Preparation Of Proanthocyanidins Nanoemulsion

In this research, the proanthocyanidins nanoemulsion was prepared by nanotechnology, and its quality stability, security, release properties and pharmacodynamics were systemically studied. The study includes five parts, and the abstracts are as follows:Part 1: Study on the blank nanoemulsion carriers.The AEO-7, PEG400MS, LAE-9 ,EL-40,EL-35 and APG were used as surfactant,the glycerine,synth eticnbutyl alcohol and 1,3-butyleneglycol were used as cosurfactant, the isopropyl myristate and Mineral oil were used as oil. The formulations of the nanoemulsion was optimized by studying the pseudotertiary phase diagrams, the factors of influencing nanoemulsion formation were investingated such surfactant, cossurfactant, oil,etc. Stability of nanoemulsion were studied. The experimental results indicated the formation of nanoemulsion was dependent on the HLB values of surfactants ,the nature of oils and cosurfactants ,the weight ratio of surfactant to cosurfactant and the type of additives in the water phase. The four nanoemulsions systems of AEO-7/IPM/water,EL-40/IPM/water,EL-35/span80/IPM/water and EL-40/span80/IPM/Mineral oil/water were limpidity and stability.The average diameter of the sample was below 100nm, The Drop shape and particle size were investigated by transmission electron microscope. which accorded with that of nanoemulsion.Part 2: The preparation and quality evaluation on proanthocyanidins nanoemulsionThe formulations of the proanthocyanidins nanoemulsion was optimized by studying the pseudotertiary phase diagrams, the effect of various elements on the formation of the nanoemulsiom was investigated. Stability of proanthocyanidins nanoemulsiom were studied. The Ultraviolet absorption wavelength, standard curve, recovery and accuracy were studied by Ultraviolet spectrophotometer. The optimization of formulation was EL-35/span80/IPM/Mineral oil/water nanoemulsion system. Proanthocyanidins nanoemulsiom was limpidity and very stable after three months storage. Electron microscopy presented of the proanthocyanidins nanoemulsiom as small spherical drops with a diameter between 1~100nm, which accorded with that of nanoemulsion. The proanthocyanidins has the maximal absorption in 550nm. The good linear range was 30～350μg/mL,r=0. 9996.The average recovery is 99.32%.and the RSD is 2.31%. So, the proanthocyanidins nanoemulsion prepared was stable and the means of UV spectrophotometry established was equal to analyse the content of proanthocyanidins.Part 3: Study on the transdermal speed of proanthocyanidins nanoemulsion in vitro by TT-6(B) pervasion pool.With proanthocyanidins aqueous solution as positive controls. Proanthocyanidins was determined by Ultraviolet spectrophotometer. The result showed that the average transdermal speed of proanthocyanidins aqueous solution, proanthocyanidins nanoemulsion were 174.6μg﹒cm-2﹒h-1 and 207.59μg﹒cm-2﹒h-1.So, compared to proanthocyanidins aqueous solution, proanthocyanidins nanoemulsion has the faster transdermal speed. It was proper to be used as a transdermal preparation.Part 4: The safety evaluation on proanthocyanidins nanoemulsionThe safety of proanthocyanidins nanoemulsion were evaluated by cell toxicity experiment, skin irritation experiment, eye irritation experiment and skin allergy experiment,. The result showed that the cell toxicity was smaller than 2 level, not obvious toxicity; the stimulation to the party of rabbit's skin and eye are all non-toxic, no skin allergy response . The proanthocyanidins nanoemulsion is nontoxic to skin of domestic rabbit, eye and cell. The proanthocyanidins nanoemulsion was safe.Part 5:Proanthocyanidins nanoemulsion protect against UVR damage in mice skin.Healthy mice were divivded into four groups randomly and gavages respectively ,those were negative control group , model group , proanthocyanidins nanoemulsion group and VC group .except negative group ,the others were irradiated . the activity of Superoxide Dismutase (SOD) and the contents of Malondialdehyde (MDA) in mice skin were measured by biochemical test method in each group of the experiment. The result showed that,in model group ,the activity of SOD was descreased ,while the content of the MDA was increased seriously(p<0.05). Compared with the model group ,the content of MDA was reduced in proanthocyanidins nanoemulsion group and in VC group ( p<0.05), the activity of SOD was increased in proanthocyanidins nanoemulsion group and in in VC group(p<0.05).The activity of SOD and content of MDA in proanthocyanidins nanoemulsion group had no difference with that in in VC group.So , proanthocyanidins nanoemulsion could eliminate free radicals itself; on the other hand ,by increasing the activity of SOD ,it could inhibit the oxidative damages of ultraviolet .