article · Inflammopharmacology
Diosmin is an anti-inflammatory flavonoid that suffers from poor bioavailability because it requires an extreme pH of 12 to dissolve. To overcome this limitation for topical psoriasis management, diosmin was formulated into nanocrystals using an anti-solvent precipitation technique stabilized with hydroxypropyl methylcellulose. The resulting formulation achieved a particle size of approximately 277 nanometres, favourable colloidal features, and strong drug release. When evaluated in a rat model of imiquimod-induced psoriasis, a gel incorporating these nanocrystals significantly outperformed plain diosmin powder gel. The highest nanocrystal dose delivered the strongest anti-inflammatory response, markedly decreasing psoriasis severity scores and serum inflammatory cytokines. It restored balance between regulatory T cells and T helper 17 cells while modulating key signalling pathways and boosting negative regulators of inflammation in skin tissue.
Psoriasis is a chronic inflammatory skin condition that requires effective, targeted topical treatments. Natural flavonoids like diosmin offer therapeutic potential but are hampered by severe solubility issues that limit drug uptake. Nanocrystal formulation directly addresses this physical delivery barrier, improving drug release and demonstrating clear anti-inflammatory efficacy in animal models, providing a foundation for developing better topical psoriasis interventions.
This technology could enable pharmaceutical manufacturers to produce topical gel therapies for psoriasis and related inflammatory dermatological disorders. The ultimate end users would be clinicians and patients seeking targeted topical treatments. The research is currently at an early, preclinical stage, having been tested only in laboratory rats, meaning extensive formulation scale-up, safety evaluation, and clinical trials in humans are necessary before commercial deployment.
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Diosmin is a flavonoid with promising anti-inflammatory and antioxidant properties. However, it has difficult physicochemical characteristics since its solubility demands a pH level of 12, which has an impact on the drug's bioavailability. The aim of this work is the development and characterization of diosmin nanocrystals using anti-solvent precipitation technique to be used for topical treatment of psoriasis. Results revealed that diosmin nanocrystals stabilized with hydroxypropyl methylcellulose (HPMC E15) in ratio (diosmin:polymer; 1:1) reached the desired particle size (276.9 ± 16.49 nm); provided promising colloidal properties and possessed high drug release profile. Additionally, in-vivo assessment was carried out to evaluate and compare the activities of diosmin nanocrystal gel using three different doses and diosmin powder gel in alleviating imiquimod-induced psoriasis in rats and investigating their possible anti-inflammatory mechanisms. Herein, 125 mg of 5% imiquimod cream (IMQ) was applied topically for 5 consecutive days on the shaved backs of rats to induce psoriasis. Diosmin nanocrystal gel especially in the highest dose used offered the best anti-inflammatory effect. This was confirmed by causing the most statistically significant reduction in the psoriasis area severity index (PASI) score and the serum inflammatory cytokines levels. Furthermore, it was capable of maintaining the balance between T helper (Th17) and T regulatory (Treg) cells. Moreover, it tackled TLR7/8/NF-κB, miRNA-31, AKT/mTOR/P70S6K and elevated the TNFAIP3/A20 (a negative regulator of NF-κB) expression in psoriatic skin tissues. This highlights the role of diosmin nanocrystal gel in tackling imiquimod-induced psoriasis in rats, and thus it could be a novel promising therapy for psoriasis.
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DOI: 10.1007/s10787-023-01198-w
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