Synthesis of novel dendrimers having aspartate grafts and their ability to enhance the aqueous solubility of model drugs.
In this study, a series of aspartate based dendrimers with different cores were synthesized in a convergent approach and well characterized by NMR and MS techniques. The aqueous solubility of the model drugs (L-Histidine, Naproxen, Methotrexate) was measured in the presence of this kind of dendrimers at room temperature in PBS buffers at pH 6, 7 and 8. Results clearly confirmed that the solubility enhancement was due to presence of dendrimers at different pH compared to their corresponding aqueous solubility at different pH. The results indicated that the aspartate based dendrimers could be considered as an effective supplement of PAMAM dendrimers in solubility enhancement and drug delivery. The surface groups played an important role in dendrimer-mediated solubility enhancement.
Ouyang
Liang
L
Key Laboratory of Drug Targeting and Drug Delivery System of Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China.
Ma
Lifang
L
Jiang
Bo
B
Li
Yanhua
Y
He
Dongsheng
D
Guo
Li
L
D001224:Aspartic Acid / Q000737:chemistry*; D050091:Dendrimers / Q000138:chemical synthesis* / Q000737:chemistry*; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry; D006639:Histidine / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008727:Methotrexate / Q000737:chemistry; D009288:Naproxen / Q000737:chemistry; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D012995:Solubility; D013499:Surface Properties; D013696:Temperature; D014867:Water / Q000737:chemistry*
D050091:Dendrimers; D004337:Drug Carriers; D010455:Peptides; D004364:Pharmaceutical Preparations; D014867:Water; D001224:Aspartic Acid; D006639:Histidine; D009288:Naproxen; D008727:Methotrexate