In vitro characterization of PEGylated phospholipid micelles for improved drug solubilization: Effects of PEG chain length and PC incorporation

Ashok, Beena; Arleth, Lise; Hjelm, Rex P.; Rubinstein, Israel; Önyüksel, Hayat

doi:10.1002/jps.20150

Cited by 230 publications

(234 citation statements)

References 21 publications

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“…1d-f). Rod or worm-like micelles formed from the increasing ratio of phospholipid in PEGylated phospholipid have been demonstrated by the works of Hristoval et al (15) and Ashok et al (16,17), which are in agreement with our observations.…”

Section: Preparation and Characterization Of Peg-pe-based Micelles Ensupporting

confidence: 93%

Stability Influences the Biodistribution, Toxicity, and Anti-tumor Activity of Doxorubicin Encapsulated in PEG-PE Micelles in Mice

et al. 2012

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Purpose To investigate the influences of stability of doxorubicin (DOX) retained in PEG-PE/HSPC micelles on its biodistribution, toxicity and anti-tumor activity in mice. Methods We incorporated HSPC into PEG-PE micelles at various molar ratios by a self-assembly procedure. Micelles were characterized by dynamic light scattering, transmission electron microscope, atomic force microscopy. Agarose gel electrophoresis assay was used to detect stable retention of DOX in micellar preparations. Biodistribution, toxicity and antitumor activity of doxorubicin encapsulated in PEG-PE/HSPC micelles in mice were investigated. Results HSPC incorporation not only changed the size and shape of PEG-PE micelles, but also decreased the ability of DOX stable retained in PEG-PE micelles, resulting in a great discrepancy in biodistribution, toxicity and anti-tumor activity among micellar DOX preparations. DOX encapsulated in PEG-PE micelles (M 1 -DOX), with narrower size distribution and greater stability, demonstrated better cytotoxicity in vitro and low systemic toxicity with superior anti-tumor metastasis activity in vivo. Conclusions Encapsulation of DOX into PEG-PE micelles showed the best therapeutic activity and lowest systemic toxicity compared to other HSPC-incorporated PEG-PE micellar preparations. Stable retention of drugs within micelles is important and is determined by compatibility between drugs and polymer blocks.

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Section: Preparation and Characterization Of Peg-pe-based Micelles Ensupporting

confidence: 93%

Stability Influences the Biodistribution, Toxicity, and Anti-tumor Activity of Doxorubicin Encapsulated in PEG-PE Micelles in Mice

et al. 2012

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“…PEG has been in use for several decades as a surfactant and for steric stabilisation and conjugation of ligands to drug nanocarriers [18]. DSPE-PEG is a PEGylated phospholipid frequently used to develop drug nanocarrier systems due to its ability to form micellar rather than bilayered structures by self assembly in a suitable aqueous environment [19].…”

Section: Introductionmentioning

confidence: 99%

Ascorbyl palmitate/DSPE-PEG nanocarriers for oral iron delivery: Preparation, characterisation and in vitro evaluation

Zariwala

Farnaud

Merchant

et al. 2014

Colloids and Surfaces B: Biointerfaces

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“…This behavior was reproducible, although the precise shifts varied. The impact of oxidation on the PL of monodisperse SiNCs is well documented [67], but a redshift accompanied by a decrease in emission intensity has been associated with nanocrystal aggregation in aqueous environments [68][69][70][71][72]. The gray curves in Fig.…”

Section: Resultsmentioning

confidence: 89%

Interaction of polymer-coated silicon nanocrystals with lipid bilayers and surfactant interfaces

et al. 2016

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We use photoluminescence (PL) microscopy to measure the interaction between PEGylated silicon nanocrystals (SiNCs) and two model surfaces; lipid bilayers and surfactant interfaces. By characterizing the photostability, transport, and size-dependent emission of the PEGylated nanocrystal clusters, we demonstrate the retention of red PL suitable for detection and tracking with minimal blueshift after a year in an aqueous environment. The predominant interaction measured for both interfaces is short-range repulsion, consistent with the ideal behavior anticipated for PEGylated phospholipid coatings. However, we also observe unanticipated attractive behavior in a small number of scenarios for both interfaces. We attribute this anomaly to defective PEG coverage on a subset of the clusters, suggesting a possible strategy for enhancing cellular uptake by controlling the homogeneity of the PEG corona. In both scenarios, the shape of the apparent potential is modeled through the free or bound diffusion of the clusters near the confining interface.

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In vitro characterization of PEGylated phospholipid micelles for improved drug solubilization: Effects of PEG chain length and PC incorporation

Cited by 230 publications

References 21 publications

Stability Influences the Biodistribution, Toxicity, and Anti-tumor Activity of Doxorubicin Encapsulated in PEG-PE Micelles in Mice

Stability Influences the Biodistribution, Toxicity, and Anti-tumor Activity of Doxorubicin Encapsulated in PEG-PE Micelles in Mice

Ascorbyl palmitate/DSPE-PEG nanocarriers for oral iron delivery: Preparation, characterisation and in vitro evaluation

Interaction of polymer-coated silicon nanocrystals with lipid bilayers and surfactant interfaces

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