ArticleInternational journal of nanomedicine2022
Cyclic RGD-Decorated Liposomal Gossypol AT-101 Targeting for Enhanced Antitumor Effect.
Article in International journal of nanomedicine, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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18 citing papers in PubMed, 34 citations in OpenAlex.
- Engineering exosomes for cancer therapy - Modification technologies and subcellular targeting strategies: A review.International journal of pharmaceutics: X · 2026Review
- AT-101 inhibits the proliferation and invasion of tongue squamous carcinoma cells by targeting the miR-21-5p/FDX1 axis.Scientific reports · 2026Article
- Calcium/Aluminum-Cored Asymmetric Bilayer Nanoparticles for Codelivery of Ziyuglycoside II and PD-L1 siRNA Exert Anti-Breast Tumor Effects.Pharmaceutics · 2026Article
- Formulation Progress, Challenges, and Perspectives of Anti-Inflammatory Natural Products.Drug design, development and therapy · 2026Review
- Multifunctional saikosaponin D-liposomes for hepatocellular carcinoma: Formulation optimization, characterization, and in vitroInternational journal of pharmaceutics: X · 2025Article
- Nanoparticle-based drug delivery systems in urologic oncology: From targeted therapy to precision theranostics.Materials today. Bio · 2025Review
- Active Targeting Strategies for Improving the Bioavailability of Curcumin: A Systematic Review.Foods (Basel, Switzerland) · 2025Review
- Review
- In Vitro and In Vivo Evaluation of Lactoferrin-Modified Liposomal Etomidate with Enhanced Brain-Targeting Effect for General Anesthesia.Pharmaceutics · 2024Article
- Preliminary Study on Pharmacokinetics and Antitumor Pharmacodynamics of Folic Acid Modified Crebanine Polyethyleneglycol-Polylactic Acid Hydroxyacetic Acid Copolymer Nanoparticles.International journal of nanomedicine · 2024Article
- Liposomal Nanomaterials: A Rising Star in Glioma Treatment.International journal of nanomedicine · 2024Review
- Implantation of hydrogel-liposome nanoplatform inhibits glioblastoma relapse by inducing ferroptosis.Asian journal of pharmaceutical sciences · 2023Article
- Suppression of triple-negative breast cancer aggressiveness by LGALS3BP via inhibition of the TNF-α-TAK1-MMP9 axis.Cell death discovery · 2023Article
- Active targeting schemes for nano-drug delivery systems in osteosarcoma therapeutics.Journal of nanobiotechnology · 2023Review
- Advances in mitophagy and mitochondrial apoptosis pathway-related drugs in glioblastoma treatment.Frontiers in pharmacology · 2023Review
- Strategic developments in the drug delivery of natural product dihydromyricetin: applications, prospects, and challenges.Drug delivery · 2022Review
- Recent advances in NIR-II fluorescence based theranostic approaches for glioma.Frontiers in chemistry · 2022Review
- Urokinase-loaded cyclic RGD-decorated liposome targeted therapy forFrontiers in bioengineering and biotechnology · 2022Article
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Authors and funding
14 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
introduction(-)-Gossypol (AT-101), the (-)-enantiomer of the natural compound gossypol, has shown significant inhibitory effects on various types of cancers such as osteosarcoma, myeloma, glioma, lung cancer, and prostate cancer. However, the clinical application of (-)-gossypol was often hindered by its evident side effects and the low bioavailability via oral administration, which necessitated the development of suitable (-)-gossypol preparations to settle the problems. In this study, injectable cyclic RGD (cRGD)-decorated liposome (cRGD-LP) was prepared for tumor-targeted delivery of (-)-gossypol.
methodsThe cRGD-LP was prepared based on cRGD-modified lipids. For comparison, a non-cRGD-containing liposome (LP) with a similar chemical composition to cRGD-LP was specially designed. The physicochemical properties of (-)-gossypol-loaded cRGD-LP (Gos/cRGD-LP) were investigated in terms of the drug loading efficiency, particle size, morphology, drug release, and so on. The inhibitory effect of Gos/cRGD-LP on the proliferation of tumor cells in vitro was evaluated using different cell lines. The biodistribution of cRGD-LP in vivo was investigated via the near-infrared (NIR) fluorescence imaging technique. The antitumor effect of Gos/cRGD-LP in vivo was evaluated in PC-3 tumor-bearing nude mice.
resultsGos/cRGD-LP had an average particle size of about 62 nm with a narrow size distribution, drug loading efficiency of over 90%, and sustained drug release for over 96 h. The results of NIR fluorescence imaging demonstrated the enhanced tumor targeting of cRGD-LP in vivo. Moreover, Gos/cRGD-LP showed a significantly enhanced inhibitory effect on PC-3 tumors in mice, with a tumor inhibition rate of over 74% and good biocompatibility.
conclusionThe incorporation of cRGD could significantly enhance the tumor-targeting effect of the liposomes and improve the antitumor effect of the liposomal (-)-gossypol in vivo, which indicated the potential of Gos/cRGD-LP that warrants further investigation for clinical applications of this single-isomer drug.
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