Comparative Assessment of Active Targeted Redox Sensitive Polymersomes Based on pPEGMA-S-S-PLA Diblock Copolymer with Marketed Nanoformulation.
Biomacromolecules
; 19(7): 2549-2566, 2018 07 09.
Article
em En
| MEDLINE
| ID: mdl-29648799
ABSTRACT
In the present work, polymersomes based on self-assembled, folate-targeted, redox-responsive, ATRP-based amphiphilic diblock copolymer poly(polyethylene glycol)-S-S-polylactide with disulfide linkage were developed for efficient doxorubicin (DOX) delivery and compared with marketed DOXIL nanoformulation. The polymersomes formulation was optimized by quality by design approach providing monodisperse nanostructures of â¼110 nm and enhanced DOX loading of â¼20%. Polymersomes showed excellent stability as per the ICH guidelines over the extended storage period of 3 months. The in vitro drug release profile confirmed the redox sensitive behavior of polymersomes providing â¼80% drug release in endosomal pH 5 with 10 mmol GSH as compared to â¼20% release at pH 7.4. The targeted polymersomes achieved enhanced cellular internalization in folate receptor overexpressing cell lines, MDA-MB-231 and HeLa, providing â¼24% higher tumor reduction than DOXIL in Ehrlich ascites tumor bearing Swiss albino mice.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Poliésteres
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Ácidos Polimetacrílicos
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Doxorrubicina
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Lipossomos
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Antineoplásicos
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
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Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article