ABSTRACT
OBJECTIVE: The objective of the present investigation was to develop a stable and optimized drug-loaded nanoemulsion system using the phase inversion temperature (PIT) method. SIGNIFICANCE: The PIT method has been widely used for the development of food-grade nanoemulsion systems. For the first time, a simple and cost-effective, PIT method was used for the development of a stable drug-loaded nanoemulsion system. METHODS: Box-Behnken experimental design was used for the development of an optimized drug-loaded nanoemulsion system by the PIT method. The independent variables were optimized for responses by using the desirability function. The hydrophobic drug, benidipine was used as a modal drug. Optimized oil phase (blend of long-chain triglycerides oil, medium-chain triglycerides oil and essential oil) was used for the development of oil in water (O/W) nanoemulsion system. RESULTS: Optimum nanoemulsion formulation was stable, transparent and contained 50% of oil to surfactant percentage with a droplet size of 96.57 ± 1.61 nm. The optimum formulation also showed higher in-vitro drug diffusion from dialysis membrane as compared to the marketed formulation. Nanoemulsion droplets were observed as spherical in the transmission electron microscopy (TEM) images. Box-Behnken statistical analysis revealed that all the independent variables had a significant impact on characteristics of nanoemulsion and the predicated value of independent variables was found to be valid. CONCLUSION: It was concluded that the PIT method produces a stable and efficient drug-loaded nanoemulsion system. Further, the optimized oil phase can be used as an alternative to costly, commercial medium-chain triglycerides (MCT) oils, for the development of a stable nanoemulsion system.
Subject(s)
Oils, Volatile , Research Design , Emulsions , Particle Size , TemperatureABSTRACT
Nanoemulsion drug delivery systems are advanced modes for delivering and improving the bioavailability of hydrophobic drugs and the drug which have high first pass metabolism. The nanoemulsion can be prepared by both high energy and low energy methods. High energy method includes high-pressure homogenization, microfluidization, and ultrasonication whereas low energy methods include the phase inversion emulsification method and the self-nanoemulsification method. Low energy methods should be preferred over high energy methods as these methods require less energy, so are more efficient and do not require any sophisticated instruments. However high energy methods are more favorable for food grade emulsion as they require lower quantities of surfactant than low energy methods. Techniques for formulation of nanoemulsion drug delivery system are overlapping in nature, especially in the case of low energy methods. In this review, we have classified different methods for formulation of nanoemulsion systems based on energy requirements, nature of phase inversion, and self-emulsification.
