ArticleInternational journal of nanomedicine2012
Cyclic RGD peptide-modified liposomal drug delivery system: enhanced cellular uptake in vitro and improved pharmacokinetics in rats.
Article in International journal of nanomedicine, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
32 citing papers in PubMed, 89 citations in OpenAlex.
- Injectable Hydrogels for Breast Cancer Therapy: From Tumor Microenvironment-Responsive and Actively Targeted Drug Delivery to Immunotherapy and Theranostics.Pharmaceutics · 2026Review
- Decoupling Bioactivity and Processability: RGD Click-Functionalized Coatings for a 3D-Printed PCL Scaffold.Biomacromolecules · 2025Article
- Advancements in Liposomal Nanomedicines: Innovative Formulations, Therapeutic Applications, and Future Directions in Precision Medicine.International journal of nanomedicine · 2025Review
- Increased Cellular Uptake of ApoE3- or c(RGD)-Modified Liposomes for Glioblastoma Therapy Depending on the Target Cells.Pharmaceutics · 2024Article
- Development of 5-Fluorouracil/pH-Responsive Adjuvant-Embedded Extracellular Vesicles for Targeting αPharmaceutics · 2024Article
- RGD-based self-assembling nanodrugs for improved tumor therapy.Frontiers in pharmacology · 2024Review
- Peptide Self-Assembled Nanocarriers for Cancer Drug Delivery.The journal of physical chemistry. B · 2023Review
- Functionalization of Nanoparticulate Drug Delivery Systems and Its Influence in Cancer Therapy.Pharmaceutics · 2022Review
- Integrin-αvβ3 as a Therapeutic Target in Glioblastoma: Back to the Future?Pharmaceutics · 2022Review
- Review
- An Underestimated Factor: The Extent of Cross-Reactions Modifying APIs in Surface-Modified Liposomal Preparations Caused by Comprised Activated Lipids.Molecules (Basel, Switzerland) · 2020Article
- Engineering Smart Targeting Nanovesicles and Their Combination with Hydrogels for Controlled Drug Delivery.Pharmaceutics · 2020Review
- Improving the therapeutic efficiency of noncoding RNAs in cancers using targeted drug delivery systems.Drug discovery today · 2020Review
- Nanoparticle-based Cell Trackers for Biomedical Applications.Theranostics · 2020Review
- Pharmacokinetic stability of macrocyclic peptide triazole HIV-1 inactivators alone and in liposomes.Journal of peptide science : an official publication of the European Peptide Society · 2019Article
- Peptide-Based Drug-Delivery Systems in Biotechnological Applications: Recent Advances and Perspectives.Molecules (Basel, Switzerland) · 2019Review
- P1c peptide decorated liposome targeting αvβ3-expressing tumor cellsRSC advances · 2018Article
- Surface Functionalization and Targeting Strategies of Liposomes in Solid Tumor Therapy: A Review.International journal of molecular sciences · 2018Review
- A peptide-CpG-DNA-liposome complex vaccine targeting TM4SF5 suppresses growth of pancreatic cancer in a mouse allograft model.OncoTargets and therapy · 2018Article
- Evaluation of the use of therapeutic peptides for cancer treatment.Journal of biomedical science · 2017Review
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundIntegrins α(v)β(3) and α(v)β(5), both of which specifically recognize the Arg-Gly-Asp (RGD) motif, are overexpressed on many solid tumors and in tumor neovasculature. Thus, coupling the RGD motif to the liposomal surface for achieving active targeting can be a promising strategy for the treatment of tumors.
methodsCyclo(Arg-Gly-Asp-D-Phe-Cys) (cRGD) was covalently coupled with the liposomal membrane surface, followed by coating with poly(ethylene glycol) (PEG) using the post-insertion technique. The coupling efficiency of cRGD was determined. Doxorubicin as a model anticancer drug was loaded into liposomes using an ammonium sulfate gradient method to investigate the encapsulation efficiency, cellular uptake by the integrin-overexpressing human glioma cell line U87MG in vitro, and pharmacokinetic properties in Sprague-Dawley rats.
resultscRGD was conjugated to the liposomal surface by a thiol-maleimide coupling reaction. The coupling efficiency reached 98%. The encapsulation efficiency of doxorubicin in liposomes was more than 98%. The flow cytometry test result showed that cRGD-modified liposomes (RGD-DXRL-PEG) had higher cell uptake by U87MG cells, compared with nontargeted liposomes (DXRL-PEG). The cellular uptake was significantly inhibited in the presence of excess free cRGD. Both the targeted (t(1/2) = 24.10 hours) and non-targeted (t(1/2) = 25.32 hours) liposomes showed long circulating properties in rat plasma. The area under the curve of the targeted and nontargeted liposomes was 6.4-fold and 8.3-fold higher than that of doxorubicin solution, respectively.
conclusionThis study indicates preferential targeting and long circulating properties for cRGD-modified liposomes in vivo, which could be used as a potential targeted liposomal drug delivery system to treat human glioma.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.