Preparation and characterization of niosomes containing ribavirin for liver targeting

Abstract

The objectives of this research were to prepare ribavirin niosomes and evaluate the influence of niosomal encapsulation on drug liver targeting in rats. Ribavirin niosomes were prepared by the thin film hydration method using span 60, cholesterol, and dicetyl phosphate in molar ratios of (1:1:0), (4:2:0), (1:1:0.1), and (4:2:1). The prepared niosomes were characterized in vitro for vesicle size, drug entrapment, drug release profiles, and vesicular stability at refrigerator temperature. The results indicated that niosomes of the molar ratio (4:2:1) had a significantly (p < 0.05) higher entrapment percentage of ribavirin than the other molar ratios, moreover, they revealed sustained release characteristics as well as longer release pattern than other niosomal formulations. Accordingly, niosomes of molar ratio (4:2:1) was selected for in vivo liver targeting study. Separately, niosomal ribavirin dispersion and free ribavirin solution were administered as a single dose of 30 mg/kg by intraperitoneal injection into two groups of rats to compare the liver ribavirin concentration. The obtained results show that the niosomal formulation significantly increased ribavirin liver concentration (6-fold) in comparison with ribavirin-free solution. Based on the previous results, the use of niosomes as a drug delivery system for ribavirin has significant liver targeting properties, this is expected to improve the efficacy of low doses of ribavirin and minimize its toxic side-effects at higher doses.

Recent advances in non-ionic surfactant vesicles (niosomes): self-assembly, fabrication, characterization, drug delivery applications and limitations

“…The concentration of ribavirin in the rat liver obtained from the ribavirin niosomes was 6-fold higher than that obtained from the ribavirin solution after an intraperitoneal injection of a single dose equivalent to 30 mg/kg of the drug. This demonstrates effective liver targeting properties for niosomes (Hashim et al, 2010).…”

Development of a biocompatible creatinine-based niosomal delivery system for enhanced oral bioavailability of clarithromycin

“…However, the chemical stability as well as the relatively low cost of the materials used to prepare niosomes may make them more attractive than liposomes for pharmaceutical and cosmetic applications (Hashim et al, 2010;Valdés et al, 2014;Yasam et al, 2014).…”

“…Niosomes enhance the oral in-vivo therapeutic efficacy of drugs by delayed clearance from the circulation by virtue of peculiar shape and size and protecting them from harsh biological environment (El-Ridy et al;. Therefore it is desirable to design niosomal formulations of Clarithromycin in order to improve the physicochemical properties, enhance intestinal absorption and thereafter increase bioavailability of the drug.…”

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“…Niosomes have attracted a great deal of attention in the delivery of dermal drugs because of many advantages, like they are biodegradable, biocompatible, non-toxic, non-immunogenic in nature and effective in the modulation of drug release properties 4 . In recent years, niosomes received a great attention as potential drug delivery systems for different routes of administration, such as intravenous and intramuscular, subcutaneous, intraperitoneal 5 and transdermal 6 .…”