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17 pages, 5022 KiB

Open AccessArticle

Impact of Pluronic F-127 on the Stability of Quercetin-Loaded Liposomes: Insights from DSC Preformulation Studies

by Effrosyni-Maria Kosti, Heliana Sotiropoulou, Ioannis Tsichlis, Maria Tsakiri, Nikolaos Naziris and Costas Demetzos

Materials 2024, 17(22), 5454; https://doi.org/10.3390/ma17225454 - 8 Nov 2024

Viewed by 383

Abstract

The aim of the present study is to evaluate the stability of DMPC:Pluronic F-127 and DPPC:Pluronic F-127 liposomes, both with and without incorporated quercetin. Quercetin belongs to the class of flavonoids and has shown antioxidant, antiviral, anti-inflammatory, anti-cancer, and antimicrobial activities. Dynamic light [...] Read more.

The aim of the present study is to evaluate the stability of DMPC:Pluronic F-127 and DPPC:Pluronic F-127 liposomes, both with and without incorporated quercetin. Quercetin belongs to the class of flavonoids and has shown antioxidant, antiviral, anti-inflammatory, anti-cancer, and antimicrobial activities. Dynamic light scattering, electrophoretic light scattering, and differential scanning calorimetry (DSC) were utilized to investigate the cooperative behavior between liposomal components and its effect on stability. All formulations were stored at 4 °C and 25 °C and studied over 42 days. Furthermore, the interaction of the final formulations with serum proteins was assessed to evaluate the potential of Pluronic F-127 as a stabilizer in these liposomal nanosystems. This study highlights the impact of DSC in preformulation evaluations by correlating thermal behavior with quercetin incorporation and variations in size and the polydispersity index. According to the results, quercetin increased the fluidity and stability of liposomal nanosystems, while Pluronic F-127 was not sufficient for effective steric stabilization. Additionally, DSC thermograms revealed the integration of Pluronic F-127 into lipid membranes and showed phase separation in the DMPC nanosystem. In conclusion, the results indicate that the DPPC:Pluronic F-127:quercetin nanosystem exhibited the desired physicochemical and thermotropic properties for the effective delivery of quercetin for pharmaceutical purposes. Full article

(This article belongs to the Special Issue Νanoparticles for Biomedical Applications)

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20 pages, 4558 KiB

Open AccessArticle

Neomycin Intercalation in Montmorillonite: The Role of Ion Exchange Capacity and Process Conditions

by Alicja Rapacz-Kmita, Marcin Gajek, Magdalena Dudek, Roksana Kurpanik, Stanisława Kluska and Ewa Stodolak-Zych

Materials 2024, 17(17), 4207; https://doi.org/10.3390/ma17174207 - 25 Aug 2024

Viewed by 1098

Abstract

The study examined the possibility of intercalation of montmorillonite with neomycin in an aqueous drug solution and the factors influencing the effectiveness of this process, such as the ion exchange capacity and process conditions, including the time and temperature of incubation with the [...] Read more.

The study examined the possibility of intercalation of montmorillonite with neomycin in an aqueous drug solution and the factors influencing the effectiveness of this process, such as the ion exchange capacity and process conditions, including the time and temperature of incubation with the drug. X-ray diffractometry (XRD), infrared spectroscopy (FTIR), thermal analysis (DSC/TG), and Zeta potential measurement were used to confirm drug intercalation as well as to investigate the nature of clay–drug interactions. The obtained conjugates with the most favorable physicochemical properties were also tested for antibacterial response against Gram-negative bacteria (Escherichia coli) to confirm that the bactericidal properties of neomycin were retained after intercalation and UV–VIS spectrophotometry was used to examine the kinetics of drug release from the carrier. The results of the conducted research clearly indicate the successful intercalation of neomycin in montmorillonite and indicate the influence of process parameters on the properties of not only the conjugates themselves but also the properties of the intercalated drug, particularly its bactericidal activity. Ultimately, a temperature of 50 °C was found to be optimal for effective drug intercalation and the conjugates obtained within 2 h showed the highest antibacterial activity, indicating the highest potential of the thus-obtained montmorillonite conjugates as neomycin carriers. Full article

(This article belongs to the Special Issue Νanoparticles for Biomedical Applications)

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12 pages, 2314 KiB

Open AccessArticle

Development of a Resveratrol Nanoformulation for the Treatment of Diabetic Retinopathy

by Juliana Gonzalez-Perez, A. M. Lopera-Echavarría, Said Arevalo-Alquichire, Pedronel Araque-Marín and Martha E. Londoño

Materials 2024, 17(6), 1420; https://doi.org/10.3390/ma17061420 - 20 Mar 2024

Cited by 1 | Viewed by 1559

Abstract

Diabetic retinopathy (RD) is a microvascular disease that can cause the formation of fragile neovessels, increasing the risk of hemorrhages and leading to vision loss. Current therapies are based on the intravitreal injection of anti-VEGF (vascular endothelial growth factor), which is invasive and [...] Read more.

Diabetic retinopathy (RD) is a microvascular disease that can cause the formation of fragile neovessels, increasing the risk of hemorrhages and leading to vision loss. Current therapies are based on the intravitreal injection of anti-VEGF (vascular endothelial growth factor), which is invasive and can cause secondary effects. The development of new treatments that complement the current therapies is necessary to improve the patient’s outcomes. Nanostructured formulations offer several advantages regarding drug delivery and penetration. In this research, a resveratrol nanosuspension (RSV-NS) was prepared and characterized using dynamic light scattering, field emission scanning electron microscopy, and infrared spectroscopy. The RSV-NS had an average particle size of 304.0 ± 81.21 nm with a PDI of 0.225 ± 0.036, and a spherical-like morphology and uniform particle distribution. Cell viability, proliferation, and migration were tested on endothelial cells (HMRECs). RSV-NS in a concentration of less than 18.75 µM did not have a cytotoxic effect on HMRECs. Likewise, proliferation and migration were significantly reduced compared to the unstimulated control at 37.5 µM. The RSV-NS did not present cytotoxic effects but decreased cell proliferation and migration, indicating that it could provide an important contribution to future medical implementations and could have a high potential to treat this disease. Full article

(This article belongs to the Special Issue Νanoparticles for Biomedical Applications)

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18 pages, 3720 KiB

Open AccessArticle

Enhanced Codelivery of Gefitinib and Azacitidine for Treatment of Metastatic-Resistant Lung Cancer Using Biodegradable Lipid Nanoparticles

by Ehab M. Elzayat, Abdelrahman Y. Sherif, Fahd A. Nasr, Mohamed W. Attwa, Doaa H. Alshora, Sheikh F. Ahmad and Ali S. Alqahtani

Materials 2023, 16(15), 5364; https://doi.org/10.3390/ma16155364 - 30 Jul 2023

Cited by 5 | Viewed by 1697

Abstract

Lung cancer is a formidable challenge in clinical practice owing to its metastatic nature and resistance to conventional treatments. The codelivery of anticancer agents offers a potential solution to overcome resistance and minimize systemic toxicity. The encapsulation of these agents within nanostructured lipid [...] Read more.

Lung cancer is a formidable challenge in clinical practice owing to its metastatic nature and resistance to conventional treatments. The codelivery of anticancer agents offers a potential solution to overcome resistance and minimize systemic toxicity. The encapsulation of these agents within nanostructured lipid carriers (NLCs) provides a promising strategy to enhance lymphatic delivery and reduce the risk of relapse. This study aimed to develop an NLC formulation loaded with Gefitinib and Azacitidine (GEF-AZT-NLC) for the treatment of metastatic-resistant lung cancer. The physicochemical properties of the formulations were characterized, and in vitro drug release was evaluated using the dialysis bag method. The cytotoxic activity of the GEF-AZT-NLC formulations was assessed on a lung cancer cell line, and hemocompatibility was evaluated using suspended red blood cells. The prepared formulations exhibited nanoscale size (235–272 nm) and negative zeta potential values (−15 to −31 mV). In vitro study revealed that the GEF-AZT-NLC formulation retained more than 20% and 60% of GEF and AZT, respectively, at the end of the experiment. Hemocompatibility study demonstrated the safety of the formulation for therapeutic use, while cytotoxicity studies suggested that the encapsulation of both anticancer agents within NLCs could be advantageous in treating resistant cancer cells. In conclusion, the GEF-AZT-NLC formulation developed in this study holds promise as a potential therapeutic tool for treating metastatic-resistant lung cancer. Full article

(This article belongs to the Special Issue Νanoparticles for Biomedical Applications)

