Amphotericin B-incorporated polymeric micelles composed of poly(d,l-lactide-co-glycolide)/dextran graft copolymer

Choi, Ki-Seok; Bang, Je-Yong; Kim, Pyoung-Il; Kim, Chan; Song, Chae-Eun

doi:10.1016/j.ijpharm.2007.12.011

Cited by 51 publications

(33 citation statements)

References 14 publications

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“…Investigators have employed different watersoluble polymers to develop encapsulated, conjugated AmBbased delivery systems, but have met with little success. [40][41][42][43][44][45][46][47][48] In some of the earlier efforts, polymers synergized the toxicity of AmB, 49 while in others the AmB was unable to retain the beneficial physicochemical properties associated with its liposomal form (AmB-L). 50 Although, AmB-cyclodextrin complexes showed improved water solubility, 49,51 they were found to be toxic to human red blood cells.…”

Section: Resultsmentioning

confidence: 99%

Self-assembled amphotericin B-loaded polyglutamic acid nanoparticles: preparation, characterization and in vitro potential against Candida albicans

Zia¹,

Khan²,

Zubair³

et al. 2015

IJN

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In the present study, we developed a self-assembled biodegradable polyglutamic acid (PGA)-based formulation of amphotericin B (AmB) and evaluated its in vitro antifungal potential against Candida albicans . The AmB-loaded PGA nanoparticles were prepared in-house and had a mean size dimension of around 98±2 nm with a zeta potential of −35.2±7.3 mV. Spectroscopic studies revealed that the drug predominantly acquires an aggregated form inside the formulation with an aggregation ratio above 2. The PGA-based AmB formulation was shown to be highly stable in phosphate-buffered saline as well as in serum (only 10%–20% of the drug was released after 10 days). The AmB–PGA nanoparticles were less toxic to red blood cells (<15% lysis at an AmB concentration of 100 μg/mL after 24 hours) when compared with Fungizone ® , a commercial antifungal product. An MTT assay showed that the viability of mammalian cells (KB and RAW 264.7) was negligibly affected at AmB concentrations as high as 200 μg/mL. Histopathological examination of mouse kidney revealed no signs of tissue necrosis. The AmB–PGA formulation showed potent antimicrobial activity similar to that of Fungizone against C. albicans . Interestingly, AmB-bearing PGA nanoparticles were found to inhibit biofilm formation to a considerable extent. In summary, AmB–PGA nanoparticles showed highly attenuated toxicity when compared with Fungizone, while retaining equivalent active antifungal properties. This study indicates that the AmB–PGA preparation could be a promising treatment for various fungal infections.

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Section: Resultsmentioning

confidence: 99%

Self-assembled amphotericin B-loaded polyglutamic acid nanoparticles: preparation, characterization and in vitro potential against Candida albicans

Zia¹,

Khan²,

Zubair³

et al. 2015

IJN

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“…A modified nanoprecipitation method was used to entrap AMB into the PLGA-TPGS NPs. 10,11 Briefly, a preweighed amount of AMB powder and 100 mg of PLGA-TPGS copolymer were dissolved in 10 mL of acetone by adding into the dispersing phase (10 mL of anhydrous ethanol), under moderate sonication and stirring at room temperature. This mixture was added into 60 mL of 0.05% nonsolvent-TPGS aqueous solution, under stirring.…”

Section: Preparation Of Amb-npsmentioning

confidence: 99%

“…[5][6][7] In addition, the stability, tissue permeability, degradation rate, and toxicity of NPs themselves are also concerns in this field. [8][9][10] The recently developed diblock copolymer D-α-tocopheryl polyethylene glycol 1000 succinate-b-poly(ε-caprolactone-ran-glycolide) (TPGS-b-(PCL-ran-PGA) [hereafter, referred to as PLGA-TPGS]) has received special attention as a promising antimicrobial agent, due to its good biocompatibility and biodegradability. 7 Therefore, the synthesis of uniform PLGA-TPGS copolymer NPs (PLGA-TPGS NPs) with specific requirements in terms of size, shape, and physical and chemical properties is of great interest in the development of new drugs.…”

