Pectin Nanoparticle-Loaded Soft Coral <i>Nephthea</i> sp. Extract as <i>In Situ</i> Gel Enhances Chronic Wound Healing: <i>In Vitro</i>, <i>In Vivo</i>, and <i>In Silico</i> Studies

• Main Authors: Nevine H. Hassan (Author), Seham S. El-Hawary (Author), Mahmoud Emam (Author), Mohamed A. Rabeh (Author), Mohamed A. Tantawy (Author), Mohamed Seif (Author), Radwa M. A. Abd-Elal (Author), Gerhard Bringmann (Author), Usama Ramadan Abdelmohsen (Author), Nabil M. Selim (Author)
• Format: Book
• Published: MDPI AG, 2023-07-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

This study shed light for the first time on the <i>in vivo</i> diabetic wound healing potential activity of natural marine soft coral polymeric nanoparticle <i>in situ</i> gel using an excision wound model. A <i>Nephthea</i> sp. methanol-methylene chloride extract loaded with pectin nanoparticles (LPNs) was created. For the preparation of <i>in situ</i> gel, ion-gelation techniques, the entrapment efficiency, the particle size, the polydispersity index, the zeta potential, the <i>in-vitro</i> drug release, and a transmission electron microscope were used and the best formula was selected. Using (UPLC-Q/TOF-MS), 27 secondary metabolites responsible for extract biological activity were identified. Isolation and identification of arachidic acid, oleic acid, nervonic acid, and bis-(2-ethylhexyl)-phthalate (DEHP) of <i>Nephthea</i> sp. was firstly reported here using NMR and mass spectral analyses. Moreover, LPN <i>in situ</i> gel has the best effects on regulating the proinflammatory cytokines (NF-κB, TNF-α, IL-6, and IL-1β) that were detected on days 7 and 15. The results were confirmed with an <i>in vitro</i> enzymatic inhibitory effect of the extract against glycogen synthase kinase (GSK-3) and matrix metalloproteinase-1 (MMP-1), with IC₅₀ values of 0.178 ± 0.009 and 0.258 ± 0.011 µg/mL, respectively. The molecular docking study showed a free binding energy of −9.6 kcal/mol for chabrolosteroid E, with the highest binding affinity for the enzyme (GSK-3), while isogosterone B had −7.8 kcal/mol for the enzyme (MMP-1). A pharmacokinetics study for chabrolohydroxybenzoquinone F and isogosterone B was performed, and it predicted the mode of action of wound healing activity.

Item Description

10.3390/ph16070957
1424-8247