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Nanostructured lipid carriers loaded with CoQ10

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huang yung chi

on 8 January 2014

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Transcript of Nanostructured lipid carriers loaded with CoQ10

Nanostructured lipid carriers loaded with CoQ10
Experiment
Method:analyzed

*Viability

*Intracellular reactive oxygen species (ROS)

*Oxidative DNA damage

*Mitochondrial functionality in human dermal fibroblasts (HDF)

Experiment
Result :

*NLC alone, whether exposed or not exposed to UVA

*Decrease in cell viability associated with enhanced oxidative stress

*Did not lead to oxidative DNA damage nor mitochondrial impairment.

Reduced CoQ10-NLC
*Reduced CoQ10-NLC,differently from oxidized CoQ10-NLC

*Counteract UVA-associated mitochondrial depolarization

*Suggesting a potential role of this molecule in antiageing cosmetological formulations
SLN-The first generation
優點:
*High biocompatibility、good physical stability

*Possibility of controlled release of drug and active substances

*Large scale production

*Cheap raw materials

Nanostructured lipid carriers (NLC)
Function:
*Drug delivery
*Promote increased bioavailability
*Epithelial penetration of lipophilic compounds

Drawback:
*Cytotoxicity(especially under in vivo usage conditions)

bioactive compounds
*Biological activities (antioxidants, anti inflammatory, enzymatic cofactors)

Application:
*Pharmaceutical

*Cosmeceutical preparations

*Lipophilic compounds such as tocotrienols, tocopherols, carotenoids, polyphenols, quinones and sterols


Application
缺點:

*Drug expulsion phenomena

*Particles concentration in the aqueous dispersion ranging from about 1% to a maximum of only 30%

*Insufficient total drug payload


*Combine the advantage of colloidal drug carrier systems,but the drawbacks are avioded or minimized

*Blend of solid and liquid lipid

*Minimizing drug expulsion phenomena

*Increasing drug loading

*Promoting the bioavailability

*The dermal delivery of CoQ10


NLC-the second generation
The Feature of CoQ10
*The fundamental role in mitochondrial bioenergetics

*Well-acknowledged antioxidant properties

*Increase production of basal membrane components

*Fibroblast proliferation

*Protect cells against oxidative damage.

Clinical Applications:
*Cardiovascular disease

*Neuromuscular degenerative diseases

*Infertility.

Cosmetic Applications:
*Reduce photoaging in vivo with a corresponding decrease in wrinkle depth

Particle size distribution and zeta potential measurements
Cell viability assay

Cell cultures
NLC preparation
1. Precirol ◎ATO 5(5.1g) was melted at 75°C + Miglyol◎812(2.25g) + CoQ10(500g)

2.Dispersed in the hot(75°C) surfactant solution(Lutrol ©F68,4% w/w and Tween 80,3% w/w)and use a high-speed stirrer at 8000 rpm.

3.Use a UP 400 S and maintaining the temperature at least 5°C.

4.Cooled in ice bath and dispersed in cold water(400ml) under high-speed homogenization at 8000 rpm for 5 min.

MATERIALS
*Precirol ©ATO 5

*Miglyol©812

*Lutrol ©F68

*Tween 80

*Reduced and oxidized CoQ10

CoenzymeQ10 supplementation
UVA exposure
Comet Assay
Cell Viability Assay
Intracellular ROS assay
Results
Preparation and characterization of CoQ10ox/red-NLC
Mitochondrial membrane potential assay
線粒體膜電位測定法
Intracellular ROS assay
Comet assay
Discussion
PCS analyses
This test evaluates mitochondrial function as a measurement of cell viability, since intracellular dehydrogenases located within the mitochondria of only viable cells are able to reduce MTT leading to the formation of purple formazan crystals.

In order to determine the possible genotoxic effects of NLC, DNA damage in terms of double strand breaks (DSBs), single strand breaks (SSBs) and oxidized purine bases was studied.
NLC可能會因為奈米顆粒裡面有抗氧化的成分而干擾細胞內氧化還原反應的平衡,所以說,如果減少輔酶Q10,不管有沒有帶有氧化輔酶Q10的NLC都會使氧化還原反應增加改變

在抗氧化劑方面,輔酶Q10脂質體比輔酶Q10氧化SLN更加促進傳輸系統傳輸

對於使用NLC上,藥物傳輸和生物相容性的研究占有一個很重要的角色


*SLN和NLC使用頻繁或在劑量高下可能會釋放細胞毒性的降解產物;在低濃度下,不一定導致細胞死亡。

*在UVA照射下,NLC處理過細胞比未處理過的細胞易存活。


*輔酶Q10(泛醌)的還原形式對NLC是一個好的保護作用,但是所採用的輔酶Q10濃度減少,是不能保護細胞免受由紫外線照射氧化。
黃永琪、陳于臻、東颯夏、李姿葶、王意茹
Mitochondrial membrane potential assay
資料出處
International Journal of Pharmaceutics 455 (2013) 348– 356
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