Nebulization of ultradeformable liposomes: The influence of aerosolization mechanism and formulation excipients

Elhissi, A.M.A.a b, Giebultowicz, J.a c e, Stec, A.A.a c , Wroczynski, P.e, Ahmed, W.a d, Alhnan, M.A.a b, Phoenix, D.a and Taylor, K.M.G.a f (2012) Nebulization of ultradeformable liposomes: The influence of aerosolization mechanism and formulation excipients. International Journal of Pharmaceutics, 436 (1-2). pp. 519-526. ISSN 03785173

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Ultradeformable liposomes are stress-responsive phospholipid vesicles that have been investigated extensively in transdermal delivery. In this study, the suitability of ultradeformable liposomes for pulmonary delivery was investigated. Aerosols of ultradeformable liposomes were generated using air-jet, ultrasonic or vibrating-mesh nebulizers and their stability during aerosol generation was evaluated using salbutamol sulphate as a model hydrophilic drug. Although delivery of ultradeformable liposome aerosols in high fine particle fraction was achievable, the vesicles were very unstable to nebulization so that up to 98 drug losses were demonstrated. Conventional liposomes were relatively less unstable to nebulization. Moreover, ultradeformable liposomes tended to aggregate during nebulization whilst conventional vesicles demonstrated a "size fractionation" behaviour, with smaller liposomes delivered to the lower stage of the impinger and larger vesicles to the upper stage. A release study conducted for 2 h showed that ultradeformable liposomes retained only 30 of the originally entrapped drug, which was increased to 53 by inclusion of cholesterol within the formulations. By contrast, conventional liposomes retained 60-70 of the originally entrapped drug. The differences between ultradeformable liposomes and liposomes were attributed to the presence of ethanol or Tween 80 within the elastic vesicle formulations. Overall, this study demonstrated, contrary to our expectation, that materials included with the aim of making the liposomes more elastic and ultradeformable to enhance delivery from nebulizers were in fact responsible for vesicle instability during nebulization and high leakage rates of the drug. © 2012 Elsevier B.V. All rights reserved.

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Keywords:alcohol, cholesterol, excipient, liposome, nanoparticle, polysorbate 80, salbutamol sulfate, ultradeformable liposome, unclassified drug, aerosol, article, drug delivery system, drug determination, drug formulation, drug manufacture, drug release, drug synthesis, high performance liquid chromatography, nebulization, priority journal, Aerosols, Albuterol, Bronchodilator Agents, Chemistry, Pharmaceutical, Drug Stability, Excipients, Hydrophobic and Hydrophilic Interactions, Liposomes, Nebulizers and Vaporizers, Particle Size, Technology, Pharmaceutical
Subjects:F Physical Sciences > F200 Materials Science
J Technologies > J510 Materials Technology
Divisions:College of Science > School of Mathematics and Physics
ID Code:27160
Deposited On:25 Jul 2018 11:05

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