Encapsulation of low lipophilic and slightly water-soluble dihydroartemisinin in PLGA nanoparticles with phospholipid to enhance encapsulation efficiency and in vitro bioactivity.
J Microencapsul
; 33(1): 43-52, 2016 Feb.
Article
em En
| MEDLINE
| ID: mdl-26626402
ABSTRACT
CONTEXT PLGA nanoparticles have been widely utilised to encapsulate lipophilic drugs for sustained release. OBJECTIVE:
This study was to enhance encapsulation efficiency and drug loading for the poorly lipophilic drug dihydroartemisinin (DHA) in PLGA nanoparticles, where amphiphilic phospholipid was employed as the intermediate. MATERIALS ANDMETHODS:
DHA-phospholipid complex formulation was optimised using the response surface method. DHA-phospholipid complex-nanoparticles (DHA-PLC-NPs) were prepared using the solvent evaporation method.RESULTS:
The particle size, zeta potential, entrapment efficiency and drug loading of the nanoparticles were 265.3 ± 7.9 nm, -21.4 ± 6.3 mV, 74.2 ± 6.5% and 2.80 ± 0.35%, respectively. Compared with the rapidly released free form, DHA underwent sustained release from the nanoparticles. DHA-PLC-NPs presented stronger cell proliferative inhibition than DHA treatment alone and apoptosis was obviously induced after DHA-PLC-NPs treatment.CONCLUSION:
Phospholipid complexes are useful intermediate to improve the lipophilicity of drugs, the interaction with the hydrophobic core of PLGA and the encapsulation efficiency of poorly lipophilic drugs in polymeric nanoparticles.Palavras-chave
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Base de dados:
MEDLINE
Assunto principal:
Fosfolipídeos
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Ácido Poliglicólico
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Portadores de Fármacos
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Ácido Láctico
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Artemisininas
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Nanopartículas
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article