Solid lipid microparticles as a sustained release system for pulmonary drug delivery.
The controlled release of drugs for pulmonary delivery is a research field which has been so far rather unexploited but is currently becoming increasingly attractive. The introduction part of this research article first details the potential advantages of solid lipid microparticles (SLMs) as drug carrier compared to liposomes and polymeric microspheres. The aim of this work is to use SLMs to impart a sustained release profile to a model drug, salbutamol acetonide (SA). SA was synthesized from salbutamol in order to increase the lipophilicity of this molecule and thereby to increase its incorporation efficiency into SLMs. SA-loaded SLMs were then produced by a hot emulsion technique followed by high-shear homogenisation and the manufacturing parameters were optimized using the experimental design methodology in order to reach a suitable particle size for pulmonary administration. Scanning electron micrographs showed that SLMs are spherical, have a smooth surface and that SA crystallizes outside of the particles when the drug loading is higher than 20%. This was confirmed by X-ray diffraction. SA in vitro release study from SLMs showed that the release rate increased with SA loading but remained in every case lower than the dissolution rate of pure SA.
Jaspart
Séverine
S
Laboratory of Pharmaceutical Technology, Department of Pharmacy, University of Liège, Belgium. sjaspart@ulg.ac.be
Bertholet
Pascal
P
Piel
Géraldine
G
Dogné
Jean-Michel
JM
Delattre
Luc
L
Evrard
Brigitte
B
D000280:Administration, Inhalation; D000420:Albuterol / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry / Q000378:metabolism; D001993:Bronchodilator Agents / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D006801:Humans; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D012137:Respiratory System / Q000378:metabolism*; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods
D001993:Bronchodilator Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008055:Lipids; D000420:Albuterol