Formulation and Optimization of Eudragit RS PO‐Tenofovir Nanocarriers Using Box‐Behnken Experimental Design

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 for in vitro drug 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 observed in vitro for up to 80 hours.

A Review on Optimization of Drug Delivery System With Experimental Designs

“…It is economical then CCD because t requires less number of Trial. Implementation of BBD in tenofovir preparation and fabrication of nateglinide nanoparticles [29,30].…”

Preparation, Statistical Optimization and Characterization of Propolis-Loaded Solid Lipid Nanoparticles Using Box-Behnken Design

“…In suggested equations, the negative or positive sign for coefficients indicates a negative or positive effect on the response respectively. 35 …”

Development of Nitazoxanide Loaded Polymeric Nanocarriers: Box Behnken Experimental Design Based Optimisation and Characterisation

“…The concept behind the selection criteria of polymer is that the Eudragit RL 100 is a positively charge polymer to synthesise nanoparticles which rises the interface between mucin and nanoparticles thus increases the drug bioavailability [8]. Due to biodegradable, aqueous solubility, minimal cell adhesion produces non -toxic effect, stability towards temperature variation and easy entanglement with nanoparticles surface PVA is selected as an another polymer [5,8].…”

“…However, polymeric containing nanoparticles improve drug therapeutic efficacy, site specific targeting effect and decreased toxicity as well as occurrence of adverse drug effect [4]. The versatile features of polymeric nanoparticles such as defence of active molecules from deprivation, enhancement in pervasion of the active molecules across gastro intestinal tract, prolonged release of the entrapped drug, decrease in dosing incidence, increase solubility in water which astounded the physiological barriers to deliver the drugs at the target sites etc [5]. Therefore, the selection of polymers for encapsulation does depends upon the various factors for design of nanomaterials and their biocompatibility [6].…”

“…The ammonium groups are present as salts and make the polymers permeable [7]. It is less soluble in water but swells in digestive fluids and independent at the physiological pH but the cationic charge facilitates rapid permeation through the intestinal mucosa [5]. The drug payload can be transported through the process of diffusion.…”