Nontoxic gemini cationic biodegradable polyurethane drug carriers: Synthesis, self-assembly and in vitro cytotoxicity

Background: Pyrvinium pamoate (PP) is an old drug approved by the FDA for the treatment of pinworm infections. Recently, PP has been introduced as an antitumor agent. However, low aqueous solubility severely limits its potential effects. In this study, we developed a liposomal formulation of pyrvinium pamoate to investigate its in vitro cytotoxicity and in vivo efficacy against melanoma cells. Materials & Methods: As drug carriers, liposomes were fabricated using thin-film method. PP was encapsulated within liposomes using remote loading method. We evaluated morphology, particle size, and Zeta potential of the liposomes. Additionally, high-performance liquid chromatography (HPLC) was employed for qualitative and quantitative analysis. Then we investigated our liposomal PP for its in vitro cytotoxicity as well as the tumor growth inhibition in C57BL/6 mice bearing B16F0 melanoma tumors. Results: Based on the analytical result, the liposomal drug delivery system is a homogeneous and stable colloidal suspension of PP particles. Images of Atomic force microscopy and particle size data showed that all the prepared nanocarrier were spherical with a diameter of approximately 101 nm. According to both in vitro and in vivo studies, nanoliposomal PP exhibited an improved anti-proliferative potential against B16F10 melanoma tumor compared with free PP. Conclusion: Liposomal encapsulation improves water solubility of PP and enhances its anti-cancer activity.

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Ionically Crosslinked Chitosan Membranes Used as Drug Carriers for Cancer Therapy Application

Materials ◽

10.3390/ma11102051 ◽

2018 ◽

Vol 11 (10) ◽

pp. 2051 ◽

Cited By ~ 8

Author(s):

Alecsandra Ferreira Tomaz ◽

Sandra Sobral de Carvalho ◽

Rossemberg Cardoso Barbosa ◽

Suédina L. Silva ◽

Marcos Sabino Gutierrez ◽

...

Keyword(s):

Cancer Therapy ◽

Drug Release ◽

Delivery System ◽

Drug Carriers ◽

In Vitro Cytotoxicity ◽

Cytotoxicity Studies ◽

Chitosan Membranes ◽

Crosslinked Chitosan ◽

Cross Linker

The aim of this paper was to prepare, by the freeze-drying method, ionically crosslinked chitosan membranes with different contents of pentasodium tripolyphosphate (TPP) and loaded with 1,4-naphthoquinone (NQ14) drug, in order to evaluate how the physical crosslinking affects NQ14 release from chitosan membranes for cancer therapy application. The membranes were characterized by Fourier transform infrared spectroscopy (FTIR), wide-angle X-ray diffraction (WAXD), scanning electron microscopy (SEM), swelling degree, and through in vitro drug release and cytotoxicity studies. According to the results, the molecular structure, porosity and hydrophilicity of the chitosan membranes were affected by TPP concentration and, consequently, the NQ14 drug release behavior from the membranes was also affected. The release of NQ14 from crosslinked chitosan membranes decreased when the cross-linker TPP quantity increased. Thus, depending on the TPP amount, the crosslinked chitosan membranes would be a potential delivery system to control the release of NQ14 for cancer therapy application. Lastly, the inhibitory potential of chitosan membranes ionically crosslinked with TPP and loaded with NQ14 against the B16F10 melanoma cell line was confirmed through in vitro cytotoxicity studies assessed via MTT assay. The anti-proliferative effect of prepared membranes was directly related to the amount of cross-linker and among all membranes prepared, such that one crosslinked with 0.3% of TPP may become a potential delivery system for releasing NQ14 drug for cancer therapy.

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Paclitaxel-tyroserleutide Conjugates Self-assembly into Nanocarrier for Drug Delivery

Letters in Drug Design & Discovery ◽

10.2174/1570180815666180803124625 ◽

2019 ◽

Vol 16 (8) ◽

pp. 882-891

Author(s):

Yongjia Liu ◽

Leilei Shi ◽

Bangshang Zhu ◽

Yue Su ◽

Hui Li ◽

...

