ArticlePharmaceutical research2005
Enhanced intracellular uptake of sterically stabilized liposomal Doxorubicin in vitro resulting in improved antitumor activity in vivo.
Article in Pharmaceutical research, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 71 citations in OpenAlex.
- Intratumoral Pi deprivation benefits chemoembolization therapy via increased accumulation of intracellular doxorubicin.Drug delivery · 2022Article
- Review
- Tumor gene therapy by systemic delivery of plasmid DNA with cell-penetrating peptides.FASEB bioAdvances · 2019Article
- Application of pharmacokinetic and pharmacodynamic analysis to the development of liposomal formulations for oncology.Pharmaceutics · 2014Article
- Improved efficacy and reduced toxicity of doxorubicin encapsulated in sulfatide-containing nanoliposome in a glioma model.PloS one · 2014Article
- Systems pharmacological analysis of paclitaxel-mediated tumor priming that enhances nanocarrier deposition and efficacy.The Journal of pharmacology and experimental therapeutics · 2013Article
- Thermal targeting of an acid-sensitive doxorubicin conjugate of elastin-like polypeptide enhances the therapeutic efficacy compared with the parent compound in vivo.Molecular cancer therapeutics · 2012Article
- Challenges in development of targeted liposomal therapeutics.The AAPS journal · 2012Review
- Targeting colon cancer cells using PEGylated liposomes modified with a fibronectin-mimetic peptide.International journal of pharmaceutics · 2009Article
- Multifunctional polymeric micelles for enhanced intracellular delivery of doxorubicin to metastatic cancer cells.Pharmaceutical research · 2008Article
- Tumor-specific antibody-mediated targeted delivery of Doxil reduces the manifestation of auricular erythema side effect in mice.International journal of pharmaceutics · 2008Article
- Enhanced cytotoxicity of monoclonal anticancer antibody 2C5-modified doxorubicin-loaded PEGylated liposomes against various tumor cell lines.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2007Article
- Tumor-specific anti-nucleosome antibody improves therapeutic efficacy of doxorubicin-loaded long-circulating liposomes against primary and metastatic tumor in mice.Molecular pharmaceuticsArticle
- Extracellularly activated nanocarriers: a new paradigm of tumor targeted drug delivery.Molecular pharmaceuticsReview
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo investigate the correlation between the in vitro intracellular uptake and the in vivo antitumor activity of anticancer drugs delivered by sterically stabilized liposomes (SSL).
methodsArginine-glycine-aspartic acid (RGD) peptide or RGD mimetic (RGDm) was coupled onto the surface of SSL to obtain the cell-binding carrier to facilitate the intracellular delivery of the encapsulated drugs. DOX-loaded SSL (SSL-DOX), DOX-loaded RGD-modified SSL (RGD-SSL-DOX) and DOX-loaded RGDm-modified SSL (RGDm-SSL-DOX) were prepared by lipid film dispersion followed by remote loading of DOX. The intracellular uptake of DOX from the various liposomal formulations was evaluated in vitro with melanoma B16 cells, and the pharmacokinetics, biodistribution, and antitumor activity were compared in C57BL/6 mice carrying melanoma B16 tumors.
resultsIn vitro intracellular uptake of DOX by B16 cells and in vivo antitumor activity in terms of tumor growth inhibition and mice survival time prolongation for various liposomal DOX were in the following order: RGD-SSL-DOX > RGDm-SSL-DOX > SSL-DOX. The mean survival time of the mice treated with RGD-SSL-DOX, RGDm-SSL-DOX, and SSL-DOX was 55, 49, and 44 days, respectively. The three liposomal DOX formulations produced very close DOX accumulation in tumor, which is significantly higher than that of free DOX. RGD- or RGDm-SSL-DOX demonstrated prolonged circulation time similar to that of SSL-DOX, whereas they showed significantly lower DOX level in blood and remarkably higher uptake by spleen than SSL-DOX.
conclusionsEnhanced intracellular uptake of DOX encapsulated in SSL could produce an improved therapeutic effect for the melanoma B16 tumors. Enhancing intracellular delivery of the anticancer drugs encapsulated in SSL may be a promising strategy to improve their therapeutic efficacy for solid tumors.
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