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23 pages, 7244 KiB

Open AccessArticle

Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis

by Perwez Alam, Mohd Imran, Samreen Jahan, Ali Akhtar and Zafrul Hasan

Gels 2023, 9(10), 791; https://doi.org/10.3390/gels9100791 - 01 Oct 2023

Viewed by 1515

Abstract

In this study, hesperidin was loaded into a transethosome and was developed employing the rotary evaporator method. The formulation was optimized using the Box–Behnken design (BBD). The optimized HSD-TE formulation has a spherical shape, vesicle size, polydispersity index, entrapment efficiency, and zeta potential [...] Read more.

In this study, hesperidin was loaded into a transethosome and was developed employing the rotary evaporator method. The formulation was optimized using the Box–Behnken design (BBD). The optimized HSD-TE formulation has a spherical shape, vesicle size, polydispersity index, entrapment efficiency, and zeta potential within the range of 178.98 nm; the PDI was 0.259 with a zeta potential of −31.14 mV and % EE of 89.51%, respectively. The in vitro drug release shows that HSD-TE exhibited the release of 81.124 ± 3.45% in comparison to HSD suspension. The ex vivo skin permeation showed a 2-fold increase in HSD-TE gel permeation. The antioxidant activity of HSD-TE was found to be 79.20 ± 1.77% higher than that of the HSD solution. The formulation showed 2-fold deeper HSD-TE penetration across excised rat skin membranes in confocal laser microscopy scanning, indicating promising in vivo prospects. In a dermatokinetic study, HSD-TE gel was compared to HSD conventional gel where TE significantly boosted HSD transport in the epidermis and dermal layers. The formulation showed greater efficacy than free HSD in the inhibition of microbial growth, as evidenced by antibacterial activity on the Gram-negative and positive bacteria. These investigations found that the HSD-TE formulation could enhance the topical application in the management of cutaneous bacterial infections. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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13 pages, 5447 KiB

Open AccessArticle

Collagen Hydrolysate Effects on Photodynamic Efficiency of Gallium (III) Phthalocyanine on Pigmented Melanoma Cells

by Vanya Mantareva, Ivan Iliev, Inna Sulikovska, Mahmut Durmuş and Tsanislava Genova

Gels 2023, 9(6), 475; https://doi.org/10.3390/gels9060475 - 09 Jun 2023

Cited by 1 | Viewed by 1104

Abstract

The conjugation of photosensitizer with collagen seems to be a very promising approach for innovative topical photodynamic therapy (PDT). The study aims to evaluate the effects of bovine collagen hydrolysate (Clg) on the properties of gallium (III) phthalocyanine (GaPc) on pigmented melanoma. The [...] Read more.

The conjugation of photosensitizer with collagen seems to be a very promising approach for innovative topical photodynamic therapy (PDT). The study aims to evaluate the effects of bovine collagen hydrolysate (Clg) on the properties of gallium (III) phthalocyanine (GaPc) on pigmented melanoma. The interaction of GaPc with Clg to form a conjugate (GaPc-Clg) showed a reduction of the intensive absorption Q-band (681 nm) with a blue shift of the maximum (678 nm) and a loss of shape of the UV-band (354 nm). The fluorescence of GaPc, with a strong emission peak at 694 nm was blue shifted due to the conjugation which lower intensity owing to reduce quantum yield (0.012 vs. 0.23, GaPc). The photo- and dark cytotoxicity of GaPc, Glg and GaPc-Clg on pigmented melanoma cells (SH-4) and two normal cell lines (BJ and HaCaT) showed a slight decrease of cytotoxicity for a conjugate, with low selectivity index (0.71 vs. 1.49 for GaPc). The present study suggests that the ability of collagen hydrolysate to form gels minimizes the high dark toxicity of GaPc. Collagen used for conjugation of a photosensitizer might be an essential step in advanced topical PDT. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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15 pages, 2147 KiB

Open AccessArticle

Resveratrol-Loaded Chia Seed Oil-Based Nanogel as an Anti-Inflammatory in Adjuvant-Induced Arthritis

by Obaid Afzal, Abdulamalik S. A. Altamimi, Mubarak A. Alamri, Ali Altharawi, Manal A. Alossaimi, Md Sayeed Akhtar, Fauzia Tabassum, Waleed H. Almalki and Tanuja Singh

