Research

17 pages, 27681 KiB

Open AccessArticle

Poly-L-Lysine–Lactobionic Acid-Capped Selenium Nanoparticles for Liver-Targeted Gene Delivery

by Shaigan Naidoo, Aliscia Daniels, Saffiya Habib and Moganavelli Singh

Int. J. Mol. Sci. 2022, 23(3), 1492; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23031492 - 27 Jan 2022

Cited by 20 | Viewed by 3521

Liver cancer is currently regarded as the second leading cause of cancer-related mortality globally and is the sixth most diagnosed malignancy. Selenium nanoparticles (SeNPs) have attracted favorable attention as nanocarriers for gene therapy, as they possess beneficial antioxidant and anticancer properties. This study [...] Read more.

Liver cancer is currently regarded as the second leading cause of cancer-related mortality globally and is the sixth most diagnosed malignancy. Selenium nanoparticles (SeNPs) have attracted favorable attention as nanocarriers for gene therapy, as they possess beneficial antioxidant and anticancer properties. This study aimed to design, functionalize and characterize SeNPs to efficiently bind, protect and deliver pCMV–Luc DNA to hepatocellular carcinoma (HepG2) cells. The SeNPs were synthesized by ascorbic acid reduction and functionalized with poly-L-lysine (PLL) to stabilize and confer positive charges to the nanoparticles. The SeNPs were further decorated with lactobionic acid (LA) to target the asialoglycoprotein receptors abundantly expressed on the surface of the hepatocytes. All SeNPs were spherical, in the nanoscale range (<130 nm) and were capable of successfully binding, compacting and protecting the pDNA against nuclease degradation. The functionalized SeNP nanocomplexes exhibited minimal cytotoxicity (<30%) with enhanced transfection efficiency in the cell lines tested. Furthermore, the targeted SeNP (LA–PLL–SeNP) nanocomplex showed significant (* p < 0.05, ** p < 0.01, **** p < 0.0001) transgene expression in the HepG2 cells compared to the receptor-negative embryonic kidney (HEK293) cells, confirming receptor-mediated endocytosis. Overall, these functionalized SeNPs exhibit favorable features of suitable gene nanocarriers for the treatment of liver cancer. Full article

(This article belongs to the Special Issue Nanostructured Formulations in Pharmaceutical, Medical and Cosmetic Applications)

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14 pages, 6656 KiB

Open AccessArticle

Curcumin Loaded Nanocarriers with Varying Charges Augmented with Electroporation Designed for Colon Cancer Therapy

by Julita Kulbacka, Kazimiera A. Wilk, Urszula Bazylińska, Magda Dubińska-Magiera, Stanisław Potoczek and Jolanta Saczko

Int. J. Mol. Sci. 2022, 23(3), 1377; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23031377 - 26 Jan 2022

Cited by 9 | Viewed by 3112

Abstract

(1) Background: The size and surface charge are the most significant parameters of nanocarriers that determine their efficiency and potential application. The poor cell uptake of encapsulated drugs is the main limitation in anticancer treatment. The well-defined properties of nanocarriers will enable to [...] Read more.

(1) Background: The size and surface charge are the most significant parameters of nanocarriers that determine their efficiency and potential application. The poor cell uptake of encapsulated drugs is the main limitation in anticancer treatment. The well-defined properties of nanocarriers will enable to target specific tissue and deliver an active cargo. (2) Methods: In the current study, poly(D,L -lactide) (PLA) nanocarriers loaded with curcumin (CUR) and differing surface charge were evaluated for transport efficacy in combination with electroporation (EP) in dependence on the type of cells. The obtained CUR-loaded nanoparticles with diameters ranging from 195 to 334 nm (derived from dynamic light scattering (DLS)) were characterized by atomic force microscopy (AFM) (morphology and shape) and Doppler electrophoresis (ζ-potential) as well as UV-vis spectroscopy (CUR encapsulation efficiency (about 90%) and photobleaching rate). The drug delivery properties of the obtained PLA nanocarriers enhanced by electroporation were assessed in human colon cancer cells (LoVo), excitable normal rat muscle cells (L6), and free of voltage-gated ion channels cells (CHO-K1). CLSM studies, viability, and ROS release were performed to determine the biological effects of nanocarriers. (3) Results: The highest photodynamic activity indicated anionic nanocarriers (1a) stabilized by C₁₂(COONa)₂ surfactant. Nanocarriers were cytotoxic for LoVo cells and less cytotoxic for normal cells. ROS release increased in cancer cells with the increasing electric field intensity, irradiation, and time after EP. Muscle L6 cells were less sensitive to electric pulses. (4) Conclusions: EP stimulation for CUR-PLA nanocarriers transport was considered to improve the regulated and more effective delivery of nanosystems differing in surface charge. Full article

