Long-term albendazole therapy for diffuse parenchymal neurocysticercosis in an immunocompetent patient:A case report

Rationale:Neurocysticercosis is a neglected tropical disease caused by the larvae of Taenia solium and may occur in immunocompetent people.We report a case of diffuse parenchymal neurocysticercosis mimicking tuberculous meningitis in an immunocompetent patient.Patient concerns:A 24-year-old immunocompetent woman presented with serial focal to generalized seizure,left body weakness,left abducens palsy,chronic cough,and body weight loss.She came from an area where she was unlikely to have contact with Taenia solium.Diagnosis:Diffuse parenchymal neurocysticercosis.Intervention:Valproic acid,dexamethasone and 15 months of albendazole therapy.Outcome:Complete recovery without any neurological sequelae.

对Albendazole治疗脑豚囊虫病的疗效评价

<正> 在我国脑豚囊虫病的发病率并不低,且致残率亦较高,因此,研究治疗脑豚囊虫病的药物是个重要课题,既往有报告用吡喹酮治疗,但结果不太理想。本文试用

Formulation and evaluation of Albendazole microcapsules for colon delivery using chitosan

Objective:To formulate and evaluate Albendazole microcapsules using chitosan,a natural polymer for colon-specific delivery for better treatment of helminthiasis,filariasis,colorectal cancer,avoiding the side effects.Methods:The Albendazole microcapsules were prepared by the use of different concentrations of sodium alginate,chitosan and hydroxypropyl methylcellulose(HPMC).The polysaccharides chitosan reacted with sodium alginate in the presence of calcium chloride to form microcapsules with a polyelectrolyte complex membrane by electrostatic interactions between the two oppositely charged polymers.The microcapsules were then studied for entrapment efficiency,drug-polymer compatibility and surface morphology. In vitro drug release study in presence and absence of cecal content were also studied.Further, kinetic modellings were employed to find out release mechanisms.Results:Albendazole loaded microspheres showd high entrapment efficiency(72.8%) and the microcapsules were free flowing,non aggregated and spherical,between 600 and 1 000μm in diameter.The surface of microcapsules were found to be porous and wavy.The FT-IR spectrum showed that there is no interaction between the polymer and the drug.The in vitro drug release study found to be affected by change in chitosan,sodium alginate and HPMC concentration.The microcapsules with 2.5% sodium alginate and 0.4% chitosan shown minimum release in gastrointestinal simulated condition but shows maximum drug release at the end of 24th hour in presence of cecal content.The rate of drug release follows Korsmeyer-peppas model that was the drug release is by diffusion and erosion.Conclusions:The study reveals that Albendazole loaded chitosanalginate based microsphere can be used effectively for the colon targeting.

Current status of the efficacy and effectiveness of albendazole and mebendazole for the treatment of Ascaris lumbricoides in North-Western Indonesia

Objective:To investigate the efficacy and effectiveness of albendazole and mebendazole in the treatment of Ascaris lumbricoides(A.lumbricoides) in the North-Western Indonesia.Methods: 229 primary school children who were positive for A.lumbricoides in their stool were recruited in the study.123 children received single-dose of 400 mg albendazole and 106 children received single-dose 500 mg of mebendazole.After 1 week,their stools were examined for the cure rate (CR) and egg reduction rate(ERR).Egg culture was also performed and observation was made on week-1,-3,-4.Results:have shown a non-significant difference in CR 96.7%vs.100%:and ERR of 99.3%vs.100.0%for albendazole and mebendazole groups respectively(P】0.05).In-vitro egg culture has shown trends of decrease in the percentage of the unfertilized eggs and in≥2 cell eggs in both treatment groups(P【0.05).The embryonated eggs from the albendazole groups has shown an increase from 7.3%on week-1 to 13.8%on week-4,whilst the mebendazole group has shown a constant increase during the whole 4 weeks of culture from 7.5%to 28.3%(P【0.01). Conclusions:No evidence of drug resistance is noted so far from the area of North-Western part of Indonesia.In addition,although both drugs showed incomplete ovicidal effects,single-dose albendazole is better than mebendazole in sterilizing A.lumbricoides eggs.