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13 pages, 2565 KiB

Open AccessArticle

Design and Development of Low- and Medium-Viscosity Alginate Beads Loaded with Pluronic^® F-127 Nanomicelles

by Flora Kalogeropoulou, Dimitra Papailiou, Chrystalla Protopapa, Angeliki Siamidi, Leto-Aikaterini Tziveleka, Natassa Pippa and Marilena Vlachou

Materials 2023, 16(13), 4715; https://doi.org/10.3390/ma16134715 - 29 Jun 2023

Cited by 5 | Viewed by 1952

Abstract

The anionic polymer sodium alginate, a linear copolymer of guluronic and mannuronic acids, is primarily present in brown algae. Copolymers are used in the sodium alginate preparation process to confer on the material strength and flexibility. Micelles and other polymeric nanoparticles are frequently [...] Read more.

The anionic polymer sodium alginate, a linear copolymer of guluronic and mannuronic acids, is primarily present in brown algae. Copolymers are used in the sodium alginate preparation process to confer on the material strength and flexibility. Micelles and other polymeric nanoparticles are frequently made using the triblock copolymer Pluronic^® F-127. The purpose of the present study is to determine the effect of sodium alginate’s viscosity (low and medium) and the presence of Pluronic^® F-127 micelles on the swelling behavior of the prepared pure beads and those loaded with Pluronic^® F-127 micelles. The Pluronic^® F-127 nanomicelles have a size of 120 nm. The swelling studies were carried out at pH = 1.2 (simulated gastric fluid-SGF) for two hours and at pH = 6.8 (simulated intestinal fluid-SIF) for four more hours. The swelling of both low- and medium-viscosity alginate beads was minor at pH = 1.2, irrespective of the use of Pluronic^® F-127 nanomicelles. At pH = 6.8, without Pluronic^® F-127, the beads showed an enhanced swelling ratio for the first four hours, which was even higher in the medium-viscosity alginate beads. With the addition of Pluronic^® F-127, the beads were dissolved in the first and second hour, in the case of the low- and medium-alginate’s viscosity, respectively. In other words, the behavior of the mixed hydrogels was the same during the swelling experiments. Therefore, the presence of Pluronic^® F-127 nanomicelles and medium-viscosity sodium alginate leads to a higher swelling ratio. A model drug, acetyl salicylic acid (ASA), was also encapsulated in the mixed beads and ASA’s release studies were performed. In conclusion, the prepared systems, which are well characterized, show potential as delivery platforms for the oral delivery of active pharmaceutical ingredients and biopharmaceuticals. Full article

(This article belongs to the Special Issue Νanoparticles for Biomedical Applications)

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19 pages, 4462 KiB

Open AccessArticle

Unimolecular Micelles from Randomly Grafted Arborescent Copolymers with Different Core Branching Densities: Encapsulation of Doxorubicin and In Vitro Release Study

by Mosa Alsehli and Mario Gauthier

Materials 2023, 16(6), 2461; https://doi.org/10.3390/ma16062461 - 20 Mar 2023

Cited by 1 | Viewed by 1724

Abstract

A series of amphiphilic arborescent copolymers of generations G1 and G2 with an arborescent poly(γ-benzyl L-glutamate) (PBG) core and poly(ethylene oxide) (PEO) chain segments in the shell, PBG-g-PEO, were synthesized and evaluated as drug delivery nanocarriers. The PBG building blocks were [...] Read more.

A series of amphiphilic arborescent copolymers of generations G1 and G2 with an arborescent poly(γ-benzyl L-glutamate) (PBG) core and poly(ethylene oxide) (PEO) chain segments in the shell, PBG-g-PEO, were synthesized and evaluated as drug delivery nanocarriers. The PBG building blocks were generated by ring-opening polymerization of γ-benzyl L-glutamic acid N-carboxyanhydride (Glu-NCA) initiated with n-hexylamine. Partial or full deprotection of the benzyl ester groups followed by coupling with PBG chains yielded a comb-branched (arborescent polymer generation zero or G0) PBG structure. Additional cycles of deprotection and grafting provided G1 and G2 arborescent polypeptides. Side chains of poly(ethylene oxide) were then randomly grafted onto the arborescent PBG substrates to produce amphiphilic arborescent copolymers. Control over the branching density of G0PBG was investigated by varying the length and the deprotection level of the linear PBG substrates used in their synthesis. Three G0PBG cores with different branching densities, varying from a compact and dense to a loose and more porous structure, were thus synthesized. These amphiphilic copolymers behaved similar to unimolecular micelles in aqueous solutions, with a unimodal number- and volume-weighted size distributions in dynamic light scattering measurements. It was demonstrated that these biocompatible copolymers can encapsulate hydrophobic drugs such as doxorubicin (DOX) within their hydrophobic core with drug loading efficiencies of 42–65%. Sustained and pH-responsive DOX release was observed from the unimolecular micelles, which suggests that they could be useful as drug nanocarriers for cancer therapy. Full article

