Preparation and Biopharmaceutical Evaluation of Novel Polymeric Nanoparticles Containing Etoposide for Targeting Cancer Cells

Ayyappan, T.; Saravanabhavan, Shanmugam; Thangarasu, Vetrichelvan

doi:10.4274/tjps.galenos.2018.21043

Cited by 8 publications

(6 citation statements)

References 22 publications

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“…Also, peak intensity is affected by crystallinity, drug crystal size and also merely by the NC powder packing in the well sample holder, the latter is not a reliable parameter to understand the crystallinity of the drug 40 . The diffraction pattern obtained for the ETO was comparable to those reported in the literature 41 . If the ETO nanoparticles are definitely crystalline in the solid state, the redispersion in solution ought to not affect their crystallinity.…”

Section: Resultssupporting

confidence: 85%

Preparation of parenteral nanocrystal suspensions of etoposide from the excipient free dry state of the drug to enhance in vivo antitumoral properties

Martin

Séguin

Annereau

et al. 2020

Sci Rep

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Nanoparticle technology in cancer chemotherapy is a promising approach to enhance active ingredient pharmacology and pharmacodynamics. Indeed, drug nanoparticles display various assets such as extended blood lifespan, high drug loading and reduced cytotoxicity leading to better drug compliance. In this context, organic nanocrystal suspensions for pharmaceutical use have been developed in the past ten years. Nanocrystals offer new possibilities by combining the nanoformulation features with the properties of solid dispersed therapeutic ingredients including (i) high loading of the active ingredient, (ii) its bioavailability improvement, and (iii) reduced drug systemic cytotoxicity. However, surprisingly, no antitumoral drug has been marketed as a nanocrystal suspension until now. Etoposide, which is largely used as an anti-cancerous agent against testicular, ovarian, small cell lung, colon and breast cancer in its liquid dosage form, has been selected to develop injectable nanocrystal suspensions designed to be transferred to the clinic. The aim of the present work is to provide optimized formulations for nanostructured etoposide solutions and validate by means of in vitro and in vivo evaluations the efficiency of this multiphase system. Indeed, the etoposide formulated as a nanosuspension by a bottom-up approach showed higher blood life span, reduced tumor growth and higher tolerance in a murine carcinoma cancer model. The results obtained are promising for future clinical evaluation of these etoposide nanosuspensions.

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Section: Resultssupporting

confidence: 85%

Preparation of parenteral nanocrystal suspensions of etoposide from the excipient free dry state of the drug to enhance in vivo antitumoral properties

Martin

Séguin

Annereau

et al. 2020

Sci Rep

View full text Add to dashboard Cite

show abstract

“…It was reported as the intensity-weighted average (Z-AVE) [N (degree of freedom) = 3] in Table 4, and size distribution has been shown in Figure S9. The PdI value (n = 10) was 0.5 and was therefore in the range of PdI recently reported for promising ETO nanoparticles formulations [79]. In addition, by DLS technique, the Z-potential (mV) of CPX 5 particles was also measured, for the purpose of having an idea of physical stability of 5 in aqueous solution, for investigating the possible tendency of the particles to form aggregates, and for finding its possible toxicity.…”

Section: Estimation Of Eto Amount In Cpx 5 (Dl%) and Of Entrapment Efmentioning

confidence: 59%

“…In other cases, the ETO EE% was either very low (4-14%) [77] or, though high (75-84%) [78], were not as high as the EE% achieved in this study by using dendrimer 4. Only recently, Thiyagarajan et al [79], have prepared a series of polymeric nanoparticles containing ETO for targeting cancer cells that had a high DL% (62-90%) and in some cases very high EE% (49-94%).…”

Section: Estimation Of Eto Amount In Cpx 5 (Dl%) and Of Entrapment Efmentioning

confidence: 99%

Polyester-Based Dendrimer Nanoparticles Combined with Etoposide Have an Improved Cytotoxic and Pro-Oxidant Effect on Human Neuroblastoma Cells

