Novel Therapeutic Approach to Inflammation and Pain

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (31 January 2025) | Viewed by 9579

Special Issue Editors


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Guest Editor
Department of Biochemical Sciences, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy
Interests: polyphenols; natural products; NaDES; inflammation; oxidative stress
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
1. Department of Physiology and Pharmacology, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy
2. Department of Biochemical Sciences, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy
Interests: inflammation; pain; natural compounds; osteoarthritis; cellular pathways
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Inflammation and pain are two closely related issues that are often intricately linked in certain pathologies and are therefore frequently studied together in scientific research. It has been determined that they are interconnected by a complex signaling network based on a variety of molecules, receptors, and cellular pathways, which play fundamental roles in the onset and development of pathological conditions such as, for example, cancer, osteoarthritis, metabolic disorders, and autoimmune disease. However, although many advances have been made in this research field, the whole mechanisms responsible for inflammatory and painful signaling have not been fully clarified. Moreover, from a therapeutical perspective, currently available analgesic and anti-inflammatory drugs are often characterized by various side effects that limit their clinical administration. In this context, understanding these mechanisms and identifying new therapeutic targets would pave the way for new discoveries in the pharmaceutical field to provide innovative alternatives to inflammation and pain treatment. At the same time, it is important to discover and develop new molecules with increasingly minimal side effects.

In this Special Issue of Pharmaceutics, we invite authors to submit original research articles or reviews in the fields of pain and inflammation. Research areas may include (but are not limited to) the following topics:

  • Study of alternative targets or novel therapeutic strategies;
  • New pharmaceutical formulations;
  • Drug delivery systems as well as drug repositioning approaches.

Hoping for your active participation, we look forward to receiving your contributions.

Dr. Roberto Mattioli
Dr. Alessia Mariano
Guest Editors

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Keywords

  • inflammation
  • pain
  • chronical disease
  • drug repositioning
  • intracellular pathways
  • drug delivery systems
  • novel therapeutic strategies

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Published Papers (4 papers)

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Research

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9 pages, 1072 KiB  
Article
Clinical Evidence Regarding Spermidine–Hyaluronate Gel as a Novel Therapeutic Strategy in Vestibulodynia Management
by Filippo Murina, Alessandra Graziottin, Nicla Toni, Maria Teresa Schettino, Luca Bello, Alessandra Marchi, Barbara Del Bravo, Dania Gambini, Lara Tiranini and Rossella Elena Nappi
Pharmaceutics 2024, 16(11), 1448; https://doi.org/10.3390/pharmaceutics16111448 - 12 Nov 2024
Viewed by 1262
Abstract
Background: Vestibulodynia (VBD) represents a summation and overlapping of trigger factors (infections, hormonal disturbances, allergies, genetic aspects, psychological vulnerability, and others) with broad individual variability. As there are no standard treatment options for VBD, the disease is still in need of appropriate therapeutic [...] Read more.
Background: Vestibulodynia (VBD) represents a summation and overlapping of trigger factors (infections, hormonal disturbances, allergies, genetic aspects, psychological vulnerability, and others) with broad individual variability. As there are no standard treatment options for VBD, the disease is still in need of appropriate therapeutic tools. Objectives: A prospective observational trial was performed to confirm the efficacy of a topical gel containing a spermidine–hyaluronate complex (UBIGEL donna™) as either a stand-alone or companion treatment through a multicenter study on a large sample population. Methods: For women with VBD (n = 154), the treatment consisted of approximately two months (4 + 4 weeks) of applications according to the posology of UBIGEL. Evaluation of symptoms was performed on relevant clinical endpoints: dyspareunia and vulvovaginal pain/burning by a visual scale (VAS); vestibular trophism by a vestibular trophic health (VeTH) score; vulvoscopy through a cotton swab test; and the level of hypertonic pelvic floor by a physical graded assessment of levator ani hypertonus. Results: A total of 154 patients treated with UBIGEL donna™ showed significant improvements across all five evaluated parameters, including pain, dyspareunia, swab test results, muscle hypertonicity, and vestibular trophism. Pain and dyspareunia scores decreased by 46.5% and 33.5%, respectively, while significant improvements were also observed in the other parameters (p < 0.0001). These improvements were consistent across various stratifications, including age and disease duration. Conclusions: The findings of the present study suggest that UBIGEL donna™ is effective in alleviating pain and dyspareunia, as well as reducing vestibular hypersensitivity in women with VBD. Although UBIGEL donna™ alone cannot serve as a comprehensive substitute for all recommended therapies, we suggest that multimodal therapy strategies may be crucial for attaining substantial improvement in any aspect of the condition. Full article
(This article belongs to the Special Issue Novel Therapeutic Approach to Inflammation and Pain)
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23 pages, 4043 KiB  
Article
Development and Evaluation of Two-Phase Gel Formulations for Enhanced Delivery of Active Ingredients: Sodium Diclofenac and Camphor
by Giedre Kasparaviciene, Yuliia Maslii, Nataliia Herbina, Daiva Kazlauskiene, Mindaugas Marksa and Jurga Bernatoniene
Pharmaceutics 2024, 16(3), 366; https://doi.org/10.3390/pharmaceutics16030366 - 5 Mar 2024
Cited by 4 | Viewed by 2970
Abstract
The formulation of biphasic gels as potential semi-solid carriers for hydrophilic and lipophilic active substances is promising for the development of pharmaceutical preparations. The aim of this study was to design a stable bigel composition and to determine the influence of the organogel/hydrogel [...] Read more.
The formulation of biphasic gels as potential semi-solid carriers for hydrophilic and lipophilic active substances is promising for the development of pharmaceutical preparations. The aim of this study was to design a stable bigel composition and to determine the influence of the organogel/hydrogel ratio on the gel’s physical-chemical and structural-mechanical properties. The investigated compositions of organogel/hydrogel remained stable at ratios ranging from 5/95 to 40/60. After texture and microstructure analysis, bigels with 20/80 and 25/75 ratios were selected as carriers for the active ingredients, sodium diclofenac and camphor, for use as topical preparations for the treatment of muscle-joint inflammation and pain. Although other researchers have published data on the preparation and evaluation of bigels, there are no scientific results on the development of a two-phase gel with our proposed combination of APIs. Sodium diclofenac release was found to be higher when combined with camphor, which revealed the advantages of the biphasic formulation. The pseudoplastic behavior, thixotropy, and thermal stability of flow of the studied bigel samples was investigated by rheological analysis. Ongoing stability studies confirmed the minimal 6-month period. Full article
(This article belongs to the Special Issue Novel Therapeutic Approach to Inflammation and Pain)
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Review

