1. IN VITRO AND IN VIVO DEVELOPMENT OF A CHEWING-SYSTEM FOR EVALUATING
Presentation Number: 1014
Session Code:
P10-269
IN VITRO AND IN VIVO DEVELOPMENT OF A CHEWING-SYSTEM FOR EVALUATING
THE RELEASE KINETICS OF BIOACTIVE MOLECULES (CPP-ACP; Qt) CONTAINING GUMS.
Ferrazzano GF1, Cantile T1, Di Stasio M2, Moccia S2, Volpe MG2, Ingenito A1.
1) University of Naples “Federico II”, Department of Pediatric Dentistry, Naples - Italy.
2) Institute of Food Sciences, CNR, Avellino – Italy.
Back-Ground
There is a growing interest in the development of artificial chewing systems in order to simulate human mastication behavior to assess anti-caries active principles release from food and/or pharmacological functional matrices.
AIM
The aim was to develop a novel in vitro chewing-system, compared to the in vivo mastication, for evaluating the release of anti-cariogenic active principles [Casein-Phosphopeptides-Amorphous-Calcium-Phosphate (CPP-ACP) and Quercetin (Qt)](1-3).
DESIGN
CPP-ACP (at 5, 10, and 20%) and Qt (at 0.5 and 1%) containing gums were used (Tab.1). In vitro and in vivo experimental protocols were designed to test the percentages of Ca (from CPP-ACP) and Qt released and their delivery rate from a chewing gum. The in vitro experiments were performed using a specifically designed chewing apparatus to test the release of Ca and Qt in artificial saliva in function of chewed time. This apparatus consisted of a thermostatted cell in which a vertically oriented piston holding an upper chewing plate was mounted; a second chewing plate was mounted on the lower cell surface. The cells were filled with 50 ml of artificial saliva and the chewing-gum was loaded onto the lower chewing surface (Fig.1). The chewing procedure consisted of up and down strokes of the upper surface providing mastication of the chewing gum. The chew frequency was 50±2 strokes per min. The release medium was used for the assessment of Ca and Qt concentrations. In vivo chewing was performed by three volunteers. Each volunteer chewed 1 gr of gum for given periods of time (5', 10', 20' and 30'). The chewed gums were used for the assessment of residual Ca and Qt concentrations.
Table 1. Chewing gum composition.
Fig. 1: Photographs of chewing apparatus
and thermostatted test cell.
RESULTS
In the in vitro study the Ca released was 24–26% at 5', 30–45% at 10', 58–72% at 20', and 59–74% at 30’. In 30' of chewing, the Qt, being more soluble, is delivered in a larger amount (70–90%) than Ca (Fig. 2-3).
In the vivo study the Ca and Qt contained in the chewed gum were complementary to that measured in vitro (Ca: 77–89% at 5‘, 52–70% at 10’, 20–39% at 20', and 18–35% at 30'; Qt: 62–73% at 5', 27–48% at 10', 9–17% at 20', and 8–12% at 30' (Fig. 4-5).
Fig. 2: In vitro release of Ca from gum formulations in artificial saliva .
Fig. 3: In vitro release of Qt from gum formulations in artificial saliva.
Fig. 4: In vivo release of Ca from gum formulations by a chew-out study.
Fig. 5: In vivo release of Qt from gum formulations by a chew-out study.
Conclusion
This study demonstrated that the in vitro chewing apparatus was comparable to in vivo human mastication. Both Ca and Qt were released during chewing, although Ca was released from the chewing gum in a slower and more controlled manner than Qt. This research concludes that both drugs were efficiently released during the mastication process to fully exploit their activity.
REFERENCES
1) Chewing gum, medicated, drug release, European Pharmacopoeia, fourth ed. 2002, pp ) Ferrazzano GF, Amato I, Cantile T, Sangianantoni G, Ingenito A. In vivo remineralising effect of GC tooth mousse on early dental enamel lesions: SEM analysis. Int Dent J 2011;61(4): ) Cushnie TP, Lamb AJ. Antimicrobial activity of flavonoids. Int J Antimicrob Agents 2005;26(5):