Development and evaluation of nanosized niosomal dispersion for oral delivery of Ganciclovir

Abstract

Encapsulation of Ganciclovir in lipophilic vesicular structure may be expected to enhance the oral absorption and prolong the existence of the drug in the systemic circulation. So the purpose of the present study was to improve the oral bioavailability of Ganciclovir by preparing nanosized niosomal dispersion. Niosomes were prepared from Span40, Span60, and Cholesterol in the molar ratio of 1:1, 2:1, 3:1, and 3:2 using reverse evaporation method. The developed niosomal dispersions were characterized for entrapment efficiency, size, shape, in vitro drug release, release kinetic study, and in vivo performance. Optimized formulation (NG8; Span60:Cholesterol 3:2 molar ratio) has shown a significantly high encapsulation of Ganciclovir (89±2.13%) with vesicle size of 144±3.47 nm (polydispersity index [PDI]=0.08). The in vitro release study signifies sustained release profile of niosomal dispersions. Release profile of prepared formulations have shown that more than 85.2±0.015% drug was released in 24 h with zero-order release kinetics. The results obtained also revealed that the types of surfactant and Cholesterol content ratio altered the entrapment efficiency, size, and drug release rate from niosomes. In vivo study on rats reveals five-time increment in bioavailability of Ganciclovir after oral administration of optimized formulation (NG8) as compared with tablet. The effective drug concentration (>0.69 µg/mL in plasma) was also maintained for at least 8 h on administration of the niosomal formulation. In conclusion, niosomes can be proposed as a potential oral delivery system for the effective delivery of Ganciclovir.

Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge 

“…Thus, compared with suspension, there appeared to be significantly enhanced oral bioavailability of CRV from the niosomal formulation. These observations were consistent with previous findings that niosomes enhance the oral bioavailability of ganciclovir 49 and paclitaxel. 50 Improved CRV absorption and higher plasma drug concentrations after niosomal formulation may be due to the main carrier components (surfactants) acting as penetration enhancers.…”

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

“…124 Similarly, nanosized ganciclovir niosomes were developed to enhance bioavailability of ganciclovir in plasma for at least 8 hours after administration. 131 …”

Ocular pharmacoscintigraphic and aqueous humoral drug availability of ganciclovir-loaded mucoadhesive nanoparticles in rabbits

“…The resulting vesicles were incubated for 2 h with a 0.2% w/w chitosan solution (in glacial acetic acid, 0.5% v/v, pH 5.5). GCV entrapment (%) was then estimated as per the method reported by Akhter et al (1).…”

“…GCV-NDs were prepared by the reverse-phase evaporation technique (1). Briefly, GCV-loaded niosomes were prepared by dissolving Span 60 and cholesterol in the ratio of 3:2 w/w in diethyl ether and adding 2 mL of PBS (pH 7.4) containing GCV.…”

“…Conventional treatment involves the oral administration of GCV at a dose of 3 g/day. However, this relatively high dose regimen is associated with the occurrence of side effects including bone marrow suppression and neutropenia (1,3). Compared to systemic treatment, intravitreal injection of GCV provides higher intraocular drug concentrations but repeated intravitreal injections are poorly tolerated (4).…”