Composition for external application comprising transcription factor decoy as active ingredient
A technology of transcription factors and compositions, applied in the direction of medical preparations containing active ingredients, organic active ingredients, medical preparations with non-active ingredients, etc., can solve problems such as not being completely satisfactory
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Embodiment 1
[0191] Example 1: Non-aqueous liquid composition of NF-κB decoy
[0192]NF-κB decoys are compounds that are easily soluble in water, and it is difficult to prepare non-aqueous topical preparations with it. However, the NF-κB decoy can be dissolved in the following fatty acid-based ionic liquid to achieve liquefaction of the NF-κB decoy.
[0193] (1) Non-aqueous external preparation composition utilizing levulinic acid-based ionic liquid (single ionic liquid):
[0194] Levulinic acid and equimolar amounts of each of diethanolamine and triethanolamine were weighed out and mixed, and each resulting mixture was heated at 80° C. for 20 minutes to produce two kinds of levulinic acid-based ionic liquids.
[0195] About 10 mg of NF-κB decoy shown in SEQ ID NO: 1 was weighed out, added to about 1.0 g of each of the two levulinic acid-based ionic liquids, and