Keyword(s):

Drug Delivery ◽

Self Assembly ◽

Water Solubility ◽

Drug Carrier ◽

Drug Loading ◽

Cancer Therapeutics ◽

Drug Carriers ◽

Pharmacokinetic Studies ◽

Assembly Method

Background: The drug-drug self-assembly was considered as a simple and efficient approach to prepare high drug loading nano-drug carriers and present new opportunities for cancer therapeutics. The strategy of PTX amphiphiles preparation would be a possible way to solve the poor water solubility of PTX. Methods: The PTX-YSL conjugate were synthesized and characterized. The PTX-YSL nanocarriers was prepared by a simple self-assembly method. In vitro cell studies and pharmacokinetic studies were evaluated for their in vitro anti-tumor activities and blood retention time. Results: The structures of PTX-YSL conjugate were confirmed by LC-MS, 1H NMR and FTIR. The size and morphology of the PTX-YSL self-assembled nanocarriers were observed with TEM and DLS. PTX-YSL nanocarriers could facilitate cellular uptake and had low cytotoxicity. PTX-YSL nanocarriers have longer blood retention for enhancing accumulation in the tumor tissues via EPR effect. Conclusion: This drug delivery system formed by PTX-YSL conjugates constitutes a promising and effective drug carrier in cancer therapy.

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Synthesis, Self-Assembly and In Vitro Cellular Uptake Kinetics of Nanosized Drug Carriers Based on Aggregates of Amphiphilic Oligomers of N-Vinyl-2-pyrrolidone

Materials ◽

10.3390/ma14205977 ◽

2021 ◽

Vol 14 (20) ◽

pp. 5977

Author(s):

Pavel P. Kulikov ◽

Anna L. Luss ◽

Levi C. Nelemans ◽

Mikhail I. Shtilman ◽

Yaroslav O. Mezhuev ◽

...

Keyword(s):

Cellular Uptake ◽

Self Assembly ◽

Targeted Delivery ◽

Drug Carriers ◽

Cellular Level ◽

Endocytic Pathway ◽

Critical Aggregation Concentration ◽

Exponential Dependence ◽

Major Mechanism

Development of nanocarrier-based drug delivery systems is a major breakthrough in pharmacology, promising targeted delivery and reduction in drug toxicity. On the cellular level, encapsulation of a drug substantially affects the endocytic processes due to nanocarrier–membrane interaction. In this study we synthesized and characterized nanocarriers assembled from amphiphilic oligomers of N-vinyl-2-pyrrolidone with a terminal thiooctadecyl group (PVP-OD). It was found that the dissolution free energy of PVP-OD depends linearly on the molecular mass of its hydrophilic part up to M¯n = 2 × 104, leading to an exponential dependence of critical aggregation concentration (CAC) on the molar mass. A model hydrophobic compound (DiI dye) was loaded into the nanocarriers and exhibited slow release into the aqueous phase on a scale of 18 h. Cellular uptake of the loaded nanocarriers and that of free DiI were compared in vitro using glioblastoma (U87) and fibroblast (CRL2429) cells. While the uptake of both DiI/PVP-OD nanocarriers and free DiI was inhibited by dynasore, indicating a dynamin-dependent endocytic pathway as a major mechanism, a decrease in the uptake rate of free DiI was observed in the presence of wortmannin. This suggests that while macropinocytosis plays a role in the uptake of low-molecular components, this pathway might be circumvented by incorporation of DiI into nanocarriers.

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SiO2-PVA-Fe(acac)3 Hybrid Based Superparamagnetic Nanocomposites for Nanomedicine: Morpho-textural Evaluation and In Vitro Cytotoxicity Assay

Molecules ◽

10.3390/molecules25030653 ◽

2020 ◽

Vol 25 (3) ◽

pp. 653 ◽

Cited By ~ 1

Author(s):

Ana-Maria Putz ◽

Cătălin Ianăși ◽

Zoltán Dudás ◽

Dorina Coricovac ◽

Claudia (Farcas) Watz ◽

...

