Abstract
The objective of present study was to develop an optimized polymeric nanoparticle system for the antiretroviral drug tenofovir. A modified nanoprecipitation method was used to prepare Eudragit RS PO nanoparticles of the drug. The effect of amount of polymer, surfactant concentration, and sonication time on particle size, particle distribution, encapsulation efficiency (EE), and zeta potential were assessed and optimized utilizing a three-factor, three-level Box-Behnken Design (BBD) of experiment. Fifteen formulations of nanoparticles were prepared as per BBD and evaluated for particle size, polydispersity index (PDI), EE, and zeta potential. The results showed that the measured mean particle sizes were in the range of 233 to 499 nm, PDI ranged from 0.094 to 0.153, average zeta potential ranged from −19.9 to −45.8 mV, and EE ranged between 98 and 99%. The optimized formulation was characterized forin vitrodrug release and structural characterization. The mean particle size of this formulation was 233 nm with a PDI of 0.0107. It had a high EE of 98% and average zeta potential of −35 mV, an indication of particle stability. The FTIR showed some noncovalent interactions between the drug and polymer but a sustained release was observedin vitrofor up to 80 hours.
Highlights
Tenofovir is one of the first-line drugs used in the treatment of the human immunodeficiency virus (HIV) infected adults
It was found that sodium dodecyl sulphate (SDS) was able to increase the drug solubility by threefold when compared to the solubility of tenofovir in water
Their results indicated that the drug had a solubility of 33.3 mg⋅mL−1 in Tween 20, which is much less when compared to our results
Summary
Tenofovir is one of the first-line drugs used in the treatment of the human immunodeficiency virus (HIV) infected adults. Various formulation and process variables such as amount of polymer, concentration of surfactant, amount of drug, stirring speed, stirring time, and temperature play a key role in determining the final physical and mechanical characteristics of nanoparticles These parameters are often screened and optimized using highly automated statistical tools and design of experiment. Box-Behnken Design (BBD) is an experimental design of response surface methodology It is one of the most popular experimental designs which is used for the development and optimization of drug delivery systems [8] and it offers the advantage of exploring more than three formulation variables to minimize the number of wet experiments to be carried out [15]. In this project we used a modified nanoprecipitation method to encapsulate tenofovir
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