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Main Authors: Sharaf, Mohamed, Al-Laith, Zainab Naser, Khan, Tehsin Ullah, Elkelish, Amr, Abdel-Maksoud, Mohamed S, Elrefaei, Nadia G, Alawam, Abdullah S, Liu, Chen-Guang
Format: Artículo científico
Language:en
Published: Bioorganic chemistry 2026
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Online Access:https://pubmed.ncbi.nlm.nih.gov/41554206/
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author Sharaf, Mohamed
Al-Laith, Zainab Naser
Khan, Tehsin Ullah
Elkelish, Amr
Abdel-Maksoud, Mohamed S
Elrefaei, Nadia G
Alawam, Abdullah S
Liu, Chen-Guang
author_facet Sharaf, Mohamed
Al-Laith, Zainab Naser
Khan, Tehsin Ullah
Elkelish, Amr
Abdel-Maksoud, Mohamed S
Elrefaei, Nadia G
Alawam, Abdullah S
Liu, Chen-Guang
Sharaf, Mohamed
Al-Laith, Zainab Naser
Khan, Tehsin Ullah
Elkelish, Amr
Abdel-Maksoud, Mohamed S
Elrefaei, Nadia G
Alawam, Abdullah S
Liu, Chen-Guang
collection PubMed - marine biology
contents Mucoadhesive lignin-liposome nanocarriers of coptisine: A multifunctional strategy against antibiotic-resistant Helicobacter pylori biofilms. Sharaf, Mohamed Al-Laith, Zainab Naser Khan, Tehsin Ullah Elkelish, Amr Abdel-Maksoud, Mohamed S Elrefaei, Nadia G Alawam, Abdullah S Liu, Chen-Guang Helicobacter pylori Biofilms Anti-Bacterial Agents Liposomes Berberine Animals Microbial Sensitivity Tests Lignin Mice Drug Resistance, Bacterial Nanoparticles Particle Size Dose-Response Relationship, Drug Molecular Structure Drug Carriers Structure-Activity Relationship Helicobacter pylori remain a major global health challenge due to rising antibiotic resistance, persistent biofilm formation, and oxidative stress-mediated gastric pathogenesis. Innovative therapeutic approaches are urgently required to overcome the limitations of conventional antibiotic regimens. We engineered a novel mucoadhesive nanocarrier (COP-LIG@LIPSNCs) by synergistically integrating biofilm-disrupting lignin nanoparticles with biocompatible liposomal vesicles to encapsulate the bioactive isoquinoline alkaloid coptisine. The formulations were comprehensively characterized using DLS, FTIR, XRD, and TEM. Antibacterial and antibiofilm were evaluated through MIC/MBC assays, time-kill kinetics, confocal bioimaging, and electron microscopy. Cytocompatibility was assessed using L929 fibroblasts, while in vivo mucoadhesion and therapeutic efficacy were investigated in a murine model. COP-LIG@LIPSNCs exhibited a stable nanoscale size (∼197 nm; PDI 0.152; ζ-potential -31.4 mV, EE% 89.2 ± 1.4 % and LE% 2.1 ± 0.08 %). COP-LIG@LIPSNCs displayed sustained behaviour, releasing 42.28 ± 4.2 % in SGF and 58.17 ± 4.1 % in SIF after 48 h, with strong mucoadhesion. Antibacterial studies demonstrated potent activity against H. pylori (MIC 32 μg/mL; MBC 64 μg/mL), achieving >92 % eradication of planktonic cells and ∼ 89 % disruption of established biofilms within 24 h. CLSM and SEM confirmed nanocarrier penetration, membrane disruption, and biofilm dispersion. Surprisingly, the H. pylori burden of the COP@LIG@LIP group was significantly lower at 1.38 × 10 CFU/g compared to negative control, indicating the effective treatment effect of killing H. pylori in vivo. COP-LIG@LIPSNCs represent a novel and multifunctional nanoplatform that synergistically combines antimicrobial, antibiofilm, and antioxidant actions. This study pioneers a sustainable strategy using lignin to create an advanced therapeutic alternative, showing significant promise for managing drug-resistant H. pylori infections.
format Artículo científico
id pubmed_41554206
institution PubMed
language en
publishDate 2026
publisher Bioorganic chemistry
record_format pubmed
spellingShingle Mucoadhesive lignin-liposome nanocarriers of coptisine: A multifunctional strategy against antibiotic-resistant Helicobacter pylori biofilms.