Efficacy of combined albendazol and praziquntel and their loaded solid lipid nanoparticles components in chemoprophylaxis of experimental hydatidosis

Objective:To evaluate the efficacy of combined ABZ and PZQ and their solid lipid nanoparticles in chemoprophylaxis of cystic echinococcosis(CE).Methods:ABZ and PZQ loaded solid lipid nanoparticles(SLNs) were prepared by high shear homogenization and microemulsion congealing techniques with some minor modification.Nanoparticles average size,polydispersity index(PDI),and particle size distribution were determined by scanning electron microscopy(SEM) and photon correlation spectroscopy.Forty females BALB/c were experimentally infected by protoscoleces(PSC) and randomly divided into four equal groups of 10 mice.After the end of the 3 months treatment period and 2 months rest,mice were sacrificed and the peritoneal cavity was opened for removal,counting,measuring,and histological analysis of hydatid cyst.Results:The results indicated that ABZ and PZQ chemoprophylaxis treatment reduced the wet weight and size of developed cysts 77.3% and 79%,respectively.The corresponding result for the ABZ and PZQ loaded SLNs was 83% and 85%,respectively.Conclusions:This study for the first time demonstrated that ABZ and PZQ loaded SLNs is superior to free ABZ and PZQ for the chemoprophylaxis of CE in mice.

Study on the inclusion interaction of methylated-β-cyclodextrins with albendazole by spectrofluorimetry and its application

The inclusion interaction between three types of methylated-β-cyclodextrins （Me-β-CDs） and albendazole （ABZ） was studied by spectrofluorimetry. The result showed that Me-β-CDs reacted with ABZ to form an inclusion complex, 1： 1 stoichiometry for Me- β-CDs-ABZ complex was established and its association constant have been determined from fluorescence data by Benesi- Hildebrand＇s method （double reciprocal plots）. It was noted that 2,6-DM-β-CD exhibited stronger binding ability than other Me-β- CDs. Based on the significant enhancement of fluorescence intensity of inclusion complex, a simple and highly sensitive fluorimetric method is proposed for the determination of ABZ in the presence of 2,6-DM-β-CD. The proposed method was successfully applied to the determination of ABZ in tablets and human urine.

Liquid chromatography-tandem mass spectrometry method for simultaneous determination of albendazole and albendazole sulfoxide in human plasma for bioequivalence studies

An improved high performance liquid chromatography-tandem mass spectrometry（LC-MS/MS） method has been developed for sensitive and rapid determination of albendazole（ABZ） and its active metabolite,albendazole sulfoxide（ABZSO）,in the positive ionization mode.The method utilized solid phase extraction（SPE） for sample preparation of the analytes and their deuterated internal standards（ISs） from100 μL human plasma.The chromatography was carried out on Hypurity C_（18） column using acetonitrile-2.0 mM ammonium acetate,pH 5.0（80：20,v/v） as the mobile phase.The assay exhibited a linear response over the concentration range of 0.200-50.0 ng/mL for ABZ and 3.00-600 ng/mL for ABZSO.The recoveries of the analytes and ISs ranged from 86.03%-89.66%and 89.85%-98.94%,respectively.Matrix effect,expressed as IS-normalized matrix factors,ranged from 0.985 to 1.042 for the both analytes.The method was successfully applied for two separate studies in healthy subjects using single dose of 400 mg conventional tablets and 400 mg chewable ABZ tablets,respectively.

Effects of albendazole,artesunate,praziquantel and miltefosine,on Opisthorchis viverrini cercariae and mature metacercariae

