Leucinostatin-A loaded nanospheres: characterization and in vivo toxicity and efficacy evaluation

Ricci, Maurizio; Blasi, Paolo; Giovagnoli, Stefano; Perioli, Luana; Vescovi, Claudia; Róssi, Carlo

doi:10.1016/j.ijpharm.2004.01.030

Cited by 21 publications

(10 citation statements)

References 27 publications

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“…Poly(lactic-co-glycolic acid) (PLGA) ( Figure 1) is a completely amorphous polymer largely used for medical and pharmaceutical applications. Because of its biocompatibility and biodegradability, it has been successfully used as base material to produce parenteral drug delivery systems (DDS) such as microparticles, 1,2 nanoparticles, 3 pellets, 4 slabs, 4 and in situ forming devices. 4 Amorphous polymers are thermally characterized by the presence of the transition temperature (Tg), which is the transition point between a highly viscous brittle structure called glassy state and a less viscous, more mobile, rubbery state.…”

Section: Introductionmentioning

confidence: 99%

Ketoprofen poly(lactide-co-glycolide) physical interaction

et al. 2007

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The aim of this work was to provide an understanding of the interaction occurring between ketoprofen and poly(lactic-co-glycolic acid) (PLGA) that leads to polymer plasticization. Experimental glass transition temperature (Tg) values were fitted with the theoretical ones predicted by the Fox and Gordon-Taylor/Kelley-Bueche equations. PLGA films containing different amounts of ketoprofen (KET) were prepared by solvent casting and characterized by scanning electron microscopy, differential scanning calorimetry, and Fourier transform infrared spectroscopy (FTIR). Differential scanning calorimetry evidenced that KET acted as a plasticizer in a similar biphasic way in both end-capped and uncapped PLGA. At KET contents of 20% to 35%, depending on the investigated polymer, the Tg was around 23 degrees C. Higher KET amounts did not lower further the Tg, and the excess of drug was found to crystallize into the polymeric matrix. Experimental Tg's deviated negatively from the predicted ones probably because of hydrogen bonding. The FTIR spectra of the films, loaded with different amounts of KET, showed a shift to higher wavenumbers for the peaks at 1697 and 1655 cm(-1) confirming the presence of some interactions, probably hydrogen bonds between the ketoprofen carboxylic group and the PLGA carbonyl groups along the polymer backbone. The hydrogen bonding between KET and PLGA is probably responsible for KET plasticizing effect. KET behaving as a lubricant may disrupt polymer chain-chain interactions, removing additional barriers to bond rotation and chain mobility.

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Section: Introductionmentioning

confidence: 99%

Ketoprofen poly(lactide-co-glycolide) physical interaction

et al. 2007

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“…[1][2][3][4][5][6][7][8] A common polymer used in the formulation of nanospheres and microspheres is the biodegradable, biocompatible polymer, polylactic-co-glycolic acid (PLGA). [5][6][7][8][9] This research is a part of the overall study of the effect of the mean diameter of the particulate delivery systems on the cellular accumulation, cytotoxicity, and efficacy of paclitaxel.…”

Section: Introductionmentioning

confidence: 99%

Particle size and temperature effect on the physical stability of PLGA nanospheres and microspheres containing Bodipy

Robinson²

2004

AAPS PharmSciTech

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The purpose of this study was to investigate the effect of particle size, storage temperature, and duration of storage on the physical stability and morphology of polylactic-co-glycolic acid (PLGA) nanospheres and microspheres. PLGA nanospheres and microspheres containing the fluorescent dye, Bodipy, were prepared in varying sizes by controlling the method and degree of agitation during the emulsification phase of preparation. Mean diameters of the particles were measured by dynamic light scattering. To evaluate the effect of storage temperature and duration of storage on the extent of aggregation, nanospheres and microspheres were stored at 4°C, 25°C, 37°C, and 50°C for 6 days and then monitored using both confocal and scanning electron microscopy. The mean ± SD diameters of PLGA particles containing Bodipy were: 266.9 ± 2.8, 351.6 ± 1.8, 988.8 ± 14.1, and 1865.9 ± 67.0 nm. The extent of aggregation of the particulate delivery system decreased as the mean diameter increased, and increased as the storage temperature increased. The maximum extent of aggregation was observed with the smallest (266 nm) nanospheres. Microspheres did not aggregate. The aggregation of nanospheres was significantly reduced by introducing an additional evaporation step during preparation, suggesting that migration of residual dichloromethane from within the nanospheres may have dissolved the PLGA on the surface. The extent of aggregation of nanospheres increased as the temperature was increased from 4°C to 50°C, and decreased as particle size increased. To avoid aggregation, PLGA nanospheres should be stored at 4°C.

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“…In the case of leucinostatin A, it has been reported that leucinostatin A-loaded nanospheres show anti-Candida albicans activity both in vitro and in vivo, but with drastic reduction of toxicity. 52 The above results reveal that leucinostatin A and B, alamethicin I and tsushimycin are promising lead compounds for a new type of antitrypanosomal activity. Further investigation of the antitrypanosomal potential of these peptide antibiotics is in progress.…”

Section: Discussionmentioning

confidence: 83%

In vitro and in vivo antitrypanosomal activities of three peptide antibiotics: leucinostatin A and B, alamethicin I and tsushimycin

et al. 2009

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In the course of our screening for antitrypanosomal compounds from soil microorganisms, as well as from the antibiotics library of the Kitasato Institute for Life Sciences, we found three peptide antibiotics, leucinostatin (A and B), alamethicin I and tsushimycin, which exhibited potent or moderate antitrypanosomal activity. We report here the in vitro and in vivo antitrypanosomal properties and cytotoxicities of leucinostatin A and B, alamethicin I and tsushimycin compared with suramin. We also discuss their possible mode of action. This is the first report of in vitro and in vivo trypanocidal activity of leucinostatin A and B, alamethicin I and tsushimycin.

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Leucinostatin-A loaded nanospheres: characterization and in vivo toxicity and efficacy evaluation

Cited by 21 publications

References 27 publications

Ketoprofen poly(lactide-co-glycolide) physical interaction

Ketoprofen poly(lactide-co-glycolide) physical interaction

Particle size and temperature effect on the physical stability of PLGA nanospheres and microspheres containing Bodipy

In vitro and in vivo antitrypanosomal activities of three peptide antibiotics: leucinostatin A and B, alamethicin I and tsushimycin

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