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Bis-MPA amphiphilic Janus dendrimers for camptothecin drug delivery

AutorLancelot, Alexandre; Claveria-Gimeno, Rafael; Abian, Olga ; Sierra, Teresa; Serrano, José Luis
Fecha de publicación2016
CitaciónEDEN5 (2016)
ResumenJanus dendrimers are composed of two dendritic blocks offering different and specific terminal groups. It is then possible to combine distinctive properties in one unique molecule in order to provoke a synergetic or an antagonist effect. Therefore, amphiphilic Janus dendrimers were synthesized combining a lipophilic dendron with a hydrophilic dendron. Such molecules can self-assemble in water. Among all the dendrimers, polyesters of 2,2-bis(hydroxymethyl)propionic acid (bis-MPA) are widely used in drug delivery as they are easy to synthesize, biocompatible and biodegradable. Camptothecin is a poorly water soluble antiviral cytotoxic drug sensible to water. The encapsulation of the drug inside amphiphilic Janus dendrimers would allow to increase the solubility of the drug in water, to protect it from hydrolysis and to reduce its cytotoxic side effect. Bis-MPA dendrons from 1st to 3rd generation were funcionalized at their periphery with glycine to form the hydrophilic block and with stearic acid (C17 chains) to form the lipophilic block. Afterwards, they were linked together with CuAAC to form a series of 4 amphiphilic Janus dendrimers with different Hydrophilic/Lipophilic Balances (HLB) and with different molecular weights. The Critical Aggregation Concentration in water was determined and the aggregates were studied by DLS and observed by TEM. They are biocompatible and do not present any antiviral activity. The influence of the size of the dendrimers and the HLB in the camptothecin encapsulation and the drug activity was studied by measuring the cytotoxicity, the antiviral activity and the release of the encapsulated drug. When HLB is too high, drug encapsulation is limited, and bigger lipophilic dendrons restrict the diffusion of the drug inside and outside the aggregates. Accordingly, three of the four dendrimers can effectively encapsulate the camptothecin using the solvent diffusion technique. This reduces camptothecin toxicity while its antiviral activity is maintained.
DescripciónResumen del trabajo presentado al V Encuentro sobre Dendrímeros, celebtrado en Zaragoza (España) del 25 al 26 de enero de 2016.
URIhttp://hdl.handle.net/10261/149037
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