Export Ready — 

Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors

Bibliographic Details
Main Author: Conceição, Carlota J. F.
Publication Date: 2023
Other Authors: Moe, Elin, Ribeiro, Paulo A., Raposo, Maria
Format: Article
Language: eng
Source: Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
Download full: http://hdl.handle.net/10362/155160
Summary: Publisher Copyright: © 2023 by the authors.
id RCAP_a1668db475f31b88deeb6eca6eb57e07
oai_identifier_str oai:run.unl.pt:10362/155160
network_acronym_str RCAP
network_name_str Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
repository_id_str https://opendoar.ac.uk/repository/7160
spelling Liposome Formulations for the Strategic Delivery of PARP1 InhibitorsDevelopment and Optimizationcancer therapyliposomesNiraparibPARP1 inhibitorsRucaparibVeliparibChemical Engineering(all)Materials Science(all)SDG 3 - Good Health and Well-beingPublisher Copyright: © 2023 by the authors.The development of a lipid nano-delivery system was attempted for three specific poly (ADP-ribose) polymerase 1 (PARP1) inhibitors: Veliparib, Rucaparib, and Niraparib. Simple lipid and dual lipid formulations with 1,2-dipalmitoyl-sn-glycero-3-phospho-rac-(1′-glycerol) sodium salt (DPPG) and 1,2-dipalmitoyl-sn-glycero-3-phosphocoline (DPPC) were developed and tested following the thin-film method. DPPG-encapsulating inhibitors presented the best fit in terms of encapsulation efficiency (>40%, translates into concentrations as high as 100 µM), zeta potential values (below −30 mV), and population distribution (single population profile). The particle size of the main population of interest was ~130 nm in diameter. Kinetic release studies showed that DPPG-encapsulating PARP1 inhibitors present slower drug release rates than liposome control samples, and complex drug release mechanisms were identified. DPPG + Veliparib/Niraparib presented a combination of diffusion-controlled and non-Fickian diffusion, while anomalous and super case II transport was verified for DPPG + Rucaparib. Spectroscopic analysis revealed that PARP1 inhibitors interact with the DPPG lipid membrane, promoting membrane water displacement from hydration centers. A preferential membrane interaction with lipid carbonyl groups was observed through hydrogen bonding, where the inhibitors’ protonated amine groups may be the major players in the PARP1 inhibitor encapsulation mode.DF – Departamento de FísicaCeFITec – Centro de Física e Investigação TecnológicaLIBPhys-UNLInstituto de Tecnologia Química e Biológica António Xavier (ITQB)RUNConceição, Carlota J. F.Moe, ElinRibeiro, Paulo A.Raposo, Maria2023-07-12T22:17:08Z2023-05-112023-05-11T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article28application/pdfhttp://hdl.handle.net/10362/155160eng2079-4991PURE: 65461447https://doi.org/10.3390/nano13101613info:eu-repo/semantics/openAccessreponame:Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)instname:FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologiainstacron:RCAAP2024-05-22T18:12:48Zoai:run.unl.pt:10362/155160Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireinfo@rcaap.ptopendoar:https://opendoar.ac.uk/repository/71602025-05-28T17:43:26.824852Repositórios Científicos de Acesso Aberto de Portugal (RCAAP) - FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologiafalse
dc.title.none.fl_str_mv Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors
Development and Optimization
title Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors
spellingShingle Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors
Conceição, Carlota J. F.
cancer therapy
liposomes
Niraparib
PARP1 inhibitors
Rucaparib
Veliparib
Chemical Engineering(all)
Materials Science(all)
SDG 3 - Good Health and Well-being
title_short Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors
title_full Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors
title_fullStr Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors
title_full_unstemmed Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors
title_sort Liposome Formulations for the Strategic Delivery of PARP1 Inhibitors
author Conceição, Carlota J. F.
author_facet Conceição, Carlota J. F.
Moe, Elin
Ribeiro, Paulo A.
Raposo, Maria
author_role author
author2 Moe, Elin
Ribeiro, Paulo A.
Raposo, Maria
author2_role author
author
author
dc.contributor.none.fl_str_mv DF – Departamento de Física
CeFITec – Centro de Física e Investigação Tecnológica
LIBPhys-UNL
Instituto de Tecnologia Química e Biológica António Xavier (ITQB)
RUN
dc.contributor.author.fl_str_mv Conceição, Carlota J. F.
Moe, Elin
Ribeiro, Paulo A.
Raposo, Maria
dc.subject.por.fl_str_mv cancer therapy
liposomes
Niraparib
PARP1 inhibitors
Rucaparib
Veliparib
Chemical Engineering(all)
Materials Science(all)
SDG 3 - Good Health and Well-being
topic cancer therapy
liposomes
Niraparib
PARP1 inhibitors
Rucaparib
Veliparib
Chemical Engineering(all)
Materials Science(all)
SDG 3 - Good Health and Well-being
description Publisher Copyright: © 2023 by the authors.
publishDate 2023
dc.date.none.fl_str_mv 2023-07-12T22:17:08Z
2023-05-11
2023-05-11T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10362/155160
url http://hdl.handle.net/10362/155160
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 2079-4991
PURE: 65461447
https://doi.org/10.3390/nano13101613
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 28
application/pdf
dc.source.none.fl_str_mv reponame:Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
instname:FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologia
instacron:RCAAP
instname_str FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologia
instacron_str RCAAP
institution RCAAP
reponame_str Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
collection Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)
repository.name.fl_str_mv Repositórios Científicos de Acesso Aberto de Portugal (RCAAP) - FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologia
repository.mail.fl_str_mv info@rcaap.pt
_version_ 1833596916938571776

Similar Items