Predicting local drug availability of locally acting lozenges: From method design to a linear level A IVIVC

Tietz, Katharina; Gutknecht, Sina Ingrid; Klein, Sandra

doi:10.1016/j.ejpb.2018.10.015

Cited by 6 publications

(1 citation statement)

References 9 publications

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“…The poor retention at the site of application of marketed solutions used as mouthwash and spray or lozenge formulations of benzydamine is, however, still a major drawback making frequent applications, in the necessary range of three to six times per day [ 26 , 28 , 29 ]. Therefore, developing novel formulations with sustained release and mucoadhesive properties would have high practical relevance while reducing the application frequency [ 30 ].…”

Section: Resultsmentioning

confidence: 99%

Intraoral Drug Delivery: Highly Thiolated κ-Carrageenan as Mucoadhesive Excipient

et al. 2023

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Aim: This study aims to design a novel thiolated κ-carrageenan (κ-CA-SH) and evaluate its potential as an excipient for the design of mucoadhesive drug delivery systems. Methods: Native κ-carrageenan (κ-CA) was thiolated with phosphorous pentasulfide in sulfolane and characterized via 1H NMR, FTIR, as well as Ellman’s test. Cytotoxicity was assessed via resazurin assay. In vitro release of the model drug, benzydamine hydrochloride, was determined. Tensile and mucosal residence time studies were performed on buccal and small intestinal mucosa. Mucoadhesive features were investigated via rheological studies with freshly isolated porcine mucus. Results: Thiolated κ-CA (κ-CA-SH) with 1213.88 ± 52 µmol/g thiol groups showed no cytotoxicity at a concentration of 1% (m/v) and low cytotoxicity up to 2% (m/v). Benzydamine hydrochloride showed slow release in solution for both polymers. Tensile studies on buccal and intestinal mucosa showed an up to 2.7-fold and 7.7-fold enhancement in the maximum detachment force (MDF) and total work of adhesion (TWA) of κ-CA-SH vs. κ-CA, respectively. The κ-CA-SH exhibited an up to 4.4-fold improved dynamic viscosity with mucus and significantly prolonged residence time on mucosa compared to native κ-CA. Conclusion: Since highly thiolated κ-CA shows a slow release of positively charged active pharmaceutical ingredients and enhanced mucoadhesive properties, it might be a promising excipient for local drug delivery in the oral cavity.

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