Novel lipid nanovesicle-loaded dissolving microarray patches for fenretinide in breast cancer chemoprevention

The retinoid fenretinide (FENR) is a promising compound for preventing breast cancer recurrence but faces challenges due to poor solubility and low bioavailability. This study explores the development of dissolving microneedles (MNs) containing FENR-loaded ethosomes for minimally invasive breast can...

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Bibliographic Details
Published in:Journal of controlled release 2024-10, Vol.374, p.76-88
Main Authors: Apolinário, Alexsandra Conceição, Naser, Yara A., Volpe-Zanutto, Fabiana, Vora, Lalitkumar K., Sabri, Akmal H., Li, Mingshan, Hutton, Aaron R.J., McCarthy, Helen O., Lopes, Luciana B., Donnelly, Ryan F.
Format: Article
Language:English
Subjects:
bioavailability
Breast cancer chemoprevention
breast neoplasms
cancer recurrence
chemoprevention
dosage forms
drugs
ethanol
Ethosomes
hydrogels
lecithins
Local transdermal therapy
micelles
Microarray patches
microarray technology
Micromolding
nanomaterials
Nanovesicles
oral administration
permeability
polysorbates
propylene glycol
solubility
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Summary:The retinoid fenretinide (FENR) is a promising compound for preventing breast cancer recurrence but faces challenges due to poor solubility and low bioavailability. This study explores the development of dissolving microneedles (MNs) containing FENR-loaded ethosomes for minimally invasive breast cancer chemoprevention, aiming to enhance local drug distribution. Ethosomes were formulated using ethanol, propylene glycol, soya lecithin, water, and polysorbate 80 micelles. MNs were created from poly(vinyl alcohol) and poly(vinylpyrrolidone) hydrogels by adding polymer powder directly into ethosomes suspensions, reducing manufacturing time and cost. Two methods were used to load ethosomes into high-density moulds: 1) only in the needle area, and 2) in both the needle area and baseplate. Dynamic light scattering confirmed nanostructures in the hydrogels and MNs. Micelle-based ethosomes dissolved MNs in 15 min, compared to 30 min for other MNs. Skin deposition studies showed greater drug deposition (up to 10 μg/patch) and enhanced skin permeation of FENR (up to 40 μg) with Method 2. In-vivo studies in rats demonstrated that oral administration resulted in plasma FENR levels below 10 ng/g in the first three hours, whereas MN administration delayed delivery, reaching a maximum plasma concentration of 52 ng/g at 48 h. Skin deposition of FENR from MNs decreased from 3 μg/g on day 1 to
ISSN:0168-3659
1873-4995
1873-4995
DOI:10.1016/j.jconrel.2024.07.080