Design of cefaclor monohydrate containing nanoparticles with extended antibacterial effect by nano-spray dryer:A nanoenglobing study

Abstract

Spray drying is an important method used in pharmaceutical product manufacturing for many years.The nano-spraydryer developed in recentyears provides ultrafine powders atnanoscale and high product yields.In thisstudy, which was aimed at prolonged release in oral use, nanoparticles-(NPs) were obtained by nanoenglobation of cefaclor monohydrate-(CEF)with EudragitRS 100-(ERS) with the help of nano-spraydrying method. The particle size (PS)of the blank formulation was 186 nm whereas PSs of CEFcontaining NPs were between 328and 389nm. The average PDI of all NP formulations werebelow 0.4 and all prepared NPs hada positive ZPvalue.The encapsulation efficiencyvalues werea range of 78-84%. In vitro release studies of NPs showed extended-release up to 24hours after the first 3hours of burst effect. The results showed that the release kinetics werefitted to the Korsmeyer-Peppas model.As a result, it was found that all pharmaceutical technology analysis results were affected by the solid concentration ratio in the feed dispersion.Antibacterial activity of NP formulations wasdetermined by microdilution method. After minimum inhibitory concentration (MIC)determination, time-dependent activity for NP-2 was investigated by the time-kill method. MIC value for NP-2 was 4-fold lower than MIC value of CEFfor Staphylococcus aureus and Escherichia coli. No growth was observed for both bacteria with NP-2during 18 hours incubation in the time-kill method.As a result, prolonged antibioticrelease and long-term antibacterialactivitywere obtained by NP-2,the optimumformulation of our study.