Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs

This thesis was devoted to the development of innovative oral delivery systems for two different molecules. In the first part, microparticles (MPs) based on xylan and Eudragit® S- 100 were produced and used to encapsulate 5-aminosalicylic acid for colon delivery. Xylan was extracted from corn cob...

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Autor principal: Silva, Acarilia Eduardo da
Outros Autores: http://lattes.cnpq.br/7417605022519087
Formato: doctoralThesis
Idioma:por
Publicado em: Universidade Federal do Rio Grande do Norte
Assuntos:
micropartículas poliméricas
sistemas lipídicos
liberação colônica
administração oral
xilana
ácido 5-aminosalicílico
anfotericina B
polymeric microparticles
lipid systems
colon delivery
oral administration
xylan
5-aminosalicylic acid
amphotericin B
CNPQ::CIENCIAS DA SAUDE
Endereço do item:https://repositorio.ufrn.br/jspui/handle/123456789/13309
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id ri-123456789-13309
record_format dspace
institution Repositório Institucional
collection RI - UFRN
language por
topic micropartículas poliméricas
sistemas lipídicos
liberação colônica
administração oral
xilana
ácido 5-aminosalicílico
anfotericina B
polymeric microparticles
lipid systems
colon delivery
oral administration
xylan
5-aminosalicylic acid
amphotericin B
CNPQ::CIENCIAS DA SAUDE
spellingShingle micropartículas poliméricas
sistemas lipídicos
liberação colônica
administração oral
xilana
ácido 5-aminosalicílico
anfotericina B
polymeric microparticles
lipid systems
colon delivery
oral administration
xylan
5-aminosalicylic acid
amphotericin B
CNPQ::CIENCIAS DA SAUDE
Silva, Acarilia Eduardo da
Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs
description This thesis was devoted to the development of innovative oral delivery systems for two different molecules. In the first part, microparticles (MPs) based on xylan and Eudragit® S- 100 were produced and used to encapsulate 5-aminosalicylic acid for colon delivery. Xylan was extracted from corn cobs and characterized in terms of its physicochemical, rheological and toxicological properties. The polymeric MPs were prepared by interfacial cross-linking polymerization and spray-drying and characterized for their morphology, mean size and distribution, thermal stability, crystallinity, entrapment efficiency and in vitro drug release. MPs with suitable physical characteristics and satisfactory yields were prepared by both methods, although the spray-dried systems showed higher thermal stability. In general, spraydried MPs would be preferable systems due to their thermal stability and absence of toxic agents used in their preparation. However, drug loading and release need to be optimized. In the second part of this thesis, oil-in-water microemulsions (O/W MEs) based on mediumchain triglycerides were formulated as drug carriers and solubility enhancers for amphotericin B (AmB). Phase diagrams were constructed using surfactant blends with hydrophiliclipophilic balance values between 9.7 and 14.4. The drug-free and drug-loaded MEs presented spherical non-aggregated droplets around 80 and 120 nm, respectively, and a low polydispersity index. The incorporation of AmB was high and depended on the volume fraction of the disperse phase. These MEs did not reduce the viability of J774.A1 macrophage-like cells for concentrations up to 25 μg/mL of AmB. Therefore, O/W MEs based on propylene glycol esters of caprylic acid may be considered as suitable delivery systems for AmB
author2 http://lattes.cnpq.br/7417605022519087
author_facet http://lattes.cnpq.br/7417605022519087
Silva, Acarilia Eduardo da
format doctoralThesis
author Silva, Acarilia Eduardo da
author_sort Silva, Acarilia Eduardo da
title Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs
title_short Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs
title_full Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs
title_fullStr Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs
title_full_unstemmed Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs
title_sort nanotechnological delivery systems for the oral administration of active molecules: polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs
publisher Universidade Federal do Rio Grande do Norte
publishDate 2014
url https://repositorio.ufrn.br/jspui/handle/123456789/13309
work_keys_str_mv AT silvaacariliaeduardoda nanotechnologicaldeliverysystemsfortheoraladministrationofactivemoleculespolymericmicroparticlesandmicroemulsionsappliedtoantiinflammatoryandantiinfectiousdrugs
_version_ 1773965508416110592
