Development and Evaluation of Minocycline Hydrochloride-Loaded In Situ Cubic Liquid Crystal for Intra-Periodontal Pocket Administration

Abstract

In the present study, an injectable in situ liquid crystal formulation was developed for local delivery of minocycline hydrochloride (MH) for chronic periodontitis treatment. The physicochemical properties, phase structures, in vitro drug release and pharmacodynamics of in situ liquid crystals were investigated. The optimal formulation (phytantriol (PT)/propylene glycol (PG)/water, 63/27/10, w/w/w) loaded with 20 mg/g MH was proved to be injectable. The precursor formulation can form a cubic phase gel in excess water in 6.97 ± 0.10 s. The results of in vitro drug release suggested the MH presented a sustained release for 4 days. Liquid crystal precursor formulation significantly reduced gingival index, probing depth and alveolar bone loss compared to the model group (p < 0.01). Besides, the pathological characteristics of model rats were improved. The results suggested that MH-loaded in situ cubic liquid crystal possessed of sustained release ability and periodontal clinical symptoms improvement. The developed in situ cubic liquid crystal may be a potentially carrier in the local delivery of MH for periodontal diseases.

In Vitro Evaluation of Antimicrobial Activity of Minocycline Formulations for Topical Application in Periodontal Therapy

“…As a local drug in periodontal therapy, different approaches have been taken, such as loaded in PLGA hydrogels [30], in in situ reversed hexagonal mesophase [31], or in liquid crystals [32]. In this study, the experimental formulations were compared with minocycline microspheres which have been commercially available for many years.…”

Minocycline-loaded PLGA electrospun membrane prevents alveolar bone loss in experimental peridontitis

“…Periocline V R is a bio-absorbable drug in the form of a sustained local drug delivery system, consisting of 20 mg/g minocycline hydrochloride in a matrix of hydroxyethyl-cellulose (Yang et al, 2018). The release rate of Periocline V R is dependent on the degradation of the matrix material, and antibacterial activity can last for approximately 7 d (Yang et al, 2018).…”

“…Periocline V R is a bio-absorbable drug in the form of a sustained local drug delivery system, consisting of 20 mg/g minocycline hydrochloride in a matrix of hydroxyethyl-cellulose (Yang et al, 2018). The release rate of Periocline V R is dependent on the degradation of the matrix material, and antibacterial activity can last for approximately 7 d (Yang et al, 2018). Periocline V R was shown to increase the concentration of MINO in the periodontal pocket, but the rate of drug release is not constant (Vandekerckhove et al, 1998;Liu et al, 2013).…”

Sustained‐release delivery of antimicrobial drugs for the treatment of periodontal diseases: Fantasy or already reality?

“…A new type of injectable gel has been recently developed by Yang et al . They used liquid crystals, which essentially flow like a liquid, but the molecules are oriented in a crystal‐like fashion.…”