dc.creator | Iglesias Blanco, Nieves | |
dc.creator | Galbis Fuster, Elsa | |
dc.creator | Díaz Blanco, Manuel Jesús | |
dc.creator | Paz Báñez, María Violante de | |
dc.creator | Galbis Pérez, Juan Antonio | |
dc.date.accessioned | 2024-01-26T08:27:27Z | |
dc.date.available | 2024-01-26T08:27:27Z | |
dc.date.issued | 2018-10-25 | |
dc.identifier.citation | Iglesias Blanco, N., Galbis Fuster, E., Díaz Blanco, M.J., Paz Báñez, M.V.d. y Galbis Pérez, J.A. (2018). Loading studies of the anticancer drug camptothecin into dual stimuli-sensitive nanoparticles. Stability scrutiny. International Journal of Pharmaceutics, 550 (1-2), 429-438. https://doi.org/10.1016/j.ijpharm.2018.08.026. | |
dc.identifier.issn | 0378-5173 | es |
dc.identifier.issn | 1873-3476 | es |
dc.identifier.uri | https://hdl.handle.net/11441/154044 | |
dc.description.abstract | In recent years, the preparation of valuable drug delivery systems (DDS) from self-assembled amphiphilic copolymers has attracted much attention since these nanomaterials provide new opportunities to solve problems
such as the lack of solubility in water of lipophilic drugs, improve their bioavailability, prolong their circulation
time and decrease the side effects associated with their administration. In the current study two types of biocompatible pH-responsive nanoparticles derived from poly(2-hydroxyethyl methacrylate) (pHEMA) have been
used as drug nano-carriers, being one of them core cross-linked to circumvent their instability upon dilution in
human fluids. The present paper deals with the optimization of the loading process of the labile, hydrophobic
and highly active anticancer drug, Camptothecin (CPT) into the nanoparticles with regard to four independent
variables: CPT/polymer ratio, sonication, temperature and loading time. Forty experiments were carried out and
a Box–Behnken experimental design was used to evaluate the significance of the independent variables related to
encapsulation efficiency and drug retention capacity. The enhanced drug loading and encapsulation efficiency
values (58% and > 92%, respectively) of CPT were achieved by the core cross-linked NPs in 2 h at 32 °C at CPT/
polymer ratio 1.5:1 w/w and 14 min of sonication. The optimized CPT-loaded NPs were studied by dynamic light
scattering and scanning electron microscopy, and an increase in size of the loaded-NP compared to the unloaded
counterparts was found. Other twenty experiments were conducted to study the enability to retain CPT into the
conjugates at different ionic strength values and times. The stability studies demonstrated that the core crosslinked nanocarriers displayed an excellent drug retention capacity (> 90%) at 25 °C for 15 days in every ionicstrength environments whereas the non-cross-linked ones were more stable at physiological ionic strength. The
optimized systems proved to be a major step forward to encapsulate and retain CPT in the NP nuclei, what makes
them ideal devices to control the delivery of CPT upon the triggered acidic conditions of solid tumors. | es |
dc.description.sponsorship | Ministerio de Economía y Competitividad de España - MAT2016-77345-C3-2-P | es |
dc.description.sponsorship | Junta de Andalucía - P12-FQM-1553 | es |
dc.format | application/pdf | es |
dc.format.extent | 10 p. | es |
dc.language.iso | eng | es |
dc.publisher | Elsevier | es |
dc.relation.ispartof | International Journal of Pharmaceutics, 550 (1-2), 429-438. | |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 Internacional | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.subject | Kinetic drug loading | es |
dc.subject | polyHEMA | es |
dc.subject | pH-responsive nanoparticles | es |
dc.subject | Drug delivery systems | es |
dc.subject | Anticancer therapy | es |
dc.subject | Core cross-linked nanoparticles | es |
dc.subject | Experimental design | es |
dc.title | Loading studies of the anticancer drug camptothecin into dual stimuli-sensitive nanoparticles. Stability scrutiny | es |
dc.type | info:eu-repo/semantics/article | es |
dc.type.version | info:eu-repo/semantics/acceptedVersion | es |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es |
dc.contributor.affiliation | Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica | es |
dc.relation.projectID | MAT2016-77345-C3-2-P | es |
dc.relation.projectID | P12-FQM-1553 | es |
dc.relation.publisherversion | https://doi.org/10.1016/j.ijpharm.2018.08.026 | es |
dc.identifier.doi | 10.1016/j.ijpharm.2018.08.026 | es |
dc.journaltitle | International Journal of Pharmaceutics | es |
dc.publication.volumen | 550 | es |
dc.publication.issue | 1-2 | es |
dc.publication.initialPage | 429 | es |
dc.publication.endPage | 438 | es |
dc.contributor.funder | Ministerio de Economía y Competitividad (MINECO). España | es |
dc.contributor.funder | Junta de Andalucía | es |