ABSTRACT
To improve the solubility and antitumor activity of ampelopsin, ampelopsin-loaded nanomicelles from the mixture of pluronic F127 and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS1000) were prepared by film-thin hydration method, in order to optimize the process conditions and physicochemical properties. The antitumor activities against MCF-7 cells between ampelopsin and nanomicelles were compared by MTT method, respectively. The results showed that the optimal nanomicelles were round with the nanometric size of (22.6±0.5) nm, encapsulation efficiency rate of (80.42±1.13)%, and drug-loading rate of (4.41±0.26)%. The solubility of ampelopsin in mixed nanomicelles significantly increased by 16 times. In different release media, the mixed nanomicelles could release more than 90% of drug in 8 h, and showed stronger cytotoxicity and inhibition against MCF-7 cells (P<0.01). The mixed nanomicelles can be used as new drug delivery system of ampelopsin.
ABSTRACT
OBJECTIVE: To examine the effects of TPGS 1000 and Soluplus on the transport of ginsenoside CK in Caco-2 cell model. METHODS: The effects of TPGS 1000 and Soluplus at different concentrations on ginsenoside CK were evaluated by using Caco-2 cell model. The concentration of ginsenoside CK in cell was examined by ultra high pressure liquid chromatography (UPLC) method. The apparent permeability coefficient (Papp) and the efflux ratio were calculated. RESULTS: When the proportion of ginsenoside CK to TPGS 1000 or Soluplus was 1:1, 1:3, and 1:9, the absorption of ginsenoside CK significantly increased. The efflux and efflux ratio both decreased significantly (P<0.05). TPGS 1000 had more significant promotion effect on the transport of ginsenoside CK than the same dose of soluplus at the same ratio (P<0.05). CONCLUSION: In Caco-2 cell model, both TPGS 1000 and Soluplus can significantly promote the absorption of ginsenoside CK.