In Vitro and In Vivo Evaluation of SP94 Modified Liposomes Loaded with N-14NCTDA, a Norcantharimide Derivative for Hepatocellular Carcinoma-Targeting.
AAPS PharmSciTech
; 21(7): 277, 2020 Oct 08.
Article
em En
| MEDLINE
| ID: mdl-33033942
ABSTRACT
The purpose of this research is to develop a liposomal drug delivery system, which can selectively target hepatocellular carcinoma (HCC) to deliver the antitumor agent N-14NCTDA, a C14 alkyl chain norcantharimide derivative of norcantharidin. N-14NCTDA-loaded liposomes were successfully prepared by lipid membrane hydration and extrusion methods. SP94, a targeting peptide for HCC cells, was attached to the liposomes loaded with N-14NCTDA by the post-insertion method to obtain SP94 modified liposomes (SP94-LPs). SP94-LPs had a significant cytotoxicity against Hep G2 cells with the IC50 of 15.395 ± 0.89 µg/mL, which is lower than that of NCTD-S (IC50 = 20.863 ± 0.56 µg/mL) and GAL-LPs (IC50 = 24.589 ± 1.02 µg/mL). Compared with conventional liposomes (Con-LPs), SP94-LPs showed greater cellular uptake in Hep G2 cells. Likewise, significant tumor suppression was achieved in H22 tumor-bearing mice which were treated with SP94-LPs. The tumor inhibition rate (IRw) of SP94-LPs was 82 ± 0.98%, obviously higher than that of GAL-LPs (69 ± 1.39%), Con-LPs (60 ± 2.78%), and NCTD-S (51 ± 3.67%). SP94-LPs exhibited a significant hepatocellular carcinoma-targeting activity in vitro and in vivo, which will provide a new alternative for hepatocellular carcinoma treatment in future. Graphical Abstract.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
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Sistemas de Liberação de Medicamentos
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Carcinoma Hepatocelular
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Compostos Bicíclicos Heterocíclicos com Pontes
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Lipossomos
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Neoplasias Hepáticas
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Antineoplásicos
Limite:
Animals
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Humans
Idioma:
En
Revista:
AAPS PharmSciTech
Assunto da revista:
FARMACOLOGIA
Ano de publicação:
2020
Tipo de documento:
Article