spelling ri-123456789-133092019-05-26T05:13:26Z Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs Silva, Acarilia Eduardo da http://lattes.cnpq.br/7417605022519087 http://lattes.cnpq.br/6907806915889763 Barratt, Gillian Saulnier, Patrick Legrand, Philippe Espuelas, Socorro micropartículas poliméricas sistemas lipídicos liberação colônica administração oral xilana ácido 5-aminosalicílico anfotericina B polymeric microparticles lipid systems colon delivery oral administration xylan 5-aminosalicylic acid amphotericin B CNPQ::CIENCIAS DA SAUDE This thesis was devoted to the development of innovative oral delivery systems for two different molecules. In the first part, microparticles (MPs) based on xylan and Eudragit® S- 100 were produced and used to encapsulate 5-aminosalicylic acid for colon delivery. Xylan was extracted from corn cobs and characterized in terms of its physicochemical, rheological and toxicological properties. The polymeric MPs were prepared by interfacial cross-linking polymerization and spray-drying and characterized for their morphology, mean size and distribution, thermal stability, crystallinity, entrapment efficiency and in vitro drug release. MPs with suitable physical characteristics and satisfactory yields were prepared by both methods, although the spray-dried systems showed higher thermal stability. In general, spraydried MPs would be preferable systems due to their thermal stability and absence of toxic agents used in their preparation. However, drug loading and release need to be optimized. In the second part of this thesis, oil-in-water microemulsions (O/W MEs) based on mediumchain triglycerides were formulated as drug carriers and solubility enhancers for amphotericin B (AmB). Phase diagrams were constructed using surfactant blends with hydrophiliclipophilic balance values between 9.7 and 14.4. The drug-free and drug-loaded MEs presented spherical non-aggregated droplets around 80 and 120 nm, respectively, and a low polydispersity index. The incorporation of AmB was high and depended on the volume fraction of the disperse phase. These MEs did not reduce the viability of J774.A1 macrophage-like cells for concentrations up to 25 μg/mL of AmB. Therefore, O/W MEs based on propylene glycol esters of caprylic acid may be considered as suitable delivery systems for AmB Conselho Nacional de Desenvolvimento Científico e Tecnológico Esta tese teve como objetivo o desenvolvimento de novos sistemas de liberação para duas moléculas distintas. Na primeira parte, micropartículas à base de xilana e Eudragit® S-100 foram produzidas para encapsular ácido 5-aminosalicílico visando à liberação cólonespecífica. A xilana foi extraída de sabugos de milho e caracterizada quanto às suas propriedades físico-químicas, reológicas e toxicológicas. Em seguida, dois métodos de microencapsulação foram utilizados: reticulação interfacial polimérica e secagem por aspersão. Os sistemas produzidos foram caracterizados quanto à morfologia, tamanho médio e distribuição, estabilidade térmica, cristalinidade, taxa de encapsulação e liberação do fármaco in vitro. Foram obtidas micropartículas com adequadas características físicas e rendimentos satisfatórios através dos dois métodos, embora os sistemas aspergidos tenham apresentado maior estabilidade térmica e sejam considerados mais interessantes devido a sua maior estabilidade térmica e ausência de agentes tóxicos. No entanto, ajustes precisam ser feitos para melhorar a encapsulação e liberação do fármaco. Na segunda parte, microemulsões do tipo óleo em água (MEs O/A) com base em triglicerídeos de cadeia média (MCT) foram produzidas visando ao carreamento de anfotericina B (AmB) e aumento da sua solubilidade. Foram obtidas MEs O/A sem e com AmB com gotículas em torno de 80 e 120 nm, respectivamente, e índices de polidispersão de 0,25 e 0,31, respectivamente. A taxa de incorporação da AmB foi alta e dependente do volume da fase dispersa. A viabilidade celular não foi afetada até 25 μg/mL da AmB. Portanto, MEs O/A a partir de MCT podem ser promissores sistemas de liberação para AmB 2014-12-17T14:13:48Z 2014-02-05 2014-12-17T14:13:48Z 2013-04-05 doctoralThesis SILVA, Acarilia Eduardo da. Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs. 2013. 186 f. Tese (Doutorado em Ciências da Saúde) - Universidade Federal do Rio Grande do Norte, Natal, 2013. https://repositorio.ufrn.br/jspui/handle/123456789/13309 por Acesso Aberto application/pdf application/pdf Universidade Federal do Rio Grande do Norte BR UFRN Programa de Pós-Graduação em Ciências da Saúde Ciências da Saúde

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