title: Preparation of azithromycin nanosuspensions by reactive precipitation method.
abstract: OBJECTIVE
  The aim of this work was to prepare azithromycin (AZI) nanosuspensions to increase the solubility and dissolution rate.
  
  
  METHODS
  AZI nanosuspensions were prepared by the combination of reactive precipitation and freeze-drying in presence of biocompatible stabilizer. Formulation and process variables affecting the characteristics of nanosuspensions were optimized. Various tests were carried out to study the physicochemical characteristics of AZI nanosuspensions.
  
  
  RESULTS
  The nanosuspensions were parenterally acceptable and autoclavable, because soybean lecithin was the stabilizer of choice and no organic solvents were used during the preparation. The mean particle size and zeta potential of the AZI nanosuspensions were about 200 nm (±20 nm) and -36.7 mV (±7.6 mV), respectively. Solid nanoparticles were obtained by lyophilization of the nanosuspensions and nanosuspensions rapidly reconstituted when the nanoparticles were dispersed in water. X-ray diffraction and differential scanning calorimetry analysis showed that the crystal state of nanoparticles was amorphous. Solubility and in vitro release studies indicated that the saturated solubility and dissolution rate increased obviously in comparison of raw AZI. The nanoparticles were physically stable over a period of 5 months as demonstrated by unchanged crystallinity and stable particle size when stored at room temperature and protected from humidity.
  
  
  CONCLUSIONS
  The results suggested that reactive precipitation is an effective way to prepare AZI nanosuspensions with increased solubility and dissolution rate.
authors.affiliation: Key Lab for Nanomaterials, Ministry of Education, Beijing University of Chemical Technology, Beijing, China.
authors.forename: Cheng-Dong
authors.initials: CD
authors.lastname: Hou
authors.forename: Jie-Xin
authors.initials: JX
authors.lastname: Wang
authors.forename: Yuan
authors.initials: Y
authors.lastname: Le
authors.forename: Hai-Kui
authors.initials: HK
authors.lastname: Zou
authors.forename: Hong
authors.initials: H
authors.lastname: Zhao
mesh_terms: D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry; D017963:Azithromycin / Q000008:administration & dosage* / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003460:Crystallization; D065546:Drug Liberation; D004355:Drug Stability; D004356:Drug Storage; D005612:Freeze Drying; D053758:Nanoparticles; D010316:Particle Size; D012995:Solubility; D013535:Suspensions; D014961:X-Ray Diffraction
chemical_list: D000900:Anti-Bacterial Agents; D013535:Suspensions; D017963:Azithromycin