Gels 2023, 9(2), 131; https://doi.org/10.3390/gels9020131 - 03 Feb 2023

Cited by 2 | Viewed by 1900

Abstract

Natural anti-inflammatory nutraceuticals may be useful in preventing rheumatoid arthritis from worsening. Resveratrol (RV) and chia seed oil, having antioxidant potential, can assist in avoiding oxidative stress-related disorders. This investigation developed and evaluated resveratrol-loaded chia seed oil-based nanoemulsion (NE) gel formulations through in [...] Read more.

Natural anti-inflammatory nutraceuticals may be useful in preventing rheumatoid arthritis from worsening. Resveratrol (RV) and chia seed oil, having antioxidant potential, can assist in avoiding oxidative stress-related disorders. This investigation developed and evaluated resveratrol-loaded chia seed oil-based nanoemulsion (NE) gel formulations through in vitro and in vivo studies. The physical stability and in vitro drug permeability of the chosen formulations (NE1 to NE10) were studied. The optimized RV-loaded nanoemulsion (NE2) had droplets with an average size of 37.48 nm that were homogeneous in shape and had a zeta potential of −18 mV. RV-NE2, with a permeability of 98.21 ± 4.32 µg/cm²/h, was gelled with 1% carbopol-940P. A 28-day anti-arthritic assessment (body weight, paw edema, and levels of pro-inflammatory mediators including TNF-α, IL-6, IL-1β, and COX-2) following topical administration of RV-NE2 gel showed significant reversal of arthritic symptoms in arthritic Wistar rats induced by Freund’s complete adjuvant injection. Therefore, RV-NE2 gel demonstrated the potential to achieve local therapeutic benefits in inflammatory arthritic conditions due to its increased topical bioavailability and balancing of pro-inflammatory mediators. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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15 pages, 1302 KiB

Open AccessArticle

Effectiveness of Epidermal Growth Factor Loaded Carboxymethylcellulose (EGF-CMC) Hydrogel in Biofilm Formation in Wounds of Diabetic Patients: A Randomized Clinical Trial

by Fernanda Soares Pessanha, Beatriz Guitton Renaud Baptista de Oliveira, Bianca Campos Oliveira, Gabriela Deutsch, Felipe Lopes Teixeira, Luciana Castilho Bokehi, Mariana Alcântara Calomino, Selma Rodrigues de Castilho, Rossana Mara da Silva Moreira Thiré, Lenise Arneiro Teixeira and Geraldo Renato de Paula

Gels 2023, 9(2), 117; https://doi.org/10.3390/gels9020117 - 01 Feb 2023

Cited by 4 | Viewed by 1583

Abstract

Diabetic patients frequently develop wounds, which can be colonized by bacteria, mainly Staphylococcus aureus and Pseudomonas aeruginosa, with the ability to form biofilms. This study aimed to evaluate the colonization and biofilm formation of Staphylococcus aureus and Pseudomonas aeruginosa in chronic wounds [...] Read more.

Diabetic patients frequently develop wounds, which can be colonized by bacteria, mainly Staphylococcus aureus and Pseudomonas aeruginosa, with the ability to form biofilms. This study aimed to evaluate the colonization and biofilm formation of Staphylococcus aureus and Pseudomonas aeruginosa in chronic wounds of diabetic patients treated with a bioactive dressing (EGF-CMC), which consisted of a 2% carboxymethylcellulose (CMC) hydrogel loaded with epidermal growth factor (EGF). This randomized clinical trial was conducted with 25 participants: 14 treated with EGF-CMC hydrogel and 11 treated with CMC hydrogel for 12 weeks. Participants with type 2 diabetes mellitus were selected. All had diabetic foot ulcers or chronic venous ulcers. Swab collections were performed on weeks 1, 6, and 12. The laboratory analyses included the identification of strains, microbial quantification, virulence gene investigation, and the evaluation of biofilm formation. In total, 13 S. aureus strains and 15 P. aeruginosa strains were isolated. There were no statistically significant differences regarding bacterial loads and virulence genes. However, EGF-CMC-hydrogel-treated wounds were colonized by strains with lower biofilm formation abilities. The probability of isolating biofilm-producing strains from CMC-hydrogel-treated wounds was 83% greater than the probability of isolating biofilm-producing strains from EGF-CMC-treated wounds. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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14 pages, 34684 KiB

