PAMAM dendrimers for the delivery of the antibacterial Triclosan

Abstract

Many oral care products incorporate an antibacterial compound to prevent the formation of dental plaque which predisposes teeth to dental caries or periodontal disease [1]. Triclosan (TCN) is a commonly used antiplaque agent in toothpastes [2,3]. Strategies to increase the delivery efficiency of antibacterials using formulation aids such as polyamidoamine (PAMAM) dendrimers are of interest.Solubilisation studies over the pH range 5-12 demonstrated an increase in the level of TCN solubilised with increasing dendrimer concentration (1 mM-5 mM). However, the dendrimer was unable to enhance TCN solubility at lower pH values and the solubilising effect observed was attributed to the ionization of TCN (pKa 8.14) resulting from dendrimer induced pH changes.End group modification of G3 PAMAM dendrimer with phenylalanine in order to promote solubility through p-p stacking between TCN and the amino acid has been carried out. Phenylalanine:G3 PAMAM conjugates of different ratios (32:1, 21:1, 16:1) were synthesized. The fully conjugated dendrimer (32:1) had poor aqueous solubility, whereas the 21:1 and 16:1 dendrimer conjugates were water soluble. The 21:1 conjugate was tested for its ability to solubilise TCN, however, again there was no increase over control buffer solutions of the same pH. An alternative approach under investigation is to directly conjugate TCN to PAMAM dendrimers via a hydrolysable linkage.

Assessment of antifungal activity of herbal and conventional toothpastes against clinical isolates of Candida albicans

“…These antimicrobial agents include metal salts, phenols, herbal extracts, enzymes, essential oils, and bisbiguanides [2,7,8] . Toothpastes have been formulated to contain a chemotherapeutic agents to improve oral health, to produce inhibitory action on plaque formation and bacteria and Candida colonisation [2,4,[9][10][11] . Objective: To detect the anticandidal activity of nine toothpastes containing sodium fluoride, sodium monofluorophosphate and herbal extracts as an active ingredients against 45 oral and non oral Candida albicans (C. albicans) isolates.…”

Dendrimer Structure Diversity and Tailorability as a Way to Fight Infectious Diseases

“…Antibacterial activity of drugs increased by the application of the above mentioned combination. Another drug molecule of antimicrobial activity that was Nanostructured Materials -Fabrication to Applicationssuccessfully solubilized by PAMAMs was triclosan [54]. Although this formulation has not been tested on bacteria, the amount of drug solubilized was remarkable and-as found in this report-highly dependent on the pH of the analysed solution.…”

Inhibitory effects of medical plants on the Candida albicans and bacterial growth in the oral cavity

“…These antimicrobial agents include metal salts, phenols, herbal extracts, enzymes, essential oils, and bisbiguanides (Stamm, 2007;Yiğit et al, 2008). Toothpaste has been formulated to contain chemotherapeutic agents to improve the oral health, to produce inhibitory action on plaque formation as well as bacteria and Candida colonization (Gardiner et al, 2008;Yiğit et al, 2008;Sadeghi and Assar, 2009;Adwan et al, 2012). However, there is a different approach to the oral hygiene.…”