Phenolic Compounds Loaded by Drug Delivery Systems Applied to Mitigate Inflammatory States

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

Deadline for manuscript submissions: closed (20 May 2023) | Viewed by 10508

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Research Institute for Medicines and Pharmaceutical Sciences (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisbon, Portugal
Interests: phenolic compounds; food supplements; antioxidant activity; metabolism; colitis; IBD; bioactivity; in vivo inflammation models; drug delivery; nutraceuticals
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Guest Editor
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisbon, Portugal
Interests: phenolic compounds; immunometabolism; food nanotechnologies; nanoencapsulation; drug delivery systems; biodisponibility; colorectal cancerolic compounds; persimmon; food science; functional foods; biochemistry; haematology; in vitro/in vivo inflammation and cancer models
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Immune-mediated inflammatory diseases (IMIDs) affect 3 to 7% of the developed world’s population and include approximately 80 conditions whose prevalence is increasing. New discoveries have been attributed to the inflammatory phenomenon, an extremely important role in the pathophysiological processes of neoplastic, neurodegenerative, infectious, autoimmune, and other diseases. Still, a considerable quantity of the patients with a particular clinically defined IMID will be unsuccessful in responding to any specific targeted mechanism of action. This can be justified, in part, as each clinically defined IMID is actually a heterogeneous syndrome rather than a molecularly defined disease entity. A fundamentally new methodology that takes the field from one that is centered on clinical signs and symptoms to one predicated on immunological and molecular mechanisms is drastically required. For this, a new form of thinking is necessary. IMIDs may be handled according to shared commonalities in their pathogenic cells and pathways, and therapeutic efforts ought to be directed at these cells and processes instead of at clinical features.

With this in mind, it is true that the ingestion of a healthy diet is suboptimal worldwide (i.e., low consumption of nuts and seeds, whole grains, and milk), while the consumption of less healthy diets (i.e., sugary beverages, processed, red meat, and salt) is more common. A diet based on the high consumption of sodium and the low consumption of fruit or whole grains is responsible for more than half of diet-related deaths and two-thirds of diet-related disability-adjusted life years (DALYs). These results are consistent around the globe.

The bioavailability of dietary compounds, in general, and phytochemicals, in particular, depends upon their release from the food matrix, their digestive stability, and the competence of transepithelial passage. The chemical structure of phenolic compounds further governs the rate and degree of intestinal absorption and the nature of metabolites circulating in plasma.

New delivery systems within the field of nanotechnology could provide higher efficiency of dietary compounds as phenolic compounds when ingested by humans, demonstrating their health benefits in well-established ways of prevention, treatment, or adjuvant in addition to conventional pharmacological treatments. A new nutritional approach may be adopted by constructing a personalized diet using these new formulations for drug delivery as micro- and nanocarriers of phenolic compounds. It is also worth noting the current changes in preferences because of the advanced knowledge surrounding the interplay between health and food, which has caused a rise in new food supply demands.

Authors are invited to submit original research articles and reviews in this prevailing and curious research field in an effort to envision future precise applications for bioactive compounds in the fight against IMIDs, new drug delivery strategies for natural products load, and new findings in phenolic profile of unknown or less known natural sources of bioactive compounds. The mechanisms of action at the cellular, molecular, and genetic levels, pharmacokinetics, and toxicokinetics are of biggest interest.

Dr. Maria-Eduardo Figueira
Dr. Rosa Direito
Guest Editors

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Keywords

  • phenolic compounds
  • inflammation
  • immune-mediated inflammatory diseases
  • cancer
  • antioxidants
  • bioactive compounds
  • drug delivery
  • food supplements
  • nanoencapsulation
  • nanotechnology
  • microtechnology
  • bioavailability
  • safety
  • biopharmaceuticals
  • pharmacokinetics
  • toxicokinetics

Published Papers (4 papers)

