Development, characterization and pharmacokinetics of mupirocin-loaded nanostructured lipid carriers (NLCs) for intravascular administration

Alcantara, Khent Primo; Zulfakar, Mohd Hanif; Castillo, Agnes L.

doi:10.1016/j.ijpharm.2019.118705

Cited by 28 publications

(14 citation statements)

References 39 publications

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“…High cost and time taken for new drug discovery also make the area of AMA research more uninteresting. 2 One of the alternatives is the reformulation of AMA to attain flexibility in application. In 1971, a researcher had isolated a novel antibacterial agent mupirocin (MP) ( 9 (Fig.…”

Section: Introductionmentioning

confidence: 99%

“…5 The drug was also found to have an elimination half-life of 20 to 40 min. 2 The noninvasive transdermal route may be an alternative for delivering MP for improved therapeutic efficacy. The route also provides ease of self-administration and removal of therapy at any time course of treatment.…”

Section: Introductionmentioning

confidence: 99%

“…Solid lipid nanoparticles (SLNs) had emerged as an alternative delivery system with a lack of the abovementioned problems of liposomes, but drug expulsion during the storage of SLNs led to poor drug loading. 2,6 Consequently, the development of nanostructured lipid carriers (NLCs) seems to be an attractive approach system to control the problem of drug expulsion. NLCs are composed of physiological and biodegradable solid lipids in which the core is dispersed with liquid lipids to minimize the possibility of polymorphic changes and recrystallization.…”

Section: Introductionmentioning

confidence: 99%

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Fabrication of Mupirocin-Loaded Nanostructured Lipid Carrier and Its In Vitro Characterization

Singh

Sharma

Gaur³

et al. 2021

ASSAY and Drug Development Technologies

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In the present study, mupirocin (MP), an antimicrobial agent, was formulated as a nanostructured lipid carrier (NLC) by using a novel method named as melt emulsion ultrafiltration method. For the formulation of NLC, glyceryl monostearate and watermelon seed oil were used as solid and liquid lipids, respectively. The method was optimized for various parameters by Taguchi design of experiment and prepared NLCs were characterized for particle size, polydispersity index (PDI), shape, zeta potential, % drug loading, and in vitro release profile. The optimized NLCs were found to be smooth, monodisperse with PDI 0.229 -0.093. NLCs were found to have an average particle size of 139 -0.75 nm and +21.9 -0.98 mV as zeta potential. The % drug loading of optimized NLCs was found to be 59% -0.13%. The optimized NLCs were able to release the drug up to 24 h. The release kinetic study revealed mixed-order kinetics. Hence, it was concluded that the novel method is simple and able to fabricate MP-loaded NLCs with sustained release property and being stable in terms of particle size, PDI, and % drug loading.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Fabrication of Mupirocin-Loaded Nanostructured Lipid Carrier and Its In Vitro Characterization

Singh

Sharma

Gaur³

et al. 2021

ASSAY and Drug Development Technologies

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“…We incorporated deoxycholic acid into the nanoformulations to obtain a negative charge of -39 mV. This value was advantageous in showing sufficient storage stability because a zeta potential of > 30 or <-30 mV indicates good electrostatic stabilization [37]. The high rate of rolipram encapsulation in the NLCs was attributed to the high lipophilicity of this compound, which allowed it to be retained in the lipid cores of the NLCs.…”

Section: Discussionmentioning

confidence: 99%

Multifunctional lipid-based nanocarriers with antibacterial and anti‐inflammatory activities for treating MRSA bacteremia in mice

