Nanotechnology is a fast-growing technology that plays an important great impact on various fields of therapeutic applications. It is capable for solving several problems related to animal health and production. There are different nano-systems such as liposomes, metallic nanoparticles, polymeric micelles, polymeric nanospheres, functionalized fullerenes, carbon nanotubes, dendrimers, polymer-coated nanocrystals and nanoshells. In this review, we mentioned different methods for the preparation and characterization of nanoparticles. This review is concerned mainly on nanoparticle systems for antibiotic delivery which suffer from poor bioavailability and many side effects. Nanoparticles are characterized by many features include their minimal size, colossal surface zone to mass extent. The development of antimicrobials in nanoparticle systems is considered an excellent alternative delivery system for antimicrobials for the treatment of microbial diseases by increasing therapeutic effect and overcoming the side effects. In this paper, we reviewed some antimicrobial nanoparticle preparations and we focused on florfenicol and neomycin nanoparticle preparations as well as chitosan and silver nanoparticles preparations to prepare, characterize and compare their different pharmacological effects.
This study examined the disposition kinetics and bioavailability of florfenicol after intravenous (i.v.), intramuscular (i.m.) and oral administration to rabbits at a dose of 30 mg/kg BW. Serial blood samples were collected through an indwelling catheter intermittently for 24 h for various routes. Plasma antibacterial concentrations were determined using a microbiological assay method with Bacillus subtilis ATCC 6633 as a reference organism. Plasma concentration-time data generated in the present study were analysed by non-compartmental methods based on statistical moment theory. Following i.v. administration, the overall elimination half-life (t1/2beta) was 1.54 h, mean residence time (MRT) was 1.69 h, mean volume of distribution at steady-state (Vdss) was 0.57 L/kg, and total body clearance (Cltot) was 0.34 L/kg/h. After i.m. and oral dosing, the terminal part of the curve should correspond to the absorption phase, instead of to the elimination phase, with terminal half-lives of 3.01 and 2.57 h, respectively. The mean absorption time (MAT) was 2.65 h for i.m. and 2.01 h for oral administration. Elimination rate constants differed with i.v., i.m. and oral administrations, suggesting a flip-flop situation. The observed mean peak plasma concentrations (Cmax obs) were 21.65 and 15.14 microg/ml achieved at a post-injection time (Tmax obs) of 0.5 h following i.m. and oral dosing, respectively. The absolute systemic availabilities were 88.25% and 50.79%, respectively, and the extent of plasma protein binding percent was 11.65%.
Prophylactic and curative capacity of water soluble formulation of Diclazuril (Diclosol 1%) and feed additive form (Clinacox, 0.5%) were tested against Eimeria infection in broiler chickens. Such testing was performed both experimentally and in the field. Toltrazuril (Baycox, 2.5%) was used as reference control drug. Water soluble formulation of Diclazuril induced a marked inhibitory effect on the different stages of the parasite life cycle in experimentally infected treated birds especially when applied on the day when blood first appeared in the faeces [fifth day post-infection (d.p.i.)] as well as on the second day of blood dropping (6 d.p.i.). Both tested dosage levels of Diclazuril water soluble formulation in drinking water (5 and 10 ppm) showed the same effect in controlling coccidial infection and reducing the total oocyst numbers, lesion and faecal scores. Moreover, there was no significant difference in the efficacy of water soluble form of Diclazuril and the reference control drug (Toltrazuril, 25 ppm). In addition, testing the water soluble formulation (5 ppm) in naturally infected poultry farm (20,000 birds), showed the same anticoccidial effect observed when using Toltrazuril, as a treatment for coccidiosis. In conclusion, addition of Diclazuril at the dose of 5 ppm in the drinking water of naturally coccidia infected bird induced the same effect as 25 ppm of Toltrazuril as a treatment for coccidiosis in chickens.
The pharmacokinetics of enrofloxacin was compared in healthy chickens, Eimeria infected chickens and in Eimeria infected chickens pre-treated with amprolium or toltrazuril following a single IV and oral administration at dose 10 mg/kg. The blood samples were taken after administration at different time intervals (5 min to 24 hours) to determine the pharmacokinetic parameters of enrofloxacin. The different concentrations of enrofloxacin were determined by using HPLC assay method. Serum concentrations versus time were analysed by a noncompartmental method. The results explored a significant decrease in serum concentrations of enrofloxacin at different time intervals and a significant change in pharmacokinetic profiles in Eimeria infected chickens compared with those values in healthy chickens whereas, amprolium improves these values. Toltrazuril leads to a significant decrease in enrofloxacin concentrations compared with infected non-treated chickens. Multiple-dose study revealed a longer withdrawal period of enrofloxacin in infected non-treated and infected chickens pre-treated with amprolium compared with the healthy group.
