Study on influence of polymer and surfactant on in vitro performance of biodegradable aqueous-core nanocapsules of tenofovirdisoproxil fumarate by response surface methodology

Grandhi Srikar,Avula Prameela Rani

doi:10.1590/s2175-97902019000118736

Abstract

The major objective of this study was to investigate the effect of biodegradable polymer type and surfactant concentration on various characteristics viz. particle size, entrapment efficiency and drug release rate constant of aqueous core nanocapsules (ACNs) containing tenofovirdisoproxil fumarate. In this study, the nanocapsules were prepared by modified multiple emulsion technique with biodegradable polymers viz. poly(lactide-co-glycolide) of two different grades (PLGA RG502H and PLGA RG503H) and poly lactic acid (PLA R203H); and the surfactant employed was span 80. The experiments were designed under response surface methodology by employing the Design Expert software. Entrapment efficiency, particle size and drug release rate constant were taken as response variables. The prepared nanocapsules were subjected to characterization studies and the obtained results were statistically analyzed by Analysis of Variance (ANOVA) for response surface 2-Factorial Interaction model. ANOVA studies showed that the influence of both factors on all the response variables were significant at p<0.05. The optimized formulation was found to have the entrapment efficiency of 71.58%, particle size of 252.41 nm and the drug release rate constant of 0.045 h-1; thus, indicating that the ACNs were obtained with finest characteristics. SEM studies showed that the particles were spherical.

Highlights

Carrier mediated drug delivery systems have received a growing significant interest in the recent years due to its ability of being utilized as carriers for the drug delivery for various causes such as targeted delivery (Li et al, 2008), improving bioavailability (Jia, 2005), crossing blood brain barrier (Dufes, 2011) and overcoming the inhibitory actions of glycoprotein-P (P-gP) for permeation of drugs into the cells (Brigger, Dubernet, Couvreur, 2002)
Compatibility studies of drug and polymer were conducted by employing I.R spectral studies
3223.48 cm-1 accounting for O-H stretching (Gomes et al, 2015; Silverstein, Webster, Kiemle, 2005). These bands accounting for the characteristic groups of Tenofovirdisoproxil fumarate (TDF) were observed at the similar positions in the spectra of individual physical mixtures of TDF with the polymers viz. PLGA RG503H, PLGA RG502H and poly lactic acid (PLA) R203H

Summary

Introduction

Carrier mediated drug delivery systems have received a growing significant interest in the recent years due to its ability of being utilized as carriers for the drug delivery for various causes such as targeted delivery (Li et al, 2008), improving bioavailability (Jia, 2005), crossing blood brain barrier (Dufes, 2011) and overcoming the inhibitory actions of glycoprotein-P (P-gP) for permeation of drugs into the cells (Brigger, Dubernet, Couvreur, 2002). The use of biodegradable polymers is advantageous because they are not deposited in the body and pose no toxicity risk, as they degrade into soluble and excretable form. These biodegradable polymeric nanoparticles can be effectively given through intravenous route in order to control the spatial and temporal delivery of the incorporated drugs. Due to their submicron size and wide possibility of modifying their surface, these can be employed to deliver drugs at varied target sites (Doppalapudi et al, 2016)

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Conclusion