title: Azithromycin cationic non-lecithoid nano/microparticles improve bioavailability and targeting efficiency.
abstract: OBJECTIVE
  The purpose of this study was to develop and evaluate the azithromycin cationic non-lecithoid nano/microparticles with high bioavailability and lung targeting efficiency.
  
  
  METHODS
  The cationic niosomes with different sizes (AMCNS-S and AMCNS-L) along with varied built-in characteristics were produced to achieve high bioavailability and lung targeting efficiency of azithromycin (AM) via two administration routes widely used in clinical practice, i.e., oral and intravenous routes, instead of transdermal route (by which the only marketed niosome-based drug delivery dermatologic products were given). The possible explanations for improved bioavailability and lung targeting efficacy were put forward here.
  
  
  RESULTS
  AMCNS-S (or AMCNS-L) had high bioavailability, for example, the oral (or intravenous) relative bioavailability of AMCNS-S (or AMCNS-L) to free AM increased to 273.19% (or 163.50%). After intravenous administration, AMCNS-S (or AMCNS-L) had obvious lung targeting efficiency, for example, the lung AM concentration of AMCNS-S (or AMCNS-L) increased 16 (or 28) times that of free AM at 12 h; the AM concentration of AMCNS-S (or AMCNS-L) in lung was higher than that in heart and kidney all the time.
  
  
  CONCLUSIONS
  The development of niosome-based AM nanocarriers provides valuable tactics in antibacterial therapy and in non-lecithoid niosomal application.
authors.affiliation: Medicine Engineering Research Center, Chongqing Medical University, Chongqing, 400016, People's Republic of China.
authors.forename: Meng
authors.initials: M
authors.lastname: Zhong
authors.forename: Yue
authors.initials: Y
authors.lastname: Feng
authors.forename: Hong
authors.initials: H
authors.lastname: Liao
authors.forename: Xueyuan
authors.initials: X
authors.lastname: Hu
authors.forename: Shengli
authors.initials: S
authors.lastname: Wan
authors.forename: Biyue
authors.initials: B
authors.lastname: Zhu
authors.forename: Mi
authors.initials: M
authors.lastname: Zhang
authors.forename: Huarong
authors.initials: H
authors.lastname: Xiong
authors.forename: Yunli
authors.initials: Y
authors.lastname: Zhou
authors.forename: Jingqing
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D017963:Azithromycin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D002412:Cations; D004337:Drug Carriers / Q000737:chemistry*; D065570:Gastric Absorption; D007275:Injections, Intravenous; D007408:Intestinal Absorption; D008081:Liposomes; D008168:Lung / Q000187:drug effects / Q000378:metabolism*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D017207:Rats, Sprague-Dawley; D013499:Surface Properties
chemical_list: D000900:Anti-Bacterial Agents; D002412:Cations; D004337:Drug Carriers; D008081:Liposomes; D017963:Azithromycin