ArticlePharmaceutics2020
Lipid Nanoparticle Inclusion Prevents Capsaicin-Induced TRPV1 Defunctionalization.
Article in Pharmaceutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 21 citations in OpenAlex.
- Review
- Diroximel Fumarate-Loaded Solid Lipid Nanoparticles (DRF-SLNs) as Potential Carriers for the Treatment of Multiple Sclerosis: Preformulation Study.International journal of molecular sciences · 2025Article
- Mediterranean Food By-products as a Valuable Source of Bioactive Compounds with Health Properties.Current medicinal chemistry · 2025Review
- Effect of Ferulic Acid Loaded in Nanoparticle on Tissue Transglutaminase Expression Levels in Human Glioblastoma Cell Line.International journal of molecular sciences · 2024Article
- Steroidal Alkaloids from Food Waste of Tomato Processing Inhibit Neuroblastoma Cell Viability.International journal of molecular sciences · 2023Article
- Nanostructured Lipid Carriers Aimed to the Ocular Delivery of Mangiferin: In Vitro Evidence.Pharmaceutics · 2023Article
- Development of Solid Lipid Nanoparticles as Dry Powder: Characterization and Formulation Considerations.Molecules (Basel, Switzerland) · 2023Article
- One-Step Encapsulation of Capsaicin into Chitosan-Oleic Acid Complex Particles: Evaluation of Encapsulation Ability and Stability.Polymers · 2022Article
- Bovine Serum Albumin-Based Nanoparticles: Preparation, Characterization, and Antioxidant Activity Enhancement of Three Main Curcuminoids fromMolecules (Basel, Switzerland) · 2022Article
- The interaction of TRPV1 and lipids: Insights into lipid metabolism.Frontiers in physiology · 2022Review
- TRP Channels as Cellular Targets of Particulate Matter.International journal of molecular sciences · 2021Review
- Astaxanthin-Loaded Stealth Lipid Nanoparticles (AST-SSLN) as Potential Carriers for the Treatment of Alzheimer's Disease: Formulation Development and Optimization.Nanomaterials (Basel, Switzerland) · 2021Article
- Transient receptor potential vanilloid subtype 1 depletion mediates mechanical allodynia through cellular signal alterations in small-fiber neuropathy.Pain reports · 2021Review
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundCapsaicin (CPS) is a highly selective agonist of the transient receptor potential vanilloid type 1 (TRPV1) with a nanomolar affinity. High doses or prolonged exposure to CPS induces TRPV1 defunctionalization and, although this effect is currently used for the treatment of thermal hyperalgesia in chronic pain conditions, it is responsible of detrimental effects, such as denervation of sensory fibers. The aim of the present study was to formulate CPS loaded lipid nanocarriers (CPS-LN) in order to optimize CPS release, thus preventing TRPV1 internalization and degradation.
methodsCPS-LNs were formulated and characterized by in vitro studies. The activation of TRPV1 receptors after CPS-LN administration was evaluated by measuring spontaneous pain that was induced by local injection into the plantar surface of the mouse hind-paw. Moreover, the expression of TRPV1 in the skin was evaluated by western blot analysis in CPS-LN injected mice and then compared to a standard CPS solution (CPS-STD).
resultsCPS inclusion in LN induced a lower pain response when compared to CPS-STD; further, it prevented TRPV1 down-regulation in the skin, while CPS-STD induced a significant reduction of TRPV1 expression.
conclusionsDrug encapsulation in lipid nanoparticles produced an optimization of CPS release, thus reducing mice pain behavior and avoiding the effects that are caused by TRPV1 defunctionalization related to a prolonged activation of this receptor.
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