Lipid Nanostructures for Antioxidant Delivery

A special issue of Antioxidants (ISSN 2076-3921).

Deadline for manuscript submissions: closed (31 December 2021) | Viewed by 23304

Special Issue Editor


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Guest Editor

Special Issue Information

Dear Colleagues,

The recent scientific literature has demonstrated the attractive potential of lipid-based nanosystems for many pharmaceutical applications. Indeed, lipid nanostructures can dissolve drugs with different physical and chemical properties, especially lipophilic active molecules, increasing their bioavailability and efficacy, controlling delivery while decreasing side-effects. The rationale in using lipid nanosystems is also related to their biocompatibility and rare toxicity, offering the chance to administer them by different routes. Many studies have demonstrated that the nanoencapsulation strategy makes it possible to protect active molecules from possible degradation, prolonging their chemical stability. On this matter, the inclusion of antioxidants within lipid nanostructures offers a tremendous opportunity. Indeed, despite their pharmaceutical potential, spanning from free radical formation hindrance to the inhibition of cancer cell proliferation and progression, antioxidant molecules are characterized by poor stability, and are degraded by many environmental factors such as oxygen, light, high temperature, and humidity. In this regard, lipid-based nanostructures such as liposomes, solid lipid nanoparticles, and nanostructured lipid carriers have been recently proposed as innovative delivery systems for antioxidant molecules. In vitro and in vivo studies have demonstrated that antioxidant encapsulation prolongs release kinetics, bioavailability, and antioxidant effects. Due to the increasing interest in this field, in this Special Issue original research papers or review articles focusing on the physico-chemical, biological, and pharmacological properties of lipid-based nanosystems containing antioxidant molecules are welcome.

Dr. Elisabetta Esposito
Guest Editor

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Keywords

  • Antioxidant molecules
  • Nanosystems
  • Oxidative stress
  • Liposome
  • Solid lipid nanoparticles
  • Nanostructured lipid carriers

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Published Papers (6 papers)

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Editorial

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3 pages, 176 KiB  
Editorial
Lipid Nanostructures for Antioxidant Delivery
by Elisabetta Esposito
Antioxidants 2022, 11(2), 238; https://doi.org/10.3390/antiox11020238 - 26 Jan 2022
Viewed by 1623
Abstract
The recent scientific literature has demonstrated the attractive potential of lipid-based nanosystems, for many pharmaceutical applications [...] Full article
(This article belongs to the Special Issue Lipid Nanostructures for Antioxidant Delivery)

