Serum Stability and Physicochemical Characterization of a Novel Amphipathic Peptide C6M1 for SiRNA Delivery

Effective delivery of siRNA (small interfering RNA) into the cells requires the translocation of siRNA into the cytosol. One potential delivery strategy uses cell-delivery peptides that facilitate this step. In the present paper, we describe the characterization of an amphipathic peptide that mediates the uptake of non-covalently bound siRNA into cells and its subsequent release into the cytosol. Biophysical characterization of peptide and peptide/siRNA mixtures at neutral and lysosomal (acidic) pH suggested the formation of α-helical structure only in endosomes and lysosomes. Surprisingly, even though the peptide enhanced the uptake of siRNA into cells, no direct interaction between siRNA and peptide was observed at neutral pH by isothermal titration calorimetry. Importantly, we show that peptide-mediated siRNA uptake occurred through endocytosis and, by applying novel endosomal-escape assays and cell-fractionation techniques, we demonstrated a pH-dependent alteration in endosome and lysosome integrity and subsequent release of siRNA and other cargo into the cytosol. These results indicate a peptide-mediated siRNA delivery through a pH-dependent and conformation-specific interaction with cellular membranes and not with the cargo.

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Formulation Strategies, Characterization, and In Vitro Evaluation of Lecithin-Based Nanoparticles for siRNA Delivery

Journal of Drug Delivery ◽

10.1155/2012/986265 ◽

2012 ◽

Vol 2012 ◽

pp. 1-9 ◽

Cited By ~ 4

Author(s):

Sebastián Ezequiel Pérez ◽

Yamila Gándola ◽

Adriana Mónica Carlucci ◽

Lorena González ◽

Daniel Turyn ◽

...

Keyword(s):

Ex Vivo ◽

Sirna Delivery ◽

Physicochemical Characterization ◽

Human Breast ◽

Efficient Delivery ◽

Interfering Rna ◽

Mcf 7

The aim of the present work was to take advantage of lecithin’s biocompatibility along with its physicochemical properties for the preparation of lecithin-based nanocarriers for small interfering RNA (siRNA) delivery. Water lecithin dispersions were prepared in different conditions, loaded with siRNA at different N/P ratios, and evaluated for loading capacity. The most appropriate ones were then assayed for cytotoxicity and characterized in terms of particle size distribution, zeta potential, and morphology. Results demonstrated that formulations prepared at pH 5.0 and 7.0 were able to load siRNA at broad N/P ratios, and cellular uptake assays showed an efficient delivery of oligos in MCF-7 human breast cancer cells; fluorescent-labeled dsRNA mainly located next to its target, near the nucleus of the cells. No signs of toxicity were observed for broad compositions of lecithin. The physicochemical characterization of the siRNA-loaded dispersions exhibited particles of nanometric sizes and pH-dependant shapes, which make them suitable for ex vivo and in vivo further evaluation.

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Physicochemical Characterization of Nanocomposite Based on Recycled Expanded Polystyrene Reinforced with Clay: Application as Methanol Fuel Cell Membrane

Modern Environmental Science and Engineering ◽

10.15341/mese(2333-2581)/04.02.2016/011 ◽

2016 ◽

Vol 2 (04) ◽

pp. 279-287

Author(s):

Mbarek Stouri ◽

Imene Bekri-Abbes ◽

Ezzeddine Srasra

Keyword(s):

Fuel Cell ◽

Cell Membrane ◽

Physicochemical Characterization ◽

Expanded Polystyrene ◽

Methanol Fuel Cell

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Optimization and Physicochemical Characterization of Chitosan and Chitosan Nanoparticles Extracted from the Crayfish Procambarus clarkii Wastes

Journal of Shellfish Research ◽

10.2983/035.038.0220 ◽

2019 ◽

Vol 38 (2) ◽

pp. 385 ◽

Cited By ~ 3

Author(s):

Marwa M. El-Naggar ◽

Wael S. I. Abou-Elmagd ◽

Ashraf Suloma ◽

Hamza A. El-Shabaka ◽

Magdy T. Khalil ◽

...

Keyword(s):

Procambarus Clarkii ◽

Chitosan Nanoparticles ◽

Physicochemical Characterization

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Morpho-anatomical, histological, phytochemical and physicochemical characterization of Dicliptera bupleuroies Nees

Pakistan Journal of Botany ◽

10.30848/pjb2021-3(23) ◽

2020 ◽

Vol 53 (3) ◽

Author(s):

Shehla Akbar ◽

Saiqa Ishtiaq

Keyword(s):

Physicochemical Characterization

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Physicochemical Characterization of Solid Dispersions of Cefdinir with PVP K-30 and PEG 4000

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2010.3.2.8 ◽

2010 ◽

Vol 3 (2) ◽

pp. 948-956

Author(s):

Kumar P ◽

S Kumar ◽

A Kumar ◽

M Chander

Keyword(s):

Solid Dispersions ◽

Physicochemical Characterization ◽

Drug Carriers ◽

Dissolution Properties ◽

Rate Of Dissolution ◽

Peg 4000 ◽

Release Studies ◽

Crystalline Nature ◽

Physical Mixtures

The purpose of this study was to prepare and characterize solid dispersions of the antibacterial agent Cefdinir with PEG 4000 and PVP K-30 with a view to improve its dissolution properties. Investigations of the properties of the dispersions were performed using release studies, X-ray powder diffraction (XRD) and Fourier transform infrared (FTIR). The results obtained showed that the rate of dissolution of Cefdinir was considerably improved when formulated in solid dispersions with PVP K-30 and PEG 4000 as compared with pure drug and physical mixtures. The results from XRD studies showed the transition of crystalline nature of drug to amorphous form, while FTIR studies demonstrated the absence of drug-carriers interaction.

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