Effect of artemether alone and in combination with grapefruit juice on hepatic drug-metabolising enzymes and biochemical aspects in experimental Schistosoma mansoni

El-Lakkany, Naglaa M.; el-Din, Sayed H. Seif; Badawy, Ahmed; Ebeid, Fatma A.

doi:10.1016/j.ijpara.2004.08.012

Cited by 33 publications

(26 citation statements)

References 37 publications

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“…These findings are in agreement with previous experiments (23,24), and human studies (25-27) related such higher PZQ concentrations to the reduction of the concentration of cytochrome P450 (CYP450) and CYP450 reductase in mice and patients infected with S. mansoni. Inhibition of hepatic drug-metabolizing enzymes (CYP450 and cytochrome b5 [Cyt b 5 ]) activities in S. mansoni-infected mice was previously reported (24,(28)(29)(30)(31).…”

Section: Discussionmentioning

confidence: 99%

Praziquantel in a Clay Nanoformulation Shows More Bioavailability and Higher Efficacy against Murine Schistosoma mansoni Infection

El-Feky

Mohamed

Nasr

et al. 2015

Antimicrob Agents Chemother

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c Consideration of existing compounds always simplifies and shortens the long and difficult process of discovering new drugs specifically for diseases of developing countries, an approach that may add to the significant potential cost savings. This study focused on improving the biological characteristics of the already-existing antischistosomal praziquantel (PZQ) by incorporating it into montmorillonite (MMT) clay as a delivery carrier to overcome its known bioavailability drawbacks. The oral bioavailability of a PZQ-MMT clay nanoformulation and its in vivo efficacy against Schistosoma mansoni were investigated. The PZQ-MMT clay nanoformulation provided a preparation with a controlled release rate, a decrease in crystallinity, and an appreciable reduction in particle size. Uninfected and infected mice treated with PZQ-MMT clay showed 3.61-and 1.96-fold and 2.16-and 1.94-fold increases, respectively, in area under the concentration-time curve from 0 to 8 h (AUC 0 -8 ) and maximum concentration of drug in serum (C max ), with a decrease in elimination rate constant (k el ) by 2.84-and 1.35-fold and increases in the absorption rate constant (k a ) and half-life (t 1/2e ) by 2.11-and 1.51-fold and 2.86-and 1.34-fold, respectively, versus the corresponding conventional PZQ-treated groups. This improved bioavailability has been expressed in higher efficacy of the drug, where the dose necessary to kill 50% of the worms was reduced by >3-fold (PZQ 50% effective dose [ED 50 ] was 20.25 mg/kg of body weight for PZQ-MMT clay compared to 74.07 mg/kg for conventional PZQ), with significant reduction in total tissue egg load and increase in total immature, mature, and dead eggs in most of the drug-treated groups. This formulation showed better bioavailability, enhanced antischistosomal efficacy, and a safer profile despite the longer period of residence in the systemic circulation. Although the conventional drug's toxicity was not examined, animal mortality rates were not different between groups receiving the test PZQ-clay nanoformulation and conventional PZQ. Schistosomiasis is a parasitic disease caused by blood flukes of the genus Schistosoma and is a serious public health problem in almost 70 countries of the tropics and subtropics without potable water and with poor sanitary conditions. It is estimated that at least 230 million people need treatment against schistosomiasis per year (1). Since an effective vaccine against schistosomiasis is lacking, the emphasis today is placed on the drug praziquantel (PZQ) (2). The low cost has made presumptive treatment on the basis of early clinical symptoms, or even universal treatment, costeffective in many situations (3).Although PZQ has proved to be especially useful in the treatment of schistosomiasis, it sometimes fails to give complete cures in treated populations. The failure of mass treatment to control schistosomiasis has been attributed to the fact that therapy is not sufficiently long-lasting (4). This effect can occur because of the low bioavailability of praziquantel d...

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Section: Discussionmentioning

confidence: 99%

Praziquantel in a Clay Nanoformulation Shows More Bioavailability and Higher Efficacy against Murine Schistosoma mansoni Infection

El-Feky

Mohamed

Nasr

et al. 2015

Antimicrob Agents Chemother

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“…Rats were regularly orally administrated with grapefruit juice at a dose level of (27 ml/kg body weight (b.w.)) (El-Lakkany et al, 2004). Group III: Animals of this group were treated with amiodarone.…”

Section: Animals and Treatmentmentioning

confidence: 99%

Effect of grapefruit juice on amiodarone induced nephrotoxicity in albino rats

Sakr

El-Gamal

2013

Toxicol Ind Health

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Amiodarone is a potent antiarrhythmic drug that is used to treat ventricular and supraventricular tachyarrhythmias. The present work studied the effect of amiodarone on the kidney of albino rats and the possible ameliorative role of grapefruit juice. Administration of amiodarone by gastric intubation (18 mg/kg body weight (b.w.), daily for 5 weeks) caused many histological alterations including intertubular leucocytic infiltrations, degeneration of the renal tubules, and atrophy of the glomeruli. Amiodarone caused marked elevation in serum creatinine and blood urea nitrogen. Histochemical examination of the renal tubules revealed depletion of glycogen and total proteins. Besides, animals administered with amiodarone showed an increase of apoptotic bands as detected by gel electrophoresis. Treating animals with amiodarone and grapefruit juice (27 ml/kg b.w.) caused an improvement in histological and histochemical appearance of the kidney together with decrease of serum creatinine and blood urea nitrogen. Moreover, the apoptosis was decreased. It is concluded from the obtained results that grapefruit juice ameliorates the nephrotoxicity of amiodarone in albino rats and this may be due to the potent antioxidant effects of its components.

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“…Juice of grapefruit (Citrus paradise) was prepared by squeezing the fresh fruit. Rats were regularly orally administered with grapefruit juice at a dose level of (27ml/Kg body weight) [17].…”

Section: Experimental Animalsmentioning

confidence: 99%

Rytmonorm-Induced Cytogenetic and Testicular Damage in Albino Rats: The Protective Effect of Grapefruit Juice

Sakr¹,

Zoail²,

El-Shafey³

2013

AJBR

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The present work studied the cytogenetic and testicular damage induced by the antiarrhythmic drug rytmonorm (RT) and the protective role of grapefruit juice in albino rats. Treating rats with RT (13.5mg/Kg bodyweight) for five weeks caused a significant increase in the percentage of chromosomal aberrations either structural or numerical and decrease the mitotic index. Using comet assays, RT caused DNA fragmentation in the lymphocytes. Testis of RT treated rats showed many histopathological and morphometric alterations. In addition, the number of sperm head abnormalities was increased. Treating animals with RT and grapefruit juice (27ml/Kg bodyweight) led to an improvement in chromosomal aberrations, mitotic index, DNA damage, and testicular alterations caused by RT. In conclusion, the results of this study indicated that grapefruit juice showed a protective effect on cytotoxicty and testicular alterations induced by RT in albino rats and this is may be due to its potent antioxidant effects.

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Effect of artemether alone and in combination with grapefruit juice on hepatic drug-metabolising enzymes and biochemical aspects in experimental Schistosoma mansoni

Cited by 33 publications

References 37 publications

Praziquantel in a Clay Nanoformulation Shows More Bioavailability and Higher Efficacy against Murine Schistosoma mansoni Infection

Praziquantel in a Clay Nanoformulation Shows More Bioavailability and Higher Efficacy against Murine Schistosoma mansoni Infection

Effect of grapefruit juice on amiodarone induced nephrotoxicity in albino rats

Rytmonorm-Induced Cytogenetic and Testicular Damage in Albino Rats: The Protective Effect of Grapefruit Juice

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