OBJECTIVETo optimize the preparation process of gemcitabine polybutylcyanoacrylate nanoparticles (GCTB- PBCA-NP).

METHODSAccording to the particle size, the entrapment efficiency and the loading quantity of GCTB-PBCA-NP, single factor analysis was carried out to optimize the component composition and preparation process based on an orthogonal design.

RESULTSThe mean particle size of the NP was (112-/+9) nm with an entrapment efficiency of (54.12-/+2.43)% and drug loading of (11.08-/+0.89)%.

CONCLUSIONAn optimized nanoparticular drug delivery system is obtained by emulsion polymerization.

Chemistry, Pharmaceutical ; Deoxycytidine ; analogs & derivatives ; chemical synthesis ; Drug Delivery Systems ; Enbucrilate ; chemical synthesis ; Nanoparticles ; chemistry

BACKGROUND/AIMS: Though endoscopic therapies such as variceal ligation and sclerotherapy has been performed, bleeding from the large esophageal and gastric varices still poses significant risk of death. Decrease of portal pressure by TIPS (transjugular intrahepatic portosystemic shunt) or surgical shunt was indicated as cause of failure of endoscopic therapies. Treatment of N-butyl-2-cyanoacrylate has been especially effective for gastric variceal bleeding, but comparison with other treatments had not been reported yet. In this study, the effect of cyanoacrylate injection therapy was cross-examined with the result of TIPS in acute esophagogastric variceal bleedings. METHODS: From April 1995 to June 2002, endoscopic cyanoacrylate injection therapy (43 cases) and TIPS (63 cases) were performed in our hospital. Each group was analysed regarding their clinical results including initial hemostasis rate, rebleeding rate, survival duration, mortality and morbidity. RESULTS: Initial hemostasis rate was 95.3% in cyanoacrylate group and 92.1% in TIPS group. Cumulative probability of rebleeding was not different between two groups. Overall complication rates associated with the procedure were 50.8% in TIPS group and 9.3% in cyanoacrylate group. There was no significant difference between two groups in their survival rates. CONCLUSIONS: Cyanoacrylate injection therapy was relatively safe, and has comparable results with TIPS for uncontrollable and severe esophagogastric variceal bleedings.
Acute Disease ; Comparative Study ; Enbucrilate/*administration & dosage/*analogs & derivatives ; Endoscopy, Digestive System ; English Abstract ; Esophageal and Gastric Varices/surgery/*therapy ; Female ; Gastrointestinal Hemorrhage/*therapy ; *Hemostasis, Endoscopic ; Humans ; Injections ; Male ; Middle Aged ; *Portasystemic Shunt, Transjugular Intrahepatic ; Tissue Adhesives/*administration & dosage

BACKGROUND/AIMS: Gastric variceal bleeding is a severe complication of cirrhosis, and it has a high mortality rate. This study was conducted to evaluate the efficacy of n-butyl-2-cyanoacrylate injection therapy for patients suffering with gastric variceal bleeding. METHODS: A total of 86 patients diagnosed with gastric variceal bleeding underwent endoscopic n-butyl-2-cyanoacrylate (Histoacryl(R)) injection therapy at our department between April, 2002 and July, 2005, with a mean follow-up period of 44 weeks (range: 2 to 136 weeks). The initial hemostasis rate and the rebleeding rate of endoscopic sclerotherapy were analyzed. Also, the cumulative survival rate was analyzed according to the status of hepatocellular carcinoma and hyponatremia, the MELD score, the Child-Pugh score and the amount of injected Histoacryl(R). RESULTS: The initial hemostasis rate of Histoacryl(R) injection therapy was 93% and the 1 month rebleeding rate was 16.1%. The total number of session for treating the initial hemostasis was 1.2+/-0.4 and the total volume of Histoacryl(R) was 2.7+/-1.2 mL. The cumulative rebleeding-free rates for the patients treated by the Histoacryl(R) injection method at 1 month, 12 months and 34 months period were 95.1%, 83.2% and 74%, respectively. The cumulative survival rates were 78.3% at 1 month, 61.9% at 12 months and 54.6% at 34 months, respectively. No thromboembolic phenomenon occurred. According to the Cox's proportional hazards analysis, only the MELD score (<15) was an independent predicting factor for survival of the patients with gastric variceal bleeding. CONCLUSIONS: Endoscopic sclerotherapy using n-butyl-2-cyanoacrylate was a safe and effective hemostatic method for patients with gastric variceal bleeding. Also, the MELD score (<15) contributed to predicting survival of the patients with gastric variceal bleeding.
Adult ; Aged ; Aged, 80 and over ; Enbucrilate/*analogs & derivatives/therapeutic use ; Esophageal and Gastric Varices/*therapy ; Female ; Gastrointestinal Hemorrhage/mortality/*therapy ; Hemostasis, Endoscopic ; Humans ; Male ; Middle Aged ; *Sclerotherapy ; Survival Rate ; Treatment Outcome