(This article belongs to the Special Issue Nanostructured Formulations in Pharmaceutical, Medical and Cosmetic Applications)

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19 pages, 4126 KiB

Open AccessArticle

Textural and Thermal Properties of the Novel Fucoidan/Nano-Oxides Hybrid Materials with Cosmetic, Pharmaceutical and Environmental Potential

by Jakub Matusiak, Urszula Maciołek, Małgorzata Kosińska-Pezda, Dariusz Sternik, Jolanta Orzeł and Elżbieta Grządka

Int. J. Mol. Sci. 2022, 23(2), 805; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23020805 - 12 Jan 2022

Cited by 7 | Viewed by 2070

Abstract

The main purpose of the research was to obtain and study hybrid materials based on three different nano-oxides commonly used in the cosmetic and pharmaceutical industries: Al₂O₃, TiO₂, and ZnO, with the natural bioactive polysaccharide fucoidan. Since [...] Read more.

The main purpose of the research was to obtain and study hybrid materials based on three different nano-oxides commonly used in the cosmetic and pharmaceutical industries: Al₂O₃, TiO₂, and ZnO, with the natural bioactive polysaccharide fucoidan. Since the mentioned oxides are largely utilized by industry, there is no doubt that the presented studies are important from an environmental point of view. On the basis of the textural studies (dynamic light scattering DLS, low temperature nitrogen adsorption, X-ray diffraction analysis XRD, scanning electron microscopy SEM) it was proved that the properties of the hybrid materials differ from the pure components of the system. Moreover, the advanced thermal analysis (TG-DTG-DSC) combined with the evolved gas analysis using Fourier transformed infrared spectroscopy (FTIR) and mass spectrometry were applied to describe the thermal decomposition of fucoidan, oxides and hybrid materials. It was found that the interactions between the polymer and the oxides results in the formation of the hybrid materials due to the functionalization of the nanoparticles surface, and that their thermal stability increased when compared to the pure substrates. Such findings definitely fill the literature void regarding the fucoidan based hybrid materials and help the industrial formulators in the preparation of new products. Full article

(This article belongs to the Special Issue Nanostructured Formulations in Pharmaceutical, Medical and Cosmetic Applications)

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17 pages, 2600 KiB

Open AccessArticle

Development and Evaluation of Repurposed Etoricoxib Loaded Nanoemulsion for Improving Anticancer Activities against Lung Cancer Cells

by Shadab Md, Nabil A. Alhakamy, Waleed S. Alharbi, Javed Ahmad, Rasheed A. Shaik, Ibrahim M. Ibrahim and Javed Ali

Int. J. Mol. Sci. 2021, 22(24), 13284; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222413284 - 10 Dec 2021

Cited by 11 | Viewed by 2712

Abstract

In the present work, novel modality for lung cancer intervention has been explored. Primary literature has established the potential role of cyclooxygenase-2 (COX-2) inhibitor in regression of multiple forms of carcinomas. To overcome its poor water solubility and boost anticancer activity, etoricoxib (ETO) [...] Read more.

