PURPOSE: A Central Composite Rotatable Design (CCRD) of Response Surface Methodology (RSM) was used purposely to optimize process parameters conditions for formulating nanoemulsion containing aripiprazole using high emulsification methods.
METHODS: This design is used to investigate the influences of four independent variables (overhead stirring time (A), shear rate (B), shear time (C), and the cycle of high-pressure homogenizer (D)) on the response variable namely, a droplet size (Y) of nanoemulsion containing aripiprazole.
RESULTS: The optimum conditions suggested by the predicted model were: 120 min of overhead stirring time, 15 min of high shear homogenizer time, 4400 rpm of high shear homogenizer rate and 11 cycles of high-pressure homogenizer, giving a desirable droplet size of nanoemulsion containing aripiprazole of 64.52 nm for experimental value and 62.59 nm for predicted value. The analysis of variance (ANOVA) showed the quadratic polynomial fitted the experimental values with F-value (9.53), a low p-value (0.0003) and a non-significant lack of-fit. It proved that the models were adequate to predict the relevance response. The optimized formulation with a viscosity value of 3.72 mPa.s and pH value of 7.4 showed good osmolality value (297 mOsm/kg) and remained stable for three months in three different temperatures (4°C, 25°C, and 45°C).
CONCLUSION: This proven that response surface methodology is an efficient tool to produce desirable droplet size of nanoemulsion containing aripiprazole for parenteral delivery application.
Methods: The designed anti-tuberculosis nanodelivery composite, MgLH-PAS, was prepared by a novel co-precipitation method using MgNO3 as well MgO as starting materials.
Results: The designed nano-formulation, PAS-MgLH, showed good antimycobacterial and antimicrobial activities with significant synergistic anti-inflammatory effects on the suppression of lipopolysaccharide (LPS) stimulated inflammatory mediators in RAW 264.7 macrophages. The designed nano-formulation was also found to be biocompatible with human normal lung cells (MRC-5) and 3T3 fibroblast cells. Furthermore, the in vitro release of PAS from PAS-MgLH was found to be sustained in human body simulated phosphate buffer saline (PBS) solutions of pH 7.4 and pH 4.8.
Discussion: The results of the present study are highly encouraging for further in vivo studies. This new nanodelivery system, MgLH, can be exploited in the delivery of other drugs and in numerous other biomedical applications as well.
Methods: The nanoparticles were characterized by X-ray diffraction (XRD) analysis, field emission scanning electron microscopy, energy dispersive X-ray fluorescence, transmission electron microscopy (TEM), vibrating sample magnetometry (VSM) and Fourier transform infrared spectroscopy.
Results: The XRD analysis indicated the presence of pure Fe3O4-NPs while the TEM images indicated that the Fe3O4-NPs are spherical with a diameter range between 3.21 and 2.22 nm. The VSM study demonstrated that the magnetic properties were enhanced with the decrease in the percentage of honey. In vitro viability evaluation of Fe3O4-NPs performed by using the MTT assay on the WEHI164 cells demonstrated no significant toxicity in higher concentration up to 140.0 ppm, which allows them to be used in some biological applications such as drug delivery.
Conclusion: The presented synthesis method can be used for the controlled synthesis of Fe3O4-NPs, which could be found to be important in applications in biotechnology, biosensor and biomedicine, magnetic resonance imaging and catalysis.