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

ABSTRACT Transdermal nicotine patches have been used in smoking cessation therapy, suggested for the treatment of skin disorders with eosinophilic infiltration and have been found to improve attention performance in patients with Alzheimer's disease and age-associated memory impairment. However, skin irritation with extended patch use is still a problem. The aim of this work was to develop a simple to prepare liquid crystalline system containing vitamin E TPGS that would be able to control nicotine delivery and reduce irritation and sensitization problems. The liquid crystalline phases were macroscopically characterized by visual analysis and examined microscopically under a polarized light microscope. Topical and transdermal delivery of nicotine were investigated in vitro using porcine ear skin mounted on a Franz diffusion cell. Nicotine skin permeation from the developed cubic phase followed zero-order kinetics (r = 0.993) and was significantly enhanced after 12 h when compared to the control formulation (nicotine solution) (p < 0.05) (138.86 ± 20.44 and 64.91 ± 4.06 μg/cm2, respectively). Cubic phase was also able to target viable skin layers in comparison to control solution (8.18 ± 1.89 and 2.63 ± 2.51 μg/cm2, respectively). Further studies to evaluate skin sensitization and irritation are now necessary.

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In vitro cytotoxicity assessment of carbon fabric coated with calcium phosphate

Carbon ◽

10.1016/j.carbon.2008.06.009 ◽

2008 ◽

Vol 46 (11) ◽

pp. 2-3

Author(s):

Hong-mei Han ◽

Gary J. Phillips ◽

Sergey V. Mikhalovsky ◽

Andrew W. Lloyd

Keyword(s):

Calcium Phosphate ◽

In Vitro Cytotoxicity ◽

Carbon Fabric ◽

Cytotoxicity Assessment

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The cytotoxic activity of pine needles ethanolic extract of Pinus merkusii on HeLa cell lines

BIO Web of Conferences ◽

10.1051/bioconf/20213303001 ◽

2021 ◽

Vol 33 ◽

pp. 03001

Author(s):

Annise Proboningrat ◽

Amaq Fadholly ◽

Sri Agus Sudjarwo ◽

Fedik Abdul Rantam ◽

Agung Budianto Achmad

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Anticancer Agents ◽

Anticancer Agent ◽

Ethanolic Extract ◽

In Vitro Cytotoxicity ◽

Hela Cell Lines ◽

Cytotoxicity Assessment ◽

Pinus Merkusii

Several efforts have been made to discover new anticancer agents based on natural ingredients. Meanwhile, previous studies have shown that different Pine genus species exhibit cytotoxic activity against various types of cancer cells. This plant is rich in phenolic compounds, especially procyanidins, flavonoids, and phenolic acids. Therefore, this study aims to investigate the in vitro cytotoxicity of Pinus merkusii needles extract on HeLa cancer cell lines. The cytotoxicity assessment was measured using MTT assay and expressed as IC50 value. The results showed that the ethanolic extract poses a dose and time-dependent cytotoxic activity with an IC50 value of 542.5 µg/ml at 48 hours of incubation. Based on this result, Pinus merkusii needles’ ethanolic extract has the potential of a novel candidate for an anticancer agent.

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Novel Mitochondrial Targeting Multifunctional Surface Charge-Reversal Polymeric Nanoparticles for Cancer Treatment

Journal of Biomedical Nanotechnology ◽

10.1166/jbn.2019.2854 ◽

2019 ◽

Vol 15 (11) ◽

pp. 2151-2163 ◽

Cited By ~ 3

Author(s):

Lei Fang ◽

Huaying Fan ◽

Chunjing Guo ◽

Linhan Cui ◽

Peng Zhang ◽

...

Keyword(s):

Cancer Treatment ◽

Targeted Delivery ◽

Polymeric Nanoparticles ◽

In Vitro Cytotoxicity ◽

Hydrodynamic Diameter ◽

Mitochondrial Targeting ◽

Anticancer Activities ◽

Charge Reversal

Polymeric nanoparticles were widely used as delivery vehicles for targeted delivery of anticancer drugs, because of their targeting property and versatility. Mitochondria are one of the important organelles that regulate the apoptosis of cancer cells and can be considered as a pivotal target for cancer treatment. A pH-responsive charge-reversal and mitochondrial targeting nanoparticles, Vitamin B6-oligomeric hyaluronic acid-dithiodipropionic acid-berberine (B6-oHA-SS-Ber), were prepared in this study. Ber is a lipophilic cation that was conjugated with oHA through disulfide bonds to produce mitochondria-targeted conjugates (oHA-SS-Ber). B6 was conjugated to oHA to obtain B6-oHA-SS-Ber and the two types of Cur-loaded nanoparticles (Cur-NPs) were formulated by the dialysis method. Due to pKa of B6, the charge they carried in the tumor tissue acidic microenvironment can be transferred from negative charge to positive charge, further targeting mitochondria. In our study, we successfully synthesized B6-HA-SS-Ber and characterized the structure by 1H-NMR. According to the results of transmission electron microscopy (TEM), we found that the B6-oHA-SS-Ber/Cur micelles could self-assembled in water to form spherical nanoparticles, with a hydrodynamic diameter of 172.9±13 nm. Moreover, in vitro cytotoxicity, cellular uptake, lysosome escape and mitochondrial distribution researches revealed the better effect of B6-oHA-SS-Ber/Cur micelles in comparison to oHA-SS-Ber/Cur. In vivo anticancer activities indicated that the B6-oHA-SS-Ber/Cur micelles exhibited effective inhibition of tumor growth.

