Lectin-conjugated microspheres for eradication of Helicobacter pylori infection and interaction with mucus

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

Using second generation mucoadhesives may enhance targeting antibiotics for eradication of Helicobacter pylori from the stomach for the treatment of peptic ulcer. The aim of this research was to prepare and characterise ethylcellulose/chitosan microspheres containing clarithromycin with their surfaces functionalised with concanavalin A to produce a floating-mucoadhesive formulation. The microspheres were prepared using an emulsification-solvent evaporation method. Particle size, surface morphology, in vitro buoyancy profile, zeta potential, drug entrapment efficiency, in vitro drug release and release kinetics of the particles were determined. Lectin was conjugated to the microsphere surface using two-stage carbodiimide activation and confirmed using FTIR, fluorescence studies and zeta potential measurements. Conjugation ranged from 11 to 15 μg Con A/mg microspheres which represents over 56% efficiency although there was some drug loss during the conjugation process. Conjugation did not have a significant effect on the buoyancy and release of drug from the microspheres using a mucus diffusion model with 53% and 40% of drug released from unconjugated and conjugated microspheres within 12 h. Conjugation improved mucoadhesion and interaction with porcine gastric mucin compared to unconjugated microspheres. The buoyancy and improved mucoadhesion of the microspheres provides potential for delivery of clarithromycin and other drugs to the stomach.

LanguageEnglish
Pages28-40
Number of pages13
JournalInternational Journal of Pharmaceutics
Volume470
Issue number1-2
DOIs
Publication statusPublished - 15 Aug 2014

Fingerprint

Helicobacter Infections
Mucus
Microspheres
Lectins
Helicobacter pylori
Clarithromycin
Pharmaceutical Preparations
Stomach
Gastric Mucins
Carbodiimides
Chitosan
Fourier Transform Infrared Spectroscopy
Concanavalin A
Peptic Ulcer
Particle Size
Swine
Fluorescence
Anti-Bacterial Agents
Research

Cite this

@article{954982aa95304aae92675e2dd04051af,
title = "Lectin-conjugated microspheres for eradication of Helicobacter pylori infection and interaction with mucus",
abstract = "Using second generation mucoadhesives may enhance targeting antibiotics for eradication of Helicobacter pylori from the stomach for the treatment of peptic ulcer. The aim of this research was to prepare and characterise ethylcellulose/chitosan microspheres containing clarithromycin with their surfaces functionalised with concanavalin A to produce a floating-mucoadhesive formulation. The microspheres were prepared using an emulsification-solvent evaporation method. Particle size, surface morphology, in vitro buoyancy profile, zeta potential, drug entrapment efficiency, in vitro drug release and release kinetics of the particles were determined. Lectin was conjugated to the microsphere surface using two-stage carbodiimide activation and confirmed using FTIR, fluorescence studies and zeta potential measurements. Conjugation ranged from 11 to 15 μg Con A/mg microspheres which represents over 56{\%} efficiency although there was some drug loss during the conjugation process. Conjugation did not have a significant effect on the buoyancy and release of drug from the microspheres using a mucus diffusion model with 53{\%} and 40{\%} of drug released from unconjugated and conjugated microspheres within 12 h. Conjugation improved mucoadhesion and interaction with porcine gastric mucin compared to unconjugated microspheres. The buoyancy and improved mucoadhesion of the microspheres provides potential for delivery of clarithromycin and other drugs to the stomach.",
keywords = "Chitosan, Concanavalin A, Ethylcelluose, Helicobacter pylori, Microspheres, Mucoadhesive",
author = "Adebisi, {Adeola O.} and Conway, {Barbara R.}",
year = "2014",
month = "8",
day = "15",
doi = "10.1016/j.ijpharm.2014.04.070",
language = "English",
volume = "470",
pages = "28--40",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

TY - JOUR

T1 - Lectin-conjugated microspheres for eradication of Helicobacter pylori infection and interaction with mucus

AU - Adebisi, Adeola O.

AU - Conway, Barbara R.

PY - 2014/8/15

Y1 - 2014/8/15

N2 - Using second generation mucoadhesives may enhance targeting antibiotics for eradication of Helicobacter pylori from the stomach for the treatment of peptic ulcer. The aim of this research was to prepare and characterise ethylcellulose/chitosan microspheres containing clarithromycin with their surfaces functionalised with concanavalin A to produce a floating-mucoadhesive formulation. The microspheres were prepared using an emulsification-solvent evaporation method. Particle size, surface morphology, in vitro buoyancy profile, zeta potential, drug entrapment efficiency, in vitro drug release and release kinetics of the particles were determined. Lectin was conjugated to the microsphere surface using two-stage carbodiimide activation and confirmed using FTIR, fluorescence studies and zeta potential measurements. Conjugation ranged from 11 to 15 μg Con A/mg microspheres which represents over 56% efficiency although there was some drug loss during the conjugation process. Conjugation did not have a significant effect on the buoyancy and release of drug from the microspheres using a mucus diffusion model with 53% and 40% of drug released from unconjugated and conjugated microspheres within 12 h. Conjugation improved mucoadhesion and interaction with porcine gastric mucin compared to unconjugated microspheres. The buoyancy and improved mucoadhesion of the microspheres provides potential for delivery of clarithromycin and other drugs to the stomach.

AB - Using second generation mucoadhesives may enhance targeting antibiotics for eradication of Helicobacter pylori from the stomach for the treatment of peptic ulcer. The aim of this research was to prepare and characterise ethylcellulose/chitosan microspheres containing clarithromycin with their surfaces functionalised with concanavalin A to produce a floating-mucoadhesive formulation. The microspheres were prepared using an emulsification-solvent evaporation method. Particle size, surface morphology, in vitro buoyancy profile, zeta potential, drug entrapment efficiency, in vitro drug release and release kinetics of the particles were determined. Lectin was conjugated to the microsphere surface using two-stage carbodiimide activation and confirmed using FTIR, fluorescence studies and zeta potential measurements. Conjugation ranged from 11 to 15 μg Con A/mg microspheres which represents over 56% efficiency although there was some drug loss during the conjugation process. Conjugation did not have a significant effect on the buoyancy and release of drug from the microspheres using a mucus diffusion model with 53% and 40% of drug released from unconjugated and conjugated microspheres within 12 h. Conjugation improved mucoadhesion and interaction with porcine gastric mucin compared to unconjugated microspheres. The buoyancy and improved mucoadhesion of the microspheres provides potential for delivery of clarithromycin and other drugs to the stomach.

KW - Chitosan

KW - Concanavalin A

KW - Ethylcelluose

KW - Helicobacter pylori

KW - Microspheres

KW - Mucoadhesive

UR - http://www.scopus.com/inward/record.url?scp=84901022710&partnerID=8YFLogxK

U2 - 10.1016/j.ijpharm.2014.04.070

DO - 10.1016/j.ijpharm.2014.04.070

M3 - Article

VL - 470

SP - 28

EP - 40

JO - International Journal of Pharmaceutics

T2 - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -