High dose Coenzyme Q10 oleogels designed for orphan therapy

Autores
Ehrenhaus Masotta, Natalia; Martinefski, Manuela Romina; Höcht, Christian; Lucangioli, Silvia Edith; Rojas, Ana Maria Luisa; Tripodi, Valeria Paula
Año de publicación
2018
Idioma
inglés
Tipo de recurso
documento de conferencia
Estado
versión publicada
Descripción
Recently, Coenzyme Q10 (CoQ10) was established by the FDA as an orphan drug and its therapeutic recommended dose increased significantly, reaching values up to 50 mg/kg/day. Patients with CoQ10 deficiency usually have swallowing difficulties, whereby the use of solid dosage forms is not the best option because they find them hard to swallow resulting in a lower adherence to the treatment. In order to satisfy the high-level requirements in adult patients and offer them a more comfortable way of treatment, a new oral CoQ10 dosage form was developed and evaluated. As CoQ10 is practically insoluble in aqueous solutions because of its lipophilic nature, oleogels were proposed to dose CoQ10. CoQ10 oleogels were prepared by its dissolution in medium-chain triglyceride (MCT) oil, using ethylcellulose for gelling and sorbitan monostearate (SMS) as surfactant. Physicochemical stability of oleogels was tested by their rheological properties, colorimetry, lipid oxidation, syneresis and remaining CoQ10 content during 12 months at 25.0°C. Pharmacokinetic profile was tested by a single-dose bioavailability study after oral intake of an oleogel containing 1g of CoQ10 and compared to the commercial capsule involving 7 healthy subjects. Thermoreversible oleogels with a maximal amount of 1 g of CoQ10 were developed with proved stability during at least 12 months of storage at 25.0°C. SMS allowed high stability to oxidation of the MCT-oil retained by the gel network, as well as low syneresis. Plastic deformation of oleogels without fracture was determined under compression, emulating the deformation behavior of the material into the oral cavity. Comparison of main pharmacokinetic parameters showed similar maximal concentration and half-life of CoQ10 after intake of both formulations and a non-significant increase in the area under the curve for the oleogel when compared with the commercial capsule. The use of these oleogels could promote the adherence to the treatment, ameliorating the discomfort perceived during swallowing by patients and could be a useful alternative for the treatment of adult patients with high CoQ10 requirements.
Fil: Ehrenhaus Masotta, Natalia. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina
Fil: Martinefski, Manuela Romina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Química Analítica y Fisicoquímica. Cátedra de Química Analítica; Argentina
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Lucangioli, Silvia Edith. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
Fil: Rojas, Ana Maria Luisa. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina
Fil: Tripodi, Valeria Paula. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
Drug Discovery for Neglected Diseases International Congress; 4th Scientific Meeting of the Research Network Natural Products against Neglected Diseases
Ciudad Autónoma de Buenos Aires
Argentina
Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Metabolismo del Fármaco
Materia
HIGH-DOSE COENZYME Q10
DYSPHAGIA
OLEOGEL
PHYSICOCHEMICAL STABILITY
PHARMACOKINETIC PROFILE
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/162956
Acceder
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network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling High dose Coenzyme Q10 oleogels designed for orphan therapyEhrenhaus Masotta, NataliaMartinefski, Manuela RominaHöcht, ChristianLucangioli, Silvia EdithRojas, Ana Maria LuisaTripodi, Valeria PaulaHIGH-DOSE COENZYME Q10DYSPHAGIAOLEOGELPHYSICOCHEMICAL STABILITYPHARMACOKINETIC PROFILEhttps://purl.org/becyt/ford/3.3https://purl.org/becyt/ford/3Recently, Coenzyme Q10 (CoQ10) was established by the FDA as an orphan drug and its therapeutic recommended dose increased significantly, reaching values up to 50 mg/kg/day. Patients with CoQ10 deficiency usually have swallowing difficulties, whereby the use of solid dosage forms is not the best option because they find them hard to swallow resulting in a lower adherence to the treatment. In order to satisfy the high-level requirements in adult patients and offer them a more comfortable way of treatment, a new oral CoQ10 dosage form was developed and evaluated. As CoQ10 is practically insoluble in aqueous solutions because of its lipophilic nature, oleogels were proposed to dose CoQ10. CoQ10 oleogels were prepared by its dissolution in medium-chain triglyceride (MCT) oil, using ethylcellulose for gelling and sorbitan monostearate (SMS) as surfactant. Physicochemical stability of oleogels was tested by their rheological properties, colorimetry, lipid oxidation, syneresis and remaining CoQ10 content during 12 months at 25.0°C. Pharmacokinetic profile was tested by a single-dose bioavailability study after oral intake of an oleogel containing 1g of CoQ10 and compared to the commercial capsule involving 7 healthy subjects. Thermoreversible oleogels with a maximal amount of 1 g of CoQ10 were developed with proved stability during at least 12 months of storage at 25.0°C. SMS allowed high stability to oxidation of the MCT-oil retained by the gel network, as well as low syneresis. Plastic deformation of oleogels without fracture was determined under compression, emulating the deformation behavior of the material into the oral cavity. Comparison of main pharmacokinetic parameters showed similar maximal concentration and half-life of CoQ10 after intake of both formulations and a non-significant increase in the area under the curve for the oleogel when compared with the commercial capsule. The use of these oleogels could promote the adherence to the treatment, ameliorating the discomfort perceived during swallowing by patients and could be a useful alternative for the treatment of adult patients with high CoQ10 requirements.Fil: Ehrenhaus Masotta, Natalia. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; ArgentinaFil: Martinefski, Manuela Romina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Química Analítica y Fisicoquímica. Cátedra de Química Analítica; ArgentinaFil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; ArgentinaFil: Lucangioli, Silvia Edith. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; ArgentinaFil: Rojas, Ana Maria Luisa. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; ArgentinaFil: Tripodi, Valeria Paula. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; ArgentinaDrug Discovery for Neglected Diseases International Congress; 4th Scientific Meeting of the Research Network Natural Products against Neglected DiseasesCiudad Autónoma de Buenos AiresArgentinaUniversidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Metabolismo del FármacoInstituto de la Química y Metabolismo del FármacoMoglioni, Albertina GladysSülsen, Valeria Patricia2018info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/conferenceObjectCongresoBookhttp://purl.org/coar/resource_type/c_5794info:ar-repo/semantics/documentoDeConferenciaapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/162956High dose Coenzyme Q10 oleogels designed for orphan therapy; Drug Discovery for Neglected Diseases International Congress; 4th Scientific Meeting of the Research Network Natural Products against Neglected Diseases; Ciudad Autónoma de Buenos Aires; Argentina; 2018; 185-186978-987-47034-0-8CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://iquimefa.conicet.gov.ar/libros-del-instituto/Internacionalinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:11:45Zoai:ri.conicet.gov.ar:11336/162956instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:11:45.819CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv High dose Coenzyme Q10 oleogels designed for orphan therapy
title High dose Coenzyme Q10 oleogels designed for orphan therapy
spellingShingle High dose Coenzyme Q10 oleogels designed for orphan therapy
Ehrenhaus Masotta, Natalia
HIGH-DOSE COENZYME Q10
DYSPHAGIA
OLEOGEL
PHYSICOCHEMICAL STABILITY
PHARMACOKINETIC PROFILE
title_short High dose Coenzyme Q10 oleogels designed for orphan therapy
title_full High dose Coenzyme Q10 oleogels designed for orphan therapy
title_fullStr High dose Coenzyme Q10 oleogels designed for orphan therapy
title_full_unstemmed High dose Coenzyme Q10 oleogels designed for orphan therapy
title_sort High dose Coenzyme Q10 oleogels designed for orphan therapy
dc.creator.none.fl_str_mv Ehrenhaus Masotta, Natalia
Martinefski, Manuela Romina
Höcht, Christian
Lucangioli, Silvia Edith
Rojas, Ana Maria Luisa
Tripodi, Valeria Paula
author Ehrenhaus Masotta, Natalia
author_facet Ehrenhaus Masotta, Natalia
Martinefski, Manuela Romina
Höcht, Christian
Lucangioli, Silvia Edith
Rojas, Ana Maria Luisa
Tripodi, Valeria Paula
author_role author
author2 Martinefski, Manuela Romina
Höcht, Christian
Lucangioli, Silvia Edith
Rojas, Ana Maria Luisa
Tripodi, Valeria Paula
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Moglioni, Albertina Gladys
Sülsen, Valeria Patricia
dc.subject.none.fl_str_mv HIGH-DOSE COENZYME Q10
DYSPHAGIA
OLEOGEL
PHYSICOCHEMICAL STABILITY
PHARMACOKINETIC PROFILE
topic HIGH-DOSE COENZYME Q10
DYSPHAGIA
OLEOGEL
PHYSICOCHEMICAL STABILITY
PHARMACOKINETIC PROFILE
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.3
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv Recently, Coenzyme Q10 (CoQ10) was established by the FDA as an orphan drug and its therapeutic recommended dose increased significantly, reaching values up to 50 mg/kg/day. Patients with CoQ10 deficiency usually have swallowing difficulties, whereby the use of solid dosage forms is not the best option because they find them hard to swallow resulting in a lower adherence to the treatment. In order to satisfy the high-level requirements in adult patients and offer them a more comfortable way of treatment, a new oral CoQ10 dosage form was developed and evaluated. As CoQ10 is practically insoluble in aqueous solutions because of its lipophilic nature, oleogels were proposed to dose CoQ10. CoQ10 oleogels were prepared by its dissolution in medium-chain triglyceride (MCT) oil, using ethylcellulose for gelling and sorbitan monostearate (SMS) as surfactant. Physicochemical stability of oleogels was tested by their rheological properties, colorimetry, lipid oxidation, syneresis and remaining CoQ10 content during 12 months at 25.0°C. Pharmacokinetic profile was tested by a single-dose bioavailability study after oral intake of an oleogel containing 1g of CoQ10 and compared to the commercial capsule involving 7 healthy subjects. Thermoreversible oleogels with a maximal amount of 1 g of CoQ10 were developed with proved stability during at least 12 months of storage at 25.0°C. SMS allowed high stability to oxidation of the MCT-oil retained by the gel network, as well as low syneresis. Plastic deformation of oleogels without fracture was determined under compression, emulating the deformation behavior of the material into the oral cavity. Comparison of main pharmacokinetic parameters showed similar maximal concentration and half-life of CoQ10 after intake of both formulations and a non-significant increase in the area under the curve for the oleogel when compared with the commercial capsule. The use of these oleogels could promote the adherence to the treatment, ameliorating the discomfort perceived during swallowing by patients and could be a useful alternative for the treatment of adult patients with high CoQ10 requirements.
Fil: Ehrenhaus Masotta, Natalia. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina
Fil: Martinefski, Manuela Romina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Química Analítica y Fisicoquímica. Cátedra de Química Analítica; Argentina
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Lucangioli, Silvia Edith. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
Fil: Rojas, Ana Maria Luisa. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina
Fil: Tripodi, Valeria Paula. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
Drug Discovery for Neglected Diseases International Congress; 4th Scientific Meeting of the Research Network Natural Products against Neglected Diseases
Ciudad Autónoma de Buenos Aires
Argentina
Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Metabolismo del Fármaco
description Recently, Coenzyme Q10 (CoQ10) was established by the FDA as an orphan drug and its therapeutic recommended dose increased significantly, reaching values up to 50 mg/kg/day. Patients with CoQ10 deficiency usually have swallowing difficulties, whereby the use of solid dosage forms is not the best option because they find them hard to swallow resulting in a lower adherence to the treatment. In order to satisfy the high-level requirements in adult patients and offer them a more comfortable way of treatment, a new oral CoQ10 dosage form was developed and evaluated. As CoQ10 is practically insoluble in aqueous solutions because of its lipophilic nature, oleogels were proposed to dose CoQ10. CoQ10 oleogels were prepared by its dissolution in medium-chain triglyceride (MCT) oil, using ethylcellulose for gelling and sorbitan monostearate (SMS) as surfactant. Physicochemical stability of oleogels was tested by their rheological properties, colorimetry, lipid oxidation, syneresis and remaining CoQ10 content during 12 months at 25.0°C. Pharmacokinetic profile was tested by a single-dose bioavailability study after oral intake of an oleogel containing 1g of CoQ10 and compared to the commercial capsule involving 7 healthy subjects. Thermoreversible oleogels with a maximal amount of 1 g of CoQ10 were developed with proved stability during at least 12 months of storage at 25.0°C. SMS allowed high stability to oxidation of the MCT-oil retained by the gel network, as well as low syneresis. Plastic deformation of oleogels without fracture was determined under compression, emulating the deformation behavior of the material into the oral cavity. Comparison of main pharmacokinetic parameters showed similar maximal concentration and half-life of CoQ10 after intake of both formulations and a non-significant increase in the area under the curve for the oleogel when compared with the commercial capsule. The use of these oleogels could promote the adherence to the treatment, ameliorating the discomfort perceived during swallowing by patients and could be a useful alternative for the treatment of adult patients with high CoQ10 requirements.
publishDate 2018
dc.date.none.fl_str_mv 2018
dc.type.none.fl_str_mv info:eu-repo/semantics/publishedVersion
info:eu-repo/semantics/conferenceObject
Congreso
Book
http://purl.org/coar/resource_type/c_5794
info:ar-repo/semantics/documentoDeConferencia
status_str publishedVersion
format conferenceObject
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/162956
High dose Coenzyme Q10 oleogels designed for orphan therapy; Drug Discovery for Neglected Diseases International Congress; 4th Scientific Meeting of the Research Network Natural Products against Neglected Diseases; Ciudad Autónoma de Buenos Aires; Argentina; 2018; 185-186
978-987-47034-0-8
CONICET Digital
CONICET
url http://hdl.handle.net/11336/162956
identifier_str_mv High dose Coenzyme Q10 oleogels designed for orphan therapy; Drug Discovery for Neglected Diseases International Congress; 4th Scientific Meeting of the Research Network Natural Products against Neglected Diseases; Ciudad Autónoma de Buenos Aires; Argentina; 2018; 185-186
978-987-47034-0-8
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://iquimefa.conicet.gov.ar/libros-del-instituto/
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
dc.coverage.none.fl_str_mv Internacional
dc.publisher.none.fl_str_mv Instituto de la Química y Metabolismo del Fármaco
publisher.none.fl_str_mv Instituto de la Química y Metabolismo del Fármaco
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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