Abstract
The present study was focused on formulating and evaluating clarithromycin (CLR) containing niosomal formulation for in vitro and in vivo pharmacokinetic behavior. Niosomal formulations (empty and drug loaded) were prepared by using different ratio of surfactant (various Span grades 20, 40, 60, and 80) and cholesterol by thin film hydration method and were evaluated for in vitro characteristics, stability studies, and in vivo study. Dicetyl phosphate (DCP) was added to the niosomal formulation. Various pharmacokinetic parameters were determined from plasma of male SD rats. Span 60 containing niosomal formulation NC2 (cholesterol to surfactant ratio 1 : 1) displayed highest entrapment efficiency with desired particle size of 4.67 μm. TEM analyses showed that niosomal formulation was spherical in shape. Niosomes containing Span 60 displayed higher percentage of drug release after 24 h as compared to other formulations. NC2 formulation was found to be stable at the end of the study on storage condition. Various pharmacokinetic parameters, namely, AUC, AUMC, and MRT of niosomal formulation, were found to be 1.5-fold, 4-fold, and 3-fold plain drug, respectively. The present study suggested that niosomal formulations provide sustained and prolonged delivery of drug with enhance bioavailability.
Highlights
In recent years, transporting the drug molecules to the desired site in the biological systems has become a very specific and sophisticated area of pharmaceutical research
Shape and morphology of empty niosomal formulations and drug loaded niosomal formulations were determined by optical microscopy and Transmission Electron Microscopy (TEM) and results were shown in Figures 1 and 2
Developed niosomal formulations were characterized with respect to particle size, shape, entrapment efficiency, and in vitro drug release profile
Summary
In recent years, transporting the drug molecules to the desired site in the biological systems has become a very specific and sophisticated area of pharmaceutical research. The role of the novel drug delivery system is limited to a drug package convenience and ease of administration but along with this it is needed to provide better therapeutic efficacy and safety by delivering the drug molecules to the target site in the most convenient manner. These novel carriers provide sustained drug release for prolonged duration in targeted tissue resulting in enhanced therapeutic efficacy and minimized side effects (as discussed by Lamprecht [1]). Tmax, AUC, AUMC, and MRT of niosomal formulation, were calculated
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