1:1). Inhalable multilamellar liposomes were generated from proliposomes in situ within a Pari LC Plus nebulizer by addition of aqueous phase, with no need for prior manual shaking. All proliposome formulations produced high aerosol and phospholipid outputs and were delivered in high fractions to the lower stage of a two-stage impinger. The SPC:Chol (1:1) liposomes tended to accumulate more in the nebulizer because of their greater rigidity, which correlated with the larger size measured at the end of nebulization. The size of aerosol droplets as measured by laser diffraction was similar for all formulations, however, at the sputtering period, the SPC:Chol (1:1) formulation produced large droplets with broadened size distribution. This study has demonstrated a simple approach to delivering high outputs of liposomes using a particulate-based proliposome technology and has shown an evidence of liposome generation from proliposomes within a medical nebulizer.
基于颗粒的前体脂质体是通过用鸡蛋卵磷脂（EPC）、大豆卵磷脂（SPC）或胆固醇等摩尔比的大豆卵磷脂（SPC:Chol，1:1）包被蔗糖载体颗粒制成的。通过添加水相，在Pari LC Plus雾化器中原位从前体脂质体生成可吸入多层脂质体，无需事先手动摇晃。所有前体脂质体制剂均产生高气溶胶和磷脂输出量，并以高比例输送到两级冲击器的较低阶段。SPC:Chol（1:1）脂质体由于其更大的刚性，往往在雾化器中积累更多，这与雾化结束时测量的较大尺寸相关。通过激光衍射测量，所有制剂的气溶胶液滴大小相似，然而，在溅射期，SPC:Chol（1:1）制剂产生大液滴，尺寸分布变宽。本研究展示了一种使用基于颗粒的前体脂质体技术输送高产量脂质体的简单方法，并证明了在医用雾化器中从前体脂质体生成脂质体的证据。