Objective:To explore larvicidal effects of anthelmintic drugs on Opisthorchis viverrini(O.viverrini) for alternative approach to interrupting its cycle for developing a field-based control program.Methods:The larvicidal activities of albendazole(A1),artesunate(Ar),praziquantel(Pzq) and miltefosine(Mf) on O.viverrini cercariae and mature metacercariae were investigated.Lethal concentrations(LC_(50) and LC_(95)) of these drugs were determined.Mature metacercariae previously exposed to various concentrations of the drugs were administered to hamsters.Worms were harvested 30 d post infection and worm recovery rates calculated.Al,Ar,Pzq and Mf produced morphological degeneration and induced shedding tails of cercariae after 24 h exposure.Results:The LC_(50) and LC_(95) of Al,Ar,Pzq and Mf on cercariae were 0.720 and 1.139,0.350 and 0.861,0.017 and 0.693,and 0.530 and 1.134 ppm,respectively.LC_(50) and LC_(95) of Ar on mature metacercariae were 303.643 and 446.237 ppm and of Mf were 289.711 and 631.781 ppm,respectively but no lethal effect in Pzq-and Al-treated groups(up to 1 ppt).No worms were found in hamsters administered Pzq-treated metacercariae.The adult worms from Al-treated metacercariae were significantly bigger in size compared to the control group(P<0.05).Fecundity and body width were greater in adults from Mf-treated metacercariae compared to the control group(P<0.05).Conclusions:The larvicidal effects of these drugs were high efficacy to O.viverrini cercariae but lesser efficacy to metacercariae.It should be further studied with the eventual aim of developing a field-based control program.

Inhibition of Albendazole and Oxfendazole on the Activity of Fumaric Reductase in Cysticercus cellulosae

The activity of fumaric reductase in Cysticercus cellulosae tissue homogenate with albendazole and oxfendazole individually was detected. Results showed that the two kinds of drugs both could inhabite the activity of fumaric reductase. The results indicate that the mechanism of action of benzimidazole carbamate drugs is probably inhabiting the complex of fumaric reductase noncompetently, thus lead to the exhaostion of energy and death.

Effect of Albendazole and Mebendazole on Hydatid Cyst of Mice

In the current study, hydatid cysts from livers and lungs of camels were obtained from Tambool slaughter house and protoscoleces were separated aseptically. 36-weeks-old Swiss mice (25 - 30 gram body weight males and females) were divided into two groups of 6 each: a prophylactic group dosed with 150 ml/kg of albendazole and mebendazole was given directly after injection with 2000 protoscoleces intraperitoneally for 10 consecutive days. The treated group was given a dose of 300 ml/kg of albendazole and mebendazole for 24 days with 4 days interval separated by 2 days and after 6 months of inoculation with protoscoleces, the two groups in addition to the control group were sacrificed and necropsied. The results revealed a significant difference in the development of hydatid cyst (p < 0.01). Inside the mice, small number of cysts was noticed in the group treated with albendazole and mebendazole compared to the control group, however, albendazole was highly efficacious than the mebendazole where the efficiency of albendazole reached 97% while the mebendazole efficiency rate was almost 50% which indicates that albendazole could be considered the drug of choice in the treatment of hydatid cyst.

Protective Effects of Vitamin E on Albendazole Adverse Effects

The present study was conducted to determine the effect of albendazole alone or in combination with vitamin E on antioxidant activity and histopathological, changes on the liver and kidney. Following oral administration of albendazole of 0.25 mg/kg body weight and Vitamin E of 0.01 mg/kg body weight used for 21 successive days to broiler chicken, the experiment was done on fifteen broiler chickens divided into three groups: group one was non-treated, group two was treated with albendazole of 0.25 mg/kg body weight and group three was treated in combination with vitamin E of 0.01 mg/kg body weight. The blood sample and tissue were taken at the end of experiment 12 hrs after the last dose. The experimental result revealed that the significant decrease of liver enzymes caused by albendazole like serum Alanine Aminotransferase (ALP), Aspartate Aminotransferase (AST), Alkaline Phosphatase (ALT), when compared with the control group, the experimental result significant decrease in kidney parameters like urea creatinine level caused by albendazole and finally there was a significant increase in antioxidant enzymes activity like CAT, SOP, GPX and a significant decrease in MDA. Histopathology results in liver-treated animals with albendazole in combination with vitamin E showed dilated, congested Portal Blood Vessels (PBV, arrow), mild to moderate Biliary Proliferation (BP, arrow), portal Round Cells Aggregation (RCA, arrow), and focal Hepatocellular Degeneration (HCD, arrow). Histopathology results of kidney-treated animals with al- bendazole in combination with vitamin E showing a mild Per Tubular Edema (PTE arrow), focal Tubular Degeneration (TD arrow), Tubular Regeneration (TR, arrow), glomerular lobulation and atrophy (GL arrow), and beside interstitial cells aggregation (RCA arrow), H & EX 200. Therefore, vitamin E should be taken by albendazole to decrease its effect.

