Structural effects on cosolubilization of dendrimer and propofol in water dilutable microemulsions as delivery vehicle

Abstract

In this study we characterized a new and improved transport vehicle for 2,6-diisopropylphenol (propofol), a hydrophobic anesthesia drug, in the absence and presence of dendrimers being a transporting agents across cells, polypropylenimine (PPI) dendrimer generation 2 (PPI-G2) into a microemulsion (ME). Three unique systems of water-dilutable compositions capable of inverting from W/O to bicontinuous and to O/W structures upon water dilutions were studied by means of electrical conductivity, electron paramagnetic resonance (EPR), and self-diffusion nuclear magnetic resonance (SD-NMR). The microviscosity, as well as the order parameter (from EPR results) increase with the increase in the dendrimer content, while inverting the structures from W/O to bicontinuous ME. Inversion from the bicontinuous mesophase to the O/W nanodroplets caused a very minor increase in the order parameter. Self-diffusion NMR measurements provided information on the diffusivity and the interactions of the different components of the ME. It was found that propofol has no effect on the diffusivity of the components since it is embedded within the core of the ME droplets. However, the dendrimer increases the diffusivity of water. In addition, we learned that at high dendrimer content, it remains solubilized; however its location at the ME/water interface moves to the water continuous phase. The study demonstrates the ability of water dilutable MEs to act as drug carriers hosting both propofol and dendrimer.