This study investigated the comparative serum disposition kinetics of ivermectin (IVM) after a single subcutaneous dose of 200 microg/kg body weight of IVM alone or in combination with an anthelmintic consisting of ivermectin and rafoxanide (200 microg/kg of IVM and 2.5 mg/kg rafoxanide) for use in calves and sheep. The IVM concentrations in serum samples were analyzed by high-performance liquid chromatography with fluorescence detection. In sheep serum, rafoxanide induced a rapid absorption of IVM when given in combined form manifested by a shorter absorption half-life time of IVM by 68.49% when given in combination as compared with IVM when given alone. In addition, there is an increase in the value of the area under the concentration curve (AUC) by 15.48% while the value of elimination rate constant was decreased by 38.2% and significantly increased the half-life time of elimination from 2.04 days for IVM alone to 3.3 days when given in combination with rafoxanide. In calves serum, the mean t1/2ab for IVM/rafoxanide was 0.131 days and for the control formulation 0.16 days, and t1/2el was 5.78 and 4.95, respectively. IVM Cmax for IVM/rafoxanide was 22.4 ng/ml and for the control formulation 19.1 ng/ml. T (max) values were 0.99 and 1.12 days, and the mean AUC values were 188.9 and 165.4 ng/ml/day. The difference in Cmax, AUC, Kab, K el, and t1/2el was significant. However, there was no statistical difference between the Tmax and t1/2ab. These findings revealed that the combination of rafoxanide with IVM in sheep and calves increased the absorption of IVM and delayed its elimination.
An efficient one-pot synthesis of N 2-(tetrazol-5-yl)-6-aryl/heteroaryl-1,3,5-triazine-2,4-diamine derivatives was developed by reacting 5-amino-1,2,3,4-tetrazole with aromatic aldehydes and cyanamide in pyridine under controlled microwave heating with high yields. X-ray crystallography confirmed the structure of the obtained products.
A comparative pharmacokinetic study of three enrofloxacin injectable solutions was carried out in six healthy Barky rams after intramuscular injection according to a single dose, randomized, crossover experimental design. The three formulations were enrofloxacin 10% (Baytril(®)), enrofloxacin 10% plus bromhexine 1% (Mucotryl(®)) and enrofloxacin 10 % solution without bromhexine (Mucotryl without bromhexine). The three formulations were given a single intramuscular dose at a dose rate of 5 mg kg(-1) b.wt. The concentrations of the drug in the serum were measured using high-performance liquid chromatography (HPLC) with fluorescence detection. The results indicate that there were no significant differences between the distribution rate constant (k(ab)) and distribution half-life (t(1/2ab)), the maximum serum concentration (C(max)) and the time to peak concentration (T(max)) between Baytril and the other two formulations. There were significant differences between the elimination half life (t(1/2el)) and elimination rate constant (k(el)), for Baytril and enrofloxacin (the exact formulation of Mucotryl without bromhexine). Enrofloxacin was rapidly absorbed following IM administration of 5 mg kg(-1) b. wt. The peak serum concentrations (C(max)) were 2.83, 2.45 and 3.12 µg ml(-1) and were attained at (t(max)) 1.15, 1.41 and 1.26 hours when given Mucotryl, Baytril and enrofloxacin (the exact formulation of Mucotryl without bromhexine) to sheep, respectively. The injectable formulations investigated were bioequivalent after their intramuscular injection to sheep at recommended dose rate. As our results showed that, values of T(max), C(max) and AUC (Area under time curve concentration) determined for both Baytril, Mucotryl, and enrofloxacin (the exact formulation of Mucotryl without bromhexine ( reference ant test products) are within the acceptable range of 0.80-1.20, this means that the tested products product under investigation was bio-equivalent. These findings showed that the efficacy of the two test formulations was similar or possibly enhanced compared with Baytril based on the pharmacokinetic parameters obtained and due to concentration dependent activity of enrofloxacin.
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