Inhaled pyrazinamide proliposome for targeting alveolar macrophages

Rojanarat, Wipaporn; Nakpheng, Titpawan; Thawithong, Ekawat; Yanyium, Niracha; Srichana, Teerapol

doi:10.3109/10717544.2012.721144

Cited by 71 publications

(34 citation statements)

References 22 publications

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“…Permeability determination of AmB (white square), AmB-KDC (black triangle), AmB-SDC (black square), AmB-SDCS (white triangle), and AmB-SC (black circle) from 15 to 120 min, respectively (mean±SD, n=3) 600 nm were efficiently phagocytosed and, in our case, nanoparticle sizes of <100 nm were efficiently phagocytosed (25). A similar result was reported by Rojanarat et al (26). These results supported the view that AmB-SDCS lipid formulation was phagocytosed by AM NR8383 cells.…”

Section: Phagocytosis Of Anti-fungal Reconstituted Dry Powder Particlsupporting

confidence: 77%

Factors Affecting Enhanced Permeation of Amphotericin B Across Cell Membranes and Safety of Formulation

et al. 2015

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Abstract. The aim of this study was to determine amphotericin B (AmB) permeation across lipid bilayer membranes mounted on Transwell® and to observe the phagocytosis of the AmB and the AmB-lipid formulations by alveolar macrophage (AM) cell lines using a fluorescence microscope. The lipid bilayer membranes were prepared from phospholipid and ergosterol as well as phospholipid and cholesterol in a ratio (67:33 mol%). AmB-lipid formulations were prepared from AmB incorporated with four lipid derivatives during a lyophilization process. In vitro cytotoxicity studies were carried out on kidney cells by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The levels of nitric oxide production by AMs exposed to these AmB-lipid formulations were determined by the Griess reaction. Phagocytosis of the AmB-lipid formulations was carried out using AM cells. The lipid bilayer membranes and AmB-lipid formulations were successfully prepared. In vitro cytotoxicity results showed less toxicity to kidney cells than pure AmB, and a 1,000-fold less production of nitric oxide by NR8383 cell lines was obtained when compared to lipopolysaccharide. Permeation results were two-to fivefold higher than for pure AmB in the ergosterol containing lipid bilayer and two-to fourfold higher than AmB in the cholesterol containing compositions, both of which were enough to kill the fungi according to their MICs and MFCs. AM phagocytosed the AmB-lipid formulations. We suggest that these products especially the AmB-sodium deoxycholate sulfate are potential candidates for targeting AM cells for the treatment of invasive pulmonary aspergillosis.

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Section: Phagocytosis Of Anti-fungal Reconstituted Dry Powder Particlsupporting

confidence: 77%

Factors Affecting Enhanced Permeation of Amphotericin B Across Cell Membranes and Safety of Formulation

et al. 2015

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“…Results of in vivo toxicity studies showed that capreomycin oleate exhibited its lowest toxic potential suggesting it be used as super generics in pulmonary tuberculosis treatment [73]. Outcomes of various miscellaneous lipid based drug delivery systems in the treatment of TB are summarized in Table 6 [74][75][76][77][78][79][80][81][82][83][84][85][86].…”

Section: Miscellaneous Lipid Based Formulationsmentioning

confidence: 99%

Exploring the Use of Lipid Based Nano-Formulations for the Management of Tuberculosis

