Departamento: Departamento de Fármacos e Medicamentos
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Faculdade de Ciências Farmacêuticas
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Campus: Araraquara
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PublicaçãoCapítulo de livro Oral drug release systems based on pectin(2014-07-01) Cury, Beatriz Stringhetti Ferreira
; Meneguin, Andréia Bagliotti ; de Oliveira Cardoso, Valéria Maria ; Prezotti, Fabíola Garavello ; Universidade Estadual Paulista (Unesp) Pectin is a natural polysaccharide and its specific enzymatic degradability by colonic microbiota makes it a promising material for designing drug release systems, mainly those intended for targeting drugs to the colon. However, in despite of pectin resistance against proteases and amylases, remaining as aggregates of macromolecules in acid medium, a great challenge to optimize the performance of pectin in such systems lies in its high hydrophilicity that, in several times, results in an undesirable premature release of drugs. Blends of pectin with other polysaccharides and cross-linking reactions are valuable tools to modulate such properties of pectin, particularly reducing its solubility. These approaches have been focus of important researches of our research group and our findings have been published in important scientific journals. Blends of pectin and retrograded starch (RS) allowed the preparation of free films with suitable mechanical properties and reduced dissolution of films in acid media, while their high resistance against enzymatic digestion by pancreatin was demonstrated. The same polymer association was exploited for preparing tablets containing sodium diclofenac (SD), and the presence of pectin reduced significantly the drug dissolution in acid medium. In another study with free films, the blends of pectin-high amylose starch (HAS) crosslinked with sodium trimetaphosphate (STMP) contributed to the reduction of their hydrophilicity. This polymer association was also exploited for preparing hydrophilic matrices from which the drug release rates in acid medium were lowered. In addition, this same cross-linked HAS/pectin blend was employed for preparing microparticles loaded with SD by immersion and the mixtures containing the same proportion of polymers allowed a more effective control of drug release rates. Furthermore, microparticles obtained by physical mixture of polymers showed the lower percentage of drug released in acid medium and this behavior was attributed to the pectin that provides a diffusion layer of high viscosity that reduces the drug release rate. The association of pectin with gellan gum for preparing mucoadhesive beads by ionotropic gelation provided a pH dependent dissolution behavior, allowing reduced drug release rates in acid media. The purpose of this review is to evidence the importance of pectin as a carrier in the design of different drug release systems, aiming the targeting of drugs. Besides, the association of pectin with other polysaccharides and the cross-linking reaction are demonstrated to be reliable strategies to modulate the properties of the systems according to specific therapeutic needs.PublicaçãoCapítulo de livro Chagas disease pharmacotherapy and its chemical structure activity relationship(2017-01-01) Scarim, Cauê Benito; Chiba, Diego Eidy ; Bosquesi, Priscila Longhin ; dos Santos, Jean Leandro ; Chin, Chung Man ; Universidade Estadual Paulista (Unesp) Therapeutic arsenal currently available for Chagas disease is restricted in only two drugs, nifurtimox and benznidazole, since 1960s and 1970s, respectively. Despite the efforts to develop new drugs, until now, no new drugs were approved. This chapter describes the history of the two drugs used, as well as their mechanism of action, toxicity and relation-structure activity (SAR). In addition, the chapter addresses new therapies in clinical research, and those which are involved in programs (consortia) to develop new treatments for Chagas' disease.PublicaçãoCapítulo de livro Therapeutic targets in chagas disease(2017-01-01) Scarim, Cauê Benito; Chiba, Diego Eidy ; Chelucci, Rafael Consolin ; dos Santos, Jean Leandro ; Chin, Chung Man ; Universidade Estadual Paulista (Unesp) Optimal pharmacotherapy occurs when we have selectivity and no toxicity. The discovery of specific pathways or enzymes that are vital forcell or parasite survival is also vital for the design of new specific, non-toxic drugs for the treatment of cancer, microbial or parasitic diseases. This chapter describes the main validated therapeutic targets in the research of new drugs for the treatment of Chagas' disease, such as cysteine proteases, ergosterol metabolic pathways, thiol-dependent mechanisms (trypanothione reductase), glycolytic pathways, transsialidase enzymes, the transport and metabolism of polyamines, among others, as well as examples from the scientific literature. This also includes what is already in clinical trials that involves the specified targets.PublicaçãoCapítulo de livro General characteristics, main virulence markers and new approaches in the control of helicobacter pylori(2020-06-26) Camargo, Bruna Almeida Furquim de; Spósito, Larissa ; Souza, Maurício Palmeira Chaves De ; Ramos, Matheus Aparecido dos Santos ; Fortunato, Giovanna Capaldi ; Chorilli, Marlus ; Bauab, Taís