Properties of poly(lactic-co-glycolic acid) nanospheres containing protease inhibitors: Camostat mesilate and nafamostat mesilate

Yin, Jiahui; Noda, Yoichi; Yotsuyanagi, Toshihisa

doi:10.1016/j.ijpharm.2006.01.047

Cited by 19 publications

(10 citation statements)

References 21 publications

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“…Since chitosan-TPP microparticles were prepared using coacervation procedure, it was easy to entrap hydrophilic small molecules of vancomycin and cefazolin into the microparticles in both the processes (encapsulation and coating procedure). High encapsulation efficiencies (Table 1) were obtained in this study in comparison with other studies where water-in-oil-in water (w/o/w) double emulsion procedures were used, wherein it is difficult to achieve high encapsulation efficiency due to high solubility of drug in the external phase, as a result majority of the drug diffuses to the external phase during emulsion and solvent evaporation process [40]. The drugs were incorporated in two ways - encapsulation and coating (adsorption) to determine their influence on the release profiles of both the drugs.…”

Section: Discussionmentioning

confidence: 51%

Effect of dual delivery of antibiotics (vancomycin and cefazolin) and BMP-7 from chitosan microparticles on Staphylococcus epidermidis and pre-osteoblasts in vitro

Mantripragada

Jayasuriya

2016

Materials Science and Engineering: C

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The main aims of this manuscript are to: i) determine the effect of commonly used antibiotics to treat osteoarticular infections on osteoblast viability, ii) study the dual release of the growth factor (BMP-7) and antibiotics (vancomycin and cefazolin) from chitosan microparticles iii) demonstrate the bioactivity of the antibiotics released in vitro on Staphylococcus epidermidis. The novelty of this work is dual delivery of growth factor and antibiotic from the chitosan microparticles in a controlled manner without affecting their bioactivity. Cefazolin and vancomycin have different therapeutic concentrations for their action in vivo and therefore, two different concentrations of the drugs were used. Osteoblast cytotoxicity test concluded that cefazolin concentrations of 50 and 100 μg/ml were found to have positive influence on osteoblast proliferation. A significant increase in osteoblast proliferation was observed in the presence of cefazolin and BMP-7 in comparison with BMP-7 alone group; indicating cefazolin might play a role in osteoblast proliferation. On the other hand, vancomycin concentration of 1000 μg/ml was found to significantly reduce (p < 0.01) osteoblast proliferation in comparison with controls. The microbial study indicated that cefazolin at a minimum concentration of 21.5 μg/ml could inhibit ~85% growth of S. epidermidis, whereas vancomycin at a concentration of 30 μg/ml was found to inhibit ~80% bacterial growth.

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Section: Discussionmentioning

confidence: 51%

Effect of dual delivery of antibiotics (vancomycin and cefazolin) and BMP-7 from chitosan microparticles on Staphylococcus epidermidis and pre-osteoblasts in vitro

Mantripragada

Jayasuriya

2016

Materials Science and Engineering: C

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“…However, microspheres prepared using the W/O/W method (Gallarate et al, 2009;Liu et al, 2006;Mun et al, 2010;Yin et al, 2006) have two major problems: a low drug loading efficiency and burst release behavior (Freiberg et al, 2004;Huang and Brazel, 2001;Park et al, 1992a, b;Wang et al, 1991).…”

Section: Resultsmentioning

confidence: 99%

Sustained release of isoniazid from polylactide microspheres prepared using solid/oil drug loading method for tuberculosis treatment

Zhang

Liu

Zhang

et al. 2016

Sci. China Life Sci.

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Polylactide (PLA) microspheres were prepared using the solid-in-oil (S/O) spray-drying method to achieve the sustained release of a hydrophilic drug for the treatment of tuberculosis, via intratracheal instillation. Isoniazid (IN), a low-molecular-weight hydrophilic drug, was used as a model drug. The effects of various sizes of micronized IN powder, different drug/polymer ratios, spray-drying process parameters, and drug-release characteristics were studied to optimize the manufacturing parameters. A high entrapment efficiency (87.3%) was obtained using this method; furthermore, the microspheres were spherical and smooth. They were individually and homogenously distributed, with a mean diameter of 5.6 μm; furthermore, they showed a satisfactory extended sustained-release phase. After administration of the microspheres to rats, pulmonary drug concentrations were maintained at a relatively stable level for up to 4 weeks.

