Morphology, gelation and cytotoxicity evaluation of D-α-Tocopheryl polyethylene glycol succinate (TPGS) – Tetronic mixed micelles

Puig-Rigall, Joan; Blanco-Prieto, María J.; Rădulescu, Aurel; Dreiss, Cécile A.; González‐Gaitano, Gustavo

doi:10.1016/j.jcis.2020.08.004

Cited by 26 publications

(24 citation statements)

References 35 publications

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“…Among different nanocarriers explored so far by different researchers, mixed micelles have gained potential interest due to the spontaneous and self-assembling property of amphiphilic copolymers into nanometric (5-100 nm) colloidal dispersions, with relatively narrow size distribution (Cagel et al, 2017;Gorain et al, 2020). The micellar structure of the carrier is spontaneously formed above the critical micellar concentration (CMC) of the polymer, thereby develop a core-shell model with the hydrophobic core to entrap the poorly water-soluble drugs with a shell constituting hydrophilic moieties (Puig-Rigall et al, 2021). The entrapped drug within the core provides the architecture for control release properties, where the hydrophilic shell stabilizes the three-dimensional spherical structure of the system (Gorain et al, 2020;Puig-Rigall et al, 2021).…”

Section: Introductionmentioning

confidence: 99%

“…The micellar structure of the carrier is spontaneously formed above the critical micellar concentration (CMC) of the polymer, thereby develop a core-shell model with the hydrophobic core to entrap the poorly water-soluble drugs with a shell constituting hydrophilic moieties (Puig-Rigall et al, 2021). The entrapped drug within the core provides the architecture for control release properties, where the hydrophilic shell stabilizes the three-dimensional spherical structure of the system (Gorain et al, 2020;Puig-Rigall et al, 2021). However, judicious selection of the polymers with biodegradable and biocompatible characteristics for the micellar delivery is of utmost importance for the safe delivery of therapeutics.…”

Section: Introductionmentioning

confidence: 99%

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Development, Optimization and Evaluation of 2-Methoxy-Estradiol Loaded Nanocarrier for Prostate Cancer

et al. 2021

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The therapeutic efficacy of antineoplastic agents possessing a selective target to the nucleus of the cancer cells could be enhanced through novel formulation approaches. Thus, toward the improvement of the anticancer potential of 2-methoxy estradiol (2 ME) on prostate cancer, the drug was entrapped into the hydrophobic micelles core formulated with Phospholipon 90G and d-α-tocopheryl polyethylene glycol succinate (TPGS). Optimization of the formulation was done by Box-Behnken statistical design using Statgraphics software to standardize percentages of TPGS and phospholipid to obtain the smallest particle size. The optimized formulation was found to be spherical with nanometer size of 152 ± 5.2 nm, and low PDI (0.234). The entrapment efficiency of the micelles was 88.67 ± 3.21% with >93% release of 2 ME within 24 h. There was a 16-fold increase in apoptosis and an 8-fold increase in necrosis of the PC-3 cells when incubated with 2 ME micellar delivery compared to control cells (2.8 ± 0.2%). This increased apoptosis was further correlated with increased BAX expression (11.6 ± 0.7) and decreased BCL-2 expression (0.29 ± 0.05) in 2 ME micelles treated cells when compared to the control group. Further, loss of mitochondrial membrane potential (∼50-fold) by the drug-loaded micelles and free drug compared to control cells was found to be due to the generation of ROS. Findings on cell cycle analysis revealed the significant arrest of the G2-M phase of the PC-3 cells when incubated with the optimized formulation. Simultaneously, a significantly increased number of cells in pre-G1 revealed the maximum apoptotic potential of the drug when delivered via micellar formulation. Finally, upregulation of caspase-9, p53, and NO, with downregulation of TNF-α, NF-κβ, and inflammatory mediators of the PC-3 cells established the superiority of the micellar approach against prostate cancer. In summary, the acquired results highlighted the potentiality of the 2 ME-micellar delivery tool for controlling the growth of prostate cancer cells for improved efficacy.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development, Optimization and Evaluation of 2-Methoxy-Estradiol Loaded Nanocarrier for Prostate Cancer

