Curcumin-loaded colloidal carrier system: formulation optimization, mechanistic insight, ex vivo and in vivo evaluation

Abstract

The present work investigated the topical delivery potential of nanoemulsion gel loaded with curcumin (CR). CR nanoemulsion (CR-NE) was prepared by spontaneous emulsification method using oil (Labrafac PG/glyceryl triacetate), surfactant:cosurfactant (S mix ) (tween 80/polyethylene glycol [PEG] 400) and water. The pseudo-ternary phase diagrams were constructed and thermodynamic stability testing was performed. Droplet size and zeta potential were evaluated using photon correlation spectroscopy and transmission electron spectroscopy. Six formulations selected with an average droplet size ≤70±2.72 nm showed a fourfold increase in skin permeation as compared to crude CR solution in oil. The formulation CR-NE4 having a flux of 117.04±2.32 µg/cm 2 /h and with maximum retention (42.87%) was selected, characterized (droplet size =41.13±3.34 nm and zeta potential =−33.1±1.45 mV), and incorporated into gel using carbopol-980 (1% w/v). Skin dynamics analyzed by confocal laser scanning microscopy showed maximum deposition of CR up to a depth of 86.98 µm and was in concordance with differential scanning calorimetry and Fourier transform infrared spectroscopy studies that confirmed lipid bilayer disruption, enhancing permeation. A 28-day anti-arthritic evaluation (body weight, paw edema, tibiotarsal joint thickness, TNF-α and IL-1β levels, and histopathology) on Freund’s complete adjuvant induced arthritic rat model after topical application of CR-NE gel in Wistar rats demonstrated substantial reversal of arthritic symptoms. Thus, CR-NE gel possesses potential for therapeutic effects locally in inflammatory arthritic disorders with improved topical bioavailability.

Effects of Carbopol^® 934 proportion on nanoemulsion gel for topical and transdermal drug delivery: a skin permeation study

“…The areas were then covered with gauze and an adhesive plaster. 17 An electric razor was used to clip the hair from the abdomen of the guinea pigs. The clipped areas were examined the next day, and guinea pigs with intact skin were chosen for the tests.…”

Current application of phytocompound-based nanocosmeceuticals for beauty and skin therapy

“…The aforementioned products prevent skin aging due to oxidative stress and premature aging. [69][70][71][72][73] The combination of polyphenols with retinols enhances skin protection. Other than nanosizing, few delivery systems have been used to develop nanoantiaging creams and lotions for the enhanced activity of bioactive compounds to deeper layers of skin.…”

“…Various nanodelivery techniques used in the formulation of cosmeceuticals are of solid lipid nanoparticles, nanostructured lipid carriers, liposomes, phytosomes, nanoemulsions, nanoniosomes, nanocapsules, and nanolipospheres. 4,57,70 Solid lipid nanoparticle-loaded resveratrol showed enhanced permeation in the porcine skin. 127 Similarly, colloidal silica emulsion loaded with quercetin also showed enhanced human skin permeation owing to the nanosizing of the compounds.…”

Phytoconstituents as pharmacotherapeutics in rheumatoid arthritis: challenges and scope of nano/submicromedicine in its effective delivery

“…In another study, curcumin loaded into nanoemulsion gel has shown fourfold higher skin permeation as compared to the curcumin solution in oil. Furthermore, antiarthritic evaluation on Freund's complete adjuvant‐induced arthritic rat model after application of curcumin nanogel in Wistar rats showed substantial removal of arthritic symptoms with enhanced topical availability at the site of application . Likewise, thymoquinone has several limitations which restrict its clinical applications.…”

“…Furthermore, antiarthritic evaluation on Freund's complete adjuvant-induced arthritic rat model after application of curcumin nanogel in Wistar rats showed substantial removal of arthritic symptoms with enhanced topical availability at the site of application. [83] Likewise, thymoquinone has several limitations which restrict its clinical applications. Polymeric nanoparticles have been developed with the help of poly(lactide-co-glycolide) (PLGA) with 97.5% entrapment efficiency revealed higher potency as compared to thymoquinone alone.…”