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21 pages, 968 KiB  
Review
Nanotechnology in Pain Management
by Andrew Torpey, Emily Bellow, Veronica Samojedny, Sukhpreet Ahluwalia, Amruta Desai, William Caldwell and Sergio Bergese
Pharmaceutics 2024, 16(11), 1479; https://doi.org/10.3390/pharmaceutics16111479 - 20 Nov 2024
Cited by 1 | Viewed by 1925
Abstract
Chronic pain is a debilitating condition that affects millions of patients worldwide, contributing to a high disease burden and millions of dollars in lost wages, missed workdays, and healthcare costs. Opioids, NSAIDs, acetaminophen, gabapentinoids, muscle relaxants, anticonvulsants, and antidepressants are the most used [...] Read more.
Chronic pain is a debilitating condition that affects millions of patients worldwide, contributing to a high disease burden and millions of dollars in lost wages, missed workdays, and healthcare costs. Opioids, NSAIDs, acetaminophen, gabapentinoids, muscle relaxants, anticonvulsants, and antidepressants are the most used medications for chronic pain and carry significant side effects, including gastric bleeding, hepatotoxicity, stroke, kidney damage, constipation, dizziness, and arrhythmias. Opioids in particular carry the risk of long-term dependence, drug tolerance, and overdose. In 2022, 81,806 people died from opioid overdose in the United States alone. Alternative treatments for chronic pain are critically needed, and nanotechnology has emerged as a promising means of achieving effective long-term analgesia while avoiding the adverse side effects associated with conventional pharmacological agents. Nanotechnology-based treatments include liposomes, Poly Lactic-co-Glycolic Acid (PLGA) and other polymeric nanoparticles, and carbon-based polymers, which can help mitigate those adverse side effects. These nanomaterials can serve as drug delivery systems that facilitate controlled release and drug stability via the encapsulation of free molecules and protein-based drugs, leading to longer-lasting analgesia and minimizing side effects. In this review, we examine the role of nanotechnology in addressing concerns associated with conventional chronic pain treatments and discuss the ongoing efforts to develop novel, nanotechnology-based treatments for chronic pain such as nanocapacitor patches, gene therapy, the use of both viral and non-viral vectors, CRISPR, and scavengers. Full article
(This article belongs to the Special Issue Novel Therapeutic Approach to Inflammation and Pain)
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28 pages, 959 KiB  
Review
The Antinociceptive Role of Nrf2 in Neuropathic Pain: From Mechanisms to Clinical Perspectives
by Kestutis Petrikonis, Jurga Bernatoniene, Dalia M. Kopustinskiene, Roberto Casale, Sergio Davinelli and Luciano Saso
Pharmaceutics 2024, 16(8), 1068; https://doi.org/10.3390/pharmaceutics16081068 - 15 Aug 2024
Cited by 5 | Viewed by 2202
Abstract
Neuropathic pain, a chronic condition resulting from nerve injury or dysfunction, presents significant therapeutic challenges and is closely associated with oxidative stress and inflammation, both of which can lead to mitochondrial dysfunction. The nuclear factor erythroid 2-related factor 2 (Nrf2) pathway, a critical [...] Read more.
Neuropathic pain, a chronic condition resulting from nerve injury or dysfunction, presents significant therapeutic challenges and is closely associated with oxidative stress and inflammation, both of which can lead to mitochondrial dysfunction. The nuclear factor erythroid 2-related factor 2 (Nrf2) pathway, a critical cellular defense mechanism against oxidative stress, has emerged as a promising target for neuropathic pain management. Nrf2 modulators enhance the expression of antioxidant and cytoprotective genes, thereby reducing oxidative damage, inflammation, and mitochondrial impairment. This review explores the antinociceptive effects of Nrf2, highlighting how pharmacological agents and natural compounds may be used as potential therapeutic strategies against neuropathic pain. Although preclinical studies demonstrate significant pain reduction and improved nerve function through Nrf2 activation, several clinical challenges need to be addressed. However, emerging clinical evidence suggests potential benefits of Nrf2 modulators in several conditions, such as diabetic neuropathy and multiple sclerosis. Future research should focus on further elucidating the molecular role of Nrf2 in neuropathic pain to optimize its modulation efficacy and maximize clinical utility. Full article
(This article belongs to the Special Issue Novel Therapeutic Approach to Inflammation and Pain)
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