In Vitro and Ex Vivo Evaluation of Novel Curcumin-Loaded Excipient for Buccal Delivery
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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.
KEY WORDSbuccal curcumin hyaluronic acid thiomer wound healing
The authors thank Josef Mayr in Mayr, Natters, Austria for the porcine mucosa.
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Declaration of Interest
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties. No writing assistance was utilized in the production of this manuscript.
- 16.Jennings P, Koppelstaetter C, Pfaller W, Morin JP, Hartung T, Ryan MP. Assessment of a new cell culture perfusion apparatus for in vitro chronic toxicity testing—part 2: toxicological evaluation. Altex-Altern Tierexp. 2004;21(2):61–6.Google Scholar
- 19.Laffleur F, Psenner J, Suchaoin W. Permeation enhancement via thiolation: in vitro and ex vivo evaluation of hyaluronic acid-cysteine ethyl ester. J Pharm Sci. 2015;104(7):2153–60.Google Scholar
- 21.Mueller C, Verroken A, Iqbal J, Bernkop-Schnuerch A. Thiolated chitosans: in vitro comparison of mucoadhesive properties. J Appl Polym Sci. 2012;124(6):5046–55.Google Scholar
- 26.Peppas NA. Mucoadhesive polymers. Abstr Pap Am Chem Soc. 1990;199:343-POLY.Google Scholar