Chitosan based micro- and nanoparticles for colon-targeted delivery of vancomycin prepared by alternative processing methods

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 92; pp. 112 - 119
• Main Authors: Cerchiara, T., Abruzzo, A., di Cagno, M., Bigucci, F., Bauer-Brandl, A., Parolin, C., Vitali, B., Gallucci, M.C., Luppi, B.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.05.2015
• Subjects: Anti-Bacterial Agents - administration & dosage; Anti-Bacterial Agents - pharmacokinetics; Chemistry, Pharmaceutical - methods; Chitosan; Chitosan - chemistry; Colon - metabolism; Drug Compounding - methods; Drug delivery; Drug Delivery Systems; Drug Liberation; Freeze Drying; Microparticles; Microscopy, Electron, Scanning; Microspheres; Nanoparticles; Particle Size; Polyphosphates - chemistry; Spectroscopy, Fourier Transform Infrared; Staphylococcus aureus - drug effects; Technology, Pharmaceutical - methods; Vancomycin; Vancomycin - administration & dosage; Vancomycin - pharmacokinetics; Nanoparticles; Drug delivery; Chitosan; Vancomycin; Microparticles
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2015.03.004

[Display omitted] •We prepared chitosan micro/nanoparticles for colon-specific delivery of vancomycin.•Particles were prepared by different methods: ionic gelation or spray-drying process.•The nanoparticles obtained by nano spray-dryer showed the best results. The aim of this work was to prepare chitosan (CH) based particulate formulations for colon delivery of vancomycin (VM). Chitosan microparticles (MPs) and nanoparticles (NPs) loaded with VM were prepared using different CH/tripolyphosphate (TPP) molar ratios and different technological processes. In particular, nanoparticles were prepared by ionic gelation and freeze-drying to recover these particles, or, alternatively, by spray-drying method. Microparticles were prepared using a different spray-dryer. Micro- and nanoparticles were characterized in terms of size distributions by photon correlation spectroscopy (PCS), while encapsulation and drug loading efficiencies were studied using a dialysis method. Fourier Transform Infrared Spectroscopy (FT-IR) was employed to determine the surface composition of the micro- and nanoparticles respectively, and the morphologies of the developed systems were studied by scanning electron microscopy (SEM). Water uptake as well as drug release profiles were also measured. Antibacterial activity against Staphylococcus aureus, a Gram-positive model strain, was evaluated. FT-IR results suggested an electrostatic interaction between VM and CH/TPP particles. Moreover, the particles were found to hold a positive zeta-potential, indicating the presence of CH on the particle surfaces. Particle size and encapsulation efficiency were mainly influenced by the different manufacturing processes employed. Nanoparticles obtained by spray-drying showed the best results in terms of water uptake and drug release rate. Moreover, they showed a good bactericidal activity against S. aureus.