This study was aimed to establish rat bladder tumor animal models to investigate the in viva antitumor effect of polyanhydride-pirarubicin (PAD-THP), a long-lasting anti-cancer implant, in the bladder tumor of animal models. The model of bladder cancer was set up with N-butly-N-(4 hydroxybutyl) nitrosamine (BBN) feeding into rats. The PAD-THP long-acting anti-cancer implants containing the drugs and the same dose of the THP naked drug were placed under the bladder mucosa of bladder tumor model in vivo. The pirarubicin plasma concentration was measured with high performance liquid chromatography (HPLC) detection in vivo. The effective drug concentration and lasting period were observed and compared in the animal bodies. The tumor sizes were measured before and after the treatment. The in viva antitumor effects were analyzed and compared. The results showed that more significant antitumor effect of PAD-THP implants on the local drug release characteristics were presented compared with that of the same dose of THP bare drug group and there were significant differences (P<0. 05) between the two methods. All the results indicated that the PAD-THP anti-cancer implants in the postoperative local treatment of bladder tumors would show prosperous in the future for clinical application.
Animals ; Antineoplastic Agents ; administration & dosage ; Butylhydroxybutylnitrosamine ; Delayed-Action Preparations ; administration & dosage ; Disease Models, Animal ; Doxorubicin ; administration & dosage ; analogs & derivatives ; Female ; Implants, Experimental ; Polyanhydrides ; administration & dosage ; Rats ; Rats, Sprague-Dawley ; Urinary Bladder Neoplasms ; chemically induced ; drug therapy ; pathology

To retain the anti-rheumatoid arthritis activity of melittin and to reduce the hemolysis and hypersusceptibility caused by melittin, a deletion peptide of melittin was synthesized. Its ant-inflammation effect was observed . A hydrophile peptide fragment of melittin was synthesized by standard solid-phase method. The product was analyzed by HPLC and MS. The relevant hemolysis and hypersusceptibility were tested. The rabbits' model of immune arthritis were established and treated. The results showed that the hemolysis rate for peptide fragment was less than 5%, the hypersusceptibility rate was less than 8%. The hydrophile peptide fragment of melittin may retain anti-rheumatoid arthritis activity and reduce the melittin-induced hemolysis and hypersusceptibility.
Animals ; Arthritis, Rheumatoid ; therapy ; Melitten ; chemical synthesis ; therapeutic use ; Peptide Fragments ; chemical synthesis ; therapeutic use ; Rabbits

This paper aims to prepare polyanhydride-Pirarubicin dose long-acting sustained-release implants for the treatment of bladder cancer and for the prevention of postoperative recurrence of bladder cancer. Pirarubicin hydrochloride (THP) and polyanhydride, in accordance with a certain proportion, were fully mixed in the agate morta and dissolved in dichloromethane, and then were cast into a film within a mold put in the dryer set at 4 degrees C. Each tablet implanted contained 5.0 mg of THP. Polyanhydride-pirarubicin sustained-release was implanted into the bladder mucosa of the rabbits, and blood and urine samples were taken at different times after the operation. The THP drug concentrations in urine and blood were determined with high-performance liquid chromatography. The THP concentration in urine was significantly higher than the THP concentration in plasma. The drug concentration in urine reached (92.5 +/- 7.4) microg/L at 250 d time after the operation. Polyanhydride-pirarubicin implants possess long-acting sustained-release level dynamics in the body. It can maintain a stable long-term drug release and can be expected to last a year and can effectively prevent recurrence of bladder cancer. The present experiments proved that the implants with sustained-release drug treatment are expected to be useful in the clinical application in prevention of bladder cancer recurrence.
Absorbable Implants ; Animals ; Antineoplastic Agents ; administration & dosage ; Chromatography, High Pressure Liquid ; methods ; Delayed-Action Preparations ; administration & dosage ; chemistry ; Doxorubicin ; administration & dosage ; analogs & derivatives ; Female ; Implants, Experimental ; Male ; Neoplasm Recurrence, Local ; prevention & control ; Polyanhydrides ; administration & dosage ; chemistry ; Postoperative Period ; Rabbits ; Random Allocation ; Urinary Bladder Neoplasms ; drug therapy ; surgery