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

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.

• Authors: Flavia Laffleur, Franziska Schmelzle, Ariane Ganner, Stefan Vanicek
• Journal: AAPS PharmSciTech (AAPS PharmSciTech) Vol. 18 Issue 6 Pg. 2102-2109 (Aug 2017) ISSN: 1530-9932 [Electronic] United States
• PMID: 28028792 (Publication Type: Journal Article)

Chemical References

• Excipients
• Curcumin

Topics

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