Purpose and Background: To study the incremental in vitro release of KSL (W), an antimicrobial decapeptide with a broad range of microbicidal activity, and CPC, a surface- active agent, from a chewing gum formulation for controlling dental plaque growth, and to determine the adsorption of KSL (W) and CPC onto hydroxyapatite (HA) discs. Methods: The incremental release of KSL (W) and CPC from the gum formulation was studied using a chewing apparatus (artificial saliva at 37°C, 50 strokes/min). The adsorption of both actives, KSL (W) and CPC, was determined by immersing the HA discs into the release medium. The amounts of KSL (W) and CPC in the release medium before and after the adsorption process at each time point were analyzed by reversed-phase HPLC. Results: Approximately 17% of KSL (W) and ~46 % of CPC that were present in the formulation were released in the first 2 minutes. This was followed by the release of an additional 28% of the peptide and ~18% CPC in the next 3 minutes. Thereafter, the amount released per unit of time declined gradually throughout 60 minutes of chewing. Approximately 9 mg of the loaded KSL (W) (10 mg/gum) and 1.8 mg of the loaded CPC (2 mg/gum) were released after 60 minutes of chewing. It was also shown that ~100% of the adsorbed KSL (W) on the HA discs at each time point was released via a desorption process into fresh artificial saliva during the chewing. Conclusion: The analysis of the incremental release data suggests that the amount of KSL (W) and CPC in the mouth will be that during the stated increment of time and any released KSL (W) from the previous increment will be eliminated or cleared from the oral cavity during the subsequent increment. This of course would represent the minimum amount since there will be some KSL (W) remaining from the previous increment which will be additional to the subsequent period. This also does not account for adsorption to the teeth and carryover to the next increment. The concentrations in the mouth have been shown to provide antimicrobial activity.

Incremental in vitro release of a decapeptide, KSL (W), and cetylpyridinium chloride, CPC, from a chewing gum formulation and their adsorption on hydroxyapatite.

BLASI, PAOLO;SCHOUBBEN, Aurelie Marie Madeleine;
2008

Abstract

Purpose and Background: To study the incremental in vitro release of KSL (W), an antimicrobial decapeptide with a broad range of microbicidal activity, and CPC, a surface- active agent, from a chewing gum formulation for controlling dental plaque growth, and to determine the adsorption of KSL (W) and CPC onto hydroxyapatite (HA) discs. Methods: The incremental release of KSL (W) and CPC from the gum formulation was studied using a chewing apparatus (artificial saliva at 37°C, 50 strokes/min). The adsorption of both actives, KSL (W) and CPC, was determined by immersing the HA discs into the release medium. The amounts of KSL (W) and CPC in the release medium before and after the adsorption process at each time point were analyzed by reversed-phase HPLC. Results: Approximately 17% of KSL (W) and ~46 % of CPC that were present in the formulation were released in the first 2 minutes. This was followed by the release of an additional 28% of the peptide and ~18% CPC in the next 3 minutes. Thereafter, the amount released per unit of time declined gradually throughout 60 minutes of chewing. Approximately 9 mg of the loaded KSL (W) (10 mg/gum) and 1.8 mg of the loaded CPC (2 mg/gum) were released after 60 minutes of chewing. It was also shown that ~100% of the adsorbed KSL (W) on the HA discs at each time point was released via a desorption process into fresh artificial saliva during the chewing. Conclusion: The analysis of the incremental release data suggests that the amount of KSL (W) and CPC in the mouth will be that during the stated increment of time and any released KSL (W) from the previous increment will be eliminated or cleared from the oral cavity during the subsequent increment. This of course would represent the minimum amount since there will be some KSL (W) remaining from the previous increment which will be additional to the subsequent period. This also does not account for adsorption to the teeth and carryover to the next increment. The concentrations in the mouth have been shown to provide antimicrobial activity.
2008
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11391/42202
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