Delivery of rifampicin–PLGA microspheres into alveolar macrophages is promising for treatment of tuberculosis

Hirota, Keiji; Hasegawa, Taizo; Nakajima, Taro; Inagawa, Hiroyuki; Kohchi, Chie; Soma, Gen‐Ichiro; Makino, Kimiko; Terada, Hiroshi

doi:10.1016/j.jconrel.2009.11.020

Cited by 115 publications

(89 citation statements)

References 28 publications

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“…If efficient particle uptake is not associated with the induction of the undesirable responses, the particles could be very useful as drug carriers. As summarized in Table 1, PLGA particles are those having such a desirable silent nature regarding inflammatory responses, although they are yet well phagocytosed by macrophages compared with polystyrene latex (PSL) particles [34,37]. Namely, the PLGA particle behaves like a "Ninja," having stealth and concealment activities.…”

Section: Induction Of Inflammatory Responses By Endocytosismentioning

confidence: 99%

“…These data are summarized from reports [34,37]. Rat alveolar macrophage cells (NR8383) were exposed to PLGA and PSL particles at a number 10 times greater than the cell number.…”

Section: Plga Psl Lpsmentioning

confidence: 99%

“…PLGA microspheres containing RFP (RFP-PLGA) were prepared by various methods such as double-emulsification and spray-drying. The PLGA MS thus prepared deliver an amount of RFP into rat alveolar macrophage NR8383 cells in vitro about 20 times greater than that added in the free form in solution [12,37]. Inhalation of PLGA MS containing the antitubercular agent rifabutin increases the drug residence time in the lungs to more than that by intravenous administration in mice due to uptake of the particles by alveolar phagocytic cells [91].…”

Section: Endocytosis-mediated Drug Actionmentioning

confidence: 99%

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Endocytosis of Particle Formulations by Macrophages and Its Application to Clinical Treatment

Hirota¹,

Terada²

2012

Molecular Regulation of Endocytosis

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Section: Induction Of Inflammatory Responses By Endocytosismentioning

confidence: 99%

“…These data are summarized from reports [34,37]. Rat alveolar macrophage cells (NR8383) were exposed to PLGA and PSL particles at a number 10 times greater than the cell number.…”

Section: Plga Psl Lpsmentioning

confidence: 99%

Section: Endocytosis-mediated Drug Actionmentioning

confidence: 99%

See 1 more Smart Citation

Endocytosis of Particle Formulations by Macrophages and Its Application to Clinical Treatment

Hirota¹,

Terada²

2012

Molecular Regulation of Endocytosis

Self Cite

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“…This approach also has the potential to reduce antibiotic resistance and Rif adverse effects, such as hepatotoxicity. New drug delivery methods that have been evaluated with Rif include; liposomes [1], PLGA microparticles [2,3], nanoparticles [4], and dendrimers [5]. These systems have been shown effective for enhancement of drug delivery to macrophages in vitro, but an improved method for effective in vivo delivery of Rif has yet to be found.…”

Section: Introductionmentioning

confidence: 99%

Glucan Particle Encapsulated Rifampicin for Targeted Delivery to Macrophages

et al. 2010

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Glucan particles (GPs) are 2-4 m spherical, hollow, porous shells extracted from Baker's yeast, Saccharomyces cerevisae. The surface of the GPs is composed primarily of 1,3--glucan and the particles are efficiently phagocytosed via receptor-mediated cell uptake by macrophages, phagocytic cells expressing glucan receptors. The hollow cavity of the GPs allows for efficient absorption and encapsulation of payload molecules. Rifampicin (Rif), a drug used in tuberculosis treatment, was encapsulated by precipitation in GPs and trapped using a calcium alginate or chitosan hydrogel to seal the pores of GPs and slow Rif release. Unplugged GP formulations immediately released Rif following particle resuspension in aqueous buffer. Alginate and chitosan sealing of GPs loaded with Rif was able to extend drug release for 24-72 h. GP-Rif formulations containing 10% w/w Rif/GP plugged with a calcium alginate hydrogel were effective at reducing colony forming units of M. tuberculosis strain mc 2 6020 in infected bone marrow macrophages ~80-90% at 24 and 72 hours. The amount of Rif delivered in the GP formulations was below the free Rif minimal inhibitory concentration demonstrating that GP targeted Rif delivery to macrophages enhances Rif antimicrobial effects. OPEN ACCESSPolymers 2010, 2 682

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“…To eradicate these intracellular infections, directly targeting to the macrophages could be a highly effective strategy. Much research has been performed to study the potential of PLGA microparticles and nanoparticles to target the alveolar macrophages, as they may remain membrane bound onto the alveolar macrophages for up to 2 weeks [231][232][233][234][235][236][237][238][239]. Makino et al showed the phagocytic uptake of rifampicin encapsulated in PLGA nanoparticles.…”

Section: Macrophage Targetingmentioning

confidence: 99%

A New Era of Pulmonary Delivery of Nano-antimicrobial Therapeutics to Treat Chronic Pulmonary Infections

Merchant

Buckton²,

Taylor³

et al. 2016

CPD

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Pulmonary infections may be fatal especially in immunocompromised patients and patients with underlying pulmonary dysfunction, such as those with cystic fibrosis, chronic obstructive pulmonary disorder, etc. According to the WHO, lower respiratory tract infections ranked first amongst the leading causes of death in 2012, and tuberculosis was included in the top 10 causes of death in low income countries, placing a considerable strain on their economies and healthcare systems. Eradication of lower respiratory infections is arduous, leading to high healthcare costs and requiring higher doses of antibiotics to reach optimal concentrations at the site of pulmonary infection for protracted periods. Hence direct inhalation to the respiratory epithelium has been investigated extensively in the past decade, and seems to be an attractive approach to eradicate and hence overcome this widespread problem. Moreover, engineering inhalation formulations wherein the antibiotics are encapsulated within nanoscale carriers could serve to overcome many of the limitations faced by conventional antibiotics, like difficulty in treating intracellular pathogens such as mycobacteria spp. and salmonella spp., biofilmassociated pathogens like Pseudomonas aeruginosa and Staphylococcus aureus, passage through the sputum associated with disorders like cystic fibrosis and chronic obstructive pulmonary disorder, systemic side effects following oral/parenteral delivery and inadequate concentrations of antibiotic at the site of infection leading to resistance. Encapsulation of antibiotics in nanocarriers may help in providing a protective environment to combat antibiotic degradation, confer controlled-release properties, hence reducing dosing frequency, and may increase uptake via specific and non-specific targeting modalities. Hence nanotechnology combined with direct administration to the airways using commercially available delivery devices, is a highly attractive formulation strategy to eradicate microorganisms from the lower respiratory tract, which might otherwise present opportunities for multi-drug resistance.

show abstract

Delivery of rifampicin–PLGA microspheres into alveolar macrophages is promising for treatment of tuberculosis

Cited by 115 publications

References 28 publications

Endocytosis of Particle Formulations by Macrophages and Its Application to Clinical Treatment

Endocytosis of Particle Formulations by Macrophages and Its Application to Clinical Treatment

Glucan Particle Encapsulated Rifampicin for Targeted Delivery to Macrophages

A New Era of Pulmonary Delivery of Nano-antimicrobial Therapeutics to Treat Chronic Pulmonary Infections

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