Maria ; Universidade Estadual Paulista (UNESP) Helicobacter pylori is classified as a Gram-negative, spiral and microaerophilic bacterium and considered one of the most common causes of gastric infections worldwide. It was isolated from gastric biopsy specimens from patients with chronic gastritis and peptic ulcers in 1983. Thereafter, H. pylori has been associated with other severe gastrointestinal tract diseases, such as chronic gastritis, mucosal lymphoma associated with gastric marginal zone, and gastric carcinoma. Besides, this bacterium is associated with extra-gastric diseases such as esophageal and colon diseases, biliary and liver diseases, neurological disorders, autoimmune and rheumatological disorders among others. H. pylori infections are estimated to affect around 50% of the world's population and, frequently has been linked to all the gastric cancer cases reported worldwide, thus constituting a public health problem.PublicaçãoCapítulo de livro Functionalization of Nanosystems in Cancer Treatment(2022-01-01) Luiz, Marcela Tavares ; Dutra, Jessyca Aparecida Paes; De Araújo, Jennifer Thayanne Cavalcante ; Di Filippo, Leonardo Delello ; Duarte, Jonatas Lobato ; Chorilli, Marlus ; Universidade de São Paulo (USP) ; Universidade Estadual Paulista (UNESP) Cancer is the major public health problem worldwide, with high rates of incidence and lethality. The leak of specificity of the treatments currently available results in several side effects and reduced efficacy. Thus, nanosystems have demonstrated great potential for the delivery of chemotherapeutic agents to tumors due to their ability to passively accumulate in the tumor through enhanced permeability and retention (EPR) effect, to carry of hydrophilic and hydrophobic drugs, and to protect the drugs against degradation. In recent decades, advances in nanosystems design have expanded their therapeutic potential due to the inclusion of targeting ligands that can be specifically recognized by receptors overexpressed on tumor cells. Among these targeting ligands, antibodies, antibodies’ fragments, peptides, and small molecules have been widely incorporated in nanosystems for promoting the active targeting to the tumors. The modification of nanosystems with these ligands can be performed before or after nanosystems’ production through non-covalent or covalent functionalization, which can result in different biological activities. In this context, the present chapter aims to present some aspects of the synthesis employed to functionalize nanosystems. In addition, we address the main targeting ligands used for promoting the active targeting of nanosystems to different cancer cells, discussing the in vitro and in vivo results obtained for each functionalization.PublicaçãoCapítulo de livro Nanoparticles for cosmetic use and its application(2019-01-01) Chiari-Andréo, Bruna Galdorfini; De Almeida-Cincotto, Maria Gabriela José ; Oshiro, João Augusto ; Taniguchi, Cibele Yumi Yamada ; Chiavacci, Leila Aparecida ; Isaac, Vera Lucia Borges ; Universidade Estadual Paulista (Unesp) ; Araraquara University (UNIARA) Nanoparticles have been cited as a tool to solve many pharmaceutical problems, also in the cosmetic field. Some advantages in using them are to vectorize or retard the release and action of a cosmetic active substance, to increase stability, effectiveness, and safety, etc. However, there are many kinds of nanoparticles that should be chosen accordingly to the need of application. Although there are advantages related to the use of nanoparticles, some difficulties could be cited, such as the scale up of the technology and safety assessment. Considering the above, this chapter aimed to show the main kinds of nanoparticles employed in the cosmetic area, highlighting the advantages obtained with their use. Also, it will discuss the scale-up and the safety assessment, mainly in relation to the pathway followed by the nanoparticle when applied on the skin.PublicaçãoCapítulo de livro Nanotechnology for cosmetics applications—a journey in innovation(2022-01-01) Longo, João Paulo Figueiró ; Camargo, Nichollas Serafim ; Ferreira, Guilherme Alves ; Cardador, Camila Magalhães ; Corrêa, Marcos Antônio; University of Brasília ; Nanoceuticals Innovation Hub ; Universidade Estadual Paulista (UNESP) The cosmetic sector was one of the first industries that adopted nanotechnology in their products. During the 1980s, some European brands incorporated liposome nanocarriers in cosmetic products. Today, thousands of companies develop and use different nanotechnologies in the cosmetic sector. Moreover, due to this historical development, a number of applications for nanoparticles have been proposed at different stages of product development. In this chapter, we will present nanocosmetic activities as an innovative strategy to improve different areas of cosmetology, from the development of new ingredients to their applications in skin or hair-care products. The main benefits include active dispersion, protection of chemical instabilities, controlled release of active ingredients, and improved product effectiveness. The objective here is to present how nanotechnology affects cosmetic development in the technological journey from the conception of the product, moving through industrial production, and finally providing benefits for end users.