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.

Background: Nanoparticles made of biodegradable polymers are the most effective colloidal drug delivery systems. The in vitro characteristics as well as in vivo presentation of these nanoparticles are majorly influenced by their formulation parameters. Objectives: The principle objective of the work was to optimize various critical formulation parameters by using statistical tools in order to develop poly (lactide-co-glycolide) (PLGA) nanocapsules loaded with tenofovir disoproxil fumarate (TDF) with effective characteristic properties. Methodology: In this work, biodegradable nanocapsules with PLGA for TDF were prepared by modified double emulsification technique. Concentration of PLGA, concentration of Pluronic F-68 in secondary emulsion and concentration of glycerol in external phase were selected as the formulation factors hence, a 3 3 full factorial design in response surface methodology was chosen as an experimental design. The prepared nanocapsules were evaluated for various characteristic properties like particle size, surface morphology, entrapment efficiency, drug release studies and DSC studies. The selected formulation parameters were optimized by a mathematical model called desirability functions approach with the set desirability of high entrapment efficiency, low drug release constant and less particle size. Results and Conclusion: Particle size, entrapment efficiency and drug release constant were found in the ranges of 249.3-376.3nm, 20.95-71.35% and 0.039-0.184 hr -1 . These selected formulation parameters were found to have significant (at p < 0.05 by ANOVA) influence on various characteristics of prepared nanocapsules. The optimized formulation found to have 63.08% of entrapment efficiency, 284.53 nm of particle size with zeta potential of -26.1 mV and 0.054 h -1 of release rate constant.

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