ABSTRACT
Chemotherapy outcomes for the treatment of glioma remains unsatisfactory due to the inefficient drug transport across the blood-brain barrier (BBB) and insufficient drug accumulation in the tumor region. Although many approaches, including various nanosystems, have been developed to promote the distribution of chemotherapeutics in the brain tumor, the delivery efficiency and the possible damage to the normal brain function still greatly restrict the clinical application of the nanocarriers. Therefore, it is urgent and necessary to discover more safe and effective BBB penetration and glioma-targeting strategies. In the present study, menthol, one of the strongest BBB penetration enhancers screened from traditional Chinese medicine, was conjugated to casein, a natural food protein with brain targeting capability. Then the conjugate self-assembled into the nanoparticles to load anti-cancer drugs. The nanoparticles were characterized to have appropriate size, spheroid shape and high loading drug capacity. Tumor spheroid penetration experiments demonstrated that penetration ability of menthol-modified casein nanoparticles (M-CA-NP) into the tumor were much deeper than that of unmodified nanoparticles. imaging further verified that M-CA-NPs exhibited higher brain tumor distribution than unmodified nanoparticles. The median survival time of glioma-bearing mice treated with HCPT-M-CA-NPs was significantly prolonged than those treated with free HCPT or HCPT-CA-NPs. HE staining of the organs indicated the safety of the nanoparticles. Therefore, the study combined the advantages of traditional Chinese medicine strategy with modern delivery technology for brain targeting, and provide a safe and effective approach for glioma therapy.
ABSTRACT
AIM: To establish the quality standard for Qidan Granules(Radix et Rhizoma Salviae Miltiorrhizae,Radix Astragali,Myrrha,Rhizoma Curcumae;Faeces Togopteri). METHODS: Myrrh,Rhizoma Curcumae and Faeces Trogopteri in Qidan Granules were identified by TLC.The content of tanshinone Ⅱ_A was determined by HPLC.The astragaloside content was determined by HPLC-ELSD. RESULTS: Myrrh,Rhizoma Curcumae and Faeces Trogopteri could be identified by TLC.There was a good linear relationship between the peak area and quantity of tanshinone Ⅱ_A at the range of 2.98-953.6 ng,r=0.999 9,and the recovery was 100.6%,RSD was(0.5%.) Also,there was a good natural logarithm linear relationship between the peak area and quantity of astragaloside at the range of 2.05-40.92 ?g,r=0.999 8,and the recovery was 102.0%,RSD was 1.8%.(CONCLUSION:) The method can be used to set up the quality standard for Qidan Granules.
ABSTRACT
AIM:To develop the method for analyzing bulleyacinitine A in plasm from mice through the treatment of subcutaneous injection of bulleyacinitine A by liquid chromatography tandem mass spectrometry(LC-MS/MS).METHODS:50 ?L mouse plasma sample added zolpidem as internal standard and pH 9.2 buffer solution was extracted with ethylether,followed by liquid chromatography and mass spectrometric detection.The mobile phase was consisted of methanol-buffer solution(85∶15)(buffer solution consisted of 20 mmol/L ammonium acetate and 0.1% formic solution).The flow rate was 300 ?L per minute.The separation column was C_ 18 column.The electrospray ionization tandem mass spectrometry and the multiple reaction monitoring mode were applied to detecting the bulleyacinitine A in plasma.RESULTS:The assay was linear from 0.1 to 1 000 ng/mL.The recovery rate was more than 80%.CONCLUSION:The method could be used to detect bulleyacinitine A level in mouse plasma,which offers advantages of sensitiveness,specificity and simpleness.
ABSTRACT
AIM:To establish a method of determining the entrapment efficiency of bulleyaconitine A multivesicular liposomes.METHODS:Bulleyaconitine multivesicular liposomes and its free bulleyaconitine were separated by centrifugalization.To calculate the entrapment efficiency,total and free bulleyaconitine were assayed by HPLC.RESULTS:At low speed,the rate of rotation did not affect the determination of entrapment efficiency.The average entrapment efficiency of three lot samples was 87.12%.CONCLUSION:Entrapment efficiency of bulleyaconitine multivesicular liposomes could be evaluated simply and quickly by centrifugalization.