Preparation, characterization, and pulmonary delivery of rifapentine liposomes modified by lauric diethanolamide / 药学学报

ABSTRACT

<p><b>AIM</b>To prepare rifapentine (RIF) liposomes modified by surfactants for studying their the water-solubility, drug loading effeciency, release rate and pulmonary drug delivery.</p><p><b>METHODS</b>The film method was used to prepare RIF liposomes. Of verious RIF liposomes morphology by lauric diethanolamide (LDEA), Tween 80 and azone, the properties were studied, envolving morphology, entrapment drug release rate and dissected lung-membrance penetration rate of swine. Pulmonary delivery study was carried out through bronchoscope.</p><p><b>RESULTS</b>The particle size of RIF-LDEA liposomes was between 15 - 50 nm. The top entrapment efficiency reached 83.0%. The apparent coefficient of membrane penetration (Kp) was 44.29. LD50 was 675 mg x kg(-1) by iv.</p><p><b>CONCLUSION</b>LDEA increased the water-solubility, loading effeciency and release rate of RIF liposomes. The prepared RIF-LDEA liposomes were suitable for the treatment of pulmonary tubrculosis through bronchoscope.</p>