ABSTRACT
OBJECTIVE: To investigate the antitumor effect of 16-dehydropregnenolone (16-DHP) liposomes. METHODS: Twelve kinds of tumor cells were used to determine the cytotoxic effect of 16-DHP liposome by MTT assay. The established tumor xenograft in nude mouse model was used to evaluate anti-tumor effect of 16-DHP liposomes after tail vein injection. RESULTS: IC50 value of 16-DHP liposomes to the human hepatoma cell HepG2, human oral carcinoma KB cell, human breast cancer T47D, human gastric cancer cell SGC7901, human fibrosarcoma cell HT1080, human ovarian cancer cell SKOV3, human prostate cancer cell PC3, human prostrate cancer cell DU145, human lung cancer cell A549, human rhabdomyosarcoma A204 cell and human cervical carcinoma cell HeLa were 44.69, 9.17, 26.22, 19.58, 28.01, 37.18, 24.58, 21.38, 54.69, 4.18 and 8.96 μg · mL-1, respectively. The relative tumor increment rate and inhibition rates of tumor weight were 93.7%, 60.52%, 37.84% and 23.05%, 48.84%, 69.70% respectively after treated with 16-DHP liposomes (7.5, 15 and 30 mg · kg-1 · d-1, 28 d). CONCLUSION: 16-DHP liposomes possess in vitro and in vivo anti-tumor activities.
ABSTRACT
Objective To optimize preparation of freeze-dried 16-dehydropregnenolone (16-DHP) liposome and evalu-ate the quality. Methods The freeze-dried liposome was prepared by rotary-evaporated film-ultrasonication with lyophilization. Single factor experiments and orthogonal design were used to optimize the prescription and preparation,and the quality was evalua-ted. Results The optimum preparation technics were as follows: the concentration of PC-98T was 6. 5% (W/ V), the quantity ratio of PC-98T to cholesteryl sodium sulfate salt was 4∶1,hydration temperature was 60 ℃ , ultrasonic time was 2 min,and the cryoprotectant was 7. 5% glucose. The average particle size, Zeta potential and encapsulation efficiency were (121. 3±48. 7) nm,-41. 9 mV and (98. 7±0. 1)% , respectively. Conclusion The formulation of freeze-dried 16-DHP liposome is reasonable, the technology is practicable and stable.
ABSTRACT
The pharmacokinetics of 16-dehydropregnenolone （16-DHP）, a sterols compound isolated from Solanum lyratum Thunb., was investigated in rats following a single intramuscular administration （40 mg/kg）. The concentration of 16-DHP in rat plasma was determined by a high performance liquid chromatography （HPLC） method with UV detection. Levonorgestrel was used as the internal standard （IS）. The pharmacokinetic parameters of 16-DHP were derived by non-compartmental method. After a single intramuscular administration, the maximum plasma concentration （Cmax） was （289±25）ng/mL, time to reach Cmax（tmax） was （0.38±0.14） h, the elimination half-life （t1/z） was （2.5±1.1）h, the area under the plasma concentration-time curve from time zero to the time of the last measurable concentration （AUC（0-t）） was （544± 73）ng· h/mL. The results indicated that 16-DHP was absorbed quickly and eliminated rapidly in rats after the intramuscular injection.
ABSTRACT
The pharmacokinetics of 16-dehydropregnenolone (16-DHP),a sterols compound isolated from Solanum lyratum Thunb.,was investigated in rats following a single intramuscular administration (40 mg/kg).The concentration of 16-DHP in rat plasma was determined by a high performance liquid chromatography (HPLC) method with UV detection.Levonorgestrel was used as the internal standard (IS).The pharmacokinetic parameters of 16-DHP were derived by non-compartmental method.After a single intramuscular administration,the maximum plasma concentration (Cmax,) was (289 ±25)ng/mL,time to reach Cmax(tmax) was (0.38±0.14) h,the elimination half-life (t1/2) was (2.5±1.1)h,the area under the plasma concentration-time curve from time zero to the time of the last measurable concentration (AUC10-t)) was (544 ± 73 )ng· h/mL.The results indicated that 16-DHP was alsorbed quickly and eliminated rapidly in rats after the intramuscular injection.