Application of Nanocarrier Systems for the Delivery of Bioactive Natural Products and Derivatives Thereof

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (20 November 2024) | Viewed by 5019

Special Issue Editors


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Guest Editor
1. Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina
2. Institute of Chemistry and Metabolism of Drugs (IQUIMEFA), University of Buenos Aires—National Scientific and Technical Research Council, Buenos Aires, Argentina
Interests: neglected diseases; antimicrobial activity; natural compounds; plant extracts; terpenoids; flavonoids; Asteraceae
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
1. CBIOS-Centro de Biociências/The Biosciences Research Center, ECTS-School of Health Sciences and Technologies, Lusófona University, Campo Grande, 376, 1749-024 Lisboa, Portugal
2. IPLUSO/NICiTeS-ERISA-Escola Superior de Saúde Ribeiro Sanches, Rua do Telhal aos Olivais, 8-8ª, 1900-693 Lisboa, Portugal
Interests: natural products chemistry; structure-activity relationships

Special Issue Information

Dear Colleagues,

Since ancient times, natural products have been used as medicines for the treatment of several illnesses. In this sense, the isolation and identification of bioactive natural compounds have played a crucial role in the drug discovery process.

Natural molecules as well as their derivatives have been used for the development of novel treatments for a variety of diseases, with cancer and infectious diseases being among the most noteworthy. Although bioactive natural compounds have many advantages, such as a low molecular weight, variety of structures and chiral centers that allow for interactions with biological targets, many of them also have drawbacks related to their poor solubility, permeability and/or stability in biological mediums.

At present, researchers are putting more efforts in developing a Novel Drug Delivery System (NDDS) for the effective and targeted delivery of old, well-established molecules to increase safety and efficacy and to reduce the needed dose, instead of inventing new drug molecules.

In recent years, nanotechnology has made great progress in the development of carriers for the transportation of drugs. These systems are especially of interest for natural compound delivery, since they can overcome their limitations by improving pharmacokinetic properties and the arrival to the site of action.

This Special Issue will cover aspects related to the application of nanotechnology systems for the delivery of natural products as potential therapeutic treatments for acute and chronic diseases. Submissions, including research papers as well as mini-reviews and review articles, will be considered.

Prof. Dr. Valeria Patricia Sülsen
Prof. Dr. Maria Do Céu Costa
Prof. Dr. Constantinos Athanassopoulos
Guest Editors

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Keywords

  • nanotechnology
  • nanocarriers
  • natural compounds
  • novel drug delivery (NDDS)
  • target delivery

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Published Papers (2 papers)