Research

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16 pages, 2338 KiB  
Article
Synergistic Antioxidant Activity and Enhanced Stability of Curcumin Encapsulated in Vegetal Oil-Based Microemulsion and Gel Microemulsions
by Cristina Scomoroscenco, Mircea Teodorescu, Sabina Georgiana Burlacu, Ioana Cătălina Gîfu, Catalin Ionut Mihaescu, Cristian Petcu, Adina Raducan, Petruta Oancea and Ludmila Otilia Cinteza
Antioxidants 2022, 11(5), 854; https://doi.org/10.3390/antiox11050854 - 27 Apr 2022
Cited by 20 | Viewed by 2797
Abstract
Curcumin, due to its antioxidant, antibacterial, anti-inflammatory, and antitumoral activity, has attracted huge attention in applications in many fields such as pharmacy, medicine, nutrition, cosmetics, and biotechnology. The stability of curcumin-based products and preservation of antioxidant properties are still challenges in practical applications. [...] Read more.
Curcumin, due to its antioxidant, antibacterial, anti-inflammatory, and antitumoral activity, has attracted huge attention in applications in many fields such as pharmacy, medicine, nutrition, cosmetics, and biotechnology. The stability of curcumin-based products and preservation of antioxidant properties are still challenges in practical applications. Stability and antioxidant properties were studied for curcumin encapsulated in O/W microemulsion systems and three related gel microemulsions. Only biodegradable and biocompatible ingredients were used for carriers: grape seed oil as oily phase, Tween 80, and Plurol® Diisostearique CG as a surfactant mix, and ethanol as a co-solvent. For the gel microemulsions, water-soluble polymers, namely Carbopol® 980 NF, chitosan, and sodium hyaluronate were used. The influence of UVC irradiation and heat treatment on the degradation kinetics of curcumin in the formulations was studied. Because of the antioxidant character of the microemulsion oily phase, the possibility of a synergistic effect between grape seed oil and curcumin was explored. In this study, the high efficiency of the studied drug delivery systems to ensure protection from external degradative factors was confirmed. Also, the influence of the encapsulation in microemulsion and derived gel microemulsion systems on the antioxidant capacity curcumin was studied, and a synergistic effect with vegetal oil was demonstrated. Full article
(This article belongs to the Special Issue Lipid Nanostructures for Antioxidant Delivery)
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15 pages, 2672 KiB  
Article
Exploiting the Anti-Inflammatory Potential of White Capsicum Extract by the Nanoformulation in Phospholipid Vesicles
by Ilaria Pappalardo, Anna Santarsiero, Maria De Luca, Maria Assunta Acquavia, Simona Todisco, Carla Caddeo, Giuliana Bianco, Vittoria Infantino, Giuseppe Martelli and Antonio Vassallo
Antioxidants 2021, 10(11), 1683; https://doi.org/10.3390/antiox10111683 - 25 Oct 2021
Cited by 4 | Viewed by 2070
Abstract
The peppers of the Capsicum species are exploited in many fields, as flavoring agents in food industry, or as decorative and therapeutic plants. Peppers show a diversified phytochemical content responsible for different biological activities. Synergic activity exerted by high levels of antioxidant compounds [...] Read more.
The peppers of the Capsicum species are exploited in many fields, as flavoring agents in food industry, or as decorative and therapeutic plants. Peppers show a diversified phytochemical content responsible for different biological activities. Synergic activity exerted by high levels of antioxidant compounds is responsible for their important anti-inflammatory property. A methanolic extract was obtained from a new pepper genotype and tested for anti-inflammatory activity. The extract was incorporated into phospholipid vesicles to increase the bioavailability of its bioactive components. Two types of phospholipid vesicles were produced, conventional liposomes and Penetration Enhancer containing Vesicles (PEVs). They were tested in human monoblastic leukemia U937 cell line, showing no cytotoxic effect. The intracellular reactive oxygen species (ROS) and nitric oxide (NO) levels were measured to value the in vitro efficacy of the vesicles in regulating inflammatory responses. Liposomal incorporation significantly reduced ROS levels in extract-treated LPS-activated cells. Furthermore, LC-MS/MS analyses demonstrated that liposomes facilitated the transport of the extract components across the cell membrane and their accumulation into the cytoplasm. Full article
(This article belongs to the Special Issue Lipid Nanostructures for Antioxidant Delivery)
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26 pages, 3674 KiB  
Article
Engineered Sumoylation-Deficient Prdx6 Mutant Protein-Loaded Nanoparticles Provide Increased Cellular Defense and Prevent Lens Opacity
by Bhavana Chhunchha, Eri Kubo, Uday B. Kompella and Dhirendra P. Singh
Antioxidants 2021, 10(8), 1245; https://doi.org/10.3390/antiox10081245 - 04 Aug 2021
Cited by 5 | Viewed by 2035
Abstract
Aberrant Sumoylation-mediated protein dysfunction is involved in a variety of oxidative and aging pathologies. We previously reported that Sumoylation-deficient Prdx6K(lysine)122/142R(Arginine) linked to the TAT-transduction domain gained stability and protective efficacy. In the present study, we formulated wild-type TAT-HA-Prdx6WT and Sumoylation-deficient Prdx6-loaded [...] Read more.
Aberrant Sumoylation-mediated protein dysfunction is involved in a variety of oxidative and aging pathologies. We previously reported that Sumoylation-deficient Prdx6K(lysine)122/142R(Arginine) linked to the TAT-transduction domain gained stability and protective efficacy. In the present study, we formulated wild-type TAT-HA-Prdx6WT and Sumoylation-deficient Prdx6-loaded poly-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) to further enhance stability, protective activities, and sustained delivery. We found that in vitro and subconjuctival delivery of Sumoylation-deficient Prdx6-NPs provided a greater protection of lens epithelial cells (LECs) derived from human and Prdx6−/−-deficient mouse lenses against oxidative stress, and it also delayed the lens opacity in Shumiya cataract rats (SCRs) than TAT-HA-Prdx6WT-NPs. The encapsulation efficiencies of TAT-HA-Prdx6-NPs were ≈56%–62%. Dynamic light scattering (DLS) and atomic force microscopy (AFM) analyses showed that the NPs were spherical, with a size of 50–250 nm and a negative zeta potential (≈23 mV). TAT-HA-Prdx6 analog-NPs released bioactive TAT-HA-Prdx6 (6%–7%) within 24 h. Sumoylation-deficient TAT-HA-Prdx6-NPs provided 35% more protection by reducing the oxidative load of LECs exposed to H2O2 compared to TAT-HA-Prdx6WT-NPs. A subconjuctival delivery of TAT-HA-Prdx6 analog-NPs demonstrated that released TAT-HA-Prdx6K122/142R could reduce lens opacity by ≈60% in SCRs. Collectively, our results demonstrate for the first time that the subconjuctival delivery of Sumoylation-deficient Prdx6-NPs is efficiently cytoprotective and provide a proof of concept for potential use to delay cataract and oxidative-related pathobiology in general. Full article
(This article belongs to the Special Issue Lipid Nanostructures for Antioxidant Delivery)
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19 pages, 7332 KiB  
Article
Ethosomes and Transethosomes for Mangiferin Transdermal Delivery
by Maddalena Sguizzato, Francesca Ferrara, Supandeep Singh Hallan, Anna Baldisserotto, Markus Drechsler, Manuela Malatesta, Manuela Costanzo, Rita Cortesi, Carmelo Puglia, Giuseppe Valacchi and Elisabetta Esposito
Antioxidants 2021, 10(5), 768; https://doi.org/10.3390/antiox10050768 - 12 May 2021
Cited by 47 | Viewed by 4559
Abstract
Mangiferin is a natural glucosyl xanthone with antioxidant and anti-inflammatory activity, making it suitable for protection against cutaneous diseases. In this study ethosomes and transethosomes were designed as topical delivery systems for mangiferin. A preformulation study was conducted using different surfactants in association [...] Read more.
Mangiferin is a natural glucosyl xanthone with antioxidant and anti-inflammatory activity, making it suitable for protection against cutaneous diseases. In this study ethosomes and transethosomes were designed as topical delivery systems for mangiferin. A preformulation study was conducted using different surfactants in association with phosphatidylcholine. Vesicle dimensional distribution was monitored by photon correlation spectroscopy, while antioxidant capacity and cytotoxicity were respectively assessed by free radical scavenging analysis and MTT on HaCaT keratinocytes. Selected nanosystems were further investigated by cryogenic transmission electron microscopy, while mangiferin entrapment capacity was evaluated by ultracentrifugation and HPLC. The diffusion kinetics of mangiferin from ethosomes and transethosomes evaluated by Franz cell was faster in the case of transethosomes. The suitability of mangiferin-containing nanovesicles in the treatment of skin disorders related to pollutants was investigated, evaluating, in vitro, the antioxidant and anti-inflammatory effect of ethosomes and transethosomes on human keratinocytes exposed to cigarette smoke as an oxidative and inflammatory challenger. The ability to induce an antioxidant response (HO-1) and anti-inflammatory status (IL-6 and NF-kB) was determined by RT-PCR and immunofluorescence. The data demonstrated the effectiveness of mangiferin loaded in nanosystems to protect cells from damage. Finally, to gain insight into the keratinocytes’ uptake of ethosome and transethosome, transmission electron microscopy analyses were conducted, showing that both nanosystems were able to pass intact within the cells. Full article
(This article belongs to the Special Issue Lipid Nanostructures for Antioxidant Delivery)
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Review

