In vitro anti-Acanthamoeba synergistic effect of chlorhexidine and cationic carbosilane dendrimers against both trophozoite and cyst forms

• Published in: International journal of pharmaceutics 2016-07, Vol.509 (1-2), p.1-7
• Main Authors: Heredero-Bermejo, I., Sánchez-Nieves, J., Soliveri, J., Gómez, R., de la Mata, F.J., Copa-Patiño, J.L., Pérez-Serrano, J.
• Format: Article
• Language: English
• Subjects: Acanthamoeba; Acanthamoeba - drug effects; Acanthamoeba keratitis; Acanthamoeba Keratitis - drug therapy; Acanthamoeba polyphaga; Anti-Infective Agents, Local - pharmacology; Carbosilane dendrimers; Cations - pharmacology; Cell Line, Tumor; Chlorhexidine - analogs & derivatives; Chlorhexidine - pharmacology; Chlorhexidne; Cysts - drug therapy; Dendrimers - pharmacology; Drug resistance; Drug Synergism; HeLa Cells; Humans; Microbicide; Silanes - pharmacology; Synergy; Trophozoites - drug effects
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2016.04.075

Combinations of chlorhexidine with ammonium and guanidine carbosilane dendrimers have remarkable cooperative effect against trophozoites and cysts of Acanthamoeba polyphaga. [Display omitted] Acanthamoeba sp. are the causative agents of severe illnesses in humans such as Acanthamoeba keratitis (AK) and granulomatous amoebic encephalitis (GAE). Medical therapy is not yet well established. Treatments of AK last for several months and generate toxicity, resistances appear due to the cysts stage and recurrences can occur. In this study has been demonstrated that the combination of chlorhexidine digluconate (CLX) and carbosilane dendrimers containing ammonium or guanidine moieties has in vitro synergistic effect against Acanthamoeba polyphaga. This synergy provokes an important reduction in the minimal trophozoite amoebicidal concentration (MTAC) of CLX, which means a reduction of their toxic effects on human cells. Moreover, some CLX/dendrimer combinations show important activity against the cyst resistance stage.