Tecnologia Simples para Revolucionar a Absorção: Inovação ao Serviço do Desenvolvimento de Fármacos Desafiadores

The project aims to uncover the full potential of an innovative technology for the development of new drug products, particularly its bioavailability enhancing effect when delivering drugs that are challenging to translate into the market (promising drugs, yet with unfavorable physicochemical properties and/or metabolism that limit their administration, bioavailability, and efficacy in humans). In particular, we intend to validate the promotion of oral/mucosal bioavailability of lipophilic drugs with high hepatic first-pass metabolization and peptides/proteins by this technology. Three drugs were selected for this project: segesterone acetate (SA) and cannabidiol (CBD) as small drugs, and Pigment epithelium-derived factor [PEDF] (including its derived neurotrophic peptides) as a candidate therapeutic protein/peptides. Therefore, while validating the innovative technology, we expect to support the development of at least 3 potential novel medicines based on this technology, with indication in important unmet medical needs (stroke all 3, but also multiple sclerosis, epilepsy, cancer, among other diseases). Regarding SA, we have preliminary encouraging results, obtained in the unfavorable context of non-starved animals, which need to be confirmed and further optimized. In fact, these first results raised other important questions to be answered: Is our formula better than other lipid-based formulations due to the favorable characteristics of our innovative technology? Can we improve these results by using other versions of the innovative nanoemulsion? Can we use the nanoemulsion preconcentrate (self-emulsifying drug delivery system) instead of the formed nanoemulsion and can we convert it to a solid product? Can we achieve better control of the plasmatic levels of SA (eg. develop a novel prolonged release formulation of the nanoemulsion)? Can we promote the oral bioavailability of other drugs with high first-pass hepatic elimination? And of labile hydrophilic macromolecules like peptides and proteins? The project has a second important aim, which is to further innovate and improve the therapeutic strategy with these drugs by the development of prolonged release formulations and/or association of drugs to potentiate both the bioavailability and therapeutic effect of the previous drugs in stroke patients. It is also our aim to give particular attention to intellectual property protection from innovative solutions that may arise from this project, and actively contact potential institutions interested in collaborating in the translation of our technology.