Inhalable Dry Powders from Lyophilized Sildenafil Loaded Liposomes Containing Resveratrol or Cholesterol
Abstract
Pulmonary drug delivery is a promising approach for the treatment of respiratory diseases allowing for passive drug targeting and enhanced drug efficacy. Background/Objectives: The aim of the present study was to develop inhalable dry powders from lyophilized sildenafil citrate (SC) loaded liposomes made of phosphatidylcholine and either cholesterol (CH) or resveratrol (RSV).
Methods:: Liposomes were prepared via a pH gradient method to increase drug entrapment efficiency and drug loading and then the lipid vesicles were lyophilized using different proportions of ethanol, mannitol and lactose as excipients. The resulting dry cakes were converted into powders and evaluated for aerodynamic performance using a custom-designed air-blowing device. Notably, this is the first time that resveratrol has been used as a substitute for cholesterol in SC loaded liposomes.
Results:: The obtained results demonstrate that RSV is a suitable component of liposome bilayer that improves drug loading and probe that lyophilized cakes containing the liposomes produced a dry powder suitable for aerosolization and pulmonary delivery of sildenafil citrate. The results found for RSV liposomes point to this polyphenol offering a potential alternative to traditional cholesterol-based liposomal formulations.
Conclusions:: This approach presents a novel strategy for pulmonary delivery of sildenafil using biocompatible and FDA-approved excipients for this administration route.
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