Lipid Microsphere Formulation Containing Rifampicin Targets Alveolar Macrophages

Takenaga, Mitsuko; Ohta, Yuki; Tokura, Yukie; Hamaguchi, Akemi; Igarashi, Rie; Disratthakit, Areeya; Doi, Norio

doi:10.1080/10717540801952530

Cited by 24 publications

(12 citation statements)

References 29 publications

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“…These microparticles exhibited sustained release of isoniazid, RIF and pyrazinamide for 3-5 days in plasma and up to 9 days in organs (Ul-Ain et al, 2003). Very recently, lipid microspheres containing RIF were showed to deliver the drug to alveolar macrophages in vitro and in vivo, and that intranasal administration to animals could achieve preferential accumulation in the lungs with less effect on the liver (Takenaga et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Microencapsulation of antibiotic rifampicin in poly(3-hydroxybutyrate-co-3-hydroxyvalerate)

et al. 2008

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The aim of this study was the preparation of microparticles containing rifampicin using a biodegradable polymer poly(3-hydroxybutyrate-co-3-hydroxyvalerate) for oral administration produced by a bacteria. The poly(3-hydroxybutyrate-co-3-hydroxyvalerate) microparticles with and without rifampicin were prepared by the emulsification and solvent evaporation method, in which chloroform and polyvinyl alcohol are used as the solvent and emulsifier, respectively. Microparticles were obtained within a size range of 20-60 microm by changing the initial poly(3-hydroxybutyrate-co-3-hydroxyvalerate), polyvinyl alcohol and rifampicin concentrations. An encapsulation efficiency value of 14% was obtained. The optimized total yield of 60% of the poly(3-hydroxybutyrate-co-3-hydroxyvalerate)/ rifampicin was obtained. A load of 0.035 mg/1 mg of PHBV was reached. Almost 90% of the drug loaded in the microparticles was released after 24 h. The size, encapsulation efficiency and ribampicin release of the microparticles varied as a function of the initial poly(3-hydroxybutyrate-co-3-hydroxyvalerate), polyvinyl alcohol and rifampicin concentrations. It was demonstrated that the microencapsulated rifampicin, although was not totally available in the medium, exhibited a similar inhibition value as free rifampicin at 24 h of incubation with S. aureus. Cytotoxicity assays demonstrated a reduction of the toxicity when rifampicin was microencapsulated in poly(3-hydroxybutyrate-co-3-hydroxyvalerate) while maintaining its antibacterial activity.

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Section: Introductionmentioning

confidence: 99%

Microencapsulation of antibiotic rifampicin in poly(3-hydroxybutyrate-co-3-hydroxyvalerate)

et al. 2008

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“…The LM-RFP was prepared and characterized as described previously by Takenaga et al (2008). Briefly, the primary RFP suspension was prepared by homogenization of the mixture of RFP (50 or 60 mg; Wako Pure Chemicals Ltd., Osaka, Japan), soybean oil (1 g; Nisshin Oillio, Kanagawa, Japan) and soybean phosphatidylcholine (120 mg; Nisshin Oillio, Kanagawa, Japan) at 15 000 rpm for 5 min.…”

Section: Lipid Microspheres Formulationmentioning

confidence: 99%

“…The LM-RFP are easily uptaken into alveolar macrophages and concentrated in lungs with a smaller distribution in livers after being administered intranasally compared to non-encapsulated RFP (Takenaga et al 2008). Another clinical usefulness of lipid microsphere-prostaglandin E 1 injection for peripheral vascular diseases treatment is known to increase the drug concentration in inflammatory tissue and decrease the side-effects (Shen et al 2005).…”

Section: Introductionmentioning

confidence: 98%

Anti-tuberculosis activity and drug interaction with nevirapine of inhalable lipid microspheres containing rifampicin in murine model

Disratthakit¹,

Doi²,

Takenaga³

et al. 2010

Journal of Microencapsulation

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Intranasal administration of lipid microspheres (LM) containing rifampicin (LM-RFP) exhibited the bacteriostatic effect against Mycobacterium tuberculosis H37Rv. The efficacies of intranasal LM-RFP in lung were markedly higher in immunodeficient BALB/c nude mice (p < 0.001), but not different in immunocompetent BALB/c mice (p = 1.000) compared to the results of oral rifampicin groups. When intranasal LM-RFP was given instead of oral rifampicin, the reductions of C(max) and AUC(0-3) of nevirapine were decreased from 32.2% to 11.9% and 30.5% to 12.4%, respectively. These results suggested that intranasal LM-RFP could improve the anti-tuberculosis activity in immunodeficient host and minimize drug interaction between rifampicin and nevirapine.

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“…Stabilization of the desired con centration of a drug in the blood and/or tissues of a patient is frequently required in order to enhance the effect of drugs. The examples of such drugs are non steroid anti inflammatory agents, antibiotics, and cytostatic preparations [6][7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Characterization of polymeric microparticles based on resorbable polyesters of oxyalkanoic acids as a platform for deposition and delivery of drugs

et al. 2012

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The effect of the preparation technique (chemical composition of a polymer, type and method of emulsion mixing, and molecular mass of a drug) on the yield, structure, and size of microparticles obtained from resorbable polyesters of microbiological origin, polyhydroxyalkanoates, is studied. It is found that the concentration of the polymer solution and the method of emulsion mixing are the most significant factors affecting the diameter of microparticles based on polyhydroxyalkanoates; the surface structure of particles depends to a higher extent on the chemical composition of the polymer. The family of microparticles from 100-200 nm to 50-70 µm in diameter is synthesized. It is shown that the rate of drug release from micropar ticles in vitro into the medium is higher in the case of 3 hydroxybutyrate copolymers with 3 hydroxyvalerate than in the case of the homopolymer of 3 hydroxybutyrate. This parameter increases with the content of 3 hydroxyvalerate units in the copolymer and the porosity and mass fraction of the drug in particles with a decrease in their sizes. For in vitro systems containing a phosphate buffer, variation in the preparation param eters makes it possible to obtain microparticles with various characteristics suitable for deposition of drugs. For microparticles obtained from polyhydroxyalkanoates and having different diameters, the mathematical description of the kinetics of drug release from the polymer matrix is provided.

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Lipid Microsphere Formulation Containing Rifampicin Targets Alveolar Macrophages

Cited by 24 publications

References 29 publications

Microencapsulation of antibiotic rifampicin in poly(3-hydroxybutyrate-co-3-hydroxyvalerate)

Microencapsulation of antibiotic rifampicin in poly(3-hydroxybutyrate-co-3-hydroxyvalerate)

Anti-tuberculosis activity and drug interaction with nevirapine of inhalable lipid microspheres containing rifampicin in murine model

Characterization of polymeric microparticles based on resorbable polyesters of oxyalkanoic acids as a platform for deposition and delivery of drugs

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