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

Naz Z, Ahmad FJ - Int J Nanomedicine (2015)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Nanomedicine Research Lab, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.

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 (Smix) (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.

No MeSH data available.


Related in: MedlinePlus

Comparative zeta size analysis and permeation study of selected CR-NEs.Notes: (A) Droplet size distribution analysis of selected curcumin-loaded nanoemulsions, CR-NE1, CR-NE2, CR-NE3, CR-NE4, CR-NE6, and CR-PLC; (B) comparative permeation profile of the same.Abbreviations: CR-NE, curcumin nanoemulsion; CR-PLC, curcumin placebo nanoemulsion; C-CR, crude curcumin solution in oil; hr, hour(s).
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f2-ijn-10-4293: Comparative zeta size analysis and permeation study of selected CR-NEs.Notes: (A) Droplet size distribution analysis of selected curcumin-loaded nanoemulsions, CR-NE1, CR-NE2, CR-NE3, CR-NE4, CR-NE6, and CR-PLC; (B) comparative permeation profile of the same.Abbreviations: CR-NE, curcumin nanoemulsion; CR-PLC, curcumin placebo nanoemulsion; C-CR, crude curcumin solution in oil; hr, hour(s).

Mentions: Six formulations, two each from Smix ratios of 2:1, 3:1, and 4:1 having an oil content (Labrafac PG: glyceryl triacetate =1:1) 9%–12% v/v and Smix range 50%–55% v/v, were selected and characterized for droplet size (Figure 2A). CR at a concentration of 0.25% w/v was mixed thoroughly with the oil phase. Then, the required amount of Smix and water was added under constant magnetic stirring.


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

Naz Z, Ahmad FJ - Int J Nanomedicine (2015)

Comparative zeta size analysis and permeation study of selected CR-NEs.Notes: (A) Droplet size distribution analysis of selected curcumin-loaded nanoemulsions, CR-NE1, CR-NE2, CR-NE3, CR-NE4, CR-NE6, and CR-PLC; (B) comparative permeation profile of the same.Abbreviations: CR-NE, curcumin nanoemulsion; CR-PLC, curcumin placebo nanoemulsion; C-CR, crude curcumin solution in oil; hr, hour(s).
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4498720&req=5

f2-ijn-10-4293: Comparative zeta size analysis and permeation study of selected CR-NEs.Notes: (A) Droplet size distribution analysis of selected curcumin-loaded nanoemulsions, CR-NE1, CR-NE2, CR-NE3, CR-NE4, CR-NE6, and CR-PLC; (B) comparative permeation profile of the same.Abbreviations: CR-NE, curcumin nanoemulsion; CR-PLC, curcumin placebo nanoemulsion; C-CR, crude curcumin solution in oil; hr, hour(s).
Mentions: Six formulations, two each from Smix ratios of 2:1, 3:1, and 4:1 having an oil content (Labrafac PG: glyceryl triacetate =1:1) 9%–12% v/v and Smix range 50%–55% v/v, were selected and characterized for droplet size (Figure 2A). CR at a concentration of 0.25% w/v was mixed thoroughly with the oil phase. Then, the required amount of Smix and water was added under constant magnetic stirring.

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Nanomedicine Research Lab, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.

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 (Smix) (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.

No MeSH data available.


Related in: MedlinePlus