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Thursday 07 November 2002

A facile method of delivery of liposomes by nebulization.

By: Desai TR, Hancock RE, Finlay WH.

J Control Release 2002 Nov 7;84(1-2):69-78

In this study, we have demonstrated a facile approach to the aerosol delivery of liposomes by nebulization. The approach involves mere dispersion of the physical mixture of phospholipid(s) and drug in saline, which results in spontaneous formation of liposomes thereby creating reservoirs for the encapsulation of drugs. Various phospholipids exhibiting different physico-chemical properties were investigated here. Two antimicrobial agents (ciprofloxacin and CM3, a novel peptide) and a bronchodilator, salbutamol sulfate, were used as model drugs to examine the nebulization properties. Nebulization properties were found to be dependent upon the nature of the phospholipids and drug. Among various phospholipids investigated, dimyristoyl phosphatidyl glycerol (DMPG), a combination of egg phosphatidylcholine (EPC) plus DMPG (i.e., EPC+DMPG) and dimyristoyl phosphatidylcholine (DMPC) plus DMPG (DMPC+DMPG) (molar ratios 1:1) showed encouraging results in terms of higher nebulization efficiency and lower leakage of drug after nebulization. The generated aerosols were characterized by an Andersen cascade impactor operated at 28.3 l/min. The mass median aerodynamic diameter (MMAD) values of the aerosol droplets obtained by nebulization of all the preparations containing DMPG reveal that these preparations are suitable for aerosol delivery by nebulization. This facile approach is expected to overcome problems associated with stability upon storage and high production costs.

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