Drug delivery by inhalation is important for treatment of various pulmonary conditions such as allergy, asthma and chronic obstructive pulmonary disease as it can administer high drug doses rapidly and directly to the site of disease while minimizing systemic exposure and toxicity associated with oral or intravenous dosing. Nevertheless, therapeutic efficacy of inhaled drugs is often limited by rapid clearance from the site of action due to absorption into systemic circulation or metabolic degradation in the lungs, thereby necessitating frequent dosing and increasing systemic liability. Drug-loaded microparticles have been explored as a mechanism to sustain local drug levels in the lungs by virtue of controlled release. However, many attempts to achieve sustained release from inhaled microparticles focused on microparticles with mucoadhesive properties, overlooking the fundamental importance of mucus clearance in the airway as an innate defense against inhaled particles [1]. In this work we describe the preparation and the characterization of a cationic solid lipid system subjected to alginate coating for sustained release of salmeterol xinafoate (SX) into the lungs. The presence of mucoadhesive polymers allows solid lipid microparticles (SLMs) to adhere better to the mucous layer on the respiratory epithelium as compared with conventional carriers. The obtained systems have been characterized in terms of size, zeta potential, mucoadhesive properties and loading capacity (LC). Afterwards, we evaluated the cytotoxicity in vitro of SX, free or entrapped into SLMs, and empty microparticles by MTS viability assays on 16-HBE (human bronchial epithelial cells) cell lines.
Enhanced pumonary delivery of Salmeterol Xinafoate(SX) by mucoadhesive microparticle
AMORE E;FERRARO M;DI VINCENZO S;GJOMARKAJ M;PACE E;BONDI' ML
2016
Abstract
Drug delivery by inhalation is important for treatment of various pulmonary conditions such as allergy, asthma and chronic obstructive pulmonary disease as it can administer high drug doses rapidly and directly to the site of disease while minimizing systemic exposure and toxicity associated with oral or intravenous dosing. Nevertheless, therapeutic efficacy of inhaled drugs is often limited by rapid clearance from the site of action due to absorption into systemic circulation or metabolic degradation in the lungs, thereby necessitating frequent dosing and increasing systemic liability. Drug-loaded microparticles have been explored as a mechanism to sustain local drug levels in the lungs by virtue of controlled release. However, many attempts to achieve sustained release from inhaled microparticles focused on microparticles with mucoadhesive properties, overlooking the fundamental importance of mucus clearance in the airway as an innate defense against inhaled particles [1]. In this work we describe the preparation and the characterization of a cationic solid lipid system subjected to alginate coating for sustained release of salmeterol xinafoate (SX) into the lungs. The presence of mucoadhesive polymers allows solid lipid microparticles (SLMs) to adhere better to the mucous layer on the respiratory epithelium as compared with conventional carriers. The obtained systems have been characterized in terms of size, zeta potential, mucoadhesive properties and loading capacity (LC). Afterwards, we evaluated the cytotoxicity in vitro of SX, free or entrapped into SLMs, and empty microparticles by MTS viability assays on 16-HBE (human bronchial epithelial cells) cell lines.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
