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- Publisher Website: 10.1016/j.ejps.2017.02.001
- Scopus: eid_2-s2.0-85014004341
- PMID: 28163163
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Article: Mixed micelles of lipoic acid-chitosan-poly(ethylene glycol) and distearoylphosphatidylethanolamine-poly(ethylene glycol) for tumor delivery
Title | Mixed micelles of lipoic acid-chitosan-poly(ethylene glycol) and distearoylphosphatidylethanolamine-poly(ethylene glycol) for tumor delivery |
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Authors | |
Keywords | Biodistribution Cancer Chitosan DSPE-PEG Hydrophobic drug Mixed micelles Uptake |
Issue Date | 2017 |
Citation | European Journal of Pharmaceutical Sciences, 2017, v. 101, p. 228-242 How to Cite? |
Abstract | Many chemotherapeutics suffer from poor aqueous solubility and tissue selectivity. Distearoylphosphatidylethanolamine-poly(ethylene glycol) (DSPE-PEG) micelles are a promising formulation strategy for the delivery of hydrophobic anticancer drugs. However, storage and in vivo instability restrict their use. The aim of this study was to prepare mixed micelles, containing a novel polymer, lipoic acid-chitosan-poly(ethylene glycol) (LACPEG), and DSPE-PEG, to overcome these limitations and potentially increase cancer cell internalisation. Drug-loaded micelles were prepared with a model tyrosine kinase inhibitor and characterized for size, surface charge, stability, morphology, drug entrapment efficiency, cell viability (A549 and PC-9 cell lines), in vivo biodistribution, ex vivo tumor accumulation and cellular internalisation. Micelles of size 30–130 nm with entrapment efficiencies of 46–81% were prepared. LACPEG/DSPE-PEG mixed micelles showed greater interaction with the drug (condensing to half their size following entrapment), greater stability, and a safer profile in vitro compared to DSPE-PEG micelles. LACPEG/DSPE-PEG and DSPE-PEG micelles had similar entrapment efficiencies and in vivo tumor accumulation levels, but LACPEG/DSPE-PEG micelles showed higher tumor cell internalisation. Collectively, these findings suggest that LACPEG/DSPE-PEG mixed micelles provide a promising platform for tumor delivery of hydrophobic drugs. |
Persistent Identifier | http://hdl.handle.net/10722/349168 |
ISSN | 2023 Impact Factor: 4.3 2023 SCImago Journal Rankings: 0.752 |
DC Field | Value | Language |
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dc.contributor.author | Elsaid, Zeeneh | - |
dc.contributor.author | Taylor, Kevin M.G. | - |
dc.contributor.author | Puri, Sanyogitta | - |
dc.contributor.author | Eberlein, Cath A. | - |
dc.contributor.author | Al-Jamal, Khuloud | - |
dc.contributor.author | Bai, Jie | - |
dc.contributor.author | Klippstein, Rebecca | - |
dc.contributor.author | Wang, Julie Tzu Wen | - |
dc.contributor.author | Forbes, Ben | - |
dc.contributor.author | Chana, Jasminder | - |
dc.contributor.author | Somavarapu, Satyanarayana | - |
dc.date.accessioned | 2024-10-17T06:56:43Z | - |
dc.date.available | 2024-10-17T06:56:43Z | - |
dc.date.issued | 2017 | - |
dc.identifier.citation | European Journal of Pharmaceutical Sciences, 2017, v. 101, p. 228-242 | - |
dc.identifier.issn | 0928-0987 | - |
dc.identifier.uri | http://hdl.handle.net/10722/349168 | - |
dc.description.abstract | Many chemotherapeutics suffer from poor aqueous solubility and tissue selectivity. Distearoylphosphatidylethanolamine-poly(ethylene glycol) (DSPE-PEG) micelles are a promising formulation strategy for the delivery of hydrophobic anticancer drugs. However, storage and in vivo instability restrict their use. The aim of this study was to prepare mixed micelles, containing a novel polymer, lipoic acid-chitosan-poly(ethylene glycol) (LACPEG), and DSPE-PEG, to overcome these limitations and potentially increase cancer cell internalisation. Drug-loaded micelles were prepared with a model tyrosine kinase inhibitor and characterized for size, surface charge, stability, morphology, drug entrapment efficiency, cell viability (A549 and PC-9 cell lines), in vivo biodistribution, ex vivo tumor accumulation and cellular internalisation. Micelles of size 30–130 nm with entrapment efficiencies of 46–81% were prepared. LACPEG/DSPE-PEG mixed micelles showed greater interaction with the drug (condensing to half their size following entrapment), greater stability, and a safer profile in vitro compared to DSPE-PEG micelles. LACPEG/DSPE-PEG and DSPE-PEG micelles had similar entrapment efficiencies and in vivo tumor accumulation levels, but LACPEG/DSPE-PEG micelles showed higher tumor cell internalisation. Collectively, these findings suggest that LACPEG/DSPE-PEG mixed micelles provide a promising platform for tumor delivery of hydrophobic drugs. | - |
dc.language | eng | - |
dc.relation.ispartof | European Journal of Pharmaceutical Sciences | - |
dc.subject | Biodistribution | - |
dc.subject | Cancer | - |
dc.subject | Chitosan | - |
dc.subject | DSPE-PEG | - |
dc.subject | Hydrophobic drug | - |
dc.subject | Mixed micelles | - |
dc.subject | Uptake | - |
dc.title | Mixed micelles of lipoic acid-chitosan-poly(ethylene glycol) and distearoylphosphatidylethanolamine-poly(ethylene glycol) for tumor delivery | - |
dc.type | Article | - |
dc.description.nature | link_to_subscribed_fulltext | - |
dc.identifier.doi | 10.1016/j.ejps.2017.02.001 | - |
dc.identifier.pmid | 28163163 | - |
dc.identifier.scopus | eid_2-s2.0-85014004341 | - |
dc.identifier.volume | 101 | - |
dc.identifier.spage | 228 | - |
dc.identifier.epage | 242 | - |
dc.identifier.eissn | 1879-0720 | - |