Exquisite Vesicular Nanomedicine by Paclitaxel Mediated Co-assembly with Camptothecin Prodrug.
Angew Chem Int Ed Engl
; 60(38): 21033-21039, 2021 09 13.
Article
em En
| MEDLINE
| ID: mdl-34278702
ABSTRACT
We report that the self-assembly of drug amphiphiles, Evans blue conjugated camptothecin prodrug (EB-CPT), can be modulated by another anticancer drug paclitaxel (PTX), resulting in ultrahigh quality of nanovesicles (NVs) with uniform shape and diameters of around 80â
nm with the EB-CPTPTX weight ratio of 11, 12, and 13, denoted as ECX NVs. Significantly, the co-assembly of EB-CPT and PTX without adding other excipients has nearly 100 % drug loading efficiency (DLE) and ultrahigh drug loading content (DLC) of PTX alone of up to 72.3±1.7â
wt % which, to our best knowledge, is among the highest level reported in literature. Moreover, the ECX NVs with the EB-CPTPTX weight ratio of 12 showed remarkable combination index of 0.59 at a level of 50 % efficacy against HCT116 cells in vitro and greatly improved tumor inhibition effect in vivo compared with two clinically approved CPT- and PTX-based anticancer nanomedicines (Onivyde and Abraxane) individually and their combinations.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Camptotecina
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Pró-Fármacos
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Paclitaxel
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Nanomedicina
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Antineoplásicos Fitogênicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article