Chemical Modification of Hydrophobic Block in Poly(Ethylene Oxide) Poly(Caprolactone) Based Nanocarriers: Effect on the Solubilization and Hemolytic Activity of Amphotericin B

Falamarzian, Arash; Lavasanifar, Afsaneh

doi:10.1002/mabi.200900387

Cited by 35 publications

(26 citation statements)

References 36 publications

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“…The resulting micelles displayed lowered CMC due to the increased rigidity and hydrophobicity of the micelle core [116]. Nevertheless, this design may significantly increase the size of polymer spheres (typically from 100 nm to the µm scale), which was reported to severely decrease the potential targeted delivery efficacy and lower the in vivo performance of the nanomedicine [30, 32, 117]. By changing the crystallinity of the hydrophobic segment, micelles with semi-crystalline core structures could be obtained.…”

Section: Strategies To Stabilize Micelles Without Crosslinkingmentioning

confidence: 99%

Strategies to improve micelle stability for drug delivery

et al. 2018

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Micelles have been studied as drug delivery carriers for decades. Their use can potentially result in high drug accumulation at the target site through the enhanced permeability and retention effect. Nevertheless, the lack of stability of micelles in the physiological environment limits their efficacy as a drug carrier. In particular, micelles tend to disassociate and prematurely release the encapsulated drugs, lowering delivery efficacy and creating toxicity concerns. Many efforts to enhance the stability of micelles have focused mainly on decreasing the critical micelle forming concentration and improving blood circulation. Herein, we review different strategies including crosslinking and non-crosslinking approaches designed to stabilize micelles and offer perspectives on future research directions.

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Section: Strategies To Stabilize Micelles Without Crosslinkingmentioning

confidence: 99%

Strategies to improve micelle stability for drug delivery

et al. 2018

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“…However, their cost has restricted widespread use (Sachs-Barrable et al, 2008; Falamarzian & Lavasanifar, 2010). AMB is also characterized by instability at gastric pH and is unable to cross the mucosal barrier of the GI tract and enter the blood stream.…”

Section: Introductionmentioning

confidence: 99%

Oral administration of amphotericin B nanoparticles: antifungal activity, bioavailability and toxicity in rats

et al. 2017

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Amphotericin B (AMB) is used most commonly in severe systemic life-threatening fungal infections. There is currently an unmet need for an efficacious (AMB) formulation amenable to oral administration with better bioavailability and lower nephrotoxicity. Novel PEGylated polylactic-polyglycolic acid copolymer (PLGA-PEG) nanoparticles (NPs) formulations of AMB were therefore studied for their ability to kill Candida albicans (C. albicans). The antifungal activity of AMB formulations was assessed in C. albicans. Its bioavalability was investigated in nine groups of rats (n ¼ 6). Toxicity was examined by an in vitro blood hemolysis assay, and in vivo nephrotoxicity after single and multiple dosing for a week by blood urea nitrogen (BUN) and plasma creatinine (PCr) measurements. The MIC of AMB loaded to PLGA-PEG NPs against C. albicans was reduced two to threefold compared with free AMB. Novel oral AMB delivery loaded to PLGA-PEG NPs was markedly systemically available compared to Fungizone Õ in rats. The addition of 2% of GA to the AMB formulation significantly (p50.05) improved the bioavailability from 1.5 to 10.5% and the relative bioavailability was4790% that of Fungizone Õ . The novel AMB formulations showed minimal toxicity and better efficacy compared to Fungizone Õ . No nephrotoxicity in rats was detected after a week of multiple dosing of AMB NPs based on BUN and PCr, which remained at normal levels. An oral delivery system of AMB-loaded to PLGA-PEG NPs with better efficacy and minimal toxicity was formulated. The addition of glycyrrhizic acid (GA) to AMB NPs formulation resulted in a significant oral absorption and improved bioavailability in rats.

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“…Higher CMC refl ected a lower thermodynamic stability of micelles according to the Gibb's free energy of micellization, [ 36 ] or indicated a lower selfassembling tendency of amphiphiles in aqueous solution. [ 37,38 ] Thus, we supposed that the introduction of PEI caused a complexation between diblock copolymer and PEI via hydrogen bonding interaction, which dramatically enhanced the hydrophilicity of copolymer and then resulted in increase of CMC.…”

Section: Resultsmentioning

confidence: 99%

Poly(ethylene imine)‐Triggered Morphological Change of Anisotropic Micelles from Direct Aqueous Self‐Assembly of an Amphiphilic Diblock Copolymer

Chen

Wang

2016

Macro Chemistry & Physics

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In this paper, “star anise”‐like anisotropic micelle (AM) from direct aqueous self‐assembly of poly(ethylene oxide)‐block‐poly(p‐dioxanone) amphiphilic diblock copolymer is presented. By adding poly(ethylene imine) (PEI), the AM shows morphological change from “star anise” to swollen sphere. The mechanism of PEI‐triggered morphological transition involving complexation and weakening of crystallizability is revealed.

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Chemical Modification of Hydrophobic Block in Poly(Ethylene Oxide) Poly(Caprolactone) Based Nanocarriers: Effect on the Solubilization and Hemolytic Activity of Amphotericin B

Cited by 35 publications

References 36 publications

Strategies to improve micelle stability for drug delivery

Strategies to improve micelle stability for drug delivery

Oral administration of amphotericin B nanoparticles: antifungal activity, bioavailability and toxicity in rats

Poly(ethylene imine)‐Triggered Morphological Change of Anisotropic Micelles from Direct Aqueous Self‐Assembly of an Amphiphilic Diblock Copolymer

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