Honokiol (HK), a well-tolerated natural product, has many multiple pharmacological activities. However, its poor water solubility and low bioavailability limit its clinical application and development. The aim of this research was to prepare the solid dispersion (SD) formulation of honokiol (HK) with poloxamer-188 (PLX) as the carrier, thereby improving its solubility and oral bioavailability. Firstly, by investigating the relationship between the addition amount of the PLX and the solubility of HK, and the effects of solid dispersions with different ratios of HK–PLX on the solubility of HK, we determined that the optimum ratio of PLX to HK was (1:4). Then, the HK–PLX (1:4) SD of HK was prepared using the solvent evaporation method. The morphology of the obtained HK–PLX (1:4) SD was different from that of free HK. The HK in the HK–PLX (1:4) SD existed in amorphous form and formed intermolecular hydrogen bonds with PLX. Additionally, the solubility values of the HK–PLX (1:4) SD were about 32.43 ± 0.36 mg/mL and 34.41 ± 0.38 mg/mL in artificial gastric juice (AGJ) and in artificial intestinal juice (AIJ), respectively. Compared with free HK, the release rate and the bioavailability was also substantially improved for HK in its SD form. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay indicated that the HK–PLX (1:4) SD showed higher inhibition of HepG2 cells than free HK. Taken together, the present study suggests that the HK–PLX (1:4) SD could become a new oral drug formulation with high bioavailability and could produce a better response for clinical applications of HK.
This study was designed to evaluate the radioprotective effect of phenolics extracted from the fruits of Malus baccata (Linn.) Borkh. (MBP-3b) against damage induced by 60Co γ-irradiation in vivo. MBP-3b could significantly improve the activity of endogenous antioxidant enzymes and the T-AOC, as well as reduce the MDA level in the liver and kidneys of irradiated mice. In addition, pretreatment with MBP-3b at a dose of 150 mg per kg bw could significantly enhance immunomodulation activity by promoting the proliferation of spenocytes and monocyte phagocytosis. The administration of MBP-3b prevented the decline induced by radiation of haematological parameters (WBC, RBC, PLT and HGB). Furthermore, MBP-3b could protect spenocytes from radiation-induced damage by inhibiting cell apoptosis. The results indicated that MBP-3b possesses strong whole body radioprotective and immunomodulatory activities. The main constituents of MBP-3b were tentatively identified as delphinidin-3,5-diglucoside, cyanidin-3-glucoside, chlorogenic acid, proanthocyanidin C1, quercetin-3-galactoside, quercetin-3-glucoside, quercetin-3-xyloside/arabinoside, phloretin-2-xyloseglucoside, quercetin-3-rhamnoside and phlorizin. MBP-3b could be used as a probable radioprotector against gamma radiation induced oxidative damage.