Preparation of amorphous cefuroxime axetil nanoparticles by controlled nanoprecipitation method without surfactants

Amorphous nanoparticles of cefuroxime axetil (CFA), a poorly water-soluble drug, were produced by the controlled nanoprecipitation method without any surfactants at room temperature. The influence of the operation parameters, such as the types of solvent and anti-solvent, the stirring speed, the sol...

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Bibliographic Details
Published in:International journal of pharmaceutics 2006-10, Vol.323 (1), p.153-160
Main Authors: Zhang, Ji-Yao, Shen, Zhi-Gang, Zhong, Jie, Hu, Ting-Ting, Chen, Jian-Feng, Ma, Zhong-Qing, Yun, Jimmy
Format: Article
Language:English
Subjects:
Biological and medical sciences
Calorimetry, Differential Scanning
Cefuroxime - administration & dosage
Cefuroxime - analogs & derivatives
Cefuroxime - chemistry
Cefuroxime axetil
Controlled nanoprecipitation
Drug Compounding - methods
General pharmacology
Medical sciences
Microscopy, Electron, Scanning
Nanoparticles
Nanoparticles - chemistry
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Poorly water-soluble drug
Solubility
Solvents - chemistry
Spectroscopy, Fourier Transform Infrared
Surface-Active Agents - chemistry
Temperature
X-Ray Diffraction
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Summary:Amorphous nanoparticles of cefuroxime axetil (CFA), a poorly water-soluble drug, were produced by the controlled nanoprecipitation method without any surfactants at room temperature. The influence of the operation parameters, such as the types of solvent and anti-solvent, the stirring speed, the solvent/anti-solvent (S/AS) volume ratio, the drug concentration and the precipitation temperature, were experimentally investigated. The results indicated that increasing the stirring speed and the S/AS volume, decreasing the drug concentration and the temperature favored to decrease the particle size from 700 to 900 nm to ∼300 nm. The XRD analyses confirmed that the as-prepared CFA was amorphous nanoparticles. Furthermore, the amorphous CFA nanoparticles exhibited significantly enhanced dissolution property when compared to the commercial spray-dried product. The results demonstrated that the controlled nanoprecipitation method is a direct and feasible technology which could be utilized for preparation of the poorly water-soluble pharmaceutical nanoparticles.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2006.05.048