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“…This two-phase release profile of PLGA nanospheres, characterized by an initial burst release followed by a sustained slow release, indicated that DOXY was dispersed in a polymeric matrix inside the PLGA nanospheres. [41, 42] The initial burst release was reduced with the increase of the PLGA LA/GA ratio and the PLGA molecular weight. PLGA85-142K NS-scaffolds with the lowest burst release and the longest release period was selected for in vitro anti-bacterial test.…”

Section: Resultsmentioning

confidence: 99%

“…[32, 33] While water-in-oil-in-water (w/o/w) double emulsion method can be readily used to entrap proteins into nanospheres, it is difficult to entrap very hydrophilic small molecules such as doxycycline into NS with an acceptable encapsulation efficiency (less than 5% showed in Table 3) since the high solubility of the drug in the external phase and its small size makes it easy for the majority of the drug to diffuse to the external phase during the emulsion and solvent evaporation process and results in very low encapsulation efficiency. [42] Some researchers made modifications to w/o/w method [23] or used other encapsulation method [21] to achieve a higher DOXY encapsulation efficiency. However, the EE increase was limited and the size of the spheres obtained became much larger, usually in the range 100 μm.…”

Section: Discussionmentioning

confidence: 99%

Novel antibacterial nanofibrous PLLA scaffolds

Feng

Sun

Bradley

et al. 2010

Journal of Controlled Release

126

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In order to achieve high local bioactivity and low systemic side effects of antibiotics in the treatment of dental, periodontal and bone infections, a localized and temporally controlled delivery system is crucial. In this study, a three-dimensional (3D) porous tissue engineering scaffold was developed with the ability to release antibiotics in a controlled fashion for long-term inhibition of bacterial growth. The highly soluble antibiotic drug, Doxycycline (DOXY), was successfully incorporated into PLGA nanospheres using a modified water-in-oil-in-oil (w/o/o) emulsion method. The PLGA nanospheres (NS) were then incorporated into prefabricated nanofibrous PLLA scaffolds with a well interconnected macroporous structure. The release kinetics of DOXY from four different PLGA NS formulations on a PLLA scaffold was investigated. DOXY could be released from the NS-scaffolds in a locally and temporally controlled manner. The DOXY release is controlled by DOXY diffusion out of the NS and is strongly dependent upon the physical and chemical properties of the PLGA. While PLGA50-6.5K, PLGA50-64K, and PLGA75-113K NSscaffolds discharge DOXY rapidly with a high initial burst release, PLGA85-142K NS-scaffold can extend the release of DOXY to longer than 6 weeks with a low initial burst release. Compared to NS alone, the NS incorporated on a 3-D scaffold had significantly reduced the initial burst release. In vitro antibacterial tests of PLGA85 NS-scaffold demonstrated its ability to inhibit common bacterial growth (S.aureus and E.coli) for a prolonged duration. The successful incorporation of DOXY onto 3-D scaffolds and its controlled release from scaffolds extends the usage of nano-fibrous scaffolds from the delivery of large molecules such as growth factors to the delivery of small hydrophilic drugs, allowing for a broader application and a more complex tissue engineering strategy.

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Properties of poly(lactic-co-glycolic acid) nanospheres containing protease inhibitors: Camostat mesilate and nafamostat mesilate

Cited by 19 publications

References 21 publications

Effect of dual delivery of antibiotics (vancomycin and cefazolin) and BMP-7 from chitosan microparticles on Staphylococcus epidermidis and pre-osteoblasts in vitro

Effect of dual delivery of antibiotics (vancomycin and cefazolin) and BMP-7 from chitosan microparticles on Staphylococcus epidermidis and pre-osteoblasts in vitro

Sustained release of isoniazid from polylactide microspheres prepared using solid/oil drug loading method for tuberculosis treatment

Novel antibacterial nanofibrous PLLA scaffolds

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