Mapeamento tecnológico contendo silibinina e proposta de pré-formulação

Abstract

Silibinin (SB) is a flavolignan with several pharmacological activities, such as antiinflammatory, cytoprotective, anti-carcinogenic, and antioxidant. Given these activities, SB can be considered a promising substance for pharmaceutical products development. However, BS has some limitations, including low aqueous solubility, consequently, low bioavailability. Thus, pharmaceutical technologies have been used to circumvent these limitations and become a viable alternative to improve the physical-chemical properties mentioned, and among the most used technologies, nanotechnology stands out. Therefore, the objective of this work was to map possible pharmaceutical technologies applied to BS through patent deposits and then propose a pre-formulation for photoprotection. The search was carried out in two free patent databases, the WIPO and the Espacenet, using the keyword 'silibinin' without restriction of the time period. In the pre-formulation study, SB polymeric nanocapsules (NP-SB) were used as nanotechnology, using poly(ε-caprolactone) as polymer. After their preparation, they were analyzed for mean diameter, span, polydispersion index (PDI), zeta potential (PZ), pH, and SB content. In the patent review, after the screening and eligibility process, 28 patents were selected for analysis, according to the purpose of the study. As initial results, the higher number of deposits was in 2016, already among the applicant countries, China obtained about 85.71% (24), and among the requesting entities, the industry was responsible for 13 patents. Regarding the technologies used for the transport and delivery of drugs, there are polymeric nanoparticles, lipid nanoparticles, liposomes, phospholipid complexes, solid dispersion and microemulsion. Finally, all patents compared the proposed formulation with the pure substance, and the results showed an increase in the solubility and bioavailability of SB when associated with these technologies. In the pre-formulation study, it was possible to ensure that the NP-SB obtained a nanometric size of 161 ± 13.6 nm with a span of 0.7 ± 0.2 nm and PDI of 0.22 ± 0.03 nm, indicating good homogeneity in the particle size distribution. Additionally, the NP-SB showed stability (PZ = -28.16 +/- 2.5 mV), pH compatible with the skin and a content of 90.8%. Thus, pharmaceutical technologies are promising trends for the development of new drugs and cosmetics.