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Research

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25 pages, 5820 KiB  
Article
Inhibition of SARS-CoV-2-Induced NLRP3 Inflammasome-Mediated Lung Cell Inflammation by Triphala-Loaded Nanoparticle Targeting Spike Glycoprotein S1
by Chuda Chittasupho, Sonthaya Umsumarng, Kamonwan Srisawad, Punnida Arjsri, Rungsinee Phongpradist, Weerasak Samee, Wipawan Tingya, Chadarat Ampasavate and Pornngarm Dejkriengkraikul
Pharmaceutics 2024, 16(6), 751; https://doi.org/10.3390/pharmaceutics16060751 - 2 Jun 2024
Cited by 1 | Viewed by 1421
Abstract
The COVID-19 pandemic, caused by SARS-CoV-2, poses a significant global health threat. The spike glycoprotein S1 of the SARS-CoV-2 virus is known to induce the production of pro-inflammatory mediators, contributing to hyperinflammation in COVID-19 patients. Triphala, an ancient Ayurvedic remedy composed of dried [...] Read more.
The COVID-19 pandemic, caused by SARS-CoV-2, poses a significant global health threat. The spike glycoprotein S1 of the SARS-CoV-2 virus is known to induce the production of pro-inflammatory mediators, contributing to hyperinflammation in COVID-19 patients. Triphala, an ancient Ayurvedic remedy composed of dried fruits from three plant species—Emblica officinalis (Family Euphorbiaceae), Terminalia bellerica (Family Combretaceae), and Terminalia chebula (Family Combretaceae)—shows promise in addressing inflammation. However, the limited water solubility of its ethanolic extract impedes its bioavailability. In this study, we aimed to develop nanoparticles loaded with Triphala extract, termed “nanotriphala”, as a drug delivery system. Additionally, we investigated the in vitro anti-inflammatory properties of nanotriphala and its major compounds, namely gallic acid, chebulagic acid, and chebulinic acid, in lung epithelial cells (A549) induced by CoV2-SP. The nanotriphala formulation was prepared using the solvent displacement method. The encapsulation efficiency of Triphala in nanotriphala was determined to be 87.96 ± 2.60% based on total phenolic content. In terms of in vitro release, nanotriphala exhibited a biphasic release profile with zero-order kinetics over 0–8 h. A549 cells were treated with nanotriphala or its active compounds and then induced with 100 ng/mL of spike S1 subunit (CoV2-SP). The results demonstrate that chebulagic acid and chebulinic acid are the active compounds in nanotriphala, which significantly reduced cytokine release (IL-6, IL-1β, and IL-18) and suppressed the expression of inflammatory genes (IL-6, IL-1β, IL-18, and NLRP3) (p < 0.05). Mechanistically, nanotriphala and its active compounds notably attenuated the expression of inflammasome machinery proteins (NLRP3, ASC, and Caspase-1) (p < 0.05). In conclusion, the nanoparticle formulation of Triphala enhances its stability and exhibits anti-inflammatory properties against CoV2-SP-induction. This was achieved by suppressing inflammatory mediators and the NLRP3 inflammasome machinery. Thus, nanotriphala holds promise as a supportive preventive anti-inflammatory therapy for COVID-19-related chronic inflammation. Full article
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Review

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21 pages, 2845 KiB  
Review
Therapeutic Applications of Nanoformulated Resveratrol and Quercetin Phytochemicals in Colorectal Cancer—An Updated Review
by Dhanalekshmi Unnikrishnan Meenakshi, Gurpreet Kaur Narde, Alka Ahuja, Khalid Al Balushi, Arul Prakash Francis and Shah Alam Khan
Pharmaceutics 2024, 16(6), 761; https://doi.org/10.3390/pharmaceutics16060761 - 4 Jun 2024
Cited by 6 | Viewed by 1967
Abstract
Natural compounds such as polyphenols play several positive roles in maintaining the oxidative and inflammatory capacity of cells, which leads to their potential use as anticancer therapeutics. There is promising evidence for the in vitro and in vivo anticancer activity of many polyphenols, [...] Read more.
Natural compounds such as polyphenols play several positive roles in maintaining the oxidative and inflammatory capacity of cells, which leads to their potential use as anticancer therapeutics. There is promising evidence for the in vitro and in vivo anticancer activity of many polyphenols, including resveratrol and quercetin, specifically in the treatment of colorectal cancer (CRC). There is a clear association between resveratrol and quercetin in interfering with the mechanistic pathways involved in CRC, such as Wnt, P13K/AKT, caspase-3, MAPK, NF-κB, etc. These molecular pathways establish the role of resveratrol and quercetin in controlling cancer cell growth, inducing apoptosis, and inhibiting metastasis. The major bottleneck in the progression of the use of resveratrol and quercetin as anticancer therapeutics is their reduced bioavailability in vivo because of their rapid metabolism in humans. Recent advancements in various nanotechnological formulations are promising for overcoming these bioavailability issues. Various nanoformulations of resveratrol and quercetin have shown an optimistic impact on reducing the solubility and improving the stability of resveratrol and quercetin in vivo. A combinatorial approach using nanoformulations of resveratrol with quercetin could potentially increase the impact of resveratrol in controlling CRC cell proliferation. This review discusses the mechanism of resveratrol and quercetin, the two bioactive polyphenolics, in colon cancer, with an emphasis on various types of nanoformulations of the two molecules targeting colon cancer. It also explores the synergistic effect of combining resveratrol and quercetin in various nanoformulations, targeting colon cancer. This research delves into the enhanced pharmacokinetics and potential chemotherapeutic benefits of these bioactive polyphenolics when used together in innovative ways. Full article
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