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Borneol-based antisolvent-induced in situ forming matrix for crevicular pocket delivery of vancomycin hydrochloride

2022; Elsevier BV; Volume: 617; Linguagem: Inglês

10.1016/j.ijpharm.2022.121603

1873-3476

Nutdanai Lertsuphotvanit, Wichai Santimaleeworagun, Worrakanya Narakornwit, Tiraniti Chuenbarn, Jongjan Mahadlek, Takron Chantadee, Thawatchai Phaechamud,

Advanced Drug Delivery Systems

Given its safety and apparent low aqueous solubility, borneol may serve as a matrix forming component of anti-solvent based in situ forming matrixes (ISMs) for crevicular pocket targeting. Drug-free and vancomycin hydrochloride-loaded borneol ISMs were evaluated for pH, density, viscosity, contact angle, surface tension, matrix formation, drug release behavior, in vitro degradability and antimicrobial activities. Density and pH values of borneol-based ISMs decreased with increasing borneol concentration. Given their markedly low viscosity could facilitate better injectability. The contact angles of the drug-free and vancomycin HCl-loaded borneol ISMs increased after being in contact with the agarose gel or the bulge tissue of porcine due to phase inversion. A dense borneol crystal matrix formed after using the highly concentrated ISM corresponded to fast matrix formation. The borneol-based ISM exhibited a sustainable drug release longer than 14 days with a diffusion-controlled release mechanism. Moreover, the developed ISM exhibited strong antimicrobial activities against various microbes. Thus, the vancomycin HCl-loaded borneol-based ISM is a potentially effective local anti-solvent-based ISM for periodontitis treatment via crevicular pocket injection.