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The preparation of 3,5-dihydroxy-4-isopropylstilbene nanoemulsion and in vitro release.

Zhang Y, Gao J, Zheng H, Zhang R, Han Y - Int J Nanomedicine (2011)

Bottom Line: The nanoemulsion was also determined by FT-Raman spectroscopy.The DHPS nanoemulsion demonstrated good stability and stable physical and chemical properties.The nanoemulsion dramatically improved the transdermal release of DHPS (from 8.02 μg · cm(-2) to 273.15 μg · cm(-2)) and could become a favorable new dosage form for DHPS.

View Article: PubMed Central - PubMed

Affiliation: College of Chemistry and Enviromental Science, Hebei University, Baoding, China.

ABSTRACT
We have reported a novel procedure to prepare 3,5-dihydroxy-4-isopropylstilbene (DHPS) nanoemulsion, using a low-energy emulsification method. Based on the phase diagram, the optimum prescription of nanoemulsion preparation was screened. With polyoxyethylenated castor oil (EL-40) as the surfactant, ethanol as the co-surfactant, and isopropyl myristate (IPM) as the oil phase, the DHPS nanoemulsion was obtained with a transparent appearance, little viscosity, and spherically uniform distribution verified by transmission electron microscopy and laser scattering analyzer. The nanoemulsion was also determined by FT-Raman spectroscopy. The DHPS nanoemulsion demonstrated good stability and stable physical and chemical properties. The nanoemulsion dramatically improved the transdermal release of DHPS (from 8.02 μg · cm(-2) to 273.15 μg · cm(-2)) and could become a favorable new dosage form for DHPS.

Show MeSH
The ternary phase diagram under different conditions.Abbreviation: L2, O/W microemulsion area.
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f2-ijn-6-649: The ternary phase diagram under different conditions.Abbreviation: L2, O/W microemulsion area.

Mentions: A good co-surfactant can improve the dispersibility of droplets and drug absorption.39 EL-40 was combined with four different co-surfactants including i-propanol, 1,2-propanediol, n-butanol and ethanol, in different mass ratios, respectively. The results are shown in Figure 2. All four co-surfactants can promote the formation of nanoemulsions when Km is taken as 9:1; the nanoemulsion region was the largest when 1,2-propanediol was used for the co-surfactant. No clear transitional phase inversion appears when Km is taken as 8:2 and n-butanol is taken as co-surfactant. At a Km of 7:3, only ethanol can arrange EL-40 in pairs to generate phase inversion. When i-propanol served as the co-surfactant, the area of nanoemulsion was relatively small and, in comparison, the areas of nanoemulsion in phase diagrams are larger when 1,2-propanediol or ethanol are used. Among these two co-surfactants, a larger amount of surfactants are required when 1,2-propanediol is used owing to its lower solubility of DHPS, which may be harmful to the skin. Therefore because ethanol is non-irritating, has gentle properties, no toxicity to the human body, and is the most common and readily available reagent, it was chosen to be the co-surfactant.


The preparation of 3,5-dihydroxy-4-isopropylstilbene nanoemulsion and in vitro release.

Zhang Y, Gao J, Zheng H, Zhang R, Han Y - Int J Nanomedicine (2011)

The ternary phase diagram under different conditions.Abbreviation: L2, O/W microemulsion area.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3107722&req=5

f2-ijn-6-649: The ternary phase diagram under different conditions.Abbreviation: L2, O/W microemulsion area.
Mentions: A good co-surfactant can improve the dispersibility of droplets and drug absorption.39 EL-40 was combined with four different co-surfactants including i-propanol, 1,2-propanediol, n-butanol and ethanol, in different mass ratios, respectively. The results are shown in Figure 2. All four co-surfactants can promote the formation of nanoemulsions when Km is taken as 9:1; the nanoemulsion region was the largest when 1,2-propanediol was used for the co-surfactant. No clear transitional phase inversion appears when Km is taken as 8:2 and n-butanol is taken as co-surfactant. At a Km of 7:3, only ethanol can arrange EL-40 in pairs to generate phase inversion. When i-propanol served as the co-surfactant, the area of nanoemulsion was relatively small and, in comparison, the areas of nanoemulsion in phase diagrams are larger when 1,2-propanediol or ethanol are used. Among these two co-surfactants, a larger amount of surfactants are required when 1,2-propanediol is used owing to its lower solubility of DHPS, which may be harmful to the skin. Therefore because ethanol is non-irritating, has gentle properties, no toxicity to the human body, and is the most common and readily available reagent, it was chosen to be the co-surfactant.

Bottom Line: The nanoemulsion was also determined by FT-Raman spectroscopy.The DHPS nanoemulsion demonstrated good stability and stable physical and chemical properties.The nanoemulsion dramatically improved the transdermal release of DHPS (from 8.02 μg · cm(-2) to 273.15 μg · cm(-2)) and could become a favorable new dosage form for DHPS.

View Article: PubMed Central - PubMed

Affiliation: College of Chemistry and Enviromental Science, Hebei University, Baoding, China.

ABSTRACT
We have reported a novel procedure to prepare 3,5-dihydroxy-4-isopropylstilbene (DHPS) nanoemulsion, using a low-energy emulsification method. Based on the phase diagram, the optimum prescription of nanoemulsion preparation was screened. With polyoxyethylenated castor oil (EL-40) as the surfactant, ethanol as the co-surfactant, and isopropyl myristate (IPM) as the oil phase, the DHPS nanoemulsion was obtained with a transparent appearance, little viscosity, and spherically uniform distribution verified by transmission electron microscopy and laser scattering analyzer. The nanoemulsion was also determined by FT-Raman spectroscopy. The DHPS nanoemulsion demonstrated good stability and stable physical and chemical properties. The nanoemulsion dramatically improved the transdermal release of DHPS (from 8.02 μg · cm(-2) to 273.15 μg · cm(-2)) and could become a favorable new dosage form for DHPS.

Show MeSH