Delivery of Antiplaque Agents from Dentifrices, Gels, and Mouthwashes

Abstract

Antiplaque agents delivered from toothpastes, gels, or mouthrinses can augment mechanical oral hygiene procedures to control the formation of supragingival plaque and the development of early periodontal disease. Clinically effective antiplaque agents are characterized by a combination of intrinsic antibacterial activity and good oral retention properties. The overall oral retention of an antiplaque agent is determined by the strength and rate of association of the agent with its receptor sites and the accessibility of these sites. The substantivity of an antiplaque agent and its clearance from the oral cavity are determined by the rate of dissociation of the agent from the receptor sites and the salivary composition and flow rate. Positively charged and non-charged organic molecules, metal ions, enzymes, and surface-active agents have all been considered as antiplaque agents. To exert clinical antiplaque activity, an antimicrobial agent must be formulated in a chemically compatible delivery vehicle to give optimal release and uptake to the sites of action in a biologically active form during its time of application. In principle, antiplaque activity may be enhanced by combining antimicrobial agents with broadly similar, but complementary, modes of action. Alternatively, the activity of a single agent may be increased by use of a retention aid to enhance oral substantivity. Substantial evidence exists to demonstrate the validity of the first approach. However, there are few data, as yet, to support the effectiveness of the second. The oral mucosa is the bulk retention site for all clinically proven antiplaque agents. Plaque, the pellicle-coated tooth surface, and saliva are probably all sites of biological action. A detailed understanding of the interactions between agents and the various receptor sites, and of the importance of these receptor sites to biological activity, is generally lacking.

In Vitro Fluoride Release and the Antibacterial Effect of Glass Ionomers Containing Chlorhexidine Gluconate

“…2 The number of salivary ms in the oral cavity is correlated to the formation of new caries lesions, and it is generally accepted that reducing the number of ms also reduces caries activity. [3][4][5] In this context, several different antimicro-bial agents have been tested in plaque reduction, [5][6][7][8] and chlorhexidine (CHX) has been proven to be the most effective and safe agent. [9][10] CHX has been shown to be the most suitable agent in reducing ms due to its increased susceptibility when compared to other oral microorganisms.…”

Randomized controlled trial to study plaque inhibition in calcium sodium phosphosilicate dentifrices

“…To improve the plaque control delivered during tooth-brushing, dentifrices are frequently 16 formulated with chemical ingredients that target the plaque bacteria (37) , with new formations continually being developed.…”

Speciation of zinc and tin(II) in dentrifices with reference to availability in saliva

“…According to Cummins and Creeth (1992): "The overall oral retention of an anti plaque agent is determined by the strength and rate of association of the agent with its receptor sites and the accessibility of these sites. The substantivity of an antiplaque agent and its clearance from the oral cavity are determined by the rate of dissociation of the agent from the receptor sites and the salivary composition and flow rate."…”

“…The bulk retention site for all clinically proven antiplaque agents is the oral mucosa with the probable sites of biological action being plaque, the pellicle-coated tooth surface and saliva. The efficacy of these agents is thought to result from the slow release of the bound antiplaque agent from these oral surfaces to give a level in saliva and in plaque capable of inhibiting bacterial growth (Cummins et al, 1992). The processes governing the oral retention and clearance of an antiplaque agent has been summarised in the following diagram by (Cummins et al, 1992).…”

“…The efficacy of these agents is thought to result from the slow release of the bound antiplaque agent from these oral surfaces to give a level in saliva and in plaque capable of inhibiting bacterial growth (Cummins et al, 1992). The processes governing the oral retention and clearance of an antiplaque agent has been summarised in the following diagram by (Cummins et al, 1992). Both the release and uptake phases are governed by first order kinetics and so the retention of an agent is concentration-driven (van Ginnekan, 1977).…”