[Preparation, characterization, and pulmonary delivery of rifapentine liposomes modified by lauric diethanolamide].
OBJECTIVE
To prepare rifapentine (RIF) liposomes modified by surfactants for studying their the water-solubility, drug loading effeciency, release rate and pulmonary drug delivery.


METHODS
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.


RESULTS
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.


CONCLUSIONS
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.
Shu
Jia-you
JY
College of Pharmacy, Wuhan University, Wuhan 430072, China. shujiayou@sina.com
Quan
Xiang-yang
XY
Shu
Yi
Y
Guang
Yi-ping
YP
Liu
You-cheng
YC
D000818:Animals; D000904:Antibiotics, Antitubercular / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers; D016503:Drug Delivery Systems / Q000379:methods*; D004983:Ethanolamines / Q000737:chemistry; D007850:Lauric Acids / Q000737:chemistry; D008081:Liposomes; D008168:Lung / Q000378:metabolism*; D010316:Particle Size; D010539:Permeability; D012293:Rifampin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D012995:Solubility; D013552:Swine
D000904:Antibiotics, Antitubercular; D004337:Drug Carriers; D004983:Ethanolamines; D007850:Lauric Acids; D008081:Liposomes; C052237:lauric acid diethanolamide; D012293:Rifampin; C018421:rifapentine