Antibacterial nanofibers of pullulan/tetracycline-cyclodextrin inclusion complexes for Fast-Disintegrating oral drug delivery

J Colloid Interface Sci. 2022 Mar 15:610:321-333. doi: 10.1016/j.jcis.2021.12.013. Epub 2021 Dec 8.

Abstract

Tetracycline is a widely used antibiotic suffering from poor water solubility and low bioavailability. Here, hydroxypropyl-beta-cyclodextrin (HPβCD) was used to form inclusion complexes (IC) of tetracycline with 2:1 M ratio (CD:drug). Then, tetracycline-HPβCD-IC was mixed with pullulan- a non-toxic, water-soluble biopolymer - to form nanofibrous webs via electrospinning. The electrospinning of pullulan/tetracycline-HPβCD-IC was yielded into defect-free nanofibers collected in the form of a self-standing and flexible material with the loading capacity of ∼ 7.7 % (w/w). Pullulan/tetracycline nanofibers was also generated as control sample having the same drug loading. Tetracycline was found in the amorphous state in case of pullulan/tetracycline-HPβCD nanofibers due to inclusion complexation. Through inclusion complexation with HPβCD, enhanced aqueous solubility and faster release profile were provided for pullulan/tetracycline-HPβCD-IC nanofibers compared to pullulan/tetracycline one. Additionally, pullulan/tetracycline-HPβCD-IC nanofibers readily disintegrated when wetted with artificial saliva while pullulan/tetracycline nanofibers were not completely absorbed by the same simulate environment. Electrospun nanofibers showed promising antibacterial activity against both gram-positive and gram-negative bacteria. Briefly, our findings indicated that pullulan/tetracycline-HPβCD-IC nanofibers could be an attractive material as orally fast disintegrating drug delivery system for the desired antibiotic treatment thanks to its promising physicochemical and antibacterial properties.

Keywords: Antibacterial; Antibiotic; Cyclodextrin; Electrospinning; Fast disintegrating; Fast dissolving; Inclusion complex; Nanofibers; Oral drug delivery; Tetracycline.

MeSH terms

  • 2-Hydroxypropyl-beta-cyclodextrin
  • Anti-Bacterial Agents / pharmacology
  • Cyclodextrins*
  • Drug Carriers
  • Drug Delivery Systems
  • Glucans
  • Gram-Negative Bacteria
  • Gram-Positive Bacteria
  • Nanofibers*
  • Solubility
  • Tetracycline / pharmacology

Substances

  • Anti-Bacterial Agents
  • Cyclodextrins
  • Drug Carriers
  • Glucans
  • 2-Hydroxypropyl-beta-cyclodextrin
  • pullulan
  • Tetracycline