Enhancement of antibacterial activity of tilmicosin against Staphylococcus aureus by solid lipid nanoparticles in vitro and in vivo

Wang, X.F.; Zhang, S.L.; Zhu, Luyan; Xie, Shuyu; Zhao, Dong; Wang, Y.; Zhou, Wenzhong

doi:10.1016/j.tvjl.2010.11.019

Cited by 80 publications

(56 citation statements)

References 21 publications

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“…The plasma concentration of enrofloxacin after enrofloxacin SLNs administration in emus showed biphasic release pattern. The initial fast (burst release) release of the drug could be due to desorption and diffusion of enrofloxacin accumulated at the oil-water interface and in the outer shell of nanoparticles (Xie et al 2008;Muller et al 2000;Han et al 2009;Wang et al 2011). The initial release should be sufficiently rapid to * For C max , a value of 14.755 lg/mL (mean peak plasma concentration at 5 min) was used for the calculation ensure that therapeutic drug levels are achieved in a timely manner in vivo.…”

Section: Discussionmentioning

confidence: 99%

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

Kumar¹,

Arivuchelvan²,

Jagadeeswaran³

et al. 2014

Appl Nanosci

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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.

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Section: Discussionmentioning

confidence: 99%

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

Kumar¹,

Arivuchelvan²,

Jagadeeswaran³

et al. 2014

Appl Nanosci

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“…7 The control nanoparticles were treated similarly as blanks for the measurements. The assay was repeated three times using different samples from independent preparations.…”

Section: Determination Of Drug Loadingmentioning

confidence: 99%

“…[7][8][9] A pharmacokinetics study examining what occurs following its subcutaneous administration in mice demonstrated that this formulation shows significantly longer systemic circulation, greater bioavailability, and lower maximum serum concentration than native tilmicosin. 8 A subsequent mouse mastitis study indicated that the TMS-HCO-NP formulation has enhanced antibacterial activity and therapeutic efficacy at a lower dose and frequency than tilmicosin alone.…”

Section: Introductionmentioning

confidence: 99%

“…8 A subsequent mouse mastitis study indicated that the TMS-HCO-NP formulation has enhanced antibacterial activity and therapeutic efficacy at a lower dose and frequency than tilmicosin alone. 7 A lower peak tilmicosin concentration may account for the reduced acute toxicity of TMS-HCO-NP. 9 Solid lipid nanoparticles (SLN) are colloidal drug delivery systems that can be prepared as either aqueous dispersions (suspensions) or dry powders.…”

Section: Introductionmentioning

confidence: 99%

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Preparation and evaluation of tilmicosin-loaded hydrogenated castor oil nanoparticle suspensions of different particle sizes

Chen¹,

Wang²,

Lu³

et al. 2014

IJN

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Three tilmicosin-loaded hydrogenated castor oil nanoparticle (TMS-HCO-NP) suspensions of different particle sizes were prepared with different polyvinyl alcohol surfactant concentrations using a hot homogenization and ultrasonic technique. The in vitro release, in vitro antibacterial activity, mammalian cytotoxicity, acute toxicity in mice, and stability study were conducted to evaluate the characteristics of the suspensions. The in vitro tilmicosin release rate, antibacterial activity, mammalian cytotoxicity, acute toxicity in mice, and stability of the suspensions were evaluated. When prepared with polyvinyl alcohol concentrations of 0.2%, 1%, and 5%, the mean diameters of the nanoparticles in the three suspensions were 920±35 nm, 452±10 nm, and 151±4 nm, respectively. The three suspensions displayed biphasic release profiles similar to that of freeze-dried TMS-HCO-NP powders, with the exception of having a faster initial release. Moreover, suspensions of smaller-sized particles showed faster initial release, and lower minimum inhibitory concentrations and minimum bactericidal concentrations. Time-kill curves showed that within 12 hours, the suspension with the 151 nm particles had the most potent bactericidal activity, but later, the suspensions with larger-sized particles showed increased antibacterial activity. None of the three suspensions were cytotoxic at clinical dosage levels. At higher drug concentrations, all three suspensions showed similar concentration-dependent cytotoxicity. The suspension with the smallest-sized particle showed significantly more acute toxicity in mice, perhaps due to faster drug release. All three suspensions exhibited good stability at 4°C and at room temperature for at least 6 months. These results demonstrate that TMS-HCO-NP suspensions can be a promising formulation for tilmicosin, and that nanoparticle size can be an important consideration for formulation development.

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“…Methods of evaluating antimicrobial activity of nanostructure materials can be divided into quantitative and qualitative methods. Microorganisms are often evaluated in the laboratory using the methods such as Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC), disc diffusion, colony counting, turbidity assay and dilution methods (6)(7)(8)(9)(10)(11)(12).…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial Activities of the Polypropylene Imine Dendrimer Aginst Bacteria Isolated From Rural Water Resources

Jebelli

Kalantar

Maleki

et al. 2015

Jundishapur J Nat Pharm Prod

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Background: Dendrimers are a new class of polymeric materials with the well-defined structure, composition and architecture. Owing to antibacterial properties of dendrimers, they can be used as alternative water and wastewater disinfection with the minimum adverse side effects. Objectives: The aim of the present study was to evaluate the antibacterial activity of second generation poly propylene imine (PPI-G2) dendrimer on predominant bacteria in drinking water resources. Materials and Methods:In this qualitative and interventional study, a total of 764 water samples were collected from rural areas in Qom Province, Iran, and bacteria were isolated and identified using standard procedures. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against gram-positive and gram-negative bacteria were determined according to clinical and laboratory standards institute (CLSI) guideline. Standard discs were prepared using different concentrations of dendrimer on MuellerHinton agar plates. Results:The most important isolated bacteria were Escherichia coli 37 (48.7%), Klebsiella oxytoca 12 (15.8%), Proteus mirabilis 3 (4%), Entrobacter aerogenes 8 (10.5%), Citrobacter freundii 4 (5.2%), Pseudomonas aeruginosa 5 (6.6%), Staphylococcus aureus 2 (2.6%), and Bacillus subtilis 5 (6.6%). Moreover, it was found that PPI-G2 showed more potent activity towards the gram-positive bacteria than the gram-negative ones. Conclusions:The PPI-G2 dendrimer with end amine groups exhibited a positive impact on the removal of dominant bacterial isolated strains. Therefore, it is possible to use these nanodendrimers as a safe and effective material for water disinfection in the future.

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Enhancement of antibacterial activity of tilmicosin against Staphylococcus aureus by solid lipid nanoparticles in vitro and in vivo

Cited by 80 publications

References 21 publications

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

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

Preparation and evaluation of tilmicosin-loaded hydrogenated castor oil nanoparticle suspensions of different particle sizes

Antimicrobial Activities of the Polypropylene Imine Dendrimer Aginst Bacteria Isolated From Rural Water Resources

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