Exemestane encapsulated vitamin E-TPGS–polymeric nanoparticles: preparation, optimization, characterization, and<i>in vitro</i>cytotoxicity assessment

In this study, amoxicillin (AMO)-loaded poly(vinyl alcohol)/sodium alginate (PVA/NaAlg) nanoparticles were prepared as a polymer-based controlled release system. The physicochemical properties of the obtained nanoparticles were investigated by XRD, DSC/TGA, particle size analyses and zeta potential measurements. The average particle sizes were in the range from 336.3 ± 25.66 to 558.3 ± 31.39 nm with negative zeta potential values from -41.86 ± 0.55 to -47.3 ± 2.76 mV. The influences of PVA/NaAlg ratio, span 80 concentration, exposure time to glutaraldehyde (GA) and the drug/polymer ratio on AMO release profiles were evaluated. In vitro drug release studies showed a controlled and pH dependent AMO release with an initial burst effect. XRD patterns and DSC thermograms of AMO-loaded nanoparticles revealed that the drug in the nanoparticles was in amorphous form, which was more stable than the crystalline form. The antibacterial activity of the optimal formulation was also investigated. The minimum inhibitory concentration (MIC) values of this formulation had the comparable antibacterial activity with that of pure AMO. These results indicate that the developed nanoparticles could be a promising candidate drug delivery system for AMO.

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“…Data were presented as the mean ± SD (n ¼ 3). nanoparticles [51,52]. This result was further confirmed by XRD analysis.…”

Section: Xrd Dsc and Tga Analysessupporting

confidence: 65%

Development and characterization of polymeric-based nanoparticles for sustained release of amoxicillin – an antimicrobial drug

Güncüm

Işıklan

Anlaş

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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“…Release of the dye was found to be bimodal: First, a burst release was observed in 6 h and release continued over 24 h (Figure 1(B)). This initial burst can be the reason for the surface adsorbed dye diffusion (Mishra et al 2016). These results have to be taken into consideration since such extracellular Dil release may influence the cell uptake results interpretation.…”

Section: Resultsmentioning

confidence: 98%

A small variation in average particle size of PLGA nanoparticles prepared by nanoprecipitation leads to considerable change in nanoparticles’ characteristics and efficacy of intracellular delivery

Sahin

Esendağlı

Yerlikaya

et al. 2017

Artificial Cells, Nanomedicine, and Biotechnology

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In this study, it was aimed to investigate characteristics and intracellular delivery of two different-sized PLGA nanoparticles in ouzo region by considering number of nanoparticles. To determine the effect of formulation parameters on average particle size, Dil labeled nanoparticles were prepared using a three-factor, two-level full factorial statistical experimental design. PLGA (230.8 ± 4.32 nm) and PLGA (157.9 ± 6.16 nm) nanoparticles were obtained by altering polymer amount based on experimental design results and characterized. Same number of PLGA and PLGA nanoparticles per cell were applied onto HEK293 cells; then, cytotoxicity, uptake kinetics and mechanism were evaluated by flow cytometry and fluorescent microscopy. Also same weight of PLGA and PLGA nanoparticles were applied and cellular uptake of these nanoparticles was evaluated. It was found that PLGA nanoparticles had higher encapsulation efficiency and slower dye release compared to PLGA nanoparticles. When they were applied at same counts per cell, PLGA nanoparticles displayed faster and higher intracellular dye transfer than PLGA nanoparticles. On the other hand, PLGA appeared to be a more effective vehicle than PLGA when applied at the same weight concentration. It was also shown that for both nanoparticles, HEK293 cells employed macropinocytic, caveolae- and clathrin-mediated endocytic pathways.

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“…Moreover, nanosized carriers show the ability to improve plasma half-life, bioavailability, therapeutic efficacy, decrease dosing frequency, and systemic toxicity [9,10]. Recently, different nanoparticles-based systems have been developed to improve the solubility and in vitro efficacy of EXE [11][12][13][14][15], but these formulations failed in providing evidence of significant therapeutic efficacy. However, as per the literature, to date, polymer-lipid hybrid nanoparticles (PLHNPs) for improved efficacy against breast cancer have not been studied.…”

Section: Introductionmentioning

confidence: 99%

Exemestane encapsulated polymer-lipid hybrid nanoparticles for improved efficacy against breast cancer: optimization, in vitro characterization and cell culture studies

et al. 2021

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Polymer-lipid hybrid nanoparticles (PLHNPs) are novel nanoplatforms for the effective delivery of a lipophilic drug in the management of a variety of solid tumors. The present work was designed to develop exemestane (EXE) encapsulated D-alpha-tocopheryl polyethylene glycol succinate (TPGS) based PLHNPs (EXE-TPGS-PLHNPs) for controlled delivery of EXE for breast cancer management. EXE-TPGS-PLHNPs were formulated by single-step nano-precipitation technique and statistically optimized by a 33 Box–Behnken design using Design expert® software. The polycaprolactone (PCL; X 1), phospholipon 90 G (PL-90G; X 2), and surfactant (X 3) were selected as independent factors while particles size (PS; Y 1), polydispersity index (PDI; Y 2), and %entrapment efficiency (%EE; Y 3) were chosen as dependent factors. The average PS, PDI, and %EE of the optimized EXE-TPGS-PLHNPs was observed to be 136.37 ± 3.27 nm, 0.110 ± 0.013, and 88.56 ± 2.15% respectively. The physical state of entrapped EXE was further validated by Fourier-transform infrared spectroscopy, differential scanning calorimetry, and powder x-ray diffraction that revealed complete encapsulation of EXE in the hybrid matrix of PLHNPs with no sign of significant interaction between drug and excipients. In vitro release study in simulated gastrointestinal fluids revealed initial fast release for 2 h after that controlled release profile up to 24 h of study. Moreover, optimized EXE-TPGS-PLHNPs exhibited excellent stability in gastrointestinal fluids as well as colloidal stability in different storage concentrations. Furthermore, EXE-TPGS-PLHNPs exhibited distinctively higher cellular uptake and time and dose-dependent cytotoxicity against MCF-7 breast tumor cells compared to EXE-PLHNPs without TPGS and free EXE. The obtained results suggested that EXE-TPGS-PLHNPs can be a promising platform for the controlled delivery of EXE for the effective treatment of breast cancer.

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Exemestane encapsulated vitamin E-TPGS–polymeric nanoparticles: preparation, optimization, characterization, andin vitrocytotoxicity assessment

Cited by 16 publications

References 45 publications

Development and characterization of polymeric-based nanoparticles for sustained release of amoxicillin – an antimicrobial drug

Development and characterization of polymeric-based nanoparticles for sustained release of amoxicillin – an antimicrobial drug

A small variation in average particle size of PLGA nanoparticles prepared by nanoprecipitation leads to considerable change in nanoparticles’ characteristics and efficacy of intracellular delivery

Exemestane encapsulated polymer-lipid hybrid nanoparticles for improved efficacy against breast cancer: optimization, in vitro characterization and cell culture studies

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