Formulation of enrofloxacin SLNs and its pharmacokinetics in emu (Dromaius novaehollandiae) birds

Abstract

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.

Enrofloxacin-Impregnated PLGA Nanocarriers for Efficient Therapeutics and Diminished Generation of Reactive Oxygen Species

“…In this study, the value of diffusion exponent ( n ) in the Korsmeyer–Peppas model was lower than 0.45, which indicated the drug release from NPs follows the behavior of Fickian diffusion. , Initial burst release of ENRO from PLGA­(ENRO)­NPs in the first few hours could be due to dissolution of the drug loaded in the NPs, which follows the Fickian diffusion. After which, low and sustained release of ENRO from the NPs can be attributed to the polymer erosion/degradation over time. , It has been reported that the diffusion of free ENRO is about 94% in first 2 h and 100% diffusion is observed within 24 h . This report of free ENRO shows that PLGA­(ENRO) NPs have sustained release over the period of 4 days.…”

Poly(N-vinylcaprolactam) containing solid lipid polymer hybrid nanoparticles for controlled delivery of a hydrophilic drug gemcitabine hydrochloride

“…Generally, formulations with zeta potential greater than +25 mV and lower than −25 mV are considered stable due to electrostatic repulsion between the particles, since lower zeta potential may cause aggregation of the particles through van der Waal interactions. 47 Particle size in the range of 238 ± 12.13 to 319 ± 12.47 nm and % encapsulation efficiency (% EE) in the range of 28 ± 4.24 to 46.5 ± 6.19 were obtained in the designed nine formulations. It was suggested by the software that quadratic model was best fitted for all the responses studied.…”

Investigation of Synthesis Parameters for Modification of Chitosan with Enrofloxacin

“…It is biodegradable and used to treat infection of urinary tract, skin and respiratory. Moreover, it has antibacterial activity against gram-positive and gram-negative bacteria [7,8]. This research has an idea to modify chitosan with enrofloxacin for increase antibacterial efficacy.…”