article · Journal of Pharmaceutical Investigation
This study developed a transdermal drug delivery system for fluocinolone acetonide, a corticosteroid used to manage rheumatoid arthritis, aiming to bypass the poor solubility and bioavailability associated with oral delivery. Researchers created polyethylene glycol-decorated hyalurosomes carrying the drug using an ethanol injection method, optimising surfactant types and hyaluronic acid quantities. The best formulation achieved high drug entrapment and a nanoscale particle size, and was subsequently integrated into cellulose acetate and polycaprolactone nanofibers to support sustained release. When applied transdermally in a rat model of adjuvant-induced arthritis, the nanofiber system led to marked improvements in joint histopathology. It reduced levels of inflammatory markers including mTORC1, TNF-alpha, and NF-kappaB, while simultaneously increasing levels of the anti-inflammatory marker IL-10 and TRIM24, demonstrating enhanced management of arthritis symptoms.
Rheumatoid arthritis is typically managed with oral anti-inflammatory drugs that suffer from poor absorption and trigger undesirable systemic side effects. By formulating a corticosteroid into transdermal nanofibers that deliver the drug through the skin, this approach could offer sustained local relief, suppress joint inflammation, and reduce the harmful effects associated with oral administration.
This technology could enable topical or patch-based therapeutics for pharmaceutical companies formulating treatments for rheumatoid arthritis. The research demonstrates sustained transdermal delivery and therapeutic efficacy in a rat disease model, indicating that the formulation is at an applied, preclinical testing stage and would require clinical safety and efficacy trials before real-world adoption.
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Abstract Purpose This study aimed to develop a transdermal delivery system for fluocinolone acetonide (FLA), a corticosteroid used in treating inflammatory conditions like rheumatoid arthritis (RA), to overcome the limitations of oral administration, such as poor solubility and bioavailability. Methods FLA-loaded PEG decorated hyalurosomes (FLA-PHs) were fabricated using ethanol injection, incorporating various Brij® surfactants and different amounts of hyaluronic acid (HA) based on a full factorial design. The impact of independent variables, HA amount (mg) (X 1 ) and Brij type (X 2 ) were inspected for entrapment efficiency (EE%), particle size (PS), and zeta potential (ZP). The optimum FLA-PHs were then incorporated into ε-polycaprolactone (PCL) and cellulose acetate (CA) nanofibers to enhance sustained transdermal delivery (FLA-NFs). Results The optimum FLA-PHs exhibited EE% of 83.58 ± 0.69%, PS of 169.00 ± 1.41 nm, and ZP of -22.90 ± 0.14 mV. Morphological assessment of FLA-NFs showed promising results in terms of surface roughness. In a Freund-induced rat model of adjuvant-induced arthritis, transdermal treatment with FLA-NFs significantly improved joint histopathological analyses. Furthermore, it suppressed inflammatory markers such as mTORC1, TNF-α, and NF-κB while upregulating TRIM24 and the anti-inflammatory IL-10. Conclusion FLA-NFs present a promising strategy for enhancing the transdermal delivery of FLA for managing RA, offering potential improvements in efficacy and reduced systemic side effects compared to conventional oral administration.
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DOI: 10.1007/s40005-024-00693-8
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