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24 pages, 2140 KiB  
Review
Solid Lipid Nanoparticles as Carriers of Natural Phenolic Compounds
by Alexandra Borges, Victor de Freitas, Nuno Mateus, Iva Fernandes and Joana Oliveira
Antioxidants 2020, 9(10), 998; https://doi.org/10.3390/antiox9100998 - 15 Oct 2020
Cited by 87 | Viewed by 8905
Abstract
Phenolic compounds are one of the most widespread classes of compounds in nature, with several beneficial biological effects being associated with their anti-oxidant and anti-carcinogenic activities. Their application in the prevention or treatment of numerous chronic diseases have been studied, but a major [...] Read more.
Phenolic compounds are one of the most widespread classes of compounds in nature, with several beneficial biological effects being associated with their anti-oxidant and anti-carcinogenic activities. Their application in the prevention or treatment of numerous chronic diseases have been studied, but a major drawback is still the low bioavailability of these compounds, as well as their instability towards pH, temperature, and light in some cases. Nanotechnology has emerged as an alternative to overcome these limitations, and the use of lipidic encapsulation systems is a promising technique to achieve an efficient drug delivery, protecting molecules from external factors and improving their bioavailability. In this review, solid lipid nanoparticles and nanostructured lipid carriers are highlighted as an important tool for the improvement of the bioavailability and stability of natural phenolic compounds, including their preparation methods and functionalization approaches and the discussion of several applications for putative use in cosmetic and pharmacologic products. Full article
(This article belongs to the Special Issue Lipid Nanostructures for Antioxidant Delivery)
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