Praziquantel and Albendazole Pills Can Cure Cancer

Objective:To prevent and treat various types of cancer safely,reliably,and at low cost.Method:Early and mid-stage cancer patients took praziquantel and albendazole every day,late cancer patients only took albendazole every day,while with the traditional Chinese medicine“ginseng jade bamboo particle”to eliminate the adverse reactions and side effects caused by the above two western medicines,continue for more than three months.Conclusion:Praziquantel and albendazole have good therapeutic and cancer prevention effects in actual clinical trials.

In vivo therapeutic effects of albendazole in combination with IFN-on cystic echinococcosis in mice

Objective:This study was aimed to evaluate the in vivo therapeutic effects of the combination of ABZ with interferon(IFN)-αon cystic echinococcosis(CE)in mice.Methods:After 5-month secondary infection with protoscolices,Balb/c mice were randomly divided into four groups:ABZtreated group,IFN-α-treated group,ABZ+IFN-αgroup and untreated control group.Drugs in different treated groups were respectively administered for 2 months.Blood was respectively taken from caudal veins in mice at treatment time points of 0 d,7 d,14 d,28 d,36 d,48 d and 60 d,in order to detect the changes in the level of antibodies in the serum.Mice were then sacrificed after the end of treatment,and related indicators were detected to evaluate the therapeutic effects.Results:In comparison with untreated control group(p<.01)and ABZ-treated group(p<.05),ABZ+IFN-αgroup showed a more significant decrease in the number of cysts,cyst size and cyst weight.After transmission electron microscopy(TEM)of the cysts in different treated groups,it was found that,there was an obvious change in cyst ultrastructure in ABZ+IFN-αgroup.ELISA experimental results showed that,in ABZ+IFN-αgroup,there was a significant decrease in IL-10 in serums and splenocytes(p<.01);In comparison with untreated control group,ABZ+IFN-αgroup showed a more significant decrease in the levels of IgE,IgG and its subtypes(p<.01).Conclusions:In this study,the combination of ABZ with IFN-αwas proved to be an effective CE treatment option.

Albendazole versus metronidazole treatment of adult giardiasis:An open randomized clinical study

To investigate the efficacy and tolerability of albendazoleand metranidazole treatment in giardiasis.

肝泡型包虫病的诊治进展

肝包虫病为慢性寄生虫病,由多房棘球蚴的幼虫引发,此病具有相当高的致残率和死亡风险,又被称作“虫癌”。临床上将肝包虫病分为肝泡型包虫病和肝囊型包虫病,肝包虫病在世界各地广泛流行,我国主要在西部农牧区居民群体中发生,对该地区居民的生存质量构成了巨大的威胁。目前临床上治疗肝包虫病以手术治疗方式为主,伴随着外科诊治技术的迅速发展和对肝包虫病研究不断深入,其诊治方案也不断完善。本文将主要综述肝泡型包虫病的诊断和治疗进展,旨在为临床医务人员提供参考,以尽早发现和治疗,降低疾病对患者产生的不良影响,改善患者预后。

A novel tumor-targeting treatment strategy uses energy restriction via co-delivery of albendazole and nanosilver

Although nanotechnology has been rapidly developed and applied in tumor targeting, the outcome of chemotherapy remains greatly restricted by the toxicity of cytotoxic drugs in normal tissues and cells. Therefore, the development of alternative delivery systems, with few side effects in normal cells, has attracted increasing attention. Energy restriction is a novel and promising approach to cancer treatment, which can restrict tumor growth via inhibition of cellular energy metabolism. In this study, a novel tumor targeting system, based on folate-conjugated bovine serum albumin （BSA）, was developed to co-deliver albendazole and nanosilver simultaneously, to restrain the energy metabolism of tumor cells. This nanosystem showed stronger anti-tumor efficacy than those using nanoparticles without folic acid modification, nanosilver, or albendazole, both in vitro and in vivo. This nanosystem depleted cellular ATP via direct inhibition of glycolytic enzymes and mitochondrial damage, resulting in inhibition of proliferation, cell-cycle arrest, and apoptosis of tumor cells. The enhanced anti-tumor activity contributed to the tumor-targeting ability of this system, resulting in specific energy inhibition in tumor cells. Toxicity evaluation was performed to confirm the safety of this system. This nanosystem provides an efficient and safe strate~ for tumor therapy.