Sharaf, Mohamed
Al-Laith, Zainab Naser
Khan, Tehsin Ullah
Elkelish, Amr
Abdel-Maksoud, Mohamed S
Elrefaei, Nadia G
Alawam, Abdullah S
Liu, Chen-Guang
Helicobacter pylori
Biofilms
Anti-Bacterial Agents
Liposomes
Berberine
Animals
Microbial Sensitivity Tests
Lignin
Mice
Drug Resistance, Bacterial
Nanoparticles
Particle Size
Dose-Response Relationship, Drug
Molecular Structure
Drug Carriers
Structure-Activity Relationship
Mucoadhesive lignin-liposome nanocarriers of coptisine: A multifunctional strategy against antibiotic-resistant Helicobacter pylori biofilms. Sharaf, Mohamed Al-Laith, Zainab Naser Khan, Tehsin Ullah Elkelish, Amr Abdel-Maksoud, Mohamed S Elrefaei, Nadia G Alawam, Abdullah S Liu, Chen-Guang Helicobacter pylori Biofilms Anti-Bacterial Agents Liposomes Berberine Animals Microbial Sensitivity Tests Lignin Mice Drug Resistance, Bacterial Nanoparticles Particle Size Dose-Response Relationship, Drug Molecular Structure Drug Carriers Structure-Activity Relationship Helicobacter pylori remain a major global health challenge due to rising antibiotic resistance, persistent biofilm formation, and oxidative stress-mediated gastric pathogenesis. Innovative therapeutic approaches are urgently required to overcome the limitations of conventional antibiotic regimens. We engineered a novel mucoadhesive nanocarrier (COP-LIG@LIPSNCs) by synergistically integrating biofilm-disrupting lignin nanoparticles with biocompatible liposomal vesicles to encapsulate the bioactive isoquinoline alkaloid coptisine. The formulations were comprehensively characterized using DLS, FTIR, XRD, and TEM. Antibacterial and antibiofilm were evaluated through MIC/MBC assays, time-kill kinetics, confocal bioimaging, and electron microscopy. Cytocompatibility was assessed using L929 fibroblasts, while in vivo mucoadhesion and therapeutic efficacy were investigated in a murine model. COP-LIG@LIPSNCs exhibited a stable nanoscale size (∼197 nm; PDI 0.152; ζ-potential -31.4 mV, EE% 89.2 ± 1.4 % and LE% 2.1 ± 0.08 %). COP-LIG@LIPSNCs displayed sustained behaviour, releasing 42.28 ± 4.2 % in SGF and 58.17 ± 4.1 % in SIF after 48 h, with strong mucoadhesion. Antibacterial studies demonstrated potent activity against H. pylori (MIC 32 μg/mL; MBC 64 μg/mL), achieving >92 % eradication of planktonic cells and ∼ 89 % disruption of established biofilms within 24 h. CLSM and SEM confirmed nanocarrier penetration, membrane disruption, and biofilm dispersion. Surprisingly, the H. pylori burden of the COP@LIG@LIP group was significantly lower at 1.38 × 10 CFU/g compared to negative control, indicating the effective treatment effect of killing H. pylori in vivo. COP-LIG@LIPSNCs represent a novel and multifunctional nanoplatform that synergistically combines antimicrobial, antibiofilm, and antioxidant actions. This study pioneers a sustainable strategy using lignin to create an advanced therapeutic alternative, showing significant promise for managing drug-resistant H. pylori infections.
title Mucoadhesive lignin-liposome nanocarriers of coptisine: A multifunctional strategy against antibiotic-resistant Helicobacter pylori biofilms.
topic Helicobacter pylori
Biofilms
Anti-Bacterial Agents
Liposomes
Berberine
Animals
Microbial Sensitivity Tests
Lignin
Mice
Drug Resistance, Bacterial
Nanoparticles
Particle Size
Dose-Response Relationship, Drug
Molecular Structure
Drug Carriers
Structure-Activity Relationship
url https://pubmed.ncbi.nlm.nih.gov/41554206/