Optimum conditions for efficient phagocytosis of rifampicin-loaded PLGA microspheres by alveolar macrophages

Hirota, Keiji; Hasegawa, Taizo; Hinata, Hideyuki; Ito, Fuminori; Inagawa, Hiroyuki; Kochi, Chie; Soma, Gen‐Ichiro; Makino, Kimiko; Terada, Hiroshi

doi:10.1016/j.jconrel.2007.01.013

Cited by 154 publications

(103 citation statements)

References 46 publications

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“…The AR-12/MPs used in this study showed an encapsulation efficiency similar to that in our previous work (29) and were shown to be 265 nm in diameter (Fig. 1), which is an ideal size for uptake via macrophages but not by nonphagocytic cells (36)(37)(38). Particle formulation through sonication generates a polydispersed particle population; however, Champion et al noted that the main determinant for uptake by macrophages is shape, and thus, polydispersed particle populations of the same shape that lie within the optimal uptake range for macrophages should be taken up at similar rates (38).…”

Section: Discussionsupporting

confidence: 79%

Needle-Free Delivery of Acetalated Dextran-Encapsulated AR-12 Protects Mice from Francisella tularensis Lethal Challenge

Hoang

Curry

Collier

et al. 2016

Antimicrob Agents Chemother

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Section: Discussionsupporting

confidence: 79%

Needle-Free Delivery of Acetalated Dextran-Encapsulated AR-12 Protects Mice from Francisella tularensis Lethal Challenge

Hoang

Curry

Collier

et al. 2016

Antimicrob Agents Chemother

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“…Macrophage cells are able to ingest large particles having a diameter between 1 m and 10 m to eliminate invaders from outside the body [13,14]. The optimal sizes of the particles for the uptake by alveolar macrophages range between 3 m and 6 m [15], but those by peritoneal macrophages and peripheral blood mononuclear cells are reportedly from 0.3 m to 1.1 m [16][17][18]. The uptake mechanism of the particles, such as 3-m particles, was interpreted by the Derjaguin-Landau-Verwey-Overbeek (DLVO) theory [19].…”

Section: Particle Sizementioning

confidence: 99%

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

Hirota¹,

Terada²

2012

Molecular Regulation of Endocytosis

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“…Achieving an effective concentration of drug by oral administration and a complete cure is complicated by the difficulty of delivering drugs to the sites deep within the lungs where Mycobacterium tuberculosis resides. Several studies have attempted to improve the delivery of drugs into the lungs [19][20][21][22][23][24][25][26][27][28][29][30][31][32][33]. Such targeted delivery of drugs is expected to improve the treatment of TB, decrease the necessary doses, and reduce systemic sideeffects.…”

Section: Introductionmentioning

confidence: 99%

Application of a Four-fluid Nozzle Spray Drier to Prepare Inhalable Rifampicin-containing Mannitol Microparticles

2008

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Abstract. The purpose of this study was to use a four-fluid nozzle spray drier as a new one-step method for preparing rifampicin (RFP)-containing mannitol microparticles. A RFP-acetone/methanol (2:1) solution and aqueous solutions of mannitol (MAN) were simultaneously supplied through different liquid passages of a four-fluid nozzle spray drier and then dried to obtain MAN microparticles containing RFP. Using a cascade impactor, the in vitro aerosol performance of RFP powder and RFP-MAN microparticles with 1:5, 1:10, and 1:20 ratios was compared. The in vivo retention of RFP in the lungs of rats after intratracheal administration of 1:20 RFP-MAN microparticles was also compared. The RFP-MAN microparticles had better aerosol performance than RFP powder and delivery to the lung stages improved as the fraction of MAN was increased. For the 1:20 RFP-MAN microparticles, deposition in stages 2-7 was approximately 43%, which is sufficient for treatment. Approximately 8% of the RFP-MAN microparticles were deposited in stages 6-7, which corresponds to alveoli containing alveolar macrophages. The initial retention of RFP in the lung following pulmonary delivery of 1:20 RFP-MAN microparticles was higher than following oral or intravenous administration of RFP, but the elimination was rapid, resulting in the disappearance of RFP from the lung within 4 h. The plasma concentrationtime profile of RFP after intratracheal administration of 1:20 RFP-MAN microparticles was consistent with the profile for RFP retention in the lung. Addition of cholesterol or phosphatidylcholine to RFP had little effect on its retention in the lung. The RFP-MAN microparticles were effective for delivery of RFP to the lung, but the RFP rapidly removed from the lung into the blood circulation. This study demonstrated that RFP-containing MAN microparticles prepared in one step using the four-fluid nozzle spray drier efficiently deliver RFP to the lung, although methods must be developed to prolong its retention and improve targeting to alveolar macrophages.

show abstract

Optimum conditions for efficient phagocytosis of rifampicin-loaded PLGA microspheres by alveolar macrophages

Cited by 154 publications

References 46 publications

Needle-Free Delivery of Acetalated Dextran-Encapsulated AR-12 Protects Mice from Francisella tularensis Lethal Challenge

Needle-Free Delivery of Acetalated Dextran-Encapsulated AR-12 Protects Mice from Francisella tularensis Lethal Challenge

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

Application of a Four-fluid Nozzle Spray Drier to Prepare Inhalable Rifampicin-containing Mannitol Microparticles

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