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Encapsulation of low lipophilic and slightly water-soluble dihydroartemisinin in PLGA nanoparticles with phospholipid to enhance encapsulation efficiency and in vitro bioactivity
Wang L.2; Wang Y.2; Wang X.1; Sun L.2; Zhou Z.2; Lu J.2; Zheng Y.2
2016-01-02
Source PublicationJournal of Microencapsulation
ISSN14645246 02652048
Volume33Issue:1Pages:43-52
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 and methods: 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.

KeywordCancer Encapsulation Nanoparticle Phospholipids Plga
DOI10.3109/02652048.2015.1114042
URLView the original
Indexed BySCI
WOS Research AreaChemistry ; Engineering ; Pharmacology & Pharmacy
WOS SubjectChemistry, Applied ; Engineering, Chemical ; Pharmacology & Pharmacy
WOS IDWOS:000371816700004
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Cited Times [WOS]:7   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Peking University
2.Universidade de Macau
Recommended Citation
GB/T 7714
Wang L.,Wang Y.,Wang X.,et al. Encapsulation of low lipophilic and slightly water-soluble dihydroartemisinin in PLGA nanoparticles with phospholipid to enhance encapsulation efficiency and in vitro bioactivity[J]. Journal of Microencapsulation,2016,33(1):43-52.
APA Wang L..,Wang Y..,Wang X..,Sun L..,Zhou Z..,...&Zheng Y..(2016).Encapsulation of low lipophilic and slightly water-soluble dihydroartemisinin in PLGA nanoparticles with phospholipid to enhance encapsulation efficiency and in vitro bioactivity.Journal of Microencapsulation,33(1),43-52.
MLA Wang L.,et al."Encapsulation of low lipophilic and slightly water-soluble dihydroartemisinin in PLGA nanoparticles with phospholipid to enhance encapsulation efficiency and in vitro bioactivity".Journal of Microencapsulation 33.1(2016):43-52.
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