ABSTRACT
Objective To investigate the efficacy and safety of HCPT combined with 5-fluorouracil(5-Fu) in treatment of bladder cancer .Methods Selected 92 patients with advanced bladder cancer in our hospi-tal from February 2011 to August 2015 , equally divided into observation group and control group of 46 patients based on the random number table ,the control group were received 5-Fu intravesical chemotherapy ,The obser-vation group were given the HCPT combined with 5-Fu chemotherapy ,the chemotherapy infusion were once a week,continuous perfusion were observed for 3 months.Results The response rates in the observation group was 95.7%and the control group was 76.1%,the observation group were significantly higher than the control group (P0.05),all adverse reactions after symptomatic treatment were improved .All patients were followed up for 1 year,The mortality and recurrence rates in the observation group were 8.7%and 4.3%re-spectively,while the control group were 30.4%and 17.4%,the mortality and recurrence rates of the observation group were significantly lower than the control group (P<0.05).Conclusion HCPT combined with 5 -Fu chemotherapy for bladder cancer has strong anti -cancer effect and without increase the incidence of adverse re-actions,it can promote the improvement of the long -term prognosis,so it is a safe and effective topical bladder chemotherapy drugs .
ABSTRACT
OBJECTIVE: To establish an HPLC method for determing irinotecan (CPT-11) and its metabolite 7-ethyl-10 HCPT in rat liver microsome incubation system, and to optimize the incubation conditions. METHODS: CPT-11and SN-38 were determined by HPLC. Single factor design was used to optimize the incubation conditions. RESULTS: The linear range of CPT-11 and 7-ethyl-10 HCPT in rat liver microsome incubation system were 20-4000 ng · mL-1 and 2-400 ng · mL-1, respectively. The optimal incubation conditions were as follows: 10 μmol · L-1 CPT-11, 0.02 mg liver microsomes and incubation for 15 min. CONCLUSION: The HPLC method is accurate and suitable for the determination of CPT-11and 7-ethyl-10 HCPT in rat liver microsomes. The incubation condition can be applied in drug interaction studies of irinotecan.
ABSTRACT
OBJECTIVE: To synthesize a new drug delivery system of polyaldehyde Dex coupled with SA-10-HCPT and to study the HCPT release in vitro and the anti-tumor activity in vivo. METHODS: The new drug delivery system was prepared by polyaldehyde Dex coupled with SA-HCPT, grafted with mPEG-adipic dihydrazide monohydrazone and cross-linked with adipic dihydrazide. RESULTS: The conjugate formed micelle with a diameter of 100 nm in water,which could achieve passive targeting of tumor tissue concentration. The drug loading efficiency achieved 5.63%. The drug release processes accorded with kinetic equation Rc=Atn1/(B+Ctn2) in the buffer solution. The release rate of HCPT from this conjugate in pH 5.4 buffer was much higher than that in the environment of pH 7.4 and pH 4.5. The tumor inhibition of the conjugate was similar to that of HCPT while the toxicity in vivo was significantly reduced. CONCLUSION: The structure of the conjugate is unstable in acidic environment, and the drug is released pH-sensitively. The mice survival rate is significantly improved because of the significant slow-release property. Therefore, the conjugate can be developed as a novel prodrug.
ABSTRACT
Objective: To prepare microcapsules for controlled release of 10-hydroxycamptothecin (HCPT), and determine its encapsulation efficiency and drug release profile in vitro. Methods: The microcapsules loaded with HCPT were prepared using a novel coating technology based on the layer-by-layer (LBL) deposition of oppositely charged polylysine (PLL) and alginate (ALG) polyelectrolytes with good biocompatibility onto microcrystal templates. Results: The microcapsules fabricated by this method had visible core-shell structure observed by scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM); The entrapment efficiency of the microcapsules was as high as (68.41 ± 0.72)%; The release rate of HCPT decreased as the bilayers increased in vitro. Conclusion: The microcapsules of HCPT prepared by LBL have higher entrapment efficiency and are characterized with controlled drug release, which has potential for future application.
ABSTRACT
0.05). No significant differences were detected in the median time of remission, median survival time and 1-, 2-year survival rates between the groups. Moreover, no significant differences were detected in the grade Ⅲ～Ⅳ leukopenia, grade Ⅲ～Ⅳ thrombocytopenia, grade Ⅲ～Ⅳ nausea and vomiting and grade Ⅲ～Ⅳ constipation between the groups. Conclusions:The response rate of the MVP regimen is slightly lower than the HMVP regimen, but the HMVP regimen is not noticeably superior. It may increase the toxicity such as leukopenia, nausea/vomiting and constipation, as wellas being more expensive. In short, MVP regimen should be selected between the regimens in the chemotherapy of advanced NSCLC.
