ArticleDrug design, development and therapy2021
Self-Nanoemulsifying Drug Delivery System of Genkwanin: A Novel Approach for Anti-Colitis-Associated Colorectal Cancer.
Article in Drug design, development and therapy, 2021. 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.
- Formulation approaches for colon-specific drug delivery: conventional to nanocarrier systems.RSC advances · 2026Review
- Plant-Derived Bioactive Compounds in Inflammation-Related Cancers: Mechanisms and Therapeutic Potential.Plants (Basel, Switzerland) · 2026Review
- Lipid-Based Nanocarriers for Curcumin Delivery: A Promising Strategy in The Management of Inflammatory Diseases.International journal of nanomedicine · 2026Review
- Cell membrane biomimetic nanoplatforms: a new strategy for immune escape and precision targeted therapy.Materials today. Bio · 2025Review
- Quality by Design (QbD)-Based Development of a Self-Nanoemulsifying Drug Delivery System for the Ocular Delivery of Flurbiprofen.Pharmaceutics · 2025Article
- The Application of Nano Drug Delivery Systems in Female Upper Genital Tract Disorders.Pharmaceutics · 2024Review
- Nanomedicine for colon-targeted drug delivery: strategies focusing on inflammatory bowel disease and colon cancer.Nanomedicine (London, England) · 2024Review
- Therapeutic Implications of Dietary Polyphenols-Loaded Nanoemulsions in Cancer Therapy.ACS applied bio materials · 2024Review
- Targeting the Gut: A Systematic Review of Specific Drug Nanocarriers.Pharmaceutics · 2024Review
- Review
- Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability.Pharmaceutics · 2023Article
- Therapeutic effects of natural polyphenols on colorectal adenomas: Focus on preclinical studies (Review).Oncology reports · 2023Review
- Phenolic Phytochemicals for Prevention and Treatment of Colorectal Cancer: A Critical Evaluation of In Vivo Studies.Cancers · 2023Review
- Self-Nanoemulsifying Drug Delivery System for Enhanced Bioavailability of Madecassic Acid: In vitro and in vivo Evaluation.International journal of nanomedicine · 2023Article
- Self-nanoemulsifying drug delivery system (SNEDDS) mediated improved oral bioavailability of thymoquinone: optimization, characterization, pharmacokinetic, and hepatotoxicity studies.Drug delivery and translational research · 2023Article
- Improved Trimethylangelicin Analogs for Cystic Fibrosis: Design, Synthesis and Preliminary Screening.International journal of molecular sciences · 2022Article
- Functional Excipients and Novel Drug Delivery Scenario in Self-nanoemulsifying Drug Delivery System: A Critical Note.Pharmaceutical nanotechnology · 2022Review
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe aim of the present study was to develop an optimized Genkwanin (GKA)-loaded self-nanoemulsifying drug delivery system (SNEDDS) formulation to enhance the solubility, intestinal permeability, oral bioavailability and anti-colitis-associated colorectal cancer (CAC) activity of GKA.
methodsWe designed a SNEDDS comprised oil phase, surfactants and co-surfactants for oral administration of GKA, the best of which were selected by investigating the saturation solubility, constructing pseudo-ternary phase diagrams, followed by optimizing thermodynamic stability, emulsification efficacy, self-nanoemulsification time, droplet size, transmission electron microscopy (TEM), drug release and intestinal permeability. In addition, the physicochemical properties and pharmacokinetics of GKA-SNEDDS were characterized, and its anti-colitis-associated colorectal cancer (CAC) activity and potential mechanisms were evaluated in AOM/DSS-induced C57BL/6J mice model.
resultsThe optimized nanoemulsion formula (OF) consists of Maisine CC, Labrasol ALF and Transcutol HP in a weight ratio of 20:60:20 (w/w/w), in which ratio the OF shows multiple improvements, specifically small mean droplet size, excellent stability, fast release properties as well as enhanced solubility and permeability. Pharmacokinetic studies demonstrated that compared with GKA suspension, the relative bioavailability of GKA-SNEDDS was increased by 353.28%. Moreover, GKA-SNEDDS not only significantly prevents weight loss and improves disease activity index (DAI) but also reduces the histological scores of inflammatory cytokine levels as well as inhibiting the formation of colon tumors via inducing tumor cell apoptosis in the AOM/DSS-induced CAC mice model.
conclusionOur results show that the developed GKA-SNEDDS exhibited enhanced oral bioavailability and excellent anti-CAC efficacy. In summary, GKA-SNEDDS, using lipid nanoparticles as the drug delivery carrier, can be applied as a potential drug delivery system for improving the clinical application of GKA.
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