The aim of this study was to evaluate the potential of using solid lipid microparticles (SLM) for the delivery of controlled release formulation to the respiratory tract. Salbutamol was chosen as a drug since it is widely used for the treatment of bronchial asthma. SLM, containing salbutamol , were prepared using stearic acid as the lipidic material and phosphatidylcholine as the surfactant, by the classical melt emulsification method or the spray congealing techniques with pneumatic atomizer. Initial release studies on the SLM obtained with the traditional method based on emulsion formation indicated the lack of release modulation, with > 90% salbutamol release after 5 min. This can be traced to the hydrophilic characteristics of the drug. In order to overcome this limitation, the spray congealing technique was employed. Release studies performed on the SLM produced by the spray congealing method showed a significant reduction in release, with only 65% of the drug released after 24 h. The obtained results demonstrated that for polar drug the preparation technique plays a major role in the lipid microparticle incorporation process. In particular, spray congealing was much more effective than the classical melt emulsification procedure. This effect could be attributed to the fact that the former production method permits better drug entrapment within the particles.
Incorporation of salbutamol in solid lipid microparticles
SCALIA, Santo;
2011
Abstract
The aim of this study was to evaluate the potential of using solid lipid microparticles (SLM) for the delivery of controlled release formulation to the respiratory tract. Salbutamol was chosen as a drug since it is widely used for the treatment of bronchial asthma. SLM, containing salbutamol , were prepared using stearic acid as the lipidic material and phosphatidylcholine as the surfactant, by the classical melt emulsification method or the spray congealing techniques with pneumatic atomizer. Initial release studies on the SLM obtained with the traditional method based on emulsion formation indicated the lack of release modulation, with > 90% salbutamol release after 5 min. This can be traced to the hydrophilic characteristics of the drug. In order to overcome this limitation, the spray congealing technique was employed. Release studies performed on the SLM produced by the spray congealing method showed a significant reduction in release, with only 65% of the drug released after 24 h. The obtained results demonstrated that for polar drug the preparation technique plays a major role in the lipid microparticle incorporation process. In particular, spray congealing was much more effective than the classical melt emulsification procedure. This effect could be attributed to the fact that the former production method permits better drug entrapment within the particles.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
