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Prodrugs are pharmacological molecules that are administered in an inactive or significantly less active form. Once administered, the prodrug is metabolised in vivo into an active metabolite. Thus, prodrugs are molecules that must undergo biotransformation prior to exhibiting their therapeutic effects. Traditional prodrugs are classified in two main groups e.g. a first group of prodrugs that convert polar groups on active molecules into cleavable and apolar fragments and a second group that add solubility to the active moiety. The prodrugs, designed and developed so far by other academic and/or industrial players, are chemically modified in order to alter the chemical, physical and/or biochemical properties of the drug towards the average drug, being a quite lipophilic molecule but retaining sufficient solubility.
In contrast, SEPS Pharma chemically modifies existing drug substances to molecules that mimic the lipid components of the human daily food intake or to essential nutrition components, quite distinct from most drug substances but readily absorbed by the human body. Therefore, SEPS Pharma developed lipophilic prodrugs systems (LIPS) and self emulsifying prodrug systems (SEPS).
In comparison to self (micro) emulsifying drug delivery systems (SEDDS & SMEDDS), which are well known and commercially available but only applicable for lipophilic drug candidates, SEPS Pharma's self emulsifying prodrug systems serve solutions for both hydrophilic and lipophilic drugs. In addition, our novel prodrug systems are suitable to incorporate higher drug loads compared to S(M)EDDS.
SEPS Pharma's prodrug systems will be made with the aim of oral absorption, pulmonary delivery and sustained release after intramuscular injection. Oral adsorption of drug substances which are administered through intravenous, intramuscular or subcutaneous injection enhances its applications. In addition, pulmonary absorption is applied to prevent severe presystemic degradation, while sustained release after intramuscular injection decreases the number of daily doses, minimising variations in plasma/blood levels and improving patient compliance.
Lipophilic prodrug systems (LIPS) and self emulsifying prodrug systems (SEPS) are developed in order to: - Enhance bioavailability through
- Improving the solubility that may limit dissolution in the gastro-intestinal tract
- Increasing dissolution rate
- Improving permeability across biological membranes
- Control drug release
- Avoid the first-pass metabolism/presystemic metabolism via lymphatic absorption
Related to design and development of novel prodrug formulations SEPS Pharma performs:- Design and synthesis of lipophilic/self emulsifying prodrugs
- Testing chemical stability and solubility in gastrointestinal fluids and organic solvents
- In vitro/in vivo evaluation of synthetised prodrug
- Formulation development and optimalisation
- In vitro/in vivo evaluation of final formulation
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