“…In vitro release data obtained under sink conditions are consistent with drug release reported from different SLNs by Ji et al (2011) and Xie et al (2011b). The initial fast release (burst effect) could be attributed to the presence of a small fraction of unentrapped drug or drug embedded near the SLNs surface.…”
The study was conducted to formulate the enrofloxacin solid lipid nanoparticles (SLNs) with sustained release profile and improved pharmacological activity and evaluate the pharmacokinetic behaviour of enrofloxacin SLNs after oral routes of administration in emus. The SLNs were prepared using tripalmitin as lipid carrier, Tween 80 and Span 80 as surfactants and polyvinyl alcohol (PVA) as a stabilizer by a hot homogenization coupled with ultrasonication method. The prepared enrofloxacin SLNs formulations were characterized for further investigation in emu birds. The pharmacokinetics of native enrofloxacin was studied after i.v. and oral bolus administration at 10 mg/kg in emu birds and compared with the disposition kinetics of enrofloxacin SLNs. Enrofloxacin and its metabolite ciprofloxacin in plasma were estimated using HPLC and the pharmacokinetic parameters were calculated by a noncompartmental analysis. The results demonstrated that the particle size, polydispersity index, zeta potential, encapsulation efficiency and loading capacity of the SLNs were 154.72 ± 6.11 nm, 0.42 ± 0.11, -28.83 ± 0.60 mV, 59.66 ± 3.22 and 6.13 ± 0.32 %, respectively. AFM and TEM images showed spherical to circular particles with well-defined periphery. In vitro drug release exhibited biphasic pattern with an initial burst release of 18 % within 2 h followed by sustained release over 96 h. Pharmacokinetic results showed that the t 1/2b , AUC 0-? , V darea /F, MRT and bioavailability were 3.107, 1.894, 1.594, 2.993 and 1.895 times enhanced (p \ 0.01), while CL B and b were significantly (p \ 0.01) decreased by 1.958 and 3.056 times compared to the values of native enrofloxacin administered orally. The ratio of AUC 0-t cipro/AUC 0-t enro after administration of native enrofloxacin and enrofloxacin SLNs was less than 10 %. The t 1/2b and MRT of the metabolite were longer than those of the parent substance. The PK/PD results confirmed that the SLNs extended the enrofloxacin concentration upto 48 h against pathogens susceptible to 0.125 lg/mL in emus. The results indicated that SLNs might be a promising delivery system to prolong and enhance the pharmacological activity of enrofloxacin.
“…In vitro release data obtained under sink conditions are consistent with drug release reported from different SLNs by Ji et al (2011) and Xie et al (2011b). The initial fast release (burst effect) could be attributed to the presence of a small fraction of unentrapped drug or drug embedded near the SLNs surface.…”
The study was conducted to formulate the enrofloxacin solid lipid nanoparticles (SLNs) with sustained release profile and improved pharmacological activity and evaluate the pharmacokinetic behaviour of enrofloxacin SLNs after oral routes of administration in emus. The SLNs were prepared using tripalmitin as lipid carrier, Tween 80 and Span 80 as surfactants and polyvinyl alcohol (PVA) as a stabilizer by a hot homogenization coupled with ultrasonication method. The prepared enrofloxacin SLNs formulations were characterized for further investigation in emu birds. The pharmacokinetics of native enrofloxacin was studied after i.v. and oral bolus administration at 10 mg/kg in emu birds and compared with the disposition kinetics of enrofloxacin SLNs. Enrofloxacin and its metabolite ciprofloxacin in plasma were estimated using HPLC and the pharmacokinetic parameters were calculated by a noncompartmental analysis. The results demonstrated that the particle size, polydispersity index, zeta potential, encapsulation efficiency and loading capacity of the SLNs were 154.72 ± 6.11 nm, 0.42 ± 0.11, -28.83 ± 0.60 mV, 59.66 ± 3.22 and 6.13 ± 0.32 %, respectively. AFM and TEM images showed spherical to circular particles with well-defined periphery. In vitro drug release exhibited biphasic pattern with an initial burst release of 18 % within 2 h followed by sustained release over 96 h. Pharmacokinetic results showed that the t 1/2b , AUC 0-? , V darea /F, MRT and bioavailability were 3.107, 1.894, 1.594, 2.993 and 1.895 times enhanced (p \ 0.01), while CL B and b were significantly (p \ 0.01) decreased by 1.958 and 3.056 times compared to the values of native enrofloxacin administered orally. The ratio of AUC 0-t cipro/AUC 0-t enro after administration of native enrofloxacin and enrofloxacin SLNs was less than 10 %. The t 1/2b and MRT of the metabolite were longer than those of the parent substance. The PK/PD results confirmed that the SLNs extended the enrofloxacin concentration upto 48 h against pathogens susceptible to 0.125 lg/mL in emus. The results indicated that SLNs might be a promising delivery system to prolong and enhance the pharmacological activity of enrofloxacin.
