In Vitro and Ex Vivo Evaluation of Novel Curcumin-Loaded Excipient for Buccal Delivery

AAPS PharmSciTech. 2017 Aug;18(6):2102-2109. doi: 10.1208/s12249-016-0676-y. Epub 2016 Dec 27.

Abstract

This study aimed to develop a mucoadhesive polymeric excipient comprising curcumin for buccal delivery. Curcumin encompasses broad range of benefits such as antioxidant, anti-inflammatory, and chemotherapeutic activity. Hyaluronic acid (HA) as polymeric excipient was modified by immobilization of thiol bearing ligands. L-Cysteine (SH) ethyl ester was covalently attached via amide bond formation between cysteine and the carboxylic moiety of hyaluronic acid. Succeeded synthesis was proved by H-NMR and IR spectra. The obtained thiolated polymer hyaluronic acid ethyl ester (HA-SH) was evaluated in terms of stability, safety, mucoadhesiveness, drug release, and permeation-enhancing properties. HA-SH showed 2.75-fold higher swelling capacity over time in comparison to unmodified polymer. Furthermore, mucoadhesion increased 3.4-fold in case of HA-SH and drug release was increased 1.6-fold versus HA control, respectively. Curcumin-loaded HA-SH exhibits a 4.4-fold higher permeation compared with respective HA. Taking these outcomes in consideration, novel curcumin-loaded excipient, namely thiolated hyaluronic acid ethyl ester appears as promising tool for pharyngeal diseases.

Keywords: buccal; curcumin; hyaluronic acid; thiomer; wound healing.

MeSH terms

  • Animals
  • Caco-2 Cells
  • Curcumin / administration & dosage
  • Curcumin / chemistry
  • Curcumin / pharmacokinetics*
  • Drug Delivery Systems / methods*
  • Drug Evaluation, Preclinical / methods
  • Excipients / administration & dosage
  • Excipients / chemistry
  • Excipients / pharmacokinetics*
  • Humans
  • Mouth Mucosa / drug effects
  • Mouth Mucosa / metabolism*
  • Swine

Substances

  • Excipients
  • Curcumin