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Research

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21 pages, 3512 KiB  
Article
An In Vitro and In Silico Characterization of Salvia sclarea L. Methanolic Extracts as Spasmolytic Agents
by Milica Randjelović, Suzana Branković, Miloš Jovanović, Nemanja Kitić, Slavoljub Živanović, Tatjana Mihajilov-Krstev, Bojana Miladinović, Milica Milutinović and Dušanka Kitić
Pharmaceutics 2023, 15(5), 1376; https://doi.org/10.3390/pharmaceutics15051376 - 29 Apr 2023
Cited by 1 | Viewed by 1522
Abstract
The use of medicinal plant species and their products is widespread in the field of gastrointestinal and respiratory diseases. This study aimed to evaluate the traditional use of Salvia sclarea L., clary sage, finding the possible mechanisms of its spasmolytic and bronchodilator actions [...] Read more.
The use of medicinal plant species and their products is widespread in the field of gastrointestinal and respiratory diseases. This study aimed to evaluate the traditional use of Salvia sclarea L., clary sage, finding the possible mechanisms of its spasmolytic and bronchodilator actions in in vitro conditions supported by molecular docking analysis, along with the antimicrobial effects. Four dry extracts were prepared from the aerial parts of S. sclarea, using absolute or 80% (v/v) methanol by the method of a single-stage maceration or an ultrasound-assisted extraction. Characterization of the bioactive compounds by high-performance liquid chromatography indicated the presence of significant amounts of polyphenolics, with rosmarinic acid as the prevalent one. The spontaneous ileal contractions were best inhibited by the extract prepared with 80% methanol and maceration. The same extract was superior in the carbachol- and KCl-induced tracheal smooth muscle contractions, being the strongest bronchodilator agent. The most powerful relaxation of KCl-induced ileal contractions was achieved with the extract made of absolute methanol by maceration, while the 80% methanolic extract made with the ultrasound method generated the best spasmolytic effects in the acetylcholine-induced ileal contractions. Docking analysis suggested that apigenin-7-O-glucoside and luteolin-7-O-glucoside exhibited the highest binding affinity to voltage-gated calcium channels. Gram (+) bacteria were more susceptible to the effects of the extracts, particularly Staphylococcus aureus, in contrast to Gram (−) bacteria and Candida albicans. This is the first study to point out the influence of S. sclarea methanolic extracts on the gastrointestinal and respiratory spasm reduction, paving the way for their potential place in complementary medicine. Full article
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Review

