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Novel approaches on prodrug based drug design

“…Since IBD patients undergo prolonged periods of treatment, prodrugs are considered as the most practical approach for targeting drugs to the colon in IBD patients. The three classes of prodrugs proven effective in IBD include: (1) anti-inflammatory agents (e.g., 5-ASA, azo prodrugs, amino acids) that can result from bacteria changing the function of prodrugs or prodrugs treating inflammation which changes the ecology of the bacteria, (2) immunomodulators and immunosuppressants, and (3) antioxidants. Improved drug delivery systems are required for drugs currently in use to treat localized diseases of the colon.…”

“…Conventional drugs suffer from many drawbacks in their performance. The shortcomings include high toxicity, chemical instability, inappropriate lipophilicity or hydrophilicity, deficient oral bioavailability, inappropriate pharmacokinetic or pharmacodynamic profiles, nonspecificity, high first-pass metabolism, and undesirable smell and taste [1]. The classical prodrug design often represents a nonspecific chemical approach to mask undesirable drug properties such as limited bioavailability, lack of site specificity and chemical instability.…”

Nanomedicines for Inflammatory Arthritis: Head-to-Head Comparison of Glucocorticoid-Containing Polymers, Micelles, and Liposomes

“…13-21 In addition, the N -(2-hydroxypropyl) methacrylamide (HPMA) copolymer-based prodrugs were found to be able to avert some side effects commonly associated with GC when compared to dose-equivalent regimens of the parent drug. 20 The application of liposomes as frontrunner carrier materials for the targeted delivery of GC is a logical one, in view of their clinical track record and their well-established characteristics ( e.g.…”

“…9 Consequently, it is reasonable to assume that the covalent coupling of drugs to long-circulating polymeric carriers may offer important advantages, if the linker chemistry employed enables optimally ‘tailored’ in vivo release kinetics. 13,16,22-25 …”

Synthesis and Pharmacology of Anti-Inflammatory Steroidal Antedrugs

“…Suppression on the hypothalamic-pituitary-adrenal (HPA) axis, the immune system, aggravation of diabetes, hypertension, osteoporosis, and retardation of growth in children are few of the most deleterious side effect 3–7. A considerable research effort has been devoted to the structural modifications of glucocorticoids, with a hope of increasing their potencies while minimizing their propensity to elicit systemic adverse effects, and some success had been evident in producing potent glucocorticoids with minimum salt-retaining activity 8–11.…”