Open AccessArticle

Low-Cost Pseudo-Anthropomorphic PVA-C and Cellulose Lung Phantom for Ultrasound-Guided Interventions

by Natalia Arteaga-Marrero, Enrique Villa, Ana Belén Llanos González, Marta Elena Gómez Gil, Orlando Acosta Fernández, Juan Ruiz-Alzola and Javier González-Fernández

Gels 2023, 9(2), 74; https://doi.org/10.3390/gels9020074 - 17 Jan 2023

Cited by 1 | Viewed by 2160

Abstract

A low-cost custom-made pseudo-anthropomorphic lung phantom, offering a model for ultrasound-guided interventions, is presented. The phantom is a rectangular solidstructure fabricated with polyvinyl alcohol cryogel (PVA-C) and cellulose to mimic the healthy parenchyma. The pathologies of interest were embedded as inclusions containing gaseous, [...] Read more.

A low-cost custom-made pseudo-anthropomorphic lung phantom, offering a model for ultrasound-guided interventions, is presented. The phantom is a rectangular solidstructure fabricated with polyvinyl alcohol cryogel (PVA-C) and cellulose to mimic the healthy parenchyma. The pathologies of interest were embedded as inclusions containing gaseous, liquid, or solid materials. The ribs were 3D-printed using polyethylene terephthalate, and the pleura was made of a bidimensional reticle based on PVA-C. The healthy and pathological tissues were mimicked to display acoustic and echoic properties similar to that of soft tissues. Theflexible fabrication process facilitated the modification of the physical and acoustic properties of the phantom. The phantom’s manufacture offers flexibility regarding the number, shape, location, and composition of the inclusions and the insertion of ribs and pleura. In-plane and out-of-plane needle insertions, fine needle aspiration, and core needle biopsy were performed under ultrasound image guidance. The mimicked tissues displayed a resistance and recoil effect typically encountered in a real scenario for a pneumothorax, abscesses, and neoplasms. The presented phantom accurately replicated thoracic tissues (lung, ribs, and pleura) and associated pathologies providing a useful tool for training ultrasound-guided procedures. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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18 pages, 3691 KiB

Open AccessArticle

Electron Beam Irradiation Cross-Linked Hydrogel Patches Loaded with Red Onion Peel Extract for Transdermal Drug Delivery: Formulation, Characterization, Cytocompatibility, and Skin Permeation

by Pimpon Uttayarat, Rattanakorn Chiangnoon, Thanu Thongnopkoon, Kesinee Noiruksa, Jirachaya Trakanrungsie, Wattanaporn Phattanaphakdee, Chuda Chittasupho and Sirivan Athikomkulchai

Gels 2023, 9(1), 52; https://doi.org/10.3390/gels9010052 - 07 Jan 2023

Cited by 3 | Viewed by 2750

Abstract

The use of bioactive molecules derived from medicinal plants in wound healing has recently attracted considerable attention in both research and public interest. In this work, we demonstrated the first attempt to incorporate the extract from Thai red onion skins in hydrogel patches [...] Read more.

The use of bioactive molecules derived from medicinal plants in wound healing has recently attracted considerable attention in both research and public interest. In this work, we demonstrated the first attempt to incorporate the extract from Thai red onion skins in hydrogel patches intended for transdermal delivery. The red onion skin extract (ROSE) was first prepared and evaluated for cytotoxicity by MTT assay with both L929 and human dermal fibroblast cells. Hydrogel patches with porous microstructure and high water content were fabricated from polyvinyl alcohol (PVA) by electron beam irradiation and characterized for their physical, mechanical, morphological, and cytocompatible properties prior to the loading of ROSE. After decontamination by electron beam irradiation, the in vitro release profile exhibited the burst release of extract from ROSE-coated hydrogel patches within 5 h, followed by the sustained release up to 48 h. Finally, evaluation of skin permeation using Franz cell setup with a newborn pig skin model showed that the permeation of ROSE from the hydrogel patch increased with time and reached the maximum of 262 µg/cm², which was well below the cytotoxicity threshold, at 24 h. These results demonstrated that our ROSE-coated hydrogel patches could potentially be used in transdermal delivery. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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21 pages, 58130 KiB

