Molecules Manuscript
ID: prodrugs-20071204-Montenegro-it
Type of the paper: Review
Tentative Title:
The prodrug
approach: a strategy to improve drug skin permeation
Authors: L. Montenegro *, C. Carbone, G. Puglisi
Department of Pharmaceutical Sciences, University of Catania, V.le A.
Doria 6, 95125 Catania, Italy
E-mail:
[email protected]
Abstract: The skin is regarded as a valuable portal for drug delivery.
However, drug skin permeation is strongly limited by the formidable
barrier function of the skin and by the unsuitable physicochemical
properties of most drugs. Therefore many strategies have been proposed
to improve drug skin permeability such as the prodrug approach. The
prodrug concept involves the chemical modification of a drug into a
bioreversible form in order to change its pharmaceutical and
pharmacokinetic properties and thereby enhancing its skin permeation
and therapeutic efficacy. In this review prodrugs which have been
investigated to improve topical and transdermal drug delivery are
considered along with their potential applications in the
pharmaceutical field.
Molecules Manuscript ID: molecules-prodrugs-02-it-Rusnati
Type of the paper: Review
Tentative Title:
Polysulfated/Polysulfonated Compounds for the Development of Drugs at
the Crossroad of Tumor and Infectious Dideases
Authors: Chiara Urbinati, Paola Chiodelli, Marco Presta and Marco
Rusnati
Unit of General Pathology and Immunology, Department of Biomedical
Sciences and Biotechnology, School of Medicine, University of Brescia,
Italy
E-mail:
[email protected]
Abstract: Polyanionic compounds are an heterogeneous group of
synthetic, semisynthetic or natural molecules whose prototypes are
polysulfated heparin and polysulfonated suramin. Polyanionic compounds
can structurally vary for backbone structure and length and for
number and disposition of sulfated/sulfonated groups. Different
combinations of all these features confer to polyanionic compounds the
capacity to bind with a variable degree of specificity and affinity
many proteins such as enzymes, proteases, extracellular matrix
components, cytokines, chemokines, growth factors and their receptors.
Also, polyanionic compounds bind different components of pathogenic
microorganisms, mainly viruses. Polyanionic compounds mirror the
binding capacities of cell- or extracellular matrix-associated heparan
sulfate proteoglycans, that act indeed as receptors for many of the
proteins cited above. On these bases, polyanionic compounds have been
taken in considerations as inhibitors of different pathological
processes, in particular tumor growth, metastatization and
angiogenesis, infection, virus replication, leukocyte recruitment
and inflammation. Being some of these processes overlapping,
polyanionic compounds may act as multitarget drugs, thus able to
control a given disease by blocking different pathological processes
simultaneously. Here we discuss this possibility in light of the
available literature data.