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Novel formulation and evaluation of a Q10-loaded solid lipid nanoparticle cream: in vitro and in vivo studies.

Farboud ES, Nasrollahi SA, Tabbakhi Z - Int J Nanomedicine (2011)

Bottom Line: A simple cream of CoQ10 and a cream containing CoQ10-loaded SLNs were prepared and compared on volunteers aged 20-30 years.In vitro release profiles of CoQ10 from simple cream, SLN alone, and CoQ10-loaded SLN cream showed prolonged release for SLNs compared with the simple cream, whereas there was no significant difference between SLN alone and SLN in cream.In vivo skin hydration and elasticity studies on 25 volunteers suggested good dermal penetration and useful activity of Q10 on skin as a hydratant and antiwrinkle cream.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran. farbod@sina.tums.ac.ir

ABSTRACT
Solid lipid nanoparticles (SLNs) of coenzyme Q10 (CoQ10) were formulated by a high-pressure homogenization method. The best formulation of SLN dispersion consisted of 13% lipid (cetyl palmitate or stearic acid), 8% surfactant (Tween 80 or Tego Care 450), and water. Stability tests, particle size analysis, differential scanning calorimetry, transmission electron microscopy, and release study were conducted to find the best formulation. A simple cream of CoQ10 and a cream containing CoQ10-loaded SLNs were prepared and compared on volunteers aged 20-30 years. SLNs with particle size between 50 nm and100 nm exhibited the most suitable stability. In vitro release profiles of CoQ10 from simple cream, SLN alone, and CoQ10-loaded SLN cream showed prolonged release for SLNs compared with the simple cream, whereas there was no significant difference between SLN alone and SLN in cream. In vitro release studies also demonstrated that CoQ10-loaded SLN and SLN cream possessed a biphasic release pattern in comparison with simple cream. In vivo skin hydration and elasticity studies on 25 volunteers suggested good dermal penetration and useful activity of Q10 on skin as a hydratant and antiwrinkle cream.

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Related in: MedlinePlus

Differential scanning calorimetry thermogram of sample A (stearic acid), sample B (coenzyme Q10), sample C (solid lipid nanoparticle), and sample D (Q10-loaded solid lipid nanoparticle).
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f3-ijn-6-611: Differential scanning calorimetry thermogram of sample A (stearic acid), sample B (coenzyme Q10), sample C (solid lipid nanoparticle), and sample D (Q10-loaded solid lipid nanoparticle).

Mentions: We used DSC for detecting potential drug-excipient incompatibilities as well as melting and recrystallization behavior of crystalline materials like SLNs. As depicted in Figure 3, the DSC profiles of stearic acid as a solid lipid component of SLN formulation showed apparent endothermic peaks at about 63°C. We detected the melting point of CoQ10 at 54°C. The profile of the lyophilized powder of Q10-loaded SLN showed a single peak around 57°C, whereas the SLN without Q10 had an endothermic peak at 58°C. The height of the endotherm in the thermogram of SLN-containing Q10 was less than that in SLN without Q10, suggesting loss of crystallinity of the lipids and Q10 after incorporation into SLN.9 During the production procedure, Q10 was dissolved in the melted lipid phase. Stearic acid showed one peak at 63°C, indicating no polymorphic forms.


Novel formulation and evaluation of a Q10-loaded solid lipid nanoparticle cream: in vitro and in vivo studies.

Farboud ES, Nasrollahi SA, Tabbakhi Z - Int J Nanomedicine (2011)

Differential scanning calorimetry thermogram of sample A (stearic acid), sample B (coenzyme Q10), sample C (solid lipid nanoparticle), and sample D (Q10-loaded solid lipid nanoparticle).
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3107720&req=5

f3-ijn-6-611: Differential scanning calorimetry thermogram of sample A (stearic acid), sample B (coenzyme Q10), sample C (solid lipid nanoparticle), and sample D (Q10-loaded solid lipid nanoparticle).
Mentions: We used DSC for detecting potential drug-excipient incompatibilities as well as melting and recrystallization behavior of crystalline materials like SLNs. As depicted in Figure 3, the DSC profiles of stearic acid as a solid lipid component of SLN formulation showed apparent endothermic peaks at about 63°C. We detected the melting point of CoQ10 at 54°C. The profile of the lyophilized powder of Q10-loaded SLN showed a single peak around 57°C, whereas the SLN without Q10 had an endothermic peak at 58°C. The height of the endotherm in the thermogram of SLN-containing Q10 was less than that in SLN without Q10, suggesting loss of crystallinity of the lipids and Q10 after incorporation into SLN.9 During the production procedure, Q10 was dissolved in the melted lipid phase. Stearic acid showed one peak at 63°C, indicating no polymorphic forms.

Bottom Line: A simple cream of CoQ10 and a cream containing CoQ10-loaded SLNs were prepared and compared on volunteers aged 20-30 years.In vitro release profiles of CoQ10 from simple cream, SLN alone, and CoQ10-loaded SLN cream showed prolonged release for SLNs compared with the simple cream, whereas there was no significant difference between SLN alone and SLN in cream.In vivo skin hydration and elasticity studies on 25 volunteers suggested good dermal penetration and useful activity of Q10 on skin as a hydratant and antiwrinkle cream.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran. farbod@sina.tums.ac.ir

ABSTRACT
Solid lipid nanoparticles (SLNs) of coenzyme Q10 (CoQ10) were formulated by a high-pressure homogenization method. The best formulation of SLN dispersion consisted of 13% lipid (cetyl palmitate or stearic acid), 8% surfactant (Tween 80 or Tego Care 450), and water. Stability tests, particle size analysis, differential scanning calorimetry, transmission electron microscopy, and release study were conducted to find the best formulation. A simple cream of CoQ10 and a cream containing CoQ10-loaded SLNs were prepared and compared on volunteers aged 20-30 years. SLNs with particle size between 50 nm and100 nm exhibited the most suitable stability. In vitro release profiles of CoQ10 from simple cream, SLN alone, and CoQ10-loaded SLN cream showed prolonged release for SLNs compared with the simple cream, whereas there was no significant difference between SLN alone and SLN in cream. In vitro release studies also demonstrated that CoQ10-loaded SLN and SLN cream possessed a biphasic release pattern in comparison with simple cream. In vivo skin hydration and elasticity studies on 25 volunteers suggested good dermal penetration and useful activity of Q10 on skin as a hydratant and antiwrinkle cream.

Show MeSH
Related in: MedlinePlus