Development and evaluation of co-encapsulated stavudine and lamivudine niosomes for the controlled delivery

Stavudine and lamivudine are nucleoside reverse transcriptase inhibitors used for the treatment of HIV. We describe here the co-encapsulation of stavudine and lamivudine in niosomal MLVs composed of tween80, span60 and variable amounts of cholesterol. The main aim of this study is to reduce the dose, dosing frequency and overcome the resistance of existing single drug regimen therapy. The influence of drug-lipid ratio was studied and amount of the drug could be encapsulated was optimized. The effect of cholesterol and other process related parameters were studied to obtain the niosomal vesicles with desired quality. All the prepared formulations were characterized for their physico chemical properties such as appearance, vesicle size, vesicle size distribution, percent drug entrapment, viscosity, zeta potential, stability profile and in-vitro drug release. Stability of niosomes in terms of their drug leakage and drug retention behavior was studied as per ICH guidelines for three months by storing the niosomes at refrigerated temperature (4 ± 2 °C) and room temperature (25 ± 2 °C). Niosomes stored under refrigerated condition showed greater stability and results were found to be within the specification in both storage conditions. The maximum percentage drug entrapment (92.64%) was achieved with the formulation containing the drug –lipid ratio of 150:40% w/w. In vitro release data showed that release profile followed zero order kinetics and drug release mechanism was of diffusion. Stavudine and lamivudine niosomes with good stability and appreciable controlled drug release with good retention of the drug even after 24h were prepared successfully.

Author(s): M. Yasmin Begum

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