142986-44-5Relevant articles and documents
Solubilization and anticancer-activity enhancement of Methotrexate by novel dendrimeric nanodevices synthesized in one-step reaction
Soto-Castro, Delia,Cruz-Morales, Jorge A.,Apan, Maria Teresa Ramirez,Guadarrama, Patricia
, p. 13 - 21 (2012)
The one-step synthesis of nanodevices based on PAMAM framework for targeted cancer therapy is described. Four water-soluble nanodevices (named fractions F1 to F4) were rightly separated by size discrimination, and characterized. From biological assays of cell growth inhibition percentage, the anticancer activity of Methotrexate (chemotherapeutic drug) as part of a nanodevice, generally increases over cancer cell lines and notably, in case of human lymphocytes, the cell growth inhibition percentage decreases drastically (more than 80%), thus, the nanodevices exhibited a favorable discrimination between healthy and diseased cells. From the characterization it can be conclude that the synthesized nanodevices provide a dual scenario of drug transportation: encapsulation and conjugation.
Solubility of nicotinic acid in polyamidoamine dendrimer solutions
Yiyun, Cheng,Tongwen, Xu
, p. 1384 - 1389 (2005)
In the present study we investigated the effect of ethylenediamine (EDA) core polyamidoamine (PAMAM) dendrimers on the aqueous solubility of nicotinic acid. The aqueous solubility of nicotinic acid was measured in the presence of dendrimers at room temperature in distilled water. The effect of variables, such as pH condition, concentration, surface functional group and generation (molecule size) of dendrimer, has been investigated. Results showed that the solubility of nicotinic acid in the dendrimer solutions was proportional to dendrimer concentration, both amine and ester-terminated dendrimers caused the higher increase in nicotinic acid solubility at higher pH conditions. The order in which the dendrimers increased the solubility at a constant pH condition was G4 > G3 > G2 > G1. In addition, at each pH, the solubility of nicotinic acid was greater in the presence of amine-terminated dendrimers compared to the amine ester-terminated dendrimers possessing the same number of surface functional groups. Under suitable conditions PAMAM dendrimers can be highly effective used to enhance the solubility of nicotinic acid.
Polyamidoamine dendrimers used as solubility enhancers of ketoprofen
Yiyun, Cheng,Tongwen, Xu,Rongqiang, Fu
, p. 1390 - 1393 (2005)
Ketoprofen is a non-steroidal anti-inflammatory drug which is not freely soluble in water and creates gastrointestinal problems. In the present study we investigated the potential of polyamidoamine (PAMAM) dendrimers to increase the solubility of ketoprofen. The effect of variables, such as pH condition, concentration and generation of dendrimer, has been investigated. The experimental results showed that the solubility of ketoprofen in the dendrimer solutions was proportional to dendrimer concentration. Under suitable conditions PAMAM dendrimers can be highly effective used to enhance the solubility of ketoprofen.
Development of microwave-assisted reactions for PAMAM dendrimer synthesis
Lopez-Andarias, Javier,Guerra, Javier,Castaneda, Gregorio,Merino, Sonia,Cena, Valentin,Sanchez-Verdu, Prado
, p. 2331 - 2337 (2012)
PAMAM dendrimers up to G1 have been synthesized by the divergent method taking advantage of microwave irradiation and using the CoolMateTM accessory to avoid high temperatures and long reaction times, which usually lead to defects in the dendrimer structure. Two tools have been successfully used to determine the purity of the products in addition to NMR spectroscopy, namely MALDI-TOF mass spectrometry and capillary-zone electrophoresis. These techniques show that the dendrimers were obtained in good yields, high purity, and with near-perfect regioselectivity. Molecular engineering on a nanoscale level to produce PAMAM dendrimers that can be used as drugs requires the use of technologies that lead to highly defined products. PAMAM synthesis can be assisted by microwave irradiation at low temperature to reduce the reaction time significantly while reducing the occurrence of defects in the PAMAM skeleton.
Polyamidoamine (PAMAM) dendrimers as biocompatible carriers of quinolone antimicrobials: An in vitro study
Cheng, Yiyun,Qu, Haiou,Ma, Minglu,Xu, Zhenhua,Xu, Peng,Fang, Yujie,Xu, Tongwen
, p. 1032 - 1038 (2007)
Quinolones, an expanding class of clinically established potent antibiotics, is not freely soluble in water which prevents the design of liquid dosage forms and restricts their use in topical applications. In the present study we investigated the potential of polyamidoamine (PAMAM) dendrimers as drug carriers of quinolones (nadifloxacin and prulifloxacin) by aqueous solubility and antibacterial activity studies. Results showed that the aqueous solubility of nadifloxacin and prulifloxacin was significantly increased by PAMAM dendrimers. Microbiology studies showed that nadifloxacin and prulifloxacin still exhibit their strong antimicrobial activities in the presence of dendrimers. These studies indicated that PAMAM dendrimers might be considered as biocompatible carriers of quinolones under suitable conditions.
