| Phloretin is one kind of natural flavonoid compounds, which mainly presents in peels of apples, pears and other fruits or juices of vegetables. It is a potential anti-cancer drug with pharmacological effects of antioxidant, anti-inflammatory, anti-cancer, anti-cardiovascular disease. In addition, as a natural whitening agent, it can lighten skin spots, and can be used in all types of cosmetics. However, its applications are vastly limited because of hydrophobicity and low bioavailability. One of the applications problem is how t o improve water-solubility of phloretin to enhance its bioavailability. Water-soluble phloretin was produced with carriers of PVP K-30 and HP-β-CD, and its physicochemical property, biological actvity and intracorporal metabolism were explored in the paper.Firstly, PVP K-30, HP-β-CD as carriers to prepare water-soluble phloretin by using solid dispersion technology and packing technology. Drug Loading and solubility of watersoluble phloretin were respectively measured by UV and HPLC. The results showed that the drug loading of phloretin- PVP K-30 was 95.99% and the solubility was 0.42 mg?mL-1 when mass ratio of phloretin and PVP K-30 was 1:9, the solubility increased by 14 times compared to raw material of phloretin; the drug loading of phloretin- HP-β-CD was 95.99% and the solubility was 3.01mg?mL-1 when molar ratio of phloretin and HP-β-CD was 1: 1, the solubility increased by 100 times compared to the reference.Secondly, water-soluble phloretin was characterized by DSC, XRD and FT-IR. The result showed that phloretin was probably bonded with carrier material by hydrogen and uniformly dispersed in the carrier material by molecular or amorphous. In addition, influence factors of stability of water-soluble phloretin were investigated, such as light, temperature, pH-value and other factors. Result showed that phloretin was prone to degradation in the sunlight, high temperature, alkaline conditions. The stability was significantly improved when phloretin was prepared into water-soluble phloretin.Finally, we studied pharmacokinetic and anti-inflammatory activity of water-soluble phloretin. We established method of pretreatment of phloretin plasma samples by means of liquid-liquid extraction and method of determination ofblood concentration by means of HPLC. The Study showed that the relative bioavailability of phloretin-PVP K-30 increased sequentially from low density to high density, up to 1.97; the relative bioavailability of phloretin-HP-β-CD is better when it has a low concentration, and the relative bioavailability is 4.97. This showed that Phloretin-PVP K-30 and phloretin-HP-β-CD both could be used to improve the bioavailability of phloretin, but phloretin-HP-β-CD was significantly better than phloretin-PVP K-30. Then TPA was used to induce mouse suffering ear edema to measure anti- inflammatory activity of water-soluble phloretin. Findings showed that significant inhibitory activity of phloretin-PVP K-30(inhibition rate was 53.24%) and phloretin-HP-β-CD(inhibition rate was 59.56%) compared to phloretin(inhibition rate was 18.09%), which indicated that water-soluble phloretin can significantly improve the anti-inflammatory activity of phloretin with a high bioavailability.In conclusion, the water-soluble phloretin not only can effectively improve the solubility and stability of phloretin, but also enhance the bioavailability and anti-inflammatory effects of phloretin, which provided a theoretical basis to the application of phloretin.
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