2020

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Etoposide (ETO) is a cytotoxic drug that exerts its effect by increasing reactive oxygen species (ROS) production. Although ETO is widely used, fast metabolism, poor solubility, systemic toxicity, and multi-drug resistance induction all limit its administration dosage and its therapeutic efficiency. In order to address these issues, a biodegradable dendrimer was prepared for entrapping and protecting ETO and for enhancing its solubility and effectiveness. The achieved dendrimer complex with ETO (CPX 5) showed the typical properties of a well-functioning delivery system, i.e., nanospherical morphology (70 nm), optimal Z-potential (−45 mV), good drug loading (37%), very satisfying entrapment efficiency (53%), and a remarkably improved solubility in biocompatible solvents. In regards to its cytotoxic activity, CPX 5 was tested on neuroblastoma (NB) cells with very promising results. In fact, the dendrimer scaffold and ETO are able to exert per se a cytotoxic and pro-oxidant activity on human NB cells. When CPX 5 is combined with ETO, it shows a synergistic action, slowly releasing the drug over time and significantly improving and protracting bioactivity. On the basis of these findings, the prepared ETO reservoir represents a novel biodegradable and promising device for the delivery of ETO into NB cells.

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“…Inhibition percentages were calculated and presented in relation to the concentrations required to calculate IC 50 readings. 13 , 14 …”

Section: Methodsmentioning

confidence: 99%

Dual drug‐loaded polymeric mixed micelles for ovarian cancer: Approach to enhanced therapeutic efficacy of albendazole and paclitaxel

Gaikwad,

Chaudhari,

Shaikh

et al. 2024

J Cellular Molecular Medi

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Chemotherapy resistance remains a significant challenge in treating ovarian cancer effectively. This study addresses this issue by utilizing a dual drug‐loaded nanomicelle system comprising albendazole (ABZ) and paclitaxel (PTX), encapsulated in a novel carrier matrix of D‐tocopheryl polyethylene glycol 1000 succinate vitamin E (TPGS), soluplus and folic acid. Our objective was to develop and optimize this nanoparticulate delivery system using solvent evaporation techniques to enhance the therapeutic efficacy against ovarian cancer. The formulation process involved pre‐formulation, formulation, optimization, and comprehensive characterization of the micelles. Optimization was conducted through a 32 factorial design, focusing on the effects of polymer ratios on particle size, zeta potential, polydispersity index (PDI) and entrapment efficiency (%EE). The optimal formulation demonstrated improved dilution stability, as indicated by a critical micelle concentration (CMC) of 0.0015 mg/mL for the TPGS‐folic acid conjugate (TPGS‐FOL). Extensive characterization included differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), and Fourier‐transform infrared spectroscopy (FTIR). The release profile exhibited an initial burst followed by sustained release over 90 h. The cytotoxic potential of the formulated micelles was superior to that of the drugs alone, as assessed by MTT assays on SKOV3 ovarian cell lines. Additionally, in vivo studies confirmed the presence of both drugs in plasma and tumour tissues, suggesting effective targeting and penetration. In conclusion, the developed TPGS‐Fol‐based nanomicelles for co‐delivering ABZ and PTX show promising results in overcoming drug resistance, enhancing solubility, sustaining drug release, and improving therapeutic outcomes in ovarian cancer treatment.

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Preparation and Biopharmaceutical Evaluation of Novel Polymeric Nanoparticles Containing Etoposide for Targeting Cancer Cells

Cited by 8 publications

References 22 publications

Preparation of parenteral nanocrystal suspensions of etoposide from the excipient free dry state of the drug to enhance in vivo antitumoral properties

Preparation of parenteral nanocrystal suspensions of etoposide from the excipient free dry state of the drug to enhance in vivo antitumoral properties

Polyester-Based Dendrimer Nanoparticles Combined with Etoposide Have an Improved Cytotoxic and Pro-Oxidant Effect on Human Neuroblastoma Cells

Dual drug‐loaded polymeric mixed micelles for ovarian cancer: Approach to enhanced therapeutic efficacy of albendazole and paclitaxel

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