Duodenal varix is a rare cause of hemorrhage in patients with portal hypertension, however their rupture is serious and often life threatening. Treatments for duodenal variceal bleeding include endoscopic procedures, surgery, or interventional radiologic procedures. We report a case of duodenal varices rupture in a 45-year-old man with alcoholic liver cirrhosis who presented with melena and dizziness. Emergent upper endoscopy revealed large nodular varices with a ruptured erosion on the top in the distal second portion of duodenum. Two consecutive injections with 1.0 mL of n-butyl-2-cyanoacrylate (Histoacryl; Braun-Melsungen, Germany) mixed with 1.0 mL of lipiodol (Laboratoire-Guerbet, France) were performed intravariceally and achieved successful hemostasis. This suggests that endoscopic injection sclerotherapy with histoacryl may be an effective therapeutic option for the control of ruptured duodenal variceal bleeding.
Duodenal Diseases/etiology/*therapy ; Duodenoscopy ; Duodenum/*blood supply ; Enbucrilate/*analogs & derivatives/chemistry/therapeutic use ; Gastrointestinal Hemorrhage/etiology/*therapy ; Humans ; Liver Cirrhosis, Alcoholic/complications ; Male ; Middle Aged ; Rupture ; Sclerosing Solutions/*therapeutic use ; *Sclerotherapy ; Tissue Adhesives/therapeutic use ; Tomography, X-Ray Computed ; Varicose Veins/complications/*therapy

BACKGROUND/AIMS: Gastric variceal bleeding is an infrequent but serious complication of portal hypertension. Endoscopic injection of Histoacryl(R) (N-butyl-2-cyanoacrylate) has been approved as an effective treatment for gastric variceal bleeding. The aim of this study was to evaluate the long-term efficacy and safety of the endoscopic injection of Histoacryl(R) for the treatment of gastric varices. METHODS: Between January 1994 and January 2005, eighty-five patients with gastric varices received endoscopic injections of Histoacryl(R) . Among these 85 patients, 65 received the procedure within 1 week after gastric variceal bleeding, and 13 received as a prophylactic procedure. According to the Sarin classification, 32 patients were GOV1 and 53 were GOV2. Most of the varices were large (F2 or F3, 75 patients). The average volume of Histoacryl(R) per each session was 1.43 ml. Among 85 patients, 72 patients were followed-up and the median duration was 24.5 months. RESULTS: The rate of initial hemostasis was 98.6% and recurrent bleeding occurred in 29.2% (21 of 72). When rebleeding occurred, 76.2% was within 1 year after the initial injection. Treatment failure-related mortality rate was 1.4% (1 of 85). Twenty-seven patients died, mostly due to hepatocelluar carcinoma or liver failure. Two patients experienced pulmonary embolism and one experienced splenic infarction. They recovered without specific treatment. Rebleeding rate had a tendency to increase in patients with hepatocelluar carcinoma (p=0.051) and GOV2 (p=0.061). CONCLUSIONS: Histoacryl(R) injection therapy is a effective treatment method for gastric varices with high initial hemostasis rate and low major complications.
Adult ; Aged ; Enbucrilate/administration & dosage/*analogs & derivatives/chemistry/therapeutic ; Endoscopy, Gastrointestinal ; Esophageal and Gastric Varices/mortality/surgery/*therapy ; Female ; Gastrointestinal Hemorrhage/mortality/surgery/*therapy ; Humans ; Injections ; Male ; Middle Aged ; Predictive Value of Tests ; Retrospective Studies ; Sclerosing Solutions/administration & dosage/*therapeutic use ; Severity of Illness Index ; Survival Rate

OBJECTIVETo observe the effect of intervention therapy with Shentao Ruangan pill (SRP) and hydroxycamptothecine (HCPT) in treating 85 patients with middle-advanced large hepatocarcinoma, and to analyze the factors that could affect the prognosis.

METHODSEighty-five patients were randomly divided into the treated group (n = 52) and the control group (n = 33). The treated group was treated by oral taking of SRP combined with local perfusion of HCPT through hepatic artery catheterization, while to the control group, the conventional therapy, transcatheter arterial chemoembolization (TACE) was conducted for control. The clinical efficacy of treatment in the two groups was evaluated by the change of tumor size, the factors related with prognosis were analyzed using Cox proportional hazards model and the analysis of survival conducted by Kaplan-Meier method.

RESULTS(1) The tumor size reducing rate in the treated group was 19.2% and the tumor size stabilizing rate was 82.7%, while those in the control group was 21.2% and 81.8% respectively, comparison of the criteria between the two groups showed insignificant difference (P > 0.05); (2) The median survival time, 0.5- year, 1- year and 2- year survival rate in the treated group was 326 days, 80.95%, 41.39% and 12.42% respectively, those in the control group was 262 days, 64.29%, 25.00% and 8.33% respectively, comparison between the two groups showed significant difference (P < 0.05); (3) Among the 3 TCM types in patients, the survival time and rates in patients of Gan-excess with Pi-deficiency type was similar to those in patients of Gan-heat with blood stasis type showing insignificant difference (P > 0.05), but as compared with those in patients of Gan-Shen Yin-deficiency type, the difference was significant (P < 0.05) ; (4) Beneficial factor to the prognosis were therapeutic method, that used in the treated group was superior to that used in the control group. The risk factors to the prognosis were TCM type, clinical stage and liver function. Patients of Gan-excess with Pi-deficiency type had the optimal prognosis, those of Gan-heat with blood stasis type the next and of Gan-Shen Yin-deficiency the worst. The later the clinical stage and the worse the Child-Pugh grade of liver function was, the worse the prognosis would be.

CONCLUSION(1) SRP combined with HCPT intervention treatment is superior to the simple TACE treatment in elevating patients' survival rate and time; (2) There are some relations between TCM types and prognosis; (3) Local Chinese drug therapy combined with systemic therapy could be one of the effective measures of non-operational therapy in treating large hepatocarcinoma.

Adolescent ; Adult ; Aged ; Carcinoma, Hepatocellular ; drug therapy ; Diagnosis, Differential ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Enbucrilate ; administration & dosage ; analogs & derivatives ; Female ; Hepatic Artery ; Humans ; Injections, Intra-Arterial ; Liver Neoplasms ; drug therapy ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Prognosis ; Treatment Outcome