The N-ethoxycarbonylmorpholine moiety was evaluated as a novel prodrug moiety for carboxylic acid containing drugs represented by diclofenac (1). Compound 2, the N-ethoxycarbonylmorpholine ester of diclofenac was synthesized and evaluated as a potential prodrug. The stability of the synthesized prodrug was evaluated in solutions of pH 1 and 7.4, and in plasma. The ester's half lives were found ...

Repeated injection of polyethyleneglycol-modified (PEGylated) liposomes causes a rapid clearance of them from the bloodstream, this phenomenon is called accelerated blood clearance (ABC). In the present study, we focused on the immune system responsible for the ABC phenomenon. PEGylated liposomes were preadministered to BALB/c mice and [(3)H]-labeled ones were then administered to them 3 days a...

A sterically stabilized paclitaxel-loaded liposome tailored to target human breast cancer cells was developed, thereby promoting the efficiency of intracellular delivery of paclitaxel through receptor-mediated endocytosis. Results indicated that the targeting moiety (thiolated Herceptin) was successfully coupled to the distal reactive maleimide terminus of the poly (ethylene glycol)-phospholipi...

Many therapeutic agents are manufactured and administered in prodrug forms. In this paper, a new classification system for prodrugs is proposed to provide useful information about where in the body a prodrug is converted to the active drug. In this system, prodrugs are classified into Type I or Type II and the respective Subtypes IA, IB, IIA, IIB or IIC based on their sites of conversion into t...

Frequent side effects of radical treatment modalities and the availability of novel diagnostics have raised the interest in focal therapies for localized prostate cancer. To improve the selectivity and therapeutic efficacy of such therapies, we developed a minimally invasive procedure based on a novel polymeric photosensitizer prodrug sensitive to urokinase-type plasminogen activator (uPA). The...

In light of the continued threat antimicrobial-resistant bacteria, new strategies to expand repertoire antimicrobial compounds are necessary. Prodrugs an underexploited strategy in this effort. Here, we report on enhanced activity a prodrug toward bacteria having enzyme capable its activation. A screen led us sulfurol ester antibiotic trans-3-(4-chlorobenzoyl)acrylic acid. An endogenous esteras...

pegylated polypropyleneimine (ppi) dendritic scaffold was used for the delivery of an anti-leukemic drug, imatinib. the current study evolves and emerges the use pegylated ppi dendritic scaffold for the delivery of this drug. in this imatinib was synthesized and loaded with pegylated ppi dendritic scaffold. parameters such as ft-ir, nmr, sem, drug release, dsc and hemolytictoxicity are required...

Pegylated or non-pegylated α-interferon are frequently used medications for the treatment of both chronic hepatitis B and chronic hepatitis C. Skin disorders, which are mainly comprised of eczematous dermatitis, are frequently seen during treatment with this drug. However, drug eruption or morbilliform eruptions due to interferons have been rarely reported so far. We herein describe a patient w...