Cm¹,

Cd²,

M³

et al. 2017

J Nanosci Curr Res

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Tuberculosis (TB) is an airborne infectious disease spreading very fast from person to person, which affect the health as well as socioeconomic conditions harshly. Though varieties of antitubercular drugs (ATDs) are available for its treatment, associated stern side effects restrict the patients to receive complete therapeutic benefits. Moreover, emergence of drug-resistant tuberculosis and co-infection of TB with HIV further worsen the situations. Polymeric formulations are introduced for progressive and long-term delivery of therapeutic agents, but owing to their noted limitations, performance is not up to the mark. In this juxtaposition, lipid based nano-formulations are introduced as an alternative to the polymic formulations in the management of TB with an intention to overcome side effects related to drugs along with limitations of polymeric formulations. The lipid based formulations comprise nanoemulsions, solid-lipid nanoparticles (SLNs), nano-structured lipid carriers (NLCs), liposomes, and niosomal systems, etc.Liposomes have more promising antitubercular activity as its intended for targeted drug delivery especially to the infected part. Further mannosylation of liposomes offers tremendous results in TB chemotherapy as it directly binds to mannose receptors available on the surface of alveolar macrophages resulting mycobacterium destruction. Niosomes may have superior drug targeting ability, chemical stability, osmotic activeness and in vivo activity in comparison to that of liposomes. SLNs and manosylated SLNs are the advanced form of the lipid formulations which enhance the drug uptake at the infected organ and show significant in vivo anti-tubercular activity with reduced toxicity. Moreover, NLCs shows its satisfactory potential against MTb along with drug targeting action. Advancement on the development of miscellaneous or other vesicular lipid formulations are not encouraging in the field of tubercular chemotherapy. Hence, lipid based formulations could be successfully employed for targeted delivery of ATDs with promising anti-tubercular activity.

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“…8,10,[21][22][23] The adjusted doses of the four drugs are 2-7 times of the calculated doses according to different drug potency (2-16 mg). These were done to compromise the feasible fixed dose combination of anti-TB for inhalation which should not be too high or too low.…”

Section: )mentioning

confidence: 99%

“…The dry powder formulations used in this study were formulated using liposomal-based drug delivery systems to target the alveolar macrophages. 7,8,10,19) …”

mentioning

confidence: 99%

“…However, first-line anti-TB drugs used for inhalation have been evaluated for their safety only in cell lines and with some in vivo animal models. [7][8][9][10] Clinical trials are crucial to completely evaluate the effects of anti-TB drugs on the lungs and to establish a successful therapeutic route to achieve maximum recovery from TB. Clinical trial phase I carried out with capreomycin to treat highly drug resistant TB, indicated that inhalation of capreomycin was safe and advisable for TB therapy.…”

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confidence: 99%

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Evaluation of Proinflammatory Cytokines and Adverse Events in Healthy Volunteers upon Inhalation of Antituberculosis Drugs

Srichana

Ratanajamit

Juthong

et al. 2016

Biological & Pharmaceutical Bulletin

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Inhalation therapy is a promising drug delivery approach for tuberculosis treatment. However, there is always concern about the safety of the dosage form by inhalation as it may induce inflammation. Developing a new dosage form for inhalation must include tests for its safety especially for the tumor necrosis factor (TNF)-α and interleukine (IL)-1β. The safety of four anti-tuberculosis (anti-TB) drugs administered via inhalation was assessed in healthy volunteers. Four anti-TB drugs; isoniazid, rifampicin, pyrazinamide and levofloxacin were prepared as dry powder and evaluated for uniformity of delivered dose and in vitro drug deposition. These four anti-TB dry powder formulations for inhalation met the criteria of uniformity of delivered dose and exhibited suitable size for lung delivery. Forty healthy volunteers were recruited and each was sequentially challenged with isoniazid, rifampicin, pyrazinamide and levofloxacin in different orders. Safety was monitored by measuring the pro-inflammatory cytokines in their sputum, lung function test, blood chemistry and adverse events. This study proves that all four anti-TB dry powders did not provoke inflammatory cytokines and are safe to healthy volunteers.

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Inhaled pyrazinamide proliposome for targeting alveolar macrophages

Abstract: We suggest that PZA-proliposomes are potential candidates for pulmonary tuberculosis treatment.

Cited by 71 publications

References 22 publications

Factors Affecting Enhanced Permeation of Amphotericin B Across Cell Membranes and Safety of Formulation

Factors Affecting Enhanced Permeation of Amphotericin B Across Cell Membranes and Safety of Formulation

Exploring the Use of Lipid Based Nano-Formulations for the Management of Tuberculosis

Evaluation of Proinflammatory Cytokines and Adverse Events in Healthy Volunteers upon Inhalation of Antituberculosis Drugs

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