ArticlePharmaceutics2021
Dual-Acting Zeta-Potential-Changing Micelles for Optimal Mucus Diffusion and Enhanced Cellular Uptake after Oral Delivery.
Article in Pharmaceutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 28 citations in OpenAlex.
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- In Vitro Evaluation of Novel Nano-Sized Colloidal Assemblies Incorporating Hydrophobic Tobramycin Ion Pairs: Enhanced Cellular Uptake with Preserved Antimicrobial Activity Toward Oral Drug Delivery.Molecules (Basel, Switzerland) · 2026Article
- Physicochemical Aspects of Mixed Micelle Formation Between Amphiphilic Drugs and Surfactants.International journal of molecular sciences · 2026Review
- Formulation of Metformin-Loaded Chitosan Nanoparticles and In Vivo Evaluation of Its Hypoglycemic Effects.Molecules (Basel, Switzerland) · 2026Article
- Artificial Intelligence-Guided Optimization of Hyaluronic Acid-Coated Liposomal Linagliptin for Targeted Management of Polycystic Ovary Syndrome.AAPS PharmSciTech · 2026Article
- Factorial Design-Driven Optimization of Zein-Chitosan Nanoparticles for Oral Delivery of Silibinin.ACS omega · 2026Article
- Inhalable TPGS/DPPC Micelles Coloaded with Curcumin and Icariin for Targeted Lung Cancer Therapy.ACS omega · 2025Article
- Recent Advances in Cationic Nanoemulsions for Drug Delivery: Preparation, Properties, and Applications.Current pharmaceutical design · 2025Review
- Strategies to Enhance the Solubility and Bioavailability of Tocotrienols Using Self-Emulsifying Drug Delivery System.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Lyophilized Nasal Inserts of Atomoxetine HCl Solid Lipid Nanoparticles for Brain Targeting as a Treatment of Attention-Deficit/Hyperactivity Disorder (ADHD): A Pharmacokinetics Study on Rats.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Polymers Enhancing Bioavailability in Drug Delivery.Pharmaceutics · 2022Article
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Authors and funding
3 authors at 3 institutions in 2 countries.
Funding
Abstract
contextOvercoming the intestinal mucosal barrier can be a challenge in drug delivery. Nanoemulsions with negative zeta potentials can effectively permeate the mucus layer, but those with positive zeta potentials are better taken up by cells; a nanoemulsion with capricious zeta potential from negative to positive can achieve both good permeation and high uptake.
objectiveThis study aimed to develop dual-acting zeta-potential-amphoteric micelles enabling optimal muco-permeation and enhancement of cellular uptake.
methodsA micellar pre-concentrate was prepared from 15% Labrasol, 15% Kolliphor EL, 30% Kolliphor RH 40, and 40% dimethylsulfoxide. The micellar pre-concentrate was loaded with anionic stearic acid (SA), forming ionic complexes with cationic polymers at a ratio of 25:1 with Eudragit RS 100 and Eudragit RL 100. Blank micelles and those containing complexes were separately diluted in physiological buffers and examined for their droplet sizes, polydispersity indices (PDIs), zeta potentials, and cytotoxicity. The SA release from the micellar complexes was evaluated in 0.1 mM phosphate buffer (pH 6.8) containing 0.001% fluorescein, thereby enabling an instant decrease in fluorescence. Finally, the micelles were loaded with the model drug fluorescein diacetate (FDA) and evaluated for their muco-permeation behavior and cellular uptake.
resultsThe micellar dilutions formed micelles at the critical micelle concentration (CMC) of 312 µg/mL and showed a uniform average droplet size of 14.2 nm, with a PDI < 0.1. Micellar dilutions were non-cytotoxic when used at 1:100 in a physiological medium. Micelles loaded with ionic complexes achieved a sustained release of 95.5 ± 3.7% of the SA in 180 min. Moreover, the zeta potential of the complex-loaded micelles shifted from -5.4 to +1.8 mV, whereas the blank micelles showed a stabilized zeta potential of -10 mV. Furthermore, the negatively charged blank and complex-loaded micelles exhibited comparable muco-permeation, with an overall average of 58.2 ± 3.7% diffusion of FDA. The complex-loaded micellar droplets, however, provided a significantly higher cellular uptake of the model drug FDA (2.2-fold,
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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.