ArticlePharmaceutical research2013
Docetaxel-loaded thermosensitive and bioadhesive nanomicelles as a rectal drug delivery system for enhanced chemotherapeutic effect.
Article in Pharmaceutical research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- Anemoside B4 Rectal Thermosensitive In Situ Gel to Treat Ulcerative Colitis by Overcoming Oral Bioavailability Barriers with Absorption Enhancer-Assisted Delivery.Pharmaceutics · 2025Article
- Localized Drug Delivery in Different Gastrointestinal Cancers: Navigating Challenges and Advancing Nanotechnological Solutions.International journal of nanomedicine · 2025Review
- Development and Evaluation of Docetaxel-Loaded Nanostructured Lipid Carriers for Skin Cancer Therapy.Pharmaceutics · 2024Article
- Localized Drug Delivery Systems: An Update on Treatment Options for Head and Neck Squamous Cell Carcinomas.Pharmaceutics · 2023Review
- Article
- Advancements in Rectal Drug Delivery Systems: Clinical Trials, and Patents Perspective.Pharmaceutics · 2022Review
- Preparation, in vitro and in vivo Evaluation of Thermosensitive in situ Gel Loaded with Ibuprofen-Solid Lipid Nanoparticles for Rectal Delivery.Drug design, development and therapy · 2022Article
- Achievements in Thermosensitive Gelling Systems for Rectal Administration.International journal of molecular sciences · 2021Review
- Particle and Gel Characterization of Irinotecan-Loaded Double-Reverse Thermosensitive Hydrogel.Polymers · 2021Article
- Development, Characterization, and Evaluation of SLN-Loaded Thermoresponsive Hydrogel System of Topotecan as Biological Macromolecule for Colorectal Delivery.BioMed research international · 2021Article
- Multifunctional Biomedical Adhesives.Advanced healthcare materials · 2019Review
- Physiological and Pharmaceutical Considerations for Rectal Drug Formulations.Frontiers in pharmacology · 2019Review
- Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration.Drug delivery · 2017Article
- Docetaxel-loaded multilayer nanoparticles with nanodroplets for cancer therapy.International journal of nanomedicine · 2016Article
- Tumor-targeting, pH-sensitive nanoparticles for docetaxel delivery to drug-resistant cancer cells.International journal of nanomedicine · 2015Article
- Solid lipid nanoparticle formulations of docetaxel prepared with high melting point triglycerides: in vitro and in vivo evaluation.Molecular pharmaceutics · 2014Article
- The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles.International journal of nanomedicine · 2014Article
Corrections and comments
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Authors and funding
13 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo investigate the potential of thermosensitive and biadhesive nanomicelles in improving the bioavailability of docetaxel (DCT) and its chemotherapeutic effect.
methodDCT-loaded nanomicelles were prepared by emulsufication and characterized in terms of physico-chemical and visco-elastic parameters. The optimzed formulation was evaluated for in vivo localization, pharmacokinetic and anti-tumor efficacy.
resultsThe hydrodynamic size of DCT-loaded nanomicelles was approximately 13 nm and the nanomicelles exhibited a sufficient gelation strength (9250 mPa·s) and bioadhesive force (2100 dyn/cm²) to be retained in the upper part of rectum. We observed a high rectal bioavailability of 29% DCT compared to that following oral administration in rats, as it successfully evaded the multidrug efflux transporters and hepatic first-pass metabolism. Plasma concentration around ∼50 ng/mL was maintained throughout the study period (12 h) while Taxotere® attained subtherapeutic range within 4 h of drug administration. Results also revealed that the rectally administered DCT-loaded nanomicelles exhibited a significant anti-tumor effect (200 mm³) with a reduced toxicity profile when compared to orally administered DCT (950 mm³). Furthermore, histological study showed that the rectal mucosa was completely intact with no signs of irritation upon treatment with DCT-loaded nanomicelles.
conclusionsTaken together, our novel thermosensitive and biadhesive nanomicelles demonstrated the ability to improve the bioavailability and chemotherapeutic potential of DCT in vivo. To the best of our knowledge, this is the first report describing the rectal delivery of DCT-loaded nanomicelles.
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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.