ArticlePharmaceutics2021
Improvement of Imiquimod Solubilization and Skin Retention via TPGS Micelles: Exploiting the Co-Solubilizing Effect of Oleic Acid.
Article in Pharmaceutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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The trial behind it
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
20 citing papers in PubMed, 41 citations in OpenAlex.
- Harnessing oleic acid for facilitating topical delivery of lipid nanoparticle to the ocular posterior segment and improving anti-angiogenesis effect.International journal of pharmaceutics: X · 2026Article
- Adsorption of Mixed Micelles of Polysorbate 80 and Oleic Acid to the Air-Water Interface.Langmuir : the ACS journal of surfaces and colloids · 2026Article
- Local Chemotherapy of Skin Pre-Neoplastic Lesions and Malignancies from the Perspective of Current Pharmaceutics.Pharmaceutics · 2025Review
- Polymeric Nanoparticles Enable Targeted Visualization of Drug Delivery in Breast Cancer.Molecular pharmaceutics · 2025Article
- Recent progress in topical and transdermal approaches for melanoma treatment.Drug delivery and translational research · 2025Review
- Quercetin Nano-formulations as a Potential Approach for Skin Cancer.Pharmaceutical nanotechnology · 2025Review
- TPGS-mediated Transethosomes Enhance Transdermal Administration of CurcuminCurrent drug delivery · 2025Article
- Recent Advancements in the Diagnosis and Management of Cancer Using Biomaterials-fabricated Nanofibers: A Review.Current medicinal chemistry · 2025Review
- Imiquimod nanocrystal-loaded dissolving microneedles prepared by DLP printing.Drug delivery and translational research · 2025Article
- Effective Detoxification of Olive Mill Wastewater Using Multi-Step Surfactant-Based Treatment: Assessment of Environmental and Health Impact.Molecules (Basel, Switzerland) · 2024Article
- Imiquimod Solubility in Different Solvents: An Interpretative Approach.Pharmaceutics · 2024Article
- Amphiphilic Fluorinated Unimer Micelles as Nanocarriers of Fluorescent Probes for Bioimaging.ACS applied nano materials · 2023Article
- Nanotechnology-based ocular drug delivery systems: recent advances and future prospects.Journal of nanobiotechnology · 2023Review
- Topical Drug Delivery: Innovative Controlled Release Systems.Pharmaceutics · 2023Article
- A Scalable Platform for Fabricating Biodegradable Microparticles with Pulsatile Drug Release.Advanced materials (Deerfield Beach, Fla.) · 2023Article
- Gel Formulations for Topical Treatment of Skin Cancer: A Review.Gels (Basel, Switzerland) · 2023Review
- Advancements in nanoparticle-based treatment approaches for skin cancer therapy.Molecular cancer · 2023Review
- Development and Optimization of Imiquimod-Loaded Nanostructured Lipid Carriers Using a Hybrid Design of Experiments Approach.International journal of nanomedicine · 2023Article
- An Alternative Device for the Topical Treatment of Oral Cancer: Development and Ex-Vivo Evaluation of Imiquimod-Loaded Polysaccharides Formulations.Pharmaceutics · 2022Article
- Fluorescent Multifunctional Organic Nanoparticles for Drug Delivery and Bioimaging: A Tutorial Review.Pharmaceutics · 2022Review
Corrections and comments
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Authors and funding
9 authors at 1 institution in 2 countries.
Funding
Abstract
Imiquimod (IMQ) is an immunostimulant drug approved for the topical treatment of actinic keratosis, external genital-perianal warts as well as superficial basal cell carcinoma that is used off-label for the treatment of different forms of skin cancers, including some malignant melanocytic proliferations such as lentigo maligna, atypical nevi and other in situ melanoma-related diseases. Imiquimod skin delivery has proven to be a real challenge due to its very low water-solubility and reduced skin penetration capacity. The aim of the work was to improve the drug solubility and skin retention using micelles of d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), a water-soluble derivative of vitamin E, co-encapsulating various lipophilic compounds with the potential ability to improve imiquimod affinity for the micellar core, and thus its loading into the nanocarrier. The formulations were characterized in terms of particle size, zeta potential and stability over time and micelles performance on the skin was evaluated through the quantification of imiquimod retention in the skin layers and the visualization of a micelle-loaded fluorescent dye by two-photon microscopy. The results showed that imiquimod solubility strictly depends on the nature and concentration of the co-encapsulated compounds. The micellar formulation based on TPGS and oleic acid was identified as the most interesting in terms of both drug solubility (which was increased from few µg/mL to 1154.01 ± 112.78 µg/mL) and micellar stability (which was evaluated up to 6 months from micelles preparation). The delivery efficiency after the application of this formulation alone or incorporated in hydrogels showed to be 42- and 25-folds higher than the one of the commercial creams.
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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.