Design, synthesis and in vitro evaluation of vinyl ether type polymeric prodrugs of ibuprofen, ketoprofen and naproxen

Long circulation and cytotoxicity of PEGylated gemcitabine and its potential for the treatment of pancreatic cancer

“…3 for pH 5.0 and 7.4 depicts the efficient release of gemcitabine from PEG mainly attributed to the cleavage of the amide bond. At pH 5, similar to endo-lysosomal environment, amide bond can be easily cleaved within a few minutes to free the drugs by various lysosomal enzymes whereas the bond might be accessible to hydrolysis since the polymers reach to a degree of swelling in alkaline medium, pH 7.4 (similar to blood circulation) [63]. The prolong availability of gemcitabine due to its release from polymer conjugate in blood plasma along with in vitro condition is an important parameter.…”

Naproxen glycine conjugate-synthesis, pharmaceutical preformulation and pharmacodynamic evaluation

“…Structural modification of naproxen by conjugation, with an amino acid is aimed to temporarily mask the carboxylic group that will contribute in increasing the hydrophilicity of poorly water soluble drug in addition to minimizing its side effects. Earlier reports on development of cyclodextrin prodrug (Kamel et al, 2008), amide prodrug (Babazadeh, 2008), naproxen-propyphenazone mutual prodrug (Sheha et al, 2002), ester prodrug (Rautio et al, 2000) of naproxen either do not aim at optimizing the drug molecule for its pharmaceutical limitations, for which this project has been undertaken.…”

Biodegradable Polyesters Containing Ibuprofen and Naproxen As Pendant Groups

“…1 When repeatedly administered, severe gastrointestinal side effects such as stomach ulceration, bleeding, and perforation occur because the drug is distributed throughout the body to targeted and non-targeted sites. 6,7, 8 Therefore, the therapeutic potentials of 1 and 2 could be significantly enhanced by incorporating them into controlled-delivery systems.…”

“…Acrylic and vinyl polymers have been widely studied to conjugate 1 or 2 onto the polymer backbones. 7, 8, 16-20 Although these polymers are biocompatible, they are not biodegradable. 21 Therefore, when the entire drug is released, the polymer would remain in the body which could cause patient discomfort and adverse effects.…”