Formulation development and evaluation of lidocaine hydrochloride loaded in chitosan-pectin-hyaluronic acid polyelectrolyte complex for dry socket treatment

Nuttawut Supachawaroj; Teerasak Damrongrungruang; Sucharat Limsitthichaikoon

doi:10.1016/j.jsps.2021.07.007

Formulation development and evaluation of lidocaine hydrochloride loaded in chitosan-pectin-hyaluronic acid polyelectrolyte complex for dry socket treatment

Saudi Pharm J. 2021 Sep;29(9):1070-1081. doi: 10.1016/j.jsps.2021.07.007. Epub 2021 Jul 19.

Authors

Nuttawut Supachawaroj^{1

2}, Teerasak Damrongrungruang³, Sucharat Limsitthichaikoon¹

Affiliations

¹ Department of Pharmaceutical Technology, College of Pharmacy, Rangsit University, Thailand.
² Department of Oral Surgery, College of Dental Medicine, Rangsit University, Thailand.
³ Division of Oral Diagnosis, Department of Oral Biomedical Science, Faculty of Dentistry, Khon Kaen University, Thailand.

Abstract

The main purpose of this study was to assess a lidocaine hydrochloride-loaded chitosan-pectin-hyaluronic polyelectrolyte complex for rapid onset and sustained release in dry socket wound treatment. Nine formulations (LCs) of lidocaine hydrochloride (LH) loaded into a chitosan-pectin-hyaluronic polyelectrolyte complex (PEC) were assessed using full factorial design (two factors × three levels). The formulations ranged between 4 and 10% w/w LH and 0.5-1.5% w/w HA. The following physicochemical properties of LCs were characterized: size, zeta potential, % entrapment efficiency, viscosity, mucoadhesiveness, % drug release, morphology, storage stability, and cytotoxicity. The particle size, zeta potential, % EE, viscosity, and % mucoadhesion increased with increasing LH and HA concentrations. Rapid release of LH followed a zero-order model, and a steady-state percentage of the drug was released over 4 h. LCs were found to be non-cytotoxic compared to LH solution. LH loaded into PEC demonstrated appropriate characteristics-including suitable rate of release-and fit a zero-order model. Furthermore, it was not cytotoxic and showed good stability in a high-HA formula, making it a promising candidate for future topical oral formulations.

Keywords: 32 factorial design; Dry socket treatment; HA, hyaluronic acid; Hyaluronic acid; LC, lidocaine hydrochloride loaded in chitosan-pectin-hyaluronic acid polyelectrolyte complex; LH, lidocaine hydrochloride; Lidocaine hydrochloride; PDI, polydispersion index; PEC, Chitosan-Pectin- Hyaluronic acid Polyelectrolyte Complex; Polyelectrolyte complex; Zn, zinc sulphate.