期刊
出版社
ELSEVIER
DOI: 10.1016/j.msec.2020.110920
关键词
Amphiphilic chitosan derivatives; Pegylated chitosan; Acylated chitosan; Self-assembly; Camptothecin
资金
- Norte Portugal Regional Operational Programme (NORTE 2020) [NORTE-01-0145-FEDER-000012]
- COMPETE 2020 - Operacional Programme for Competitiveness and Internationalisation (POCI), under the PORTUGAL 2020 Partnership Agreement, through the FEDER - Fundo Europeu de Desenvolvimento Regional
- Portuguese funds through FCT Fundacao para a Ciencia e a Tecnologia/Ministerio da Ciencia, Tecnologia e Ensino Superior [UID/BIM/04293/2019]
- FCT [UID/FIS/04650/2019, POCI-01-0145-FEDER-032651]
- European Regional Development Fund (ERDF), through COMPETE 2020, under Portugal 2020
- FCT, Portugal [SFRH/BD/118721/2016, CEECIND/00814/2017, SFRH/BPD/120849/2016]
- Direccion General de Fondos Europeos
- FEDER [0245_IBEROS_1_E]
- i3S Scientific Platform Biointerfaces and Nanotechnology of the national infrastructure PPBI - Portuguese Platform of Bioimaging [PPBIPOCI-01-0145-FEDER-022122]
- Fundação para a Ciência e a Tecnologia [SFRH/BPD/120849/2016] Funding Source: FCT
Chitosan was grafted with O-methyl-O'-succinylpolyethylene glycol and oleic acid after a two-step carbodiimide coupling. The structural and physicochemical characterization of the compounds confirmed the successful conjugation of the hydrophilic and hydrophobic moieties to the chitosan backbone. The amphiphilic chitosan derivative obtained allowed the formation of polymeric micelles with an average size of 140 nm, a polydispersity index < 0.234, and a positive superficial charge. Camptothecin, used as a model hydrophobic drug, was successfully carried into the polymeric micelles with an encapsulation efficiency of 78%. The in vitro drug release was evaluated in simulated gastrointestinal fluids, exhibiting a low release of camptothecin in gastric media and a controlled release in intestinal fluids. Furthermore, it was demonstrated that chitosan micelles were able to stabilize camptothecin, protecting up to 75% of the drug from hydrolysis, preserving its active lactone form. This new chitosan amphiphilic system exhibits great potential to load hydrophobic drugs, acing as a promising delivery system.
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