Mapeamento tecnológico contendo silibinina e proposta de pré-formulação
Autor(a) principal: | |
---|---|
Data de Publicação: | 2023 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Repositório Institucional da UFS |
Texto Completo: | http://ri.ufs.br/jspui/handle/riufs/17285 |
Resumo: | 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. |
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Oliveira, Ana Maria SantosSerafini, Mairim RussoFrank, Luiza Abrahão2023-03-22T20:06:13Z2023-03-22T20:06:13Z2023-02-09OLIVEIRA, Ana Maria Santos. Mapeamento tecnológico contendo silibinina e proposta de pré-formulação. 2023. 53 f. Dissertação (Mestrado em Ciências Farmacêuticas) – Universidade Federal de Sergipe, São Cristóvão, 2023.http://ri.ufs.br/jspui/handle/riufs/17285Silibinin (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.A silibinina (SB) é um flavolignano que apresenta diversas atividades farmacológicas, como anti-inflamatória, citoprotetora, anti-carcionogênica e antioxidante. Diante dessas atividades, a SB pode ser considerada uma substância promissora para o desenvolvimento de produtos farmacêuticos. Entretanto, a SB apresenta algumas limitações, dentre elas a baixa solubilidade aquosa e, consequentemente, baixa biodisponibilidade. Dessa forma, o uso de tecnologias farmacêuticas para contornar essas limitações torna-se uma alternativa viável em prol da melhoria das propriedades físico-químicas mencionadas. Dentre as tecnologias mais utilizadas, destaca-se a nanotecnologia. Portanto, o objetivo deste trabalho foi mapear possíveis tecnologias farmacêuticas aplicadas a SB, por meio de depósitos de patentes e, em seguida, propor uma pré-formulação para a fotoproteção. A pesquisa foi realizada em duas bases de dados de patentes gratuitas, a WIPO e o Espacene, utilizando a palavra-chave ‘silibinin’, sem restrição de período temporal. No estudo de pré-formulação foi utilizada como nanotecnologia, as nanocápsulas poliméricas de SB (NP-SB) empregando como polímero a poli(εcaprolactona). Posterior a sua preparação foram analisadas quanto ao diâmetro médio, span, índice de polidispersão (PDI), potencial zeta (PZ), pH e teor de SB. Na revisão de patentes, após o processo de triagem e elegibilidade, 28 patentes foram selecionadas para análise, de acordo com o objetivo do estudo. Como resultados iniciais, o maior número de depósitos foi em 2016, já entre os países requerentes, a China obteve cerca de 85,71% (24) e dentre as entidades solicitantes, a indústria foi responsável por 13 patentes. Em relação as tecnologias empregadas, para o transporte e entrega de fármacos, estão as nanopartículas poliméricas, nanopartículas lipídicas, lipossomas, complexos fosfolipídicos, dispersão sólidas e microemulsão. Por fim, todas as patentes compararam a formulação proposta com a substância pura e os resultados mostraram aumento da solubilidade e biodisponibilidade da SB, quando associada essas tecnologias. No estudo de pré-formulação foi possível assegurar que as NP-SB obteve tamanho nanométrico de 161 ± 13,6 nm com span de 0,7 ± 0,2 nm e PDI de 0,22 ± 0,03 nm, indicando boa homogeneidade na distribuição do tamanho de partícula. Adicionalmente, as NP-SB apresentaram estabilidade (PZ = -28,16 +/- 2,5 mV), pH compatível com o da pele e um teor de 90,8%. Sendo assim, as tecnologias farmacêuticas são tendências promissoras para o desenvolvimento de novos medicamentos e cosméticos.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESSão CristóvãoporTecnologia farmacêuticaNanotecnologiaSilibininaPatentesSilibininPharmaceutical technologyPatentsNanotechnologyCIENCIAS BIOLOGICAS::FARMACOLOGIAMapeamento tecnológico contendo silibinina e proposta de pré-formulaçãoTechnological mapping containing silibinin and pre-formulation proposalinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisPós-Graduação em Ciências FarmacêuticasUniversidade Federal de Sergipereponame:Repositório Institucional da UFSinstname:Universidade Federal de Sergipe (UFS)instacron:UFSinfo:eu-repo/semantics/openAccessTEXTANA_MARIA_SANTOS_OLIVEIRA.pdf.txtANA_MARIA_SANTOS_OLIVEIRA.pdf.txtExtracted