Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release.
BACKGROUND
The application of antibiotics has been limited due to weak biodistribution and pharmacokinetics. Encapsulation of these drugs in lipid vesicles might be a good solution for obtaining the required properties. Liposomes are one of the most suitable drug-delivery systems to deliver the drug to the target organ and minimize the distribution of the drug to non-target tissues.


OBJECTIVE
The study reported here aimed to develop cefditoren pivoxil liposomes by thin-film hydration, characterize them in terms of physical interactions, and undertake in vitro and in vivo release studies.


METHODS
The pre-formulation studies were carried out using Fourier-transform infrared spectroscopy and differential scanning calorimetry. Cefditoren pivoxil liposomal formulations were formulated by thin-film hydration using biomaterials ie, soya lecithin and cholesterol in different molar ratios. The best molar ratio was determined by in vitro studies such as entrapment efficacy, particle size distribution, and diffusion.


RESULTS
From the in vitro release studies, it was found that the formulation that contained soya lecithin and cholesterol in a 1.0:0.6 molar ratio gave good entrapment of 72.33% and drug release of 92.5% at 36 hours. Further, the formulation's zeta potential and surface morphology were examined and stability and in vivo studies were undertaken evaluating the pharmacokinetic parameters, which showed promising results.


CONCLUSIONS
Formulation CPL VI showed the maximum drug-loading capacity of 72.3% with good controlled release and acceptable stability when compared with the other formulations. In vivo studies in rabbits showed that the drug release from the liposomes was successfully retarded with good controlled release behavior which can be used to treat many bacterial infections with a minimal dose.
Environmental and Analytical Chemistry Division, School of Advanced Sciences, VIT University, Vellore, India.
Gojjala
G
Venugopalarao
Centre for Material Science, KCG College of Technology, Chennai, India.
Rajasekhar
R
Lakshmipathy
Environmental and Analytical Chemistry Division, School of Advanced Sciences, VIT University, Vellore, India.
Nallani Chakravarthula
NC
Sarada
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002511:Cephalosporins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D065546:Drug Liberation; D066298:In Vitro Techniques; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D011817:Rabbits; D014018:Tissue Distribution
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D008081:Liposomes; C057710:cefditoren pivoxil
biomaterials; cholesterol; drug-delivery system; liposomes; soya lecithin