Open AccessArticle

Concentration Dependent Effect of Quaternary Amines on the Adhesion of U251-MG Cells

by Nils Stamm, Kristin Glotzbach, Andreas Faissner and Ralf Weberskirch

Gels 2022, 8(12), 827; https://doi.org/10.3390/gels8120827 - 15 Dec 2022

Cited by 2 | Viewed by 1162

Abstract

Cationic gels have seen increasing interest in recent years for 2D cell cultivation since they may represent an alternative to the well-known RGD-peptide motif functionalized gels. However, few hydrogel systems with adjustable cationic strength have been fabricated and investigated so far. In this [...] Read more.

Cationic gels have seen increasing interest in recent years for 2D cell cultivation since they may represent an alternative to the well-known RGD-peptide motif functionalized gels. However, few hydrogel systems with adjustable cationic strength have been fabricated and investigated so far. In this work, eight gels with defined concentrations of cationic groups, two of which also contained the RGD peptide, were prepared from three well-defined, soluble precursor copolymers with thiol-functionalities and PEGDA3500 as a crosslinker via thiol-ene chemistry. Live/dead stainings of U-251-MG cells on the hydrogels with different concentrations of the cationic motif were made after 3 days and 7 days of cultivation. The results show a high dependence of the number of adhesive cells and their morphology, cluster versus spread cells, on the concentration of cationic groups in the gel. This effect was more pronounced when the gels were not further dialyzed before usage. In addition, a synergistic effect of the two motifs, cationic group and RGD peptide, could be demonstrated, which together induce stronger cell adhesion than either motif alone. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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16 pages, 9342 KiB

Open AccessArticle

In Situ Biosynthesis of Photothermal Parasite for Fluorescence Imaging-Guided Photothermal Therapy of Tumors

by Yaqiong Wang, Haiyan Pan, Zhaowei Meng and Cai Zhang

Gels 2022, 8(11), 754; https://doi.org/10.3390/gels8110754 - 21 Nov 2022

Cited by 1 | Viewed by 1498

Abstract

Photothermal therapy (PTT) has been widely known as a promising therapeutic strategy for cancer treatment in recent decades. However, some organic and inorganic photothermal agents exhibit shortcomings including potential long-term toxicity and lack of biodegradability. Biocompatible extracts from plants and animals provide several [...] Read more.

Photothermal therapy (PTT) has been widely known as a promising therapeutic strategy for cancer treatment in recent decades. However, some organic and inorganic photothermal agents exhibit shortcomings including potential long-term toxicity and lack of biodegradability. Biocompatible extracts from plants and animals provide several alternatives for the reformation of photothermal agents. Bio-inspired products still have inherent problems such as low accumulation in tumors, easy diffusion, and fast elimination. Herein, we aim to develop a biocompatible photothermal agent with tumor enrichment. Enlightened by “parasitized snails”, in situ biosynthesis of photothermal agents and fluorescence imaging-guided PTT are achieved with the assistance of alginate–calcium–genipin (ACG) hydrogel. ACG hydrogel is a mixture of alginate (ALG), calcium (Ca), and genipin (GP). Given that the crosslinking product of GP and protein displays fluorescent/photothermal features, the constructed ACG hydrogel can gradually react with the tumor and then “light up” and “ignite” the tumor under specific light excitation. The ACG hydrogel can be seen as a photothermal parasite, eventually leading to the death of tumor. The photothermal therapeutic effects of ACG hydrogel reacting with tumors are successfully proven in vivo. The naturally derived GP and ALG ensure the biosafety of the ACG hydrogel-based bio-application. This work is another successful practice of nature-inspired methodological strategy for in situ biosynthesis of the photothermal agent. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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17 pages, 3288 KiB