Keyword(s):

Cell Viability ◽

Cell Line ◽

Cell Lines ◽

Drug Carriers ◽

In Vitro Cytotoxicity ◽

Mri Contrast Agents ◽

Cytotoxicity Assay ◽

Tumour Cell Line ◽

Vitro Assay

A facile sol-gel route has been applied to synthesize hybrid silica-PVA-iron oxide nanocomposite materials. A step-by-step calcination (processing temperatures up to 400 °C) was applied in order to oxidize the organics together with the iron precursor. Transmission electron microscopy, X-ray diffraction, small angle neutron scattering, and nitrogen porosimetry were used to determine the temperature-induced morpho-textural modifications. In vitro cytotoxicity assay was conducted by monitoring the cell viability by the means of MTT assay to qualify the materials as MRI contrast agents or as drug carriers. Two cell lines were considered: the HaCaT (human keratinocyte cell line) and the A375 tumour cell line of human melanoma. Five concentrations of 10 µg/mL, 30 µg/mL, 50 µg/mL, 100 µg/mL, and 200 µg/mL were tested, while using DMSO (dimethylsulfoxid) and PBS (phosphate saline buffer) as solvents. The HaCaT and A375 cell lines were exposed to the prepared agent suspensions for 24 h. In the case of DMSO (dimethyl sulfoxide) suspensions, the effect on human keratinocytes migration and proliferation were also evaluated. The results indicate that only the concentrations of 100 μg/mL and 200 μg/mL of the nanocomposite in DMSO induced a slight decrease in the HaCaT cell viability. The PBS based in vitro assay showed that the nanocomposite did not present toxicity on the HaCaT cells, even at high doses (200 μg/mL agent).

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pH- and temperature-sensitive self-assembly microcapsules/microparticles: Synthesis, characterization, in vitro cytotoxicity, and drug release properties

Journal of Biomedical Materials Research Part B Applied Biomaterials ◽

10.1002/jbm.b.31900 ◽

2011 ◽

Vol 100B (2) ◽

pp. 305-313 ◽

Cited By ~ 6

Author(s):

Liwei Ma ◽

Mingzhu Liu ◽

Xiang Shi

Keyword(s):

Drug Release ◽

Self Assembly ◽

In Vitro Cytotoxicity ◽

Temperature Sensitive

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Peptide-Based Soft Hydrogels Modified with Gadolinium Complexes as MRI Contrast Agents

Pharmaceuticals ◽

10.3390/ph13020019 ◽

2020 ◽

Vol 13 (2) ◽

pp. 19 ◽

Cited By ~ 5

Author(s):

Enrico Gallo ◽

Carlo Diaferia ◽

Enza Di Gregorio ◽

Giancarlo Morelli ◽

Eliana Gianolio ◽

...

Keyword(s):

Structural Characterization ◽

Self Assembly ◽

In Vitro Cytotoxicity ◽

Mri Contrast Agents ◽

Mri Contrast ◽

High Relaxivity ◽

Diagnostic Agents ◽

Magnetic Resonance Imaging Mri ◽

Branched Nanostructures

Poly-aromatic peptide sequences are able to self-assemble into a variety of supramolecular aggregates such as fibers, hydrogels, and tree-like multi-branched nanostructures. Due to their biocompatible nature, these peptide nanostructures have been proposed for several applications in biology and nanomedicine (tissue engineering, drug delivery, bioimaging, and fabrication of biosensors). Here we report the synthesis, the structural characterization and the relaxometric behavior of two novel supramolecular diagnostic agents for magnetic resonance imaging (MRI) technique. These diagnostic agents are obtained for self-assembly of DTPA(Gd)-PEG8-(FY)3 or DOTA(Gd)-PEG8-(FY)3 peptide conjugates, in which the Gd-complexes are linked at the N-terminus of the PEG8-(FY)3 polymer peptide. This latter was previously found able to form self-supporting and stable soft hydrogels at a concentration of 1.0% wt. Analogously, also DTPA(Gd)-PEG8-(FY)3 and DOTA(Gd)-PEG8-(FY)3 exhibit the trend to gelificate at the same range of concentration. Moreover, the structural characterization points out that peptide (FY)3 moiety keeps its capability to arrange into β-sheet structures with an antiparallel orientation of the β-strands. The high relaxivity value of these nanostructures (~12 mM−1·s−1 at 20 MHz) and the very low in vitro cytotoxicity suggest their potential application as supramolecular diagnostic agents for MRI.

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