Continuous long-term albendazole therapy in intraabdominal cystic echinococcosis

To assess the therapeutic effects of long-term albendazole therapy in intraabdominal cystic echinococcosis Methods Fifteen patients with a total of 45 cysts were treated with albendazole with dosage regimen of 20 *!mg·kg -1 ·d -1 for an average of 2 5 years Repeated CT and ultrasound scannings (US) were performed after the end of therapy The duration of follow-up was 3 6 years on average The number, size and morpiology of cysts were compared before and after treatment Results The hydatid cysts were classified according to location and CT patterns into hepatic simple cysts, hepatic cysts with daughter cysts, hepatic/abdominal cysts and splenic cysts The hepatic simple cysts responded most favorably to albendazole therapy, with an overall cure rate of 88 7% The disappearance of cysts was observed in 43 0% of cases (15/35) Sixteen cysts (45 7%) became solidified or calcified, among which 8 cysts were completely calcified, 6 showed egg shell-like calcification of the cystic walls, and 2 showed solidification and calcification of cyst contents Four patients had large hepatic cysts containing daughter cysts; the daughter cysts all disappeared after treatment, but one patient relapsed with the reappearance of daughter cysts at 4-year follow-up Two splenic cysts also calcified Two patients had peritoneal cysts; one calcified and the other one reduced in size Among 15 patients treated, 9 were cured and 6 were improved There was no serious toxic reactions with continuous long-term therapy in a small series of patients Conclusions Continuous long-term albendazole treatment of intraabdominal cystic echinococcosis is safe and effective in the treatment of hepatic simple cysts, and some daughter cysts, peritoneal secondary cysts and splenic cysts No serious toxic reactions were found

阿苯达唑的合成工艺改进

本文以廉价易购的多菌灵为起始原料,与氯磺酸磺化后“一锅法”得到目标产物阿苯达唑(1),产物结构经^(1)HNMR、^(13)CNMR及MS表征确证,总收率达67.2%(以多菌灵计),HPLC纯度99.16%。该合成工艺具有原料廉价易购、条件温和、操作简便等优点,适合工业化生产。

三氧化二砷联合阿苯达唑对细粒棘球蚴生长的影响

目的研究体外条件下三氧化二砷(ATO)联合阿苯达唑(ABZ)对细粒棘球蚴原头节生长作用的影响,初步探讨联合用药治疗肝包虫病的可行性。方法采用不同浓度的ATO(3和6μmol/L)联合ABZ在体外条件下作用于原头节,分组如下:3μmol/L ATO、6μmol/L ATO、100μmol/L ABZ、3μmol/L ATO+100μmol/L ABZ和6μmol/L ATO+100μmol/L ABZ。光镜下通过0.1%伊红染色法观察原头节的活力及形态变化;扫描电子显微镜下观察原头节的超微结构变化;各组药物作用2 d后,借助半胱氨酸天冬氨酸蛋白酶-3(caspase-3)活性检测试剂盒测定caspase-3酶活力。采用ELISA法检测原头节内抗氧化酶(SOD、HO-1)活性水平。结果6μmol/L ATO+100μmol/L ABZ组原头节的抑制作用最强,3μmol/L ATO+100μmol/L ABZ组次之。联合作用组对原头节超微结构的损伤明显大于ABZ单独作用组,6μmol/L ATO+100μmol/L ABZ作用3 d后原头节表层出现虫蚀样改变、顶突变形、头钩缺损及微毛脱落。原头节在培养4d后,联合作用组原头节caspase-3活力[(43.34±1.07)μmol/L]显著高于ABZ单药作用组[(32.58±0.73)μmol/L](F=859.754,P<0.05),且具有剂量依赖性。ATO作用后原头节内SOD、HO-1活性显著下降(P<0.05),呈现时间及剂量依赖性。结论ATO与ABZ联合可显著抑制细粒棘球蚴原头节生长,且抑制作用强于单独用药,其协同作用机制可能与改变原头节内氧化应激系统有关,然而其具体机制尚需进一步研究。