Efficient intracellular delivery of rifampicin to alveolar macrophages using rifampicin-loaded PLGA microspheres: effects of molecular weight and composition of PLGA on release of rifampicin

Makino, Kimiko; Nakajima, Taro; Shikamura, Mitsuhiko; Ito, Fuminori; Ando, Shuji; Kochi, Chie; Inagawa, Hiroyuki; Soma, Gen Ichiro; Terada, Hiroshi

doi:10.1016/j.colsurfb.2004.03.018

Cited by 130 publications

(96 citation statements)

References 13 publications

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“…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%

“…Poly (lactic-glycolic) acid (PLGA) is one of the candidates for drug-containing particle formulations, because PLGA is biodegradable and biocompatible [11]. Drug release from the particles and its sustainability can be regulated by changing the molecular weight and composition of the lactate and glycolate moieties of PLGA [12].…”

Section: Effect Of Particle Properties On Endocytosismentioning

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

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Section: Endocytosis-mediated Drug Actionmentioning

confidence: 99%

Section: Effect Of Particle Properties On Endocytosismentioning

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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“…16 One of the advantages of this polymer is that by regulating the lactide to glycolide ratio the degradation rate can be regulated. 17,18 5-FU-loaded PLGA microspheres have been developed and studied for stereotactic intracerebral implantation in C6 glioma bearing rats with very promising results as far as survival, welfare, and future applications were forecast. [19][20][21] Although 5-FU-loaded microparticles are envisaged as having great potential for drug delivery, their suitability for directing the drug to the tissues or cells via systemic circulation or mucous membrane remain hindered due to their large size.…”

Section: Introductionmentioning

confidence: 99%

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

K¹,

Jagadeeshan²,

Nair³

et al. 2011

IJN

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Nanoscaled devices have great potential for drug delivery applications due to their small size. In the present study, we report for the first time the preparation and evaluation of antitumor efficacy of 5-fluorouracil (5-FU)-entrapped poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles with dependence on the lactide/glycolide combination of PLGA. 5-FU-loaded PLGA nanoparticles with two different monomer combinations, 50-50 and 90-10 were synthesized using a modified double emulsion method, and their biological evaluation was done in glioma (U87MG) and breast adenocarcinoma (MCF7) cell lines. 5-FU-entrapped PLGA 50-50 nanoparticles showed smaller size with a high encapsulation efficiency of 66%, which was equivalent to that of PLGA 90-10 nanoparticles. Physicochemical characterization of nanoparticles using differential scanning calorimetry and X-ray diffraction suggested the presence of 5-FU in molecular dispersion form. In vitro release studies showed the prolonged and sustained release of 5-FU from nanoparticles with both the PLGA combinations, where PLGA 50-50 nanoparticles showed faster release. Nanoparticles with PLGA 50-50 combination exhibited better cytotoxicity than free drug in a dose- and time-dependent manner against both the tumor cell lines. The enhanced efficiency of PLGA 50-50 nanoparticles to induce apoptosis was indicated by acridine orange/ethidium bromide staining. Cell cycle perturbations studied using flow cytometer showed better S-phase arrest by nanoparticles in comparison with free 5-FU. All the results indicate that PLGA 50-50 nanoparticles possess better antitumor efficacy than PLGA 90-10 nanoparticles and free 5-FU. Since, studies have shown that long-term exposure of ailing tissues to moderate drug concentrations is more favorable than regular administration of higher concentration of the drug; our results clearly indicate the potential of 5-FU-loaded PLGA nanoparticles with dependence on carrier combination as controlled release formulation to multiplex the therapeutic effect of cancer chemotherapy.

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“…Monodispersed poly-lactic-co-glycolic acid (PLGA) microspheres containing rifampicin have been prepared by solvent evaporation method (Makino et al, 2004, Yoshida et al, 2006. The microspheres were spherical and their average diameter was about 2 μm.…”

Section: Polymeric Microparticles For Tuberculosis Treatmentmentioning

confidence: 99%

Polyurethane as Carriers of Antituberculosis Drugs

Batyrbekov¹,

Iskakov²

2012

Polyurethane

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Efficient intracellular delivery of rifampicin to alveolar macrophages using rifampicin-loaded PLGA microspheres: effects of molecular weight and composition of PLGA on release of rifampicin

Cited by 130 publications

References 13 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

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

Polyurethane as Carriers of Antituberculosis Drugs

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