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. 2016:2016:6492953.
doi: 10.1155/2016/6492953. Epub 2016 May 16.

In Vitro and In Vivo Evaluation of Niosomal Formulation for Controlled Delivery of Clarithromycin

Gyati Shilakari Asthana  1 , Parveen Kumar Sharma  1 , Abhay Asthana  1
Affiliations

In Vitro and In Vivo Evaluation of Niosomal Formulation for Controlled Delivery of Clarithromycin

Gyati Shilakari Asthana et al. Scientifica (Cairo). 2016.

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.

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Figures

Figure 1
Figure 1
Optical microscopy of niosomes. (a) Empty and (b) drug loaded at 45x magnification.
Figure 2
Figure 2
TEM image of NC2 formulation prepared at 1 : 1 ratio of cholesterol and Span with different magnification. (a) 40,000x and (b) 45,000x.
Figure 3
Figure 3
Effect of cholesterol and surfactant ratio on particle size of niosomes containing different series of Span.
Figure 4
Figure 4
Entrapment efficiency of niosomes containing different series of Span at various ratios.
Figure 5
Figure 5
Comparative encapsulation efficiency of various series of niosomal formulation at ratio 1 : 1 : 1 (drug : cholesterol : surfactant).
Figure 6
Figure 6
Comparative release profile of selected niosomal formulations.
Figure 7
Figure 7
Cell viability study of free drug solution; empty niosomes; drug loaded niosomes on A549 cell lines (n = 3).
See this image and copyright information in PMC

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