LAUSR

Abstract Polymeric nanoparticles were found to be an effective drug delivery system to improve the bioavailability of drugs by increasing their solubility and circulation half-life in comparison with pure cefixime. In the current investigation, cefixime was used as a model drug and orally administered polymeric nanoparticles were developed using chitosan and Azadirachta indica fruit mucilage as natural polymers to achieve enhanced permeation, solubility and sustained release of therapeutically active agent. As a result, improved half-life, bioavailability and better therapeutic index of cefixime can be achieved when compared to pure cefixime. Polymeric cefixime nanoparticles were formulated using modified coacervation technique and then evaluated for various physic-chemical parameters such as average particle size, percentage entrapment efficiency and in-vitro drug release behavior, in-vitro antimicrobial efficiency and in-vivo animal studies (i.e., pharmacokinetics, acute toxicity and the efficacy studies) in comparison to the pure cefixime. The formulations were found to have a mean particle size range of 85.6 ± 4.5 to 250.6 ± 9.3 nm, and percentage entrapment efficiency was found to be in the range of 76.2 ± 1.3% to 90.4 ± 1.5%. The in-vitro drug release data showed an initial burst release of drug followed by a sustained up to 28 h. The in-vitro antimicrobial efficiency studies for the selected formulation revealed that the formulations found to have an improved zone of inhibition with lower minimum inhibitory concentration compared to the pure cefixime. The in-vivo pharmacokinetic study of formulation revealed sustained release of cefixime into the blood stream with a 14.59-fold increase in oral bioavailability and one fold increase in half-life compared to the pure cefixime when administered orally in rats (20 mg/kg weight). The acute toxicity study revealed that the formulation was found to be safe up to 2000 mg/kg with improved efficacy. Therefore, the developed formulation might be a novel carrier that improves the oral bioavailability of cefixime and thereby improved therapeutic activity can be achieved when compared to pure cefixime.