texttext/plain87236https://ri.ufs.br/jspui/bitstream/riufs/17285/3/ANA_MARIA_SANTOS_OLIVEIRA.pdf.txt3971ac9c01231da4d56a2e91d4fbb312MD53THUMBNAILANA_MARIA_SANTOS_OLIVEIRA.pdf.jpgANA_MARIA_SANTOS_OLIVEIRA.pdf.jpgGenerated Thumbnailimage/jpeg1224https://ri.ufs.br/jspui/bitstream/riufs/17285/4/ANA_MARIA_SANTOS_OLIVEIRA.pdf.jpgc1039248910d75955e243d8dc20e90aaMD54LICENSElicense.txtlicense.txttext/plain; charset=utf-81475https://ri.ufs.br/jspui/bitstream/riufs/17285/1/license.txt098cbbf65c2c15e1fb2e49c5d306a44cMD51ORIGINALANA_MARIA_SANTOS_OLIVEIRA.pdfANA_MARIA_SANTOS_OLIVEIRA.pdfapplication/pdf1156158https://ri.ufs.br/jspui/bitstream/riufs/17285/2/ANA_MARIA_SANTOS_OLIVEIRA.pdfbce48790b7aa3bb05e7831184f8c72b6MD52riufs/172852023-03-22 17:06:28.539oai:ufs.br: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Repositório InstitucionalPUBhttps://ri.ufs.br/oai/requestrepositorio@academico.ufs.bropendoar:2023-03-22T20:06:28Repositório Institucional da UFS - Universidade Federal de Sergipe (UFS)false |
dc.title.pt_BR.fl_str_mv |
Mapeamento tecnológico contendo silibinina e proposta de pré-formulação |
dc.title.alternative.eng.fl_str_mv |
Technological mapping containing silibinin and pre-formulation proposal |
title |
Mapeamento tecnológico contendo silibinina e proposta de pré-formulação |
spellingShingle |
Mapeamento tecnológico contendo silibinina e proposta de pré-formulação Oliveira, Ana Maria Santos Tecnologia farmacêutica Nanotecnologia Silibinina Patentes Silibinin Pharmaceutical technology Patents Nanotechnology CIENCIAS BIOLOGICAS::FARMACOLOGIA |
title_short |
Mapeamento tecnológico contendo silibinina e proposta de pré-formulação |
title_full |
Mapeamento tecnológico contendo silibinina e proposta de pré-formulação |
title_fullStr |
Mapeamento tecnológico contendo silibinina e proposta de pré-formulação |
title_full_unstemmed |
Mapeamento tecnológico contendo silibinina e proposta de pré-formulação |
title_sort |
Mapeamento tecnológico contendo silibinina e proposta de pré-formulação |
author |
Oliveira, Ana Maria Santos |
author_facet |
Oliveira, Ana Maria Santos |
author_role |
author |
dc.contributor.author.fl_str_mv |
Oliveira, Ana Maria Santos |
dc.contributor.advisor1.fl_str_mv |
Serafini, Mairim Russo |
dc.contributor.advisor-co1.fl_str_mv |
Frank, Luiza Abrahão |
contributor_str_mv |
Serafini, Mairim Russo Frank, Luiza Abrahão |
dc.subject.por.fl_str_mv |
Tecnologia farmacêutica Nanotecnologia Silibinina Patentes |
topic |
Tecnologia farmacêutica Nanotecnologia Silibinina Patentes Silibinin Pharmaceutical technology Patents Nanotechnology CIENCIAS BIOLOGICAS::FARMACOLOGIA |
dc.subject.eng.fl_str_mv |
Silibinin Pharmaceutical technology Patents Nanotechnology |
dc.subject.cnpq.fl_str_mv |
CIENCIAS BIOLOGICAS::FARMACOLOGIA |
description |
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. |
publishDate |
2023 |
dc.date.accessioned.fl_str_mv |
2023-03-22T20:06:13Z |
dc.date.available.fl_str_mv |
2023-03-22T20:06:13Z |
dc.date.issued.fl_str_mv |
2023-02-09 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/masterThesis |
format |
masterThesis |
status_str |
publishedVersion |
dc.identifier.citation.fl_str_mv |
OLIVEIRA, Ana Maria Santos. Mapeamento tecnológico contendo silibinina e proposta de pré-formulação. 2023. 53 f. Dissertação (Mestrado em Ciências Farmacêuticas) – Universidade Federal de Sergipe, São Cristóvão, 2023. |
dc.identifier.uri.fl_str_mv |
http://ri.ufs.br/jspui/handle/riufs/17285 |
identifier_str_mv |
OLIVEIRA, Ana Maria Santos. Mapeamento tecnológico contendo silibinina e proposta de pré-formulação. 2023. 53 f. Dissertação (Mestrado em Ciências Farmacêuticas) – Universidade Federal de Sergipe, São Cristóvão, 2023. |
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http://ri.ufs.br/jspui/handle/riufs/17285 |
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Pós-Graduação em Ciências Farmacêuticas |
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Universidade Federal de Sergipe |
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