In the present work, novel modality for lung cancer intervention has been explored. Primary literature has established the potential role of cyclooxygenase-2 (COX-2) inhibitor in regression of multiple forms of carcinomas. To overcome its poor water solubility and boost anticancer activity, etoricoxib (ETO) was chosen as a therapeutic candidate for repurposing and formulated into a nanoemulsion (NE). The prepared ETO loaded NE was characterized for the surface charge, droplet size, surface morphology, and in vitro release. The optimized ETO loaded NE was then investigated for its anticancer potential employing A549 lung cancer cell line via cytotoxicity, apoptotic activity, mitochondrial membrane potential activity, cell migration assay, cell cycle analysis, Caspase-3, 9, and p53 activity by ELISA and molecular biomarker analysis through RT-PCR test. The developed ETO-NE formulation showed adequate homogeneity in the droplet size distribution with polydispersity index (PDI) of (0.2 ± 0.03) and had the lowest possible droplet size (124 ± 2.91 nm) and optimal negative surface charge (−8.19 ± 1.51 mV) indicative of colloidal stability. The MTT assay results demonstrated that ETO-NE exhibited substantial anticancer activity compared to the free drug. The ETO-NE showed a substantially potent cytotoxic effect against lung cancer cells, as was evident from the commencement of apoptosis/necrotic cell death and S-phase cell cycle arrests in A549 cells. The study on these molecules through RT-PCR confirmed that ETO-NE is significantly efficacious in mitigating the abundance of IL-B, IL-6, TNF, COX-2, and NF-kB as compared to the free ETO and control group. The current study demonstrates that ETO-NE represents a feasible approach that could provide clinical benefits for lung cancer patients in the future. Full article

(This article belongs to the Special Issue Nanostructured Formulations in Pharmaceutical, Medical and Cosmetic Applications)

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11 pages, 2997 KiB

Open AccessArticle

Using a Cellular System to Directly Assess the Effects of Cosmetic Microemulsion Encapsulated DeoxyArbutin

by Nai-Fang Chang, Feng-Jie Tsai, Ya-Min Zheng, Wei-Hsiang Huang and Chih-Chien Lin

Int. J. Mol. Sci. 2021, 22(23), 13110; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222313110 - 03 Dec 2021

Cited by 2 | Viewed by 1681

Abstract

DeoxyArbutin (dA) is a tyrosinase inhibitor that has effective skin-lightening activity and has no obvious cytotoxicity toward melanocytes. With the aim of directly evaluating the effects of microemulsions containing dA on cells, we developed oil-in-water (O/W) microemulsions with relatively lower cytotoxicities by using [...] Read more.

DeoxyArbutin (dA) is a tyrosinase inhibitor that has effective skin-lightening activity and has no obvious cytotoxicity toward melanocytes. With the aim of directly evaluating the effects of microemulsions containing dA on cells, we developed oil-in-water (O/W) microemulsions with relatively lower cytotoxicities by using polysorbate-series surfactants. Measurement of the transparent properties and particle size analysis at different storage time periods revealed that the developed microemulsions were stable. Moreover, the developed microemulsions had direct effects on B16-F10 mouse melanoma cells. The anti-melanogenesis activities of dA-containing microemulsions were evidently better than that of the free dA group. The results demonstrated that the developed microemulsion encapsulating dA may allow the use of deoxyArbutin instead of hydroquinone to treat dermal hyperpigmentation disorders in the future. Full article

(This article belongs to the Special Issue Nanostructured Formulations in Pharmaceutical, Medical and Cosmetic Applications)

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12 pages, 2771 KiB

Open AccessArticle

Polyaminoacid Based Core@shell Nanocarriers of 5-Fluorouracil: Synthesis, Properties and Theranostics Application

by Marta Szczęch, Alicja Hinz, Natalia Łopuszyńska, Monika Bzowska, Władysław P. Węglarz and Krzysztof Szczepanowicz

Int. J. Mol. Sci. 2021, 22(23), 12762; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222312762 - 25 Nov 2021

Cited by 3 | Viewed by 1518

Abstract

Cancer is one of the most important health problems of our population, and one of the common anticancer treatments is chemotherapy. The disadvantages of chemotherapy are related to the drug’s toxic effects, which act on cancer cells and the healthy part of the [...] Read more.

Cancer is one of the most important health problems of our population, and one of the common anticancer treatments is chemotherapy. The disadvantages of chemotherapy are related to the drug’s toxic effects, which act on cancer cells and the healthy part of the body. The solution of the problem is drug encapsulation and drug targeting. The present study aimed to develop a novel method of preparing multifunctional 5-Fluorouracil (5-FU) nanocarriers and their in vitro characterization. 5-FU polyaminoacid-based core@shell nanocarriers were formed by encapsulation drug-loaded nanocores with polyaminoacids multilayer shell via layer-by-layer method. The size of prepared nanocarriers ranged between 80–200 nm. Biocompatibility of our nanocarriers as well as activity of the encapsulated drug were confirmed by MTT tests. Moreover, the ability to the real-time observation of developed nanocarriers and drug accumulation inside the target was confirmed by fluorine magnetic resonance imaging (¹⁹F-MRI). Full article