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ANTIOXIDANT, CYTOTOXICITY, AND STABILITY EVALUATION OF GINKGO BILOBA EXTRACT-BASED MICROEMULSIONS FOR ENHANCED THERAPEUTIC ACTIVITY

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i8.19537 ◽

2017 ◽

Vol 10 (8) ◽

pp. 335 ◽

Cited By ~ 1

Author(s):

Manisha Singh ◽

Surya Pratap Singh ◽

Rachana R

Keyword(s):

Ginkgo Biloba ◽

Therapeutic Potential ◽

Ginkgo Biloba Extract ◽

In Vitro Cytotoxicity ◽

Scavenging Activity ◽

Therapeutic Implications ◽

Chromatography Analysis ◽

Ic50 Value ◽

Cytotoxicity Assessment

Objective: This study is aimed to evaluate the antioxidant (AO) potential, cytotoxicity, and stability of preformulated Ginkgo biloba standard extractmicroemulsion (GBME), to investigate if, it retains the therapeutic potential of EGB761 and remains safe and stable for a longer period.Method and Results: GBME has shown enhanced AO (85.2±0.78%, IC50=31.3±0.45 μg/ml) in comparison to EGB761 (74.1±0.51%,IC50=49.4±0.05 μg/ml) using 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assay. Similarly, 2,2-diphenyl-1-picryl-hydrazyl-hydrate(DPPH) assay has also shown that AO for GBME (94.6±0.04%, IC50=11.4±1.03 μg/ml) was higher than EGB761 (78.6±1.20%, IC50=34.6±0.81 μg/ml).Further, IC50 value of antiradical unit of GBME was much lesser (ABTS=14.3±1.05 μg/ml and DPPH=17.03±1.8 μg/ml) in comparison to EGB761(ABTS=34.1±1.62 μg/ml and DPPH=37.5±0.08 μg/ml). Equivalently, both, hydrogen peroxide scavenging activity, and nitric oxide activity wereappreciably higher for GBME than the pure extract. The in vitro cytotoxicity assessment showed that GBME is quite safe (98.68±0.76% cell viability) incomparison to EGB761 (83.29±1.02%). Thereafter, these samples were tested for stability by evaluating their AO activity along with high-performanceliquid chromatography analysis, for the major phytocompounds, after 1 year, and results suggested that AO of GBME remained stable while comparingwith the freshly prepared GBME, whereas AO of EGB761 reduced significantly as compared to freshly taken EGB761 extract implying the degradationof phytocompounds supporting decrease in AO activity.Conclusion: Therefore, the observed results suggest that GBME maintained AO and scavenging activity along with enhanced shelf life with no observedtoxicity, which can be explored further for its potential therapeutic implications in various oxidative stress-induced central nervous system disorders.

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The Synthesis, Characterization, Cytotoxic Activity Assessment and Structure–Activity Relationship of 4-Aryl-6-(2,5-dichlorothiophen-3-yl)-2-methoxypyridine-3-carbonitriles

Molecules ◽

10.3390/molecules24224072 ◽

2019 ◽

Vol 24 (22) ◽

pp. 4072

Author(s):

Al-Refai ◽

Ibrahim ◽

Azmi ◽

Osman ◽

Bakar ◽

...

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Cancer Cell Lines ◽

In Vitro Cytotoxicity ◽

Basic Medium ◽

Condensation Process ◽

Cytotoxicity Activities ◽

Cytotoxicity Assessment ◽

Relationship Of

A series of 2-methoxypyridine-3-carbonitrile (5a–i)-bearing aryl substituents were successfully synthesized in good yields by the condensation of chalcones (4a–i) with malononitrile in basic medium. The condensation process, in most cases, offers a route to a variety of methoxypyridine derivatives (6a–g) as side products in poor yields. All new compounds were fully characterized using different spectroscopic methods. Mass ESI-HMRS measurements were also performed. Furthermore, these compounds were screened for their in vitro cytotoxicity activities against three cancer cell lines; namely, those of the liver (line HepG2), prostate (line DU145) and breast (line MBA-MB-231). The cytotoxicity assessment revealed that compounds 5d, 5g, 5h and 5i exhibit promising antiproliferative effects (IC50 1–5 µM) against those three cancer cell lines.

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