“…This study provides valuable evidence for the practicable use of the Weibull model in drug release phenomena from swellable polymeric nanoparticles. Likely there are also several studies have experimentally investigated that, the release data from swellable polymeric nanoparticles fit best with the weibull model (Yang et al, 2000;Adibkia et al, 2007;Aksungur et al, 2011;Ji et al, 2011;Bei et al, 2012;Azadi et al, 2013;Sun et al, 2014;Liu et al, 2015;Ashrafi and Azadi, 2016;Jafari-Aghdam et al, 2016). Among the studied models, Weibull is regarded as a favorable model which includes parameters that are sensitive to ranges of release profile.…”
Section: Resultsmentioning
confidence: 91%
“…For more identification, when β=1, the shape of curve becomes an exponential profile. If β has a higher value than 1, the curve gets sigmoidal form and finally with the β lower than 1 the equation provides parabolic model (Kalam et al, 2007). It is obvious that the external condition is capable to influence the release kinetic and be determined by the shape parameter as well (vanBoekel, 2002).…”
This study aims to provide a comparative mathematical analysis of drug release from swellable polymeric delivery systems to find a general model applicable to multi-mechanistic release. Drug release data from various swellable polymeric nanoparticles extracted from the literatures were applied to the eight conventional models. Coefficient of determination (R 2 ) and absolute percent error (E%) were calculated for each set as well as the overall error (OE), the number of error (NE) and the akaike information criterion (AIC) for all sets. The model has the highest R 2 and the number of the error, as well as both the lowest overall error (OE) and the akaike information criterion, was considered as the best one. Among the models Weibull (W) model produced R 2 and OE values of 0.93 and 8.79, respectively. Also, the AIC value and the number of errors less than 5% for the model was -34.93 and 46.15% of a total number of data sets respectively. Mathematical modeling of drug release from a carrier is often attempted to recognize the main determinants of the drug release rate from the carrier with the final goal of the identification of the ideal set of conditions leading to the desired release profile in vivo.
“…1. There are many pores in chitosan molecules which can absorb SA directly (Ji et al 2011). When the added dosages of algicide were 15, 20, 25, 32, 40, 55 and 70 mg, the increasing trend of the release concentration in the initial adding stage was quite fast, but it became a smooth trend at 12 h. The release rates at 48 h were 74, 69, 67, 60, 56 and 51 %, respectively.…”
In this paper, the effects of salicylic acid (SA) algicide carried by cross-linked chitosan on the inhibition of Microcystis flos-aquae and the removal ability of heavy metals Pb and Ni in compound polluted water were studied. The results showed that the algicide had significant inhibitory effects on Microcystis flos-aquae: when the concentrations were 550 and 700 mg L -1 , the inhibition time was up to 13 days or more, and the inhibition rate was as high as 99 %. The algicide exhibited strong adsorption capacity to heavy metals Pb and Ni. The adsorption rates of the algicide at concentrations of 400 and 550 mg L -1 on Ni and Pb were 61 and 64.9 %, 71.2 and 72.5 % at 13 days, respectively. The algicide allows a slow release of SA and long-term inhibition of algae and has better adsorption capacity on heavy metals, thus providing a method for the effective control of eutrophication and combined heavy metal pollution in water.
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