- Solubilization and anticancer-activity enhancement of Methotrexate by novel dendrimeric nanodevices synthesized in one-step reaction
-
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.
- Soto-Castro, Delia,Cruz-Morales, Jorge A.,Apan, Maria Teresa Ramirez,Guadarrama, Patricia
-
-
Read Online
- Antimicrobial efficacy of synthesized quaternary ammonium polyamidoamine dendrimers and dendritic polymer network
-
Water treatment to mitigate microbial contaminants is a major challenge across globe paving the way to develop novel antimicrobial compounds. We aim at architecting antibacterial moiety eventually catering to vast water treatment industry. In this research study, quaternary ammonium functionalized polyamidoamine (PAMAM) dendrimer and PAMAM-ethyleneglycol dimethacrylate (EGDMA) dendritic polymer network were synthesized. These materials were characterized by various analytical techniques like ATR-FTIR, 1HNMR, DSC etc. Water soluble generation (G) 1.0 PAMAM dendrimer and water insoluble PAMAM G1.0 EGDMA dendritic polymer network were quaternized by reacting with dilute hydrochloric acid (HCl) and octyl iodide (OI) respectively. Both quaternary ammonium dendrimer products were found to exhibit potent bactericidal activity against a group of common Gram-negative and Gram-positive bacteria. 10 mg/L concentration of liquid PAMAM G1.0 QHCl was efficient to kill 100% bacteria rapidly within an incubation time of just 2 minutes. In addition, quaternary ammonium dendritic polymer network PAMAM G1.0-EGDMA Q OI demonstrated good contact killing antimicrobial property without releasing any active molecule into the surrounding medium and disinfected contaminated water within 5 minutes. Both quaternary ammonium dendrimer and dendritic polymer network showed negligible cytotoxicity in MTT assay indicating their potential as a viable antimicrobial agent.
- Zainul Abid,Jackeray, Richa,Jain, Swati,Chattopadhyay, Sruti,Asif,Singh, Harpal
-
-
Read Online
- Solubility of nicotinic acid in polyamidoamine dendrimer solutions
-
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.
- Yiyun, Cheng,Tongwen, Xu
-
-
Read Online
- Evaluation of polyamidoamine (PAMAM) dendrimers as drug carriers of anti-bacterial drugs using sulfamethoxazole (SMZ) as a model drug
-
Sulfamethoxazole (SMZ), a sulfonamide with well-known anti-bacterial properties, is not freely soluble in water and causes problems in its clinical applications. In the present study we investigated the potential of ethylenediamine (EDA) core polyamidoamine (PAMAM) dendrimers as drug carriers of SMZ by aqueous solubility, in vitro release as well as anti-bacterial activity studies. Results showed that the aqueous solubility of SMZ was approximately proportional to dendrimer concentration (a 40-fold increase in solubility in 10 mg/ml G3 PAMAM dendrimer solutions compared with that in double-distilled water at 37 °C). The in vitro release of SMZ in the presence of PAMAM dendrimers was significantly slower compared to pure SMZ dissolved in ethanol. Microbiology studies showed that PAMAM dendrimers could increase the anti-bacterial activity of SMZ (a 4- or 8-fold increase in the anti-bacterial activity of SMZ in dendrimer solution compared to pure SMZ dissolved in dimethylsulfoxide (DMSO) or 0.01 M NaOH solution). The in vitro release behavior and anti-bacterial activity studies indicated that PAMAM dendrimers might be considered as potential drug carriers of sulfonamides with a sustained release behavior under suitable conditions.
- Ma, Minglu,Cheng, Yiyun,Xu, Zhenhua,Xu, Peng,Qu, Haiou,Fang, Yujie,Xu, Tongwen,Wen, Longping
-
-
Read Online
- Polyamidoamine dendrimers used as solubility enhancers of ketoprofen
-
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.
- Yiyun, Cheng,Tongwen, Xu,Rongqiang, Fu
-
-
Read Online
- Fabrication and characterization of dendrimer-encapsulated monometallic Co nanoparticles
-
A series of cobalt (Co) nanoparticles were synthesized by employing PAMAM dendrimers with different generations (G 0.0-3.0) as templates and sodium borohydride as a reducing agent. Extensive characterizations of the products were done using TEM, FT-IR, VSM, TGA, and XPS. The magnetization curves have superparamagnetic non hysteric characteristic at lower fields and with nonsaturation characteristic at high fields. All XRD patterns indicate that amorphous structure of all products. The shake-up satellites are observed at higher energies of the XPS peaks.
- Kavas,Durmus,Tanriverdi,?enel,Sozeri,Baykal
-
-
Read Online
- Development of microwave-assisted reactions for PAMAM dendrimer synthesis
-
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.
- Lopez-Andarias, Javier,Guerra, Javier,Castaneda, Gregorio,Merino, Sonia,Cena, Valentin,Sanchez-Verdu, Prado
-
-
Read Online
- Dendrimers as potential drug carriers; encapsulation of acidic hydrophobes within water soluble PAMAM derivatives
-
This paper describes the synthesis of three neutral water soluble poly(amidoamine) (PAMAM) dendrimer derivatives. The ability of the two larger dendrimers to bind small acidic hydrophobic molecules is reported. Spectroscopic data and pH behaviour suggested that the acidic hydrophobes were forming stable ion pairs with the dendrimer's internal, basic tertiary nitrogens. With respect to forming 1:1 and 2:1 substrate/dendrimer complexes, both of the larger dendrimers were equally efficient at binding. All dendrimer/substrate complexes were completely miscible with water in all proportions (i.e. infinitely water soluble). When the bound substrates are drug moieties, then the resulting complexes could be considered as potential drug delivery systems. Flow calorimetry demonstrated that the dendrimers were able to release their hydrophobic guests when in contact with a biological cell.
- Beezer,King,Martin,Mitchel,Twyman,Wain
-
-
Read Online
- Polyamidoamine (PAMAM) dendrimers as biocompatible carriers of quinolone antimicrobials: An in vitro study
-
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.
- Cheng, Yiyun,Qu, Haiou,Ma, Minglu,Xu, Zhenhua,Xu, Peng,Fang, Yujie,Xu, Tongwen
-
-
Read Online
- Modified PAMAM dendrimers as a matrix for the photostabilization of curcumin
-
Six recently synthesised poly(amidoamine) (PAMAM) dendrimers from zero, first and second generations modified with 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione (curcumin) and 2,4-dihydroxybenzophenone (CU-1, CU-2, CU-3, CU-4, CU-5 and CU-6) have been investigated in water/dioxane (4 : 1) (v/v) solution by absorption and fluorescence spectroscopy in order to determine their photostability. It has been found that the photostability of curcumin is enhanced upon its incorporation into the dendrimer molecule, and a new additional stabilization is achieved by bonding of 2,4-dihydroxybenzophenone as a UV absorber to the dendrimer molecule. It has also been established that the generation of dendrimers impacts upon this parameter as the photostabilizing effect enhances at a higher dendrimer generation. The photostability of the dendrimers has also been investigated after their deposition onto a polyethylene terephthalate (PET) fabric. This journal is
- Dodangeh, Mohammad,Grabchev, Ivo,Gharanjig, Kamaladin,Staneva, Desislava,Tang, Ren-Cheng,Sheridan, Matthew
-
-
Read Online
