Abstract:BackgroundNanocarriers represent an attractive means of drug delivery, but their biosafety must be established before their use in clinical research.ObjectivesFour kinds of amphiphilic polymeric (PEG-PG-PCL, PEEP-PCL, PEG-PCL and PEG-DSPE) micelles with similar hydrophilic or hydrophobic structure were prepared and their in vitro and in vivo safety were evaluated and compared.MethodsIn vitro nanotoxicity evaluations included assessments of cell morphology, cell volume, inflammatory effects, cytotoxicity, apopt… Show more
“…3), DSPE-PEG micelles appeared similar in structure to previously reported (Zhao, 2013) micelles. Micelles of LACPEG/DSPE-PEG differed in morphology to DSPE-PEG and LACPEG micelles, confirming the production of a new carrier.…”
Mixed micelles of lipoic acidchitosan-poly(ethylene glycol) and distearoylphosphatidylethanolamine-poly(ethylene glycol) for tumor delivery. The address for the corresponding author was captured as affiliation for all authors. Please check if appropriate. Phasci(2017Phasci( ), doi: 10.1016Phasci( / j.ejps.2017 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.A C C E P T E D M A N U S C R I P T
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A C C E P T E D M A N U S C R I P T 2
AbstractMany chemotherapeutics suffer from poor aqueous solubility and tissue selectivity.Distearoylphosphatidylethanolamine-poly(ethylene glycol) (DSPE-PEG) micelles are a promising formulation strategy for the delivery of hydrophobic anticancer drugs. However, storage and in vivo instability restrict their use. The aim of this study was to prepare mixed micelles, containing a novel polymer, lipoic acid-chitosan-poly(ethylene glycol) (LACPEG), and DSPE-PEG, to overcome these limitations and potentially increase cancer cell internalisation. Drug-loaded micelles were prepared with a model tyrosine kinase inhibitor and characterized for size, surface charge, stability, morphology, drug
“…3), DSPE-PEG micelles appeared similar in structure to previously reported (Zhao, 2013) micelles. Micelles of LACPEG/DSPE-PEG differed in morphology to DSPE-PEG and LACPEG micelles, confirming the production of a new carrier.…”
Mixed micelles of lipoic acidchitosan-poly(ethylene glycol) and distearoylphosphatidylethanolamine-poly(ethylene glycol) for tumor delivery. The address for the corresponding author was captured as affiliation for all authors. Please check if appropriate. Phasci(2017Phasci( ), doi: 10.1016Phasci( / j.ejps.2017 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.A C C E P T E D M A N U S C R I P T
ACCEPTED MANUSCRIPT
A C C E P T E D M A N U S C R I P T 2
AbstractMany chemotherapeutics suffer from poor aqueous solubility and tissue selectivity.Distearoylphosphatidylethanolamine-poly(ethylene glycol) (DSPE-PEG) micelles are a promising formulation strategy for the delivery of hydrophobic anticancer drugs. However, storage and in vivo instability restrict their use. The aim of this study was to prepare mixed micelles, containing a novel polymer, lipoic acid-chitosan-poly(ethylene glycol) (LACPEG), and DSPE-PEG, to overcome these limitations and potentially increase cancer cell internalisation. Drug-loaded micelles were prepared with a model tyrosine kinase inhibitor and characterized for size, surface charge, stability, morphology, drug
“…After a 0.5-h incubation period, the DSPE-PEG2000/TPGS micelles showed 9.6-, 11.5-, and 5.1-fold higher uptake compared to the free dye, while TPGS micelles showed 8.1-, 10.5-, and 5.5-fold enhanced uptake, for coumarin-6 concentrations of 0.025, 0.25, and 2.5 μg/mL, respectively. The higher cellular uptake of DSPE-PEG2000/TPGS micelles compared to TPGS micelles may be due to the presence of the DSPE-PEG structure [55]. Figures 2(a) and 2(b) show that the cellular uptake of the nanoparticles by the cells is both time-and dose-dependent, similarly to phenomena previously reported [56].…”
A polymer-based nanocarrier was developed for the co-delivery of epigenetic and chemotherapeutic drugs. The sterically stabilized hybrid micelle system uses micelles composed of D-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS or TPGS) and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] (DSPE-PEG2000). In this study, suberoylanilide hydroxamic acid (SAHA) and paclitaxel were used as model drugs for combination chemotherapy to enhance therapeutic efficiency in targeting mesenchyme-like triple negative breast cancer (TNBC) cells. Combination therapy of paclitaxel and SAHA in a dual drug micelle system, (P + S) mic , exhibited an IC50 value of 0.52 μg/mL, which is about 5.91-fold more cytotoxic than the mere combination of free drugs (P + S). Furthermore, the (P + S) mic formulation was far more effective at inhibiting cell migration by more than 3.4-fold than the control. Thus, our findings show that the co-delivery of these drugs using the micelle system greatly enhances their therapeutic effect at a lower dosage, thereby minimizing toxicity. In addition, this formulation is proved to be remarkably effective in preventing cell migration at low dosage.
“…The cytotoxicity of ZnO nanomaterials is related to the surface nanostructure and the extent to be internalized by cells [9]. As the surface properties and shape of the ZnO nanocrystals significantly influence the cytotoxicity, these parameters should be maintained at the desired levels [10,11].…”
ZnO nanoparticles are widely used in biological, chemical, and medical fields, but their toxicity impedes their wide application. In this study, pristine ZnO NPs (~ 7 nm; ~ 18 nm; ~ 49 nm) and lipid-coated ZnO NPs (~ 13 nm; ~ 22 nm; ~ 52 nm) with different morphologies were prepared by chemical method and characterized by TEM, XRD, HRTEM, FTIR, and DLS. Our results showed that the lipid-coated ZnO NPs (~ 13 nm; ~ 22 nm; ~ 52 nm) groups improved the colloidal stability, prevented the aggregation and dissolution of nanocrystal particles in the solution, inhibited the dissolution of ZnO NPs into Zn 2+ cations, and reduced cytotoxicity more efficiently than the pristine ZnO NPs (~ 7 nm; ~ 18 nm; ~ 49 nm). Compared to the lipid-coated ZnO NPs, pristine ZnO NPs (~ 7 nm; ~ 18 nm; ~ 49 nm) could dose-dependently destroy the cells at low concentrations. At the same concentration, ZnO NPs (~ 7 nm) exhibited the highest cytotoxicity. These results could provide a basis for the toxicological study of the nanoparticles and direct future investigations for preventing strong aggregation, reducing the toxic effects of lipid-bilayer and promoting the uptake of nanoparticles by HeLa cells efficiently.
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