Purpose: This study was performed to investigate the effect of elastic and rigid vesicles on the penetration of the D2 dopamine agonist rotigotine across human skin and to further elucidate the mechanisms of action of the elastic vesicles.
Methods: A series of rotigotine-loaded vesicles were prepared, ranging from very elastic to very rigid. The drug penetration from these vesicles across human skin was studied in vitro using flow-through diffusion cells. Micelle and buffer solutions were investigated as controls. For the most elastic vesicle composition, two additional variables were investigated. Coapplication of drug and vesicles was compared to pretreatment, and the effect of the drug entrapment efficiency was investigated.
Results: The very elastic vesicle formulation L-595/PEG-8-L (50/50) gave steady-state fluxes of 214.4 +/- 27.8 ng/(h x cm2). This formulation was the most effective formulation and significantly better than the rigid vesicle formulations as well as the micelle and buffer controls. However, coapplication and a high drug entrapment efficiency were essential factors for an optimal drug delivery from elastic vesicle formulations.
Conclusions: Elastic vesicles are promising vehicles for transdermal drug delivery. It is essential that drug molecules are applied together with and entrapped within the vesicles themselves, suggesting that elastic vesicles act as drug carrier systems and not solely as penetration enhancers.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1023/a:1026191402557 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Elastic cartilage properties of the tip of the vocal process of the arytenoid cartilage.
Laryngoscope Investig Otolaryngol
February 2025
Objectives: This study aimed to investigate the histological and ultrastructural features of the elastic cartilage at the tip of the vocal process in the arytenoid cartilage, which is essential for laryngeal biomechanics.
Methods: Five larynges, including the vocal folds and epiglottis, were examined using transmission electron microscopy. The elastic cartilage at the tip of the vocal process was compared to the epiglottic cartilage within the same larynx to elucidate structural differences.
Exploring Elastic Lipid Nanovesicles for Enhanced Skin Permeation of Whole Plant Extract: A Comprehensive Investigation.
J Biomed Mater Res B Appl Biomater
January 2025
School of Pharmacy and Technology Management, SVKM's, NMIMS, Shirpur, Maharashtra, India.
Article Synopsis
- A new method using elastic lipid nanovesicles (ELNs) loaded with Lantana camara extract is developed to improve the permeation of active compounds through the skin.
- The study produced 15 different formulations and examined factors like vesicle size, surface characteristics, and the impact on skin permeation using a model resembling human skin (Start-M).
- Results showed that smaller vesicle sizes (100-200 nm) significantly enhanced the permeation of the extract, and that the optimal surfactant ratio led to over 75% of the extract permeating within 8 hours; the ELN formulation also demonstrated a strong reduction in skin cancer cell viability.
- Future research should focus on the long-term safety and clinical applications of ELNs
Migrasome formation is initiated preferentially in tubular junctions by membrane tension.
Biophys J
January 2025
Department of Physiology and Pharmacology, Sackler Faculty of Medicine, Tel Aviv University, Tel Aviv, Israel; Center for Physics and Chemistry of Living Systems, Tel Aviv University, Tel Aviv, Israel. Electronic address:
Migrasomes, the vesicle-like membrane micro-structures, arise on the retraction fibers (RFs), the branched nano-tubules pulled out of cell plasma membranes during cell migration and shaped by membrane tension. Migrasomes form in two steps: a local RF bulging is followed by a protein-dependent stabilization of the emerging spherical bulge. Here we addressed theoretically and experimentally the previously unexplored mechanism of bulging of membrane tubular systems.
View Article and Find Full Text PDFSpontaneous formation of small and ultrasmall unilamellar vesicles in mixtures of drug surfactant and phospholipid: Effect of chemical structure of phospholipid tails on vesicle size.
J Colloid Interface Sci
December 2024
Department of Medicinal Chemistry, Uppsala University, P.O. Box 547, 751 23, Uppsala, Sweden. Electronic address:
We have investigated the effect of length and chemical structure of phospholipid tails on the spontaneous formation of unilamellar liposomal vesicles in binary solute mixtures of cationic drug surfactant and zwitterionic phosphatidylcholine phospholipids. Binary drug surfactant-phospholipid mixtures with four different phospholipids with identical headgroups (two saturated phospholipids 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC, 14:0) and 1,2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC, 16:0), and two unsaturated lipids 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC, 18:1) and 1,2-Dierucoyl-sn-Glycero-3-Phosphatidylcholine (DEPC, 22:1)) combined with two different tricyclic antidepressant drugs (amitriptyline hydrochloride (AMT) and doxepin hydrochloride (DXP)) have been investigated with small-angle neutron scattering (SANS) and cryo-transmission electron microscopy (cryo-TEM). We observe a conspicuous impact of phospholipid tail structure on both micelle-to-vesicle transition point and vesicle size.
View Article and Find Full Text PDFInfluence of the glycocalyx on the size and mechanical properties of plasma membrane-derived vesicles.
Soft Matter
January 2025
Robert Frederick Smith School of Chemical and Biomolecular Engineering, Cornell University, Ithaca, NY 14853, USA.
Recent studies have reported that the overexpression of MUC1 glycoproteins on cell surfaces changes the morphology of cell plasma membranes and increases the blebbing of vesicles from them, supporting the hypothesis that entropic forces exerted by MUC1 change the spontaneous curvature of cell membranes. However, how MUC1 is incorporated into and influences the size and biophysical properties of plasma-membrane-blebbed vesicles is not understood. Here we report single-vesicle-level characterization of giant plasma membrane vesicles (GPMVs) derived from cells overexpressing MUC1, revealing a 40× variation in MUC1 density between GPMVs from a single preparation and a strong correlation between GPMV size and MUC1 density.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!