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confidence: 99%

“…7 Therefore, the synthesis of uniform PLGA-TPGS copolymer NPs (PLGA-TPGS NPs) with specific requirements in terms of size, shape, and physical and chemical properties is of great interest in the development of new drugs. 8,9 A variety of studies [8][9][10] have shown they have good biocompatibility and biodegradability and excellent targeted drug delivery, but the antifungal effects of AMB-loaded PLGA-TPGS NPs (AMBNPs) are mostly unknown. In this study, AMB-NPs were synthesized, and their antifungal effects on the Candida spp.…”

mentioning

confidence: 99%

“…To determine the median lethal dose (LD 50 ), mice were intravenously treated with 0.5 mL of AMB-NPs in saline at different concentrations (10,20,40, 80, 160, 320, and 640 mg/kg, n=10 per group). The survival time of each animal was recorded up to 14 days after treatment, and the total number of dead animals was recorded, to calculate the lethal dose for 50% of animals (LD 50 ).…”

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Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo

Tang¹,

Zhu²,

Sun³

et al. 2014

IJN

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Background Amphotericin B (AMB) is a polyene antibiotic with broad spectrum antifungal activity, but its clinical toxicities and poor solubility limit the wide application of AMB in clinical practice. Recently, new drug-loaded nanoparticles (NPs) – diblock copolymer D-α-tocopheryl polyethylene glycol 1000 succinate-b-poly(ε-caprolactone-ran-glycolide) (PLGA-TPGS) – have received special attention for their reduced toxicity, and increased effectiveness of drug has also been reported. This study aimed to develop AMB-loaded PLGA-TPGS nanoparticles (AMB-NPs) and evaluate their antifungal effects in vitro and in vivo. Methods AMB-NPs were prepared with a modified nanoprecipitation method and then characterized in terms of physical characteristics, in vitro drug release, stability, drug-encapsulation efficiency, and toxicity. Finally, the antifungal activity of AMB-NPs was investigated in vitro and in vivo. Results AMB-NPs were stable and spherical, with an average size of around 110 nm; the entrapment efficacy was closed to 85%, and their release exhibited a typically biphasic pattern. The actual minimum inhibitory concentration of AMB-NPs against Candida albicans was significantly lower than that of free AMB, and AMB-NPs were less toxic on blood cells. In vivo experiments indicated that AMB-NPs achieved significantly better and prolonged antifungal effects when compared with free AMB. Conclusion The AMB-PLGA-TPGS NP system significantly improves the AMB bioavailability by improving its antifungal activities and reducing its toxicity, and thus, these NPs may become a good drug carrier for antifungal treatment.

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Synthesis of N‐benzyl‐O‐carboxymethylchitosan and application in the solubilization enhancement of a poorly water‐soluble drug (triamcinolone)

Rosa

Debrassi

Silva

et al. 2011

J of Applied Polymer Sci

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N-Benzyl-O-carboxymethyl chitosan (OCChB) was synthesized through a reaction of O-carboxymethylchitosan (OCCh) and benzaldehyde by the reductive amination method. The chemical structures and physical properties of the derivatives were confirmed by Fourier transform infrared spectroscopy and 1 H-NMR. The cytotoxicity of the polymers was tested by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay at concentrations ranging from 0.01 to 1000 lg/mL. The substitution degrees of the derivatives, calculated by 1 H-NMR, were 12 and 53% for OCChB1 and OCChB2, respectively. The results show that the derivatives were not toxic at 1000 lg/mL and could decrease the surface tension by concentration on the system surface compared with OCCh. Because of this property, OCChB was applied as a solubility enhancer for triamcinolone (TC), a poorly water-soluble drug. The polymer solutions at 1.0 mg/mL increased the TC solubility up to 3.5 times for OCChB1 and 5.0 times for OCChB2 compared with its solubility in water.

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Amphotericin B-incorporated polymeric micelles composed of poly(d,l-lactide-co-glycolide)/dextran graft copolymer

Cited by 51 publications

References 14 publications

Self-assembled amphotericin B-loaded polyglutamic acid nanoparticles: preparation, characterization and in vitro potential against Candida albicans

Self-assembled amphotericin B-loaded polyglutamic acid nanoparticles: preparation, characterization and in vitro potential against Candida albicans

Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo

Synthesis of N‐benzyl‐O‐carboxymethylchitosan and application in the solubilization enhancement of a poorly water‐soluble drug (triamcinolone)

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