Open AccessArticle

Central Composite Design (CCD) for the Optimisation of Ethosomal Gel Formulation of Punica granatum Extract: In Vitro and In Vivo Evaluations

by Prawez Alam, Faiyaz Shakeel, Ahmed I. Foudah, Sultan Alshehri, Roshan Salfi, Mohammed H. Alqarni and Tariq M. Aljarba

Gels 2022, 8(8), 511; https://doi.org/10.3390/gels8080511 - 17 Aug 2022

Cited by 2 | Viewed by 1687

Abstract

This research manuscript’s objective was to develop the Punica granatum extract ethosome gel. The use of nanotechnology can improve transdermal drug delivery permeation of its major bioactive compound β-sitosterol. The optimised and developed formulations were further studied in vitro and in vivo. The [...] Read more.

This research manuscript’s objective was to develop the Punica granatum extract ethosome gel. The use of nanotechnology can improve transdermal drug delivery permeation of its major bioactive compound β-sitosterol. The optimised and developed formulations were further studied in vitro and in vivo. The assessment of the anti-inflammatory activity of the gel was performed in Albino rats. Methanolic extract was prepared and developed into an ethosome suspension and an ethosome gel. To optimise the formulation’s response in terms of particle size (nm) and entrapment efficiency (%), the central composite design (CCD) was used in 2² levels. The effects of factors such as lecithin (%) and ethanol (mL) in nine formulations were observed. Characterisation of ethosome gel was performed and the results showed the particle size (516.4 nm) and mean zeta potential (−45.4 mV). Evaluations of the gel formulation were performed. The results were good in terms of pH (7.1), viscosity (32,158 cps), spreadability (31.55 g cm/s), and no grittiness. In an in vitro study, the percentages of β-sitosterol release of ethosome gel (91.83%), suspension (82.74%), and extracts (68.15%) at 279 nm were recorded. The effects of the formulated gel on formalin-induced oedema in Albino rats showed good results in terms of anti-inflammatory activity. The comparative anti-inflammatory activity of Punica granatum extract and gel showed that the gel action was good for their topical application. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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Review

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26 pages, 6879 KiB

Open AccessReview

Bile Acid Sequestrants Based on Natural and Synthetic Gels

by Magdalena-Cristina Stanciu, Marieta Nichifor and Carmen-Alice Teacă

Gels 2023, 9(6), 500; https://doi.org/10.3390/gels9060500 - 19 Jun 2023

Cited by 3 | Viewed by 2270

Abstract

Bile acid sequestrants (BASs) are non-systemic therapeutic agents used for the management of hypercholesterolemia. They are generally safe and not associated with serious systemic adverse effects. Usually, BASs are cationic polymeric gels that have the ability to bind bile salts in the small [...] Read more.

Bile acid sequestrants (BASs) are non-systemic therapeutic agents used for the management of hypercholesterolemia. They are generally safe and not associated with serious systemic adverse effects. Usually, BASs are cationic polymeric gels that have the ability to bind bile salts in the small intestine and eliminate them by excretion of the non-absorbable polymer–bile salt complex. This review gives a general presentation of bile acids and the characteristics and mechanisms of action of BASs. The chemical structures and methods of synthesis are shown for commercial BASs of first- (cholestyramine, colextran, and colestipol) and second-generation (colesevelam and colestilan) and potential BASs. The latter are based on either synthetic polymers such as poly((meth)acrylates/acrylamides), poly(alkylamines), poly(allylamines) and vinyl benzyl amino polymers or biopolymers, such as cellulose, dextran, pullulan, methylan, and poly(cyclodextrins). A separate section is dedicated to molecular imprinting polymers (MIPs) because of their great selectivity and affinity for the template molecules used in the imprinting technique. Focus is given to the understanding of the relationships between the chemical structure of these cross-linked polymers and their potential to bind bile salts. The synthetic pathways used in obtaining BASs and their in vitro and in vivo hypolipidemic activities are also introduced. Full article

(This article belongs to the Special Issue Biofunctional Gels)

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