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

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.

Formulation and in vitro evaluation of topical nanosponge-based gel containing butenafine for the treatment of fungal skin infection

“…Amount of the drug entrapped was found to be increased with the higher particle size and EC polymer concentration. In contrast, less particle size would be responsible for low entrapment efficiency, as the small particles could have more surface area to give more prospect for drug escape from the porous nanocage ( Srikar and Rani, 2019 ). BTF being water insoluble drug that enforce its maximum entrapment in nanocarriers.…”

New Silver(I) Coordination Compound Loaded into Polymeric Nanoparticles as a Strategy to Improve In Vitro Anti-Helicobacter pylori Activity

“…In addition, the hydrophobicity of the polymer further influences this trapping. As pointed out by Srikar and Rani, the higher the hydrophobicity of the polymer, the greater the amount of drug trapped and the lower its release from the polymeric system, thus allowing higher EE values.…”

“…To determine the EE, the methodologies of Abriata et al . and Srikar and Rani were used with modifications. PN1 was centrifuged in Amicon Ultra Centrifugal Filters with a molecular weight cutoff (MWCO) of 50 kDa (Merck, Darmstadt, Germany) for 20 min at 3600 rpm using an Excelsa II, Mod.…”

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“…Polymer hydrophobicity can also influence the entrapment efficiency since the encapsulating material is highly hydrophobic; it hampers the encapsulated active molecule’s escape to the aqueous phase, achieving a low efficiency [ 190 ]. The opposite is observed when the entrapped molecule presents higher solubility in the continuous phase than in the dispersed phase, leading to an easy diffusion and good encapsulation efficiency [ 189 ].…”