et al. 2021

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Section: T/ºcmentioning

confidence: 99%

“…We next turn our attention to the water content in the two compartments [85] of the micelles (core and shell). First, the shell of both free and SAL loaded micelles is highly hydrated (Tables 2 and 3), as observed for Pluronics and other PEG-base copolymers [18,85]. No meaningful change in the water content of the shell is observed with temperature (94% at 20ºC and 93 -92%, at 50ºC), the presence of SAL (94% at 37ºC for both systems or 93-92% for free and SAL loaded aggregates, respectively at 50ºC) or with pH (free micelles: at 25ºC 94/90% and at 37ºC 94/92% at pH=1/pH=7; or in the loaded micelles: 94/96% and 94/92% at 25 and 37ºC, pH=1/pH=7, respectively).…”

Section: T/ºcmentioning

confidence: 99%

“…In order to minimize the number of floating parameters, and based on previous studies of similar polymers [18,85], the water content of the core was initially fixed to zero, in other words, the scattering length density was fixed to the value of PPO (0.4×10 -6 Å -2 ). However, this assumption does not allow the fitting of the curves at all temperatures.…”

Section: T/ºcmentioning

confidence: 99%

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Solubilisation of salicylate in F127 micelles: Effect of pH and temperature on morphology and interactions with cyclodextrin

Valero

Houston

et al. 2021

Journal of Molecular Liquids

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Synthesis, antimicrobial and anticancer activities of Tetronic 1107 Schiff bases

Alasmary

Kenawy

El‐Deeb

et al. 2022

Polymers for Advanced Techs

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As a result of the serious issues connected to the bacterial infections, there is an imperious need to improve strong and ecofriendly antimicrobial polymers to overcome the limitations of conventional antimicrobial agents. In this trend, poloxamines (Tetronics) which are X‐shaped poly(ethylene oxide)–poly(propylene oxide) diblocks linked to a focal ethylenediamine group; were successfully modified to produce Tetronic Schiff base for enhancing the biological activities of Tetronic 1107. Modification of tetronic 1107 (T1107) was proceeded throughout chloroacetylation of T1107 followed by amination using p‐phenylenediamine then the latter was treated with different aldehydes to yield Tetronic Schiff bases. Characterization of Tetronic Schiff bases was carried out by 1H‐NMR, Fourier‐transform infrared spectroscopy, X‐ray diffraction, elemental analysis and thermogravimetric analysis (TGA) analyses. The antimicrobial activities of four tested compounds coded (EK1, EK2, EK3, and EK4) were quantified using Microtiter‐assay methods. The obtained data revealed potential antimicrobial activities for tested compounds against all tested microbes with priority against Pseudomonas aeruginosa, Escherichia coli and Staphylococcus aureus. Sample coded EK4 exhibited the most effective treatment against P. aeruginosa, Candida albicans, S. aureus and E. Coli with minimal inhibitory concentration values of 6, 16, 12.5, and 1.5 μM, respectively. Furthermore, the safety results confirmed that EK4 and EK1 were the safest treatment with IC50 values of 76.01 and 62.67 μM, respectively. In addition, all tested compounds showed significant anticancer effects against MDA‐MB‐231cell line, while EK3 was effective treatment against A549 cell line with IC50 values of 39.63 μM. Meanwhile, both EK2 and EK4 showed the highest selectivity index (SI) values against MDA‐MB‐231 cell line with values 2.5 and 3.07, respectively. Interestingly, EK4 showed the maximum SI values on A549 and Hep‐G2 cell lines with values 1.62 and 1.52, respectively.

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Morphology, gelation and cytotoxicity evaluation of D-α-Tocopheryl polyethylene glycol succinate (TPGS) – Tetronic mixed micelles

Cited by 26 publications

References 35 publications

Development, Optimization and Evaluation of 2-Methoxy-Estradiol Loaded Nanocarrier for Prostate Cancer

Development, Optimization and Evaluation of 2-Methoxy-Estradiol Loaded Nanocarrier for Prostate Cancer

Solubilisation of salicylate in F127 micelles: Effect of pH and temperature on morphology and interactions with cyclodextrin

Synthesis, antimicrobial and anticancer activities of Tetronic 1107 Schiff bases

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