ABSTRACT
Objective:The therapeutic efficacy and side effects of combined chemotherapy of HCPT,MTX,LV and 5-Fu for metastatic or recurrent breast cancer were evaluated in our study.Methods:A total of 43 cases of advanced metastatic or recurrent breast cancer were treated with chemotherapy regimen consisting of HCPT 10mg/m2 iv gtt for dl～5,MTX 100mg iv dl,Leucovorin 150mg/m2 iv gtt for d2～4,5-Fu 500mg/m2 iv gtt for dl～5.The cycle was repeated every 4 weeks,and 2 cycles were given as one course.Results:The overall CR+PR was 47%.One year survival rate was 54% and the median survival interval was 19 months.The main side effects were bone marrow suppression and gastrointestinal reaction.Conclusion:The combined chemotherapy regimen consisting of HCPT etc is beneficial for metastatic breast cancer.
ABSTRACT
Objective To observe the short-term efficacy and toxicity of HEPP regimen in treatment of refractory Non-Hodgkin's Lymphoma. Methods HEPP regimen: HCPT 8 mg/m2 iv gtt d1~ d5, VP16 100 mg/d iv gtt d1~d5, PDD 20 mg/d iv gtt d1~d5, PDN 60 mg/m2 po d1~d14. The chemotherapy was repeated every 4 weeks as a cycle.The clinical effect was evaluated after 2 cycles and toxicity was observed during every cycle. Results 25 patients were eligible for toxicity evaluation and 22 patients for clinical response evaluation. The objective response rate was 60.0 %, including three cases complete remission and ten cases partial remission. Six cases achieved stable disease and three cases progressive disease. The major toxicity was bone marrow suppression, including 24.0 % grade Ⅲ/Ⅳ leukopenia and 12.0 % grade Ⅲ/Ⅳ thrombocytopenia. The incidence of nausea/vomiting, mucositis and hepatic toxicity was low. Conclusion HEPP regimen can achieve a satisfy result in the treatment of refractory Non-Hodgkin's Lymphoma. It is low toxic and well tolerated.
ABSTRACT
Purpose:To evaluate the different concentration of HCPT in rabbit blood and bladder tissue between intraarterial and intravenous penfusion groups.To indentify the probability of using HCPT as a new type of anti-tumor agent delivered by the intra-arterial pesfusion method for the treating of bladder cancer.Materials and methods:Group A:40 white female rabbits were divided into 2 groups(intraarterial and intravenous)and each was subdivided according to the time intervalsof bladder tissue sampling,of 5,15,30,60,120 minites after the drug delivering.Group B:16 white female rabbits equally divieded into 2 groups(intraarterial and intravenous)for dynamic blood sampling by the intervals of 5,15,30,60,120 minitus after the drug delivering.The intra-arterial method using an artifial bilaterial super-select internal iliac artery perfunsion model defined previouysly.The intravenous method was to deliver drugs via earmarginal vena of rabbit.1mg/kg as the concentration of the drug in bladder tissure was measured by reversed-phase HPLC.Results:The concentration of the drug in bladder tissue was significantly different between the intra-arterial and intionenous groups.Drug in the bladder tissue delivered by intra-artial method was 2.17,3.41,1.51,1.52,2.33 times as much as by intra-venous method.While drugs in blood by intra-venous method was 1.92,2.03,1.77, 1.92,1.40 times as much as by intra-arterial method.Conclusion:HCPT is suitable for trans- arterial perfusion for the treating of bladder cancer.
ABSTRACT
AIM To investigate the effect of hydroxyl camptothecinum(HCPT) on pharmocokinetics of cyclosprine A(CsA) and the membrane lipid fluidity (LFU)of red cell in rabbits. METHODS The whole blood concentration of CsA in rabbits was monitored using method of FPIA. The LFU of red cell was measured using method of DPH fluorescence polarization technique. RESULTS The pharmocokinetic parameters of CsA in group CsA+HCPT such as a, V (c), K 12 and CL (s) were significantly lower and T 1/2(a) was significantly higher ( P
ABSTRACT
Objective:To investigate the effects of 10-HCPT on the growth and proliferation of human hepatoma cell lines QGY and HepG2 in vitro.Methods:QGY and HepG2 were cultured in RPMI1640.They were treated by different concentrations of 10-HCPT for 48 hours,and by a dose of 100?g/ml of 10-HCPT for different hours.The cell growth indexes (GI) were detected by MTT colorimetric assay.The clone formation rates of QGY and HepG2 were observed by soft agar assay.Results:The GI of HepG2 and QGY cells treated by 10-HCPT with concentration 10～360?g ?g/ml and 30～360?g ?g/ml were significantly lower than that of control groups respectively ( P 0.05).The clone formation rates of QGY and HepG2 of experimental groups were significantly lower than that of control groups respectively ( P