ArticleJournal of controlled release : official journal of the Controlled Release Society2011
G3.5 PAMAM dendrimers enhance transepithelial transport of SN38 while minimizing gastrointestinal toxicity.
Article in Journal of controlled release : official journal of the Controlled Release Society, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 100 citations in OpenAlex.
- Polymeric nanocarriers in drug delivery, bioimaging, and biosensing: advances and perspectives on nanomicelles, nanogels, and dendrimers.RSC advances · 2025Review
- "Enhancing Oral Drug Absorption: Overcoming Physiological and Pharmaceutical Barriers for Improved Bioavailability".AAPS PharmSciTech · 2024Review
- Nanostructure-Mediated Transport of Therapeutics through Epithelial Barriers.International journal of molecular sciences · 2024Review
- Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics.Biomedicines · 2022Review
- Gold Nanorods for Doxorubicin Delivery: Numerical Analysis of Electric Field Enhancement, Optical Properties and Drug Loading/Releasing Efficiency.Materials (Basel, Switzerland) · 2022Article
- Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs.Biomolecules · 2021Article
- Advances in Oral Drug Delivery.Frontiers in pharmacology · 2021Review
- Development of Self-Associating SN-38-Conjugated Poly(ethylene oxide)-Poly(ester) Micelles for Colorectal Cancer Therapy.Pharmaceutics · 2020Article
- Article
- Polymer-drug conjugate therapeutics: advances, insights and prospects.Nature reviews. Drug discovery · 2019Review
- Oral administration of irinotecan in patients with solid tumors: an open-label, phase I, dose escalating study evaluating safety, tolerability and pharmacokinetics.Cancer chemotherapy and pharmacology · 2019Article
- Recent Developments in Active Tumor Targeted Multifunctional Nanoparticles for Combination Chemotherapy in Cancer Treatment and Imaging.Journal of biomedical nanotechnology · 2015Review
- Cationic nanoparticles directly bind angiotensin-converting enzyme 2 and induce acute lung injury in mice.Particle and fibre toxicology · 2015Article
- Advances in the application of nanotechnology in the diagnosis and treatment of gastrointestinal tumors.Molecular and clinical oncology · 2015Article
- Predicting cytotoxicity of PAMAM dendrimers using molecular descriptors.Beilstein journal of nanotechnology · 2015Article
- Article
- Intracellular Ca2+ release mediates cationic but not anionic poly(amidoamine) (PAMAM) dendrimer-induced tight junction modulation.Pharmaceutical research · 2014Article
- Transepithelial transport of PAMAM dendrimers across isolated rat jejunal mucosae in ussing chambers.Biomacromolecules · 2014Article
- Challenges associated with Penetration of Nanoparticles across Cell and Tissue Barriers: A Review of Current Status and Future Prospects.Nano today · 2014Article
- Poly(amido amine) dendrimers as absorption enhancers for oral delivery of camptothecin.International journal of pharmaceutics · 2013Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Poly(amido amine) (PAMAM) dendrimers have shown promise in oral drug delivery. Conjugation of SN38 to PAMAM dendrimers has the potential to improve its oral absorption while minimizing gastrointestinal toxicity. In this work we evaluated G3.5 PAMAM dendrimer-SN38 conjugates with ester-linked glycine and β-alanine spacers for their suitability in oral therapy of hepatic colorectal cancer metastases. G3.5-βAlanine-SN38 was mostly stable while G3.5-Glycine-SN38 showed 10%, 20%, and 56% SN38 release in simulated gastric, intestinal and liver environments for up to 6, 24 and 48 hours, respectively. Short-term treatment of Caco-2 cells with G3.5-SN38 conjugates did not reduce cell viability, while comparable concentrations of SN38 caused significant cytotoxicity. G3.5-Glycine-SN38 and G3.5-βAlanine-SN38 showed IC₅₀ values of 0.60 and 3.59 μM, respectively, in HT-29 cells treated for 48 h, indicating the efficacy of the drug delivery system in colorectal cancer cells with longer incubation time. Both conjugates increased SN38 transepithelial transport compared to the free drug. Transport of G3.5-Glycine-SN38 was highly concentration-dependent whereas transport of G3.5-βAlanine-SN38 was concentration-independent, highlighting the influence of drug loading and spacer chemistry on transport mechanism. Together these results show that PAMAM dendrimers have the potential to improve the oral bioavailability of potent anti-cancer drugs.
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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.