Special Issue "Prodrugs"
A special issue of Pharmaceutics (ISSN 1999-4923).
Deadline for manuscript submissions: closed (28 February 2013).
This special issue will focus on prodrug strategies to address formulation, delivery, and toxicity limitations of drug molecules.
Prodrugs are pharmacological substances administered in an inactive (or less than fully active) form which are subsequently converted into active compounds through normal metabolic processes. The classical prodrug approach involves altering physico-chemical, biopharmaceutical or pharmacokinetic properties to maximize the amount of active drug reaching its site of action and this continues to be a useful strategy. Such approaches include increasing bioavailability (by optimization of aqueous solubility and lipophilicity) and influencing duration of pharmacological effects by increasing stability or decreasing first-pass effects. The prodrug approach can also be adopted to improve organoleptic properties and to improve how selectively the drug interacts with cells or processes that are not its intended target, reduces adverse or unintended side-effects.
Prodrug technologies are becoming more important for addressing undesirable properties associated with modern potential drugs and are being considered in the early stages of the drug development process. Computational approaches can consider using a design of linkers with drugs that have poor bioavailability to release the parental drugs in programmable manner and improve their bioavailability. Targeting approaches of coupling of low-molecular weight drugs to synthetic polymers such as PEG or serum proteins through a cleavable linker are also gaining popularity. Selective activation of prodrugs in tumour tissues can also be achieved using gene-directed enzyme prodrug therapy (GDEPT), virus-directed enzyme prodrug therapy (VDEPT), and antibody-directed enzyme prodrug therapy (ADEPT). Any of these aspects of prodrug design and application are welcome in this issue.
Prof. Dr. Barbara R. Conway
Manuscript Submission Information
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- drug release
- drug delivery
- physicochemical characteristics
- drug targeting
- oral administration
- tumour targeting
- drug delivery
- poly (ethylene glycol) prodrugs
- Monoclonal Antibody Drug Conjugates