Quality by Design-Optimized Glycerosome-Enabled Nanosunscreen Gel of Rutin Hydrate

Abstract

Sunburn is caused by prolonged exposure to ultraviolet (UV) rays from the sun, resulting in redness of the skin as well as tenderness, swelling, and blistering issues. During the healing process, it can cause peeling, irritation, and some long-term effects, including premature aging, pigmentation, and a high risk of skin cancer. Rutin has antioxidant and anti-inflammatory effects, which could potentially reduce inflammation and soothe sunburned skin. The objective of the current proposal is to develop and create carbopol gel-encased glycerosomes for the treatment of sunburn. The Design of Expert (DoE) technique was used to optimize the proposed formulation and was subjected to various characterization parameters such as nanovesicles size, polydispersity index (PDI), surface charge, entrapment efficiency (EE), and surface morphology. The optimized rutin-loaded glycerosomes (opt-RUT-loaded-GMs) were further characterised for drug release, 2,2-Diphenyl-1-picrylhydrazyl (DPPH) assay, and confocal laser scanning microscopy (CLSM). The formulation showed sustained release, greater permeation into the skin, and good antioxidant activity. The dermatokinetic study of opt-RUT-loaded-GMs confirms that the Rutin hydrate had better retention in the epidermis as compared to the dermis, owing to its potential for long lasting protection after topical application. It was observed that the prepared formulation was stable, highly safe, and had good sun protection factor (SPF) values that could be used as a suitable option for topical drug administration to maximize the therapeutic efficacy of the drugs.

Would be Rutin a Feasible Strategy for Environmental-Friendly Photoprotective Samples? A Review from Stability to Skin Permeability and Efficacy in Sunscreen Systems

“…As previously discussed, rutin exhibits poor penetration/permeation through the skin, being retained within the stratum corneum and, therefore, being appropriate for topical formulations [54,[65][66][67]. The observed superficial action profile of rutin, related to its aglycone counterpart, aligns with the desired characteristics of sunscreens, which ideally should remain predominantly at the application site's surface [57,61,63,64,68]. Other factors, combined with the stability of this bioactive compound in diverse topical vehicles, support the incorporation of rutin in dermocosmetic products designed to protect the skin from UVA and UVB radiation [12,54,65].…”

“…The association of rutin with nanostructures has been used to aid the penetration of this active ingredient into deeper layers of the skin to improve the action of this compound [8,[58][59][60]. In vitro studies using nanostructures such as nanocrystal, glycerosomal, and microencapsulated nanostructured lipid carriers showed permeability enhancement of the active ingredient, demonstrating the potential of these nanocarriers for bioactive delivery [61][62][63][64]. Encapsulation in ethosomes was also found to improve rutin penetration ex vivo, which was attributed to the characteristics of the nanostructure, since these malleable vesicles can facilitate the passage of the active ingredient to deeper layers of the skin [20].…”

ULK1 Mediated Autophagy-Promoting Effects of Rutin-Loaded Chitosan Nanoparticles Contribute to the Activation of NF-κB Signaling Besides Inhibiting EMT in Hep3B Hepatoma Cells

“…[78][79][80] The final pellet with rCNPs was obtained after centrifuging the solution at 10,000 rpm for 15 mins at 4° C. The pellet was washed by centrifugation at 10,000 rpm for three times (15 mins each time) and resuspended in normal saline every time to remove unentrapped or free drug. [81][82][83] In addition, the final pellet obtained after the total 1 hour of centrifugation (4 times of 15 mins) was filtered using 0.45 and 0.22 micron filters and used for further experiments. This filtration may also aid in removal of any unwanted impurities, residues or unentrapped drug.…”