Reformulation Challenge
A Biotech Company was looking for a reformulation of a protein with therapeutic activity for the healing of complex wounds. They were interested to have a novel drug delivery system integrating their protein, as potential medicine to treat topically complex wounds. The requirements for that included to encapsulate or conjugate the active with a nanocarrier which could enhance stability, activity and topical local action of the protein.
Our Proposal
Our scientists suggested to integrate the protein in DELOS nanovesicles stabilized in an aqueous-based formulation. This lipid-based nanocarrier was an excellent candidate to integrate efficiently the protein, enabling its vehiculization through the damaged skin and maintaining it protected from protease degradation in the proteolytic environment of chronic wounds. Besides, DELOS nanovesicles present an extraordinary colloidal stability, which favors the production of high quality pharmaceutical formulations.
our developed
solution
After a feasibility study in close collaboration with the Biotech Company the following goals where achieved:
- The therapeutic protein was integrated in DELOS nanovesicles with encapsulation efficiencies higher than 90%.
- Biological activity of the protein once encapsulated was not only maintained but also increased 3-fold in relation to that of free protein.
- Stability against protease action was clearly enhanced.
- Additional antimicrobial activity was added as new function of the reformulation, crucial to prevent wound infections.
After a pharmaceutical development project, additional goals have been achieved related to quality and scale-up of this nanoformulation as a new pharmaceutical intermediate:
- A preclinical prototype has been developed to carry out efficacy and toxicological regulatory invivo tests.
- Scale-up of the manufacturing process until pilot plant scale has been performed following a Quality by Design (QbD) approach.
- GMP compliant production has been defined.
Benefits obtained
1
A new re(nano)formulation has been developed with proved superior efficacy towards complex wound healing.
2
New nanomedicines for Diabetic Foot Ulcer and Venous Ulcer containing the reformulated protein will be ready to enter clinical testing in 2020.
3
Regulatory development pathway has been defined after receiving scientific advice from drug regulation agencies.
4