Liao

Yang

et al. 2021

J Nanobiotechnol

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Background Bacteremia-induced sepsis is a leading cause of mortality in intensive care units. To control a bacterial infection, an immune response is required, but this response might contribute to organ failure. Kidneys are one of the main organs affected by bacteremia. Combination therapies with antibacterial and anti-inflammatory effects may be beneficial in treating bacteremia. This study aimed to develop nanostructured lipid carriers (NLCs) loaded with ciprofloxacin and rolipram that exert a combination of anti-methicillin-resistant Staphylococcus aureus (MRSA) and anti-inflammatory effects. Retinol was incorporated into the nanoparticles to transport retinol-binding protein 4 (RBP4) to the kidneys, which abundantly express RBP receptors. The NLCs were fabricated by high-shear homogenization and sonication, and neutrophils were used as a model to assess their anti-inflammatory effects. Mice were injected with MRSA to establish a model of bacteremia with organ injury. Results The mean nanoparticle size and zeta potential of the NLCs were 171 nm and − 39 mV, respectively. Ciprofloxacin (0.05%, w/v) and rolipram (0.02%) achieved encapsulation percentages of 88% and 96%, respectively, in the nanosystems. The minimum bactericidal concentration of free ciprofloxacin against MRSA increased from 1.95 to 15.63 µg/ml when combined with rolipram, indicating a possible drug-drug interaction that reduced the antibacterial effect. Nanoparticle inclusion promoted the anti-MRSA activity of ciprofloxacin according to time-kill curves. The NLCs were found to be largely internalized into neutrophils and exhibited superior superoxide anion inhibition than free drugs. Retinol incorporation into the nanocarriers facilitated their efficient targeting to the kidneys. The NLCs significantly mitigated MRSA burden and elastase distribution in the organs of MRSA-infected animals, and the greatest inhibition was observed in the kidneys. Bacterial clearance and neutrophil infiltration suppression attenuated the bacteremia-induced cytokine overexpression, leading to an improvement in the survival rate from 22% to 67%. Conclusions The dual role of our NLCs endowed them with greater efficacy in treating MRSA bacteremia than that of free drugs.

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“…Liposomes are promising carrier systems for the targeted administration of substances in biomedical applications. They are used to deliver drugs such as small interfering ribonucleic acids, to prevent NPs degradation and to target specific cell types [13][14][15]. Additionally, the directed combination of organic and inorganic particulate systems has several advantages.…”

Section: Introductionmentioning

confidence: 99%

Tackling Complex Analytical Tasks: An ISO/TS-Based Validation Approach for Hydrodynamic Chromatography Single Particle Inductively Coupled Plasma Mass Spectrometry

et al. 2020

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Nano-carrier systems such as liposomes have promising biomedical applications. Nevertheless, characterization of these complex samples is a challenging analytical task. In this study a coupled hydrodynamic chromatography-single particle-inductively coupled plasma mass spectrometry (HDC-spICP-MS) approach was validated based on the technical specification (TS) 19590:2017 of the international organization for standardization (ISO). The TS has been adapted to the hyphenated setup. The quality criteria (QC), e.g., linearity of the calibration, transport efficiency, were investigated. Furthermore, a cross calibration of the particle size was performed with values from dynamic light scattering (DLS) and transmission electron microscopy (TEM). Due to an additional Y-piece, an online-calibration routine was implemented. This approach allows the calibration of the ICP-MS during the dead time of the chromatography run, to reduce the required time and enhance the robustness of the results. The optimized method was tested with different gold nanoparticle (Au-NP) mixtures to investigate the characterization properties of HDC separations for samples with increasing complexity. Additionally, the technique was successfully applied to simultaneously determine both the hydrodynamic radius and the Au-NP content in liposomes. With the established hyphenated setup, it was possible to distinguish between different subpopulations with various NP loads and different hydrodynamic diameters inside the liposome carriers.

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Development, characterization and pharmacokinetics of mupirocin-loaded nanostructured lipid carriers (NLCs) for intravascular administration

Cited by 28 publications

References 39 publications

Fabrication of Mupirocin-Loaded Nanostructured Lipid Carrier and Its In Vitro Characterization

Fabrication of Mupirocin-Loaded Nanostructured Lipid Carrier and Its In Vitro Characterization

Multifunctional lipid-based nanocarriers with antibacterial and anti‐inflammatory activities for treating MRSA bacteremia in mice

Tackling Complex Analytical Tasks: An ISO/TS-Based Validation Approach for Hydrodynamic Chromatography Single Particle Inductively Coupled Plasma Mass Spectrometry

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