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摘要
The purpose of this study was to develop a new delivery system based on drug cyclodextrin (CD) complexation and loading into nanostructurecl lipid carriers (NEC) to improve the oral bioavailability of vinpocetine (VP). Three different CDs and three different methods to obtain solid vinpocetine-cyclodextrin-tartaric acid complexes (VP-CD-TA) were contrasted. The co-evaporation vinpocetine-beta-cyclodextrin-tartaric acid loaded NLC (VP-beta-CD-TA COE-loaded NLC) was obtained by emulsification ultrasonic dispersion method. VP-beta-CD-TA COP-loaded NLC was suitably characterized for particle size, polydispersity index, zeta potential, entrapment efficiency and the morphology. The crystallization of drug in VP-CD-TA and NLC was investigated by differential scanning calorimetry (DSC). The in vitro release study was carried out at pH 1.2, pH 6.8 and pH 74 medium. New Zealand rabbits were applied to investigate the pharmacokinetic behavior in vivo. The VP-beta-CD-TA COE-loaded NLC presented a superior physicochemical property and selected to further study. In the in vitro release study, VP -beta-CD TA COE-loaded NEC exhibited a higher dissolution rate in the pH 6.8 and pH 7.4 medium than VP suspension and VP-NLC. The relative bioavailability of VP- beta-CD-TA COE-loaded NLC was 592% compared with VP suspension and 92% higher than VP-NLC. In conclusion, the new formulation significantly improved bioavailability of VP for oral delivery, demonstrated a perspective way for oral delivery of poorly water-soluble drugs.
- 出版日期2014-4-25
- 单位沈阳药科大学; 辽宁科技学院
