Designing, structural determination and biological effects of rifaximin loaded chitosan- carboxymethyl chitosan nanogel

Samah Attia Algharib; Ali Dawood; Kaixiang Zhou; Dongmei Chen; Chao Li; Kuiyu Meng; Muhammad Kashif Maa; Saeed Ahmed; Lingli Huang; Shuyu Xie

doi:10.1016/j.carbpol.2020.116782

Designing, structural determination and biological effects of rifaximin loaded chitosan- carboxymethyl chitosan nanogel

Carbohydr Polym. 2020 Nov 15:248:116782. doi: 10.1016/j.carbpol.2020.116782. Epub 2020 Jul 22.

Authors

Affiliations

¹ National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, China; Department of Clinical Pathology, Faculty of Veterinary Medicine, Benha University, Moshtohor, Toukh, 13736, QG, Egypt.
² The State Key Laboratory of Agricultural Microbiology, (HZAU), Wuhan, Hubei, 430070, China; Department of Medicine and Infectious Diseases, Faculty of Veterinary Medicine, University of Sadat City, Egypt.
³ National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, China.
⁴ National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, China; MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China.
⁵ MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China. Electronic address: huanglingli@mail.hzau.edu.cn.
⁶ National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, China; MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China. Electronic address: snxsy1@126.com.

PMID: 32919570
DOI: 10.1016/j.carbpol.2020.116782

Abstract

Due to the poor solubility and permeability of rifaximin (RFX), it is not effective against intracellular pathogens although it shows strong activity against most bacteria. To develop an effective mucoadhesive drug delivery system with a targeted release in bacterial infection site, RFX-loaded chitosan (CS)/carboxymethyl-chitosan (CMCS) nanogel was designed and systematically evaluated. FTIR, DSC, and XRD demonstrated that the nanogel was formed by interactions between the positively charged NH₃⁺ on CS and CMCS, and the negatively charged COO on CMCS. RFX was encapsulated into the optimized nanogel in amorphous form. The nanogel was a uniform spherical shape with a mean diameter of 171.07 nm. It had excellent sustained release, strong mucin binding ability, and pH-responsive properties of quicker swelling and release at acidic pH. It showed low hemolytic ratio and high antioxidant activity. The present investigation indicated that the CS-nanogel could be potentially used as a promising bacterial responsiveness drug delivery system.

Keywords: Acetic acid; Bioadhesive; Carboxy methyl chitosan; Chitosan; DPPH; Mucin (from porcine stomach); Nanogel; Potassium bromide (KBr); Rifaximin; Tri polyphosphate; Triton X-100; pH-responsiveness.

MeSH terms

Anti-Bacterial Agents / administration & dosage
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacokinetics
Chitosan / analogs & derivatives*
Chitosan / chemistry*
Drug Delivery Systems / methods*
Drug Design
Drug Liberation
Hydrogen-Ion Concentration
Microscopy, Electron, Transmission
Nanogels / chemistry*
Nanogels / ultrastructure
Particle Size
Rifaximin / administration & dosage*
Rifaximin / chemistry
Rifaximin / pharmacokinetics
Solubility
Spectroscopy, Fourier Transform Infrared
X-Ray Diffraction

Substances

Anti-Bacterial Agents
Nanogels
carboxymethyl-chitosan
Chitosan
Rifaximin