Meloxicam-loaded solvent exchange-induced in situ forming beta-cyclodextrin gel and microparticle for periodontal pocket delivery

Abstract

The in situ forming system has attracted attention for periodontitis treatment owing to its sustainable drug release localisation at a periodontal pocket. Given its low aqueous solubility, beta-cyclodextrin (β-CD) may serve as a matrix former of solvent exchange-induced in situ forming gel (ISG) and microparticle (ISM). Meloxicam (Mex)-loaded-β-CD ISG and ISM were prepared using β-CD in dimethyl sulphoxide (ISG) as the internal phase and camellia oil comprising 5% glyceryl monostearate as the external phase (ISM). Mex-loaded β-CD systems comprising 40% β-CD were easily injected via a 24-gauge needle. During solvent exchange with phosphate buffer saline (pH 6.8), the highly concentrated β-CD ISG promoted the phase inversion of β-CD aggregates into matrix-like. Upon exposure to aqueous phase, the ISM system comprising 40% β-CD transformed into microparticles and extended the drug release to 7 days with minimised initial burst release following Fickian diffusion. Moreover, the potential degradability was evident from the high weight loss. High maximum deformation force with high viscous character initiated the slow diffusion rate of the solvent from the ISM system. Therefore, 40% β-CD ISM is a potential local Mex-controlled release system of anti-inflammatory drug for periodontitis treatment.

Keywords: Beta-cyclodextrin; In situ forming gel; In situ forming microparticle; Local delivery; Meloxicam; Periodontal pocket.