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30 pages, 1472 KiB  
Review
Hyaluronic Acid-Mediated Phenolic Compound Nanodelivery for Cancer Therapy
by Simona Serini, Sonia Trombino, Federica Curcio, Roberta Sole, Roberta Cassano and Gabriella Calviello
Pharmaceutics 2023, 15(6), 1751; https://doi.org/10.3390/pharmaceutics15061751 - 16 Jun 2023
Cited by 5 | Viewed by 1642
Abstract
Phenolic compounds are bioactive phytochemicals showing a wide range of pharmacological activities, including anti-inflammatory, antioxidant, immunomodulatory, and anticancer effects. Moreover, they are associated with fewer side effects compared to most currently used antitumor drugs. Combinations of phenolic compounds with commonly used drugs have [...] Read more.
Phenolic compounds are bioactive phytochemicals showing a wide range of pharmacological activities, including anti-inflammatory, antioxidant, immunomodulatory, and anticancer effects. Moreover, they are associated with fewer side effects compared to most currently used antitumor drugs. Combinations of phenolic compounds with commonly used drugs have been largely studied as an approach aimed at enhancing the efficacy of anticancer drugs and reducing their deleterious systemic effects. In addition, some of these compounds are reported to reduce tumor cell drug resistance by modulating different signaling pathways. However, often, their application is limited due to their chemical instability, low water solubility, or scarce bioavailability. Nanoformulations, including polyphenols in combination or not with anticancer drugs, represent a suitable strategy to enhance their stability and bioavailability and, thus, improve their therapeutic activity. In recent years, the development of hyaluronic acid-based systems for specific drug delivery to cancer cells has represented a pursued therapeutic strategy. This is related to the fact that this natural polysaccharide binds to the CD44 receptor that is overexpressed in most solid cancers, thus allowing its efficient internalization in tumor cells. Moreover, it is characterized by high biodegradability, biocompatibility, and low toxicity. Here, we will focus on and critically analyze the results obtained in recent studies regarding the use of hyaluronic acid for the targeted delivery of bioactive phenolic compounds to cancer cells of different origins, alone or in combination with drugs. Full article
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31 pages, 4505 KiB  
Review
Modulating Inflammation-Mediated Diseases via Natural Phenolic Compounds Loaded in Nanocarrier Systems
by Tojofaniry Fabien Rakotondrabe, Min-Xia Fan, Felix Wambua Muema and Ming-Quan Guo
Pharmaceutics 2023, 15(2), 699; https://doi.org/10.3390/pharmaceutics15020699 - 19 Feb 2023
Cited by 6 | Viewed by 2273
Abstract
The global increase and prevalence of inflammatory-mediated diseases have been a great menace to human welfare. Several works have demonstrated the anti-inflammatory potentials of natural polyphenolic compounds, including flavonoid derivatives (EGCG, rutin, apigenin, naringenin) and phenolic acids (GA, CA, etc.), among others (resveratrol, [...] Read more.
The global increase and prevalence of inflammatory-mediated diseases have been a great menace to human welfare. Several works have demonstrated the anti-inflammatory potentials of natural polyphenolic compounds, including flavonoid derivatives (EGCG, rutin, apigenin, naringenin) and phenolic acids (GA, CA, etc.), among others (resveratrol, curcumin, etc.). In order to improve the stability and bioavailability of these natural polyphenolic compounds, their recent loading applications in both organic (liposomes, micelles, dendrimers, etc.) and inorganic (mesoporous silica, heavy metals, etc.) nanocarrier technologies are being employed. A great number of studies have highlighted that, apart from improving their stability and bioavailability, nanocarrier systems also enhance their target delivery, while reducing drug toxicity and adverse effects. This review article, therefore, covers the recent advances in the drug delivery of anti-inflammatory agents loaded with natural polyphenolics by the application of both organic and inorganic nanocarriers. Even though nanocarrier technology offers a variety of possible anti-inflammatory advantages to naturally occurring polyphenols, the complexes’ inherent properties and mechanisms of action have not yet been fully investigated. Thus, expanding the quest on novel natural polyphenolic-loaded delivery systems, together with the optimization of complexes’ activity toward inflammation, will be a new direction of future efforts. Full article
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33 pages, 3469 KiB  
Review
Curcumin-Based Nanomedicines in the Treatment of Inflammatory and Immunomodulated Diseases: An Evidence-Based Comprehensive Review
by Lucas Fornari Laurindo, Gabriel Magno de Carvalho, Bárbara de Oliveira Zanuso, Maria Eduardo Figueira, Rosa Direito, Ricardo de Alvares Goulart, Daiene Santos Buglio and Sandra Maria Barbalho
Pharmaceutics 2023, 15(1), 229; https://doi.org/10.3390/pharmaceutics15010229 - 10 Jan 2023
Cited by 15 | Viewed by 4301
Abstract
Curcumin (CUR) is a polyphenol extracted from the rhizome of Curcuma longa that possesses potent anti-inflammatory and antioxidant potential. Despite CUR’s numerous beneficial effects on human health, it has limitations, such as poor absorption. Nano-based drug delivery systems have recently been applied to [...] Read more.
Curcumin (CUR) is a polyphenol extracted from the rhizome of Curcuma longa that possesses potent anti-inflammatory and antioxidant potential. Despite CUR’s numerous beneficial effects on human health, it has limitations, such as poor absorption. Nano-based drug delivery systems have recently been applied to improve CUR’s solubility and bioavailability and potentialize its health effects. This review investigated the effects of different CUR-based nanomedicines on inflammatory and immunomodulated diseases. PUBMED, EMBASE, COCHRANE, and GOOGLE SCHOLAR databases were searched, and the Scale for Assessment of Narrative Review Articles (SANRA) was used for quality assessment and PRISMA guidelines. Overall, 66 studies were included comprising atherosclerosis, rheumatoid arthritis (RA), Alzheimer’s disease (AD), Parkinson’s disease (PD), multiple sclerosis (MS), Huntington’s disease (HD), inflammatory bowel diseases (IBD), psoriasis, liver fibrosis, epilepsy, and COVID-19. The available scientific studies show that there are many known nanoformulations with curcumin. They can be found in nanosuspensions, nanoparticles, nanoemulsions, solid lipid particles, nanocapsules, nanospheres, and liposomes. These formulations can improve CUR bioavailability and can effectively be used as adjuvants in several inflammatory and immune-mediated diseases such as atheroma plaque formation, RA, dementia, AD, PD, MS, IBD, psoriasis, epilepsy, COVID-19, and can be used as potent anti-fibrotic adjuvants in fibrotic liver disease. Full article
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