[Preparation and characterization of cucurbitacin B sodium deoxycholate/phospholipid-mixed oral fast dissolving film and antitumor activity study].

A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance.Encapsulation efficiency,particle size,zeta potential,polydispersity coefficient,investigated the morphology,disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate /phospholipid-mixed micelles before and after solidified in mice were evaluated and compared.The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s.It could meet the requirements of rapidly disintegrating fully.The encapsulation efficiency,particle size,zeta potential,polydispersity coefficient of cucurbitacin B sodium deoxycholate /phospholipid-mixed micelles loaded in oral fast dissolving film were(43.36 ± 2.12)%,(108.82 ± 5.2) nm,(- 34.18 ± 1.07) mV,0.088 ± 0.012,respectively.The encapsulation efficiency,particle size,zeta potential,polydispersity coefficient of cucurbitacin B sodium deoxycholate /phospholipid-mixed micelles in solution were(41.26 ± 2.22)%,(181.82 ± 4.48) nm,(- 30.67 ± 0.81) mV,0.092 ± 0.012,respectively.The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles,cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared.Solubility of cucurbitacin B loaded in sodium deoxycholate /phospholipid-mixed micelles has also been greatly improved.The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate /phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified.These showed that the sodium deoxycholate /phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate /phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.