(This article belongs to the Special Issue Nanostructured Formulations in Pharmaceutical, Medical and Cosmetic Applications)

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21 pages, 8112 KiB

Open AccessArticle

Influence of Zwitterionic CAPB on Flocculation of the Aqueous Cationic Guar Gum/Glauconite Suspensions at Various pH

by Ewelina Godek, Elżbieta Grządka, Urszula Maciołek and Anna Bastrzyk

Int. J. Mol. Sci. 2021, 22(22), 12157; https://doi.org/10.3390/ijms222212157 - 10 Nov 2021

Cited by 5 | Viewed by 2187

Abstract

The influence of the pseudoamphoteric zwitterionic surfactant cocamidopropylbetaine (CAPB) on the stabilizing flocculating properties of the aqueous suspensions of glauconite (GT) with cationic guar gum (CGG) at various pH values was investigated. The following techniques were used: turbidimetry, UV-VIS spectrophotometry, tensiometry, electrophoretic mobility [...] Read more.

The influence of the pseudoamphoteric zwitterionic surfactant cocamidopropylbetaine (CAPB) on the stabilizing flocculating properties of the aqueous suspensions of glauconite (GT) with cationic guar gum (CGG) at various pH values was investigated. The following techniques were used: turbidimetry, UV-VIS spectrophotometry, tensiometry, electrophoretic mobility measurements, SEM, CHN, XRD, and FT-IR. It was established that CGG is an effective glauconite flocculant. Moreover, the most probable mechanism that is responsible for flocculation is bridge flocculation resulting from polymer adsorption on the glauconite surface. The adsorption process is caused by electrostatic interactions between the negatively charged glauconite surface and the positively charged polymer. The amount of CGG adsorption increases with the increase of the pH, which was confirmed by the adsorption and zeta potential measurements. The addition of CAPB increases the amount of the polymer adsorption due to the formation of intermolecular polymer–surfactant complexes; however, it reduces flocculation effectiveness. Full article

(This article belongs to the Special Issue Nanostructured Formulations in Pharmaceutical, Medical and Cosmetic Applications)

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12 pages, 2015 KiB

Open AccessArticle

Biodegradable Amphoteric Surfactants in Titration-Ultrasound Formulation of Oil-in-Water Nanoemulsions: Rational Design, Development, and Kinetic Stability

by Ewelina Waglewska and Urszula Bazylińska

Int. J. Mol. Sci. 2021, 22(21), 11776; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222111776 - 29 Oct 2021

Cited by 8 | Viewed by 2408

Abstract

Amphoteric amphiphilic compounds, due to their unique properties, may represent a group of safe and biocompatible surface-active agents for effective colloidal stabilization of nanoformulations. For this reason, the aim of this work was to develop and characterize the oil-in-water nanoemulsions based on two [...] Read more.

Amphoteric amphiphilic compounds, due to their unique properties, may represent a group of safe and biocompatible surface-active agents for effective colloidal stabilization of nanoformulations. For this reason, the aim of this work was to develop and characterize the oil-in-water nanoemulsions based on two betaine-derived surfactants with high biodegradability, i.e., cocamidopropyl betaine and coco-betaine. In the first step, we investigated ternary phase diagrams of surfactant-oil-water systems containing different weight ratios of surfactant and oil, as the betaine-type surfactant entity (S), linoleic acid, or oleic acid as the oil phase (O), and the aqueous phase (W) using the titration-ultrasound approach. All the received nanoemulsion systems were then characterized upon droplets size (dynamic light scattering), surface charge (electrophoretic light scattering), and morphology (transmission electron as well as atomic force microscopy). Thermal and spinning tests revealed the most stable compositions, which were subjected to further kinetic stability analysis, including turbidimetric evaluation. Finally, the backscattering profiles revealed the most promising candidate with a size <200 nm for potential delivery of active agents in the future cosmetic, pharmaceutical, and biomedical applications. Full article

(This article belongs to the Special Issue Nanostructured Formulations in Pharmaceutical, Medical and Cosmetic Applications)

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