(This article belongs to the Special Issue Νanoparticles for Biomedical Applications)

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19 pages, 31474 KiB

Open AccessArticle

Hyperbranched Polyelectrolyte Copolymers as Novel Candidate Delivery Systems for Bio-Relevant Compounds

by Anastasia Balafouti and Stergios Pispas

Materials 2023, 16(3), 1045; https://doi.org/10.3390/ma16031045 - 24 Jan 2023

Cited by 3 | Viewed by 1920

Abstract

In this study, reversible addition-fragmentation chain transfer (RAFT) polymerization is utilized in order to synthesize novel hyperbranched poly(oligoethylene glycol) methyl ether methacrylate-co-tert-butyl methacrylate-co-methacrylic acid) (H-[P(OEGMA-co-tBMA-co-MAA)]) copolymers in combination with selective hydrolysis reactions. The copolymers showing amphiphilicity induced by the polar OEGMA and hydrophobic [...] Read more.

In this study, reversible addition-fragmentation chain transfer (RAFT) polymerization is utilized in order to synthesize novel hyperbranched poly(oligoethylene glycol) methyl ether methacrylate-co-tert-butyl methacrylate-co-methacrylic acid) (H-[P(OEGMA-co-tBMA-co-MAA)]) copolymers in combination with selective hydrolysis reactions. The copolymers showing amphiphilicity induced by the polar OEGMA and hydrophobic tBMA monomeric units, and polyelectrolyte character due to MAA units, combined with unique macromolecular architecture were characterized by physicochemical techniques, such as size exclusion chromatography (SEC) and ¹H-NMR spectroscopy. The hyperbranched copolymers were investigated in terms of their ability to self-assemble into nanostructures when dissolved in aqueous media. Dynamic light scattering and fluorescence spectroscopy revealed multimolecular aggregates of nanoscale dimensions with low critical aggregation concentration, the size and mass of which depend on copolymer composition and solution conditions, whereas zeta potential measurements indicated pH sensitive features. In addition, aiming to evaluate their potential use as nanocarriers, the copolymers were studied in terms of their drug encapsulation and protein complexation ability utilizing curcumin and lysozyme, as a model hydrophobic drug and a model cationic protein, respectively. Full article

(This article belongs to the Special Issue Νanoparticles for Biomedical Applications)

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Review

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21 pages, 4073 KiB

Open AccessReview

Mechanochemical Synthesis of Nanoparticles for Potential Antimicrobial Applications

by Rabindra Dubadi, Songping D. Huang and Mietek Jaroniec

Materials 2023, 16(4), 1460; https://doi.org/10.3390/ma16041460 - 9 Feb 2023

Cited by 36 | Viewed by 6706

Abstract

There is an increased interest in porous materials due to their unique properties such as high surface area, enhanced catalytic properties, and biological applications. Various solvent-based approaches have been already used to synthesize porous materials. However, the use of large volume of solvents, [...] Read more.

There is an increased interest in porous materials due to their unique properties such as high surface area, enhanced catalytic properties, and biological applications. Various solvent-based approaches have been already used to synthesize porous materials. However, the use of large volume of solvents, their toxicity, and time-consuming synthesis make this process less effective, at least in terms of principles of green chemistry. Mechanochemical synthesis is one of the effective eco-friendly alternatives to the conventional synthesis. It adopts the efficient mixing of reactants using ball milling without or with a very small volume of solvents, gives smaller size nanoparticles (NPs) and larger surface area, and facilitates their functionalization, which is highly beneficial for antimicrobial applications. A large variety of nanomaterials for different applications have already been synthesized by this method. This review emphasizes the comparison between the solvent-based and mechanochemical methods for the synthesis of mainly inorganic NPs for potential antimicrobial applications, although some metal-organic framework NPs are briefly presented too. Full article

(This article belongs to the Special Issue Νanoparticles for Biomedical Applications)

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