A mannose-conjugated multi-layered polymeric nanocarrier system for controlled and targeted release on alveolar macrophages

Praphakar, Rajendran Amarnath; Shakila, Harshavardhan; Dusthackeer, V.N. Azger; Munusamy, Murugan A.; Kumar, Suresh; Rajan, Mariappan

doi:10.1039/c7py02000g

Cited by 25 publications

(12 citation statements)

References 32 publications

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“…Furthermore, the lungs have comparatively low local metabolic activity and, thereby, show no or limited first pass metabolism [ 17 ]. Finally, alveolar macrophages can be targeted for management of pulmonary TB [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

Pulmonary Targeting of Inhalable Moxifloxacin Microspheres for Effective Management of Tuberculosis

et al. 2021

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In the present study, the objective was to attain a localized lung delivery of an anti-tubercular fluoroquinolone, moxifloxacin (MXF), targeting the alveolar macrophages through a non-invasive pulmonary route using inhalable microspheres as a dry powder inhaler approach. MXF-loaded poly (lactic-co-glycolic acid) (PLGA) microspheres (MXF-PLGA-MSs) were fabricated by solvent evaporation technique and optimized by using a central composite statistical design. The morphology and particle size, as well as the flowability of the optimized microspheres, were characterized. In addition, the aerosolization performance of the optimized formula was inspected using an Andersen cascade impactor. Furthermore, in vivo fate following intrapulmonary administration of the optimized formula was evaluated. The optimized MXF-PLGA-MSs were spherical in shape with a particle size of 3.16 µm, drug loading of 21.98% and entrapment efficiency of 78.0%. The optimized formula showed a mass median aerodynamic diameter (MMAD) of 2.85 ± 1.04 µm with a favorable fine particle fraction of 72.77 ± 1.73%, suggesting that the powders were suitable for inhalation. Most importantly, in vivo studies revealed that optimized MXF-PLGA-MSs preferentially accumulated in lung tissue as manifested by a two-fold increase in the area under the curve AUC0–24h, compared to plain drug. In addition, optimized MXF-PLGA-MS sustained drug residence in the lung for up to 24 h following inhalation, compared to plain drug. In conclusion, inhalable microspheres of MXF could be a promising therapeutic approach that might aid in the effective eradiation of tuberculosis along with improving patient adherence to the treatment.

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Section: Introductionmentioning

confidence: 99%

Pulmonary Targeting of Inhalable Moxifloxacin Microspheres for Effective Management of Tuberculosis

et al. 2021

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“…Several studies demonstrated the possibility of using CNTs as a nanocarrier for TB drug delivery and were conducted to overcoming on antibacterial resistance of TB. 15,28 One study in 2019 reported that chitosan-functionalized CNTs could increase the drug permeability of INH in the treatment of TB in the bone and wound tissues. 33 Also, Barros et al, 34 demonstrated the efficacy of naphthoimidazoles together with INH and rifampin, as the main drugs for controlling tuberculosis.…”

Section: Conclusion and Future Perspectivementioning

confidence: 99%

“…13 Therefore, the importance of CNTs has been recognized in the pharmaceutical industry. 12,14,15 Multiwall carbon nanotubes (MWCNTs), as drug carriers, should first be functionalized to enhance the biological function. Induction of carboxyl and chlorine on MWCNTs could increase the carrying capacity and reduce the complications symptoms on healthy cells.…”

Section: Introductionmentioning

confidence: 99%

<p>The Effects Study of Isoniazid Conjugated Multi-Wall Carbon Nanotubes Nanofluid on <em>Mycobacterium tuberculosis</em></p>

Zomorodbakhsh¹,

Abbasian²,

Naghinejad³

et al. 2020

IJN

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Background: Tuberculosis (TB) has always been recognized as one of the fatal infectious diseases, which is caused by Mycobacterium tuberculosis (M.tb). Isonicotinic acid hydrazide or isoniazid (INH) is one of the most commonly utilized drugs in the treatment of TB. Patients need to take 300 mg daily of INH for 6 months in combination with another anti-TB drug and tolerate several side effects of INH. On the other hand, the emergence of resistant strains of anti-TB antibiotics is one of the major problems in the treatment of this disease. So, antimicrobial drug delivery by nanofluids could improve the efficacy, and reduce the adverse effects of antimicrobial drugs. The purpose of this study was to perform a novel method to synthesize INH-conjugated multi-wall carbon nanotubes (MWCNTs) for more effective drug delivery, as well as, TB treatment. Methods: INH-conjugated functionalized MWCNTs were prepared, using a reflux system. The characterization of the obtained nano-drug was performed by the elemental analyses of total nitrogen, hydrogen, carbon and sulfur (CHNS), Raman spectroscopy, Fourier transform infrared (FTIR), transmission electron microscopy (TEM), and scanning electron microscopy (SEM) methods. The nanofluid of nano-drug was prepared by the ultrasonic method, and the related antibacterial effect studies were carried out on the two strains of M.tb. Results: The antimicrobial effect of INH-conjugated MWCNTs was found to be much better at low concentrations than the pure drug in all of the strains. Conclusion: Since one of the main antimicrobial mechanisms of MWCNTs is through the destruction of the bacterial cell wall, in addition to its antimicrobial effects, it increased the drug delivery of INH at lower doses compared to drug alone. So, the nanofluid, containing INH-conjugated MWCNTs, had a better lethal effect on a variety of M.tb strains than that of the drug alone.

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“…Praphakar et al synthesized am annose-conjugated multilayered polymericd rug-delivery system based on chitosan and sodium alginatec omprising two anti-TB chemotherapeutics, rifampicin(RF) and isoniazid (INH). [87] Thismannose-coated delivery system allows the efficient macrophage-targeting delivery, the combination of multiple anti-TB agents with enhanced oral bioavailability,a nd drug release in as ustained manner.S imilarly,S arwar et al and Chaubeye tal. both developed anti-VL-reagent-loaded mannosylated nanocarriersf or receptor-mediated macrophage targeting with bettert herapeutic indexes.…”

Section: Mannose-based Nanomaterials In Other Applicationsmentioning

confidence: 99%

“…Praphakar et al. synthesized a mannose‐conjugated multilayered polymeric drug‐delivery system based on chitosan and sodium alginate comprising two anti‐TB chemotherapeutics, rifampicin (RF) and isoniazid (INH) . This mannose‐coated delivery system allows the efficient macrophage‐targeting delivery, the combination of multiple anti‐TB agents with enhanced oral bioavailability, and drug release in a sustained manner.…”

Section: Mannose‐based Nanomaterials In Biomedical Applicationsmentioning

confidence: 99%

Mannose‐Functionalized Nanoscaffolds for Targeted Delivery in Biomedical Applications

Wei

Seeberger

et al. 2018

Chemistry An Asian Journal

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Targeted drug delivery by nanomaterials has been extensively investigated as an effective strategy to surmount obstacles in the conventional treatment of cancer and infectious diseases, such as systemic toxicity, low drug efficacy, and drug resistance. Mannose‐binding C‐type lectins, which primarily include mannose receptor (MR, CD206) and dendritic cell‐specific intercellular adhesion molecule‐3‐grabbing non‐integrin (DC‐SIGN), are highly expressed on various cancer cells, endothelial cells, macrophages, and dendritic cells (DCs), which make them attractive targets for therapeutic effect. Mannosylated nanomaterials hold great potential in cancer and infection treatment on account of their direct therapeutic effect on targeted cells, modulation of the tumor microenvironment, and stimulation of immune response through antigen presentation. This review presents the recent advances in mannose‐based targeted delivery nanoplatforms incorporated with different therapies in the biomedical field.

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A mannose-conjugated multi-layered polymeric nanocarrier system for controlled and targeted release on alveolar macrophages

Abstract: To improve the performance of drug delivery systems in macrophages, targeted ligand-conjugated polymeric carriers have been realized to be vital for targeted, sustainable and controlled drug release with remarkable biocompatibility and bioavailability.

Cited by 25 publications

References 32 publications

Pulmonary Targeting of Inhalable Moxifloxacin Microspheres for Effective Management of Tuberculosis

Pulmonary Targeting of Inhalable Moxifloxacin Microspheres for Effective Management of Tuberculosis

<p>The Effects Study of Isoniazid Conjugated Multi-Wall Carbon Nanotubes Nanofluid on <em>Mycobacterium tuberculosis</em></p>

Mannose‐Functionalized Nanoscaffolds for Targeted Delivery in Biomedical Applications

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