Objective(s): 4-aminosalicylic acid (4-ASA) is an isomer of mesalazine that has recently been shown to be effective against inflammatory bowel disease (IBD), and more specifically, ulcerative colitis. However, the majority of orally administered 4-ASA is readily and extensively absorbed from the stomach and small intestine, so only a small amount is transported to the ...

The molecular information that became available over the past two decades significantly influenced the field of drug design and delivery at large, and the prodrug approach in particular. While the traditional prodrug approach was aimed at altering various physiochemical parameters, e.g., lipophilicity and charge state, the modern approach to prodrug design considers molecular/cellular factors, ...

Acemetacin is the carboxymethyl ester of indomethacin and a pro-drug precursor compound, in other words, prodrug. The pharmacologically active metabolite acemetacin also indomethacin. exerts its potent non-steroidal anti-inflammatory effects body as It known that not only prodrug indomethacin, but an agent with gastric protective mechanisms, possibly involving reduction leukocyte adhesion, by e...

Effective chemotherapy remains a key issue for successful cancer treatment in general and neuroblastoma in particular. Here we report a chemotherapeutic strategy based on catalytic antibody-mediated prodrug activation. To study this approach in an animal model of neuroblastoma, we have synthesized prodrugs of etoposide, a drug widely used to treat this cancer in humans. The prodrug incorporates...

acrylic-type polymeric systems having degradable ester bonds linked to ibuprofen were synthesized and evaluated as materials for drug delivery. ibuprofen, as a non-steroidal anti-inflammatory drug, was linked to 2-hydroxyethyl methacrylate by activated ester methodology in one-pot procedure. the resulting methacrylic derivative of ibuprofen was copolymerized with 2-hydroxyethyl methacrylate and...

Bisphosphonates are used clinically to treat disorders of calcium metabolism and malignant bone disease and are known to inhibit cancer cell growth, adhesion, and invasion. However, clinical use of these agents for the treatment of extraskeletal disease is limited because of low cell permeability. We recently described a bisphosphonamidate prodrug strategy for efficient intracellular release of...

The term prodrug was first used by Albert [1]. Prodrug can be defined as an agent that is transformed after administration, either by metabolism or by spontaneous chemical breakdown, to form a pharmacologically active drug. The prodrug itself is inactive or less active and is converted to active agent in vivo. Targeted prodrug approach is one of the new trends in the treatment of cancer. A lot ...

A biodegradable and reduction-cleavable gemcitabine (GEM) polymeric prodrug with in vivo near-infrared (NIR) imaging ability was reported. This theranostic GEM prodrug PEG-b-[PLA-co-PMAC-graft-(IR820-co-GEM)] was synthesized by ring-opening polymerization and "click" reaction. The as-prepared reduction-sensitive prodrug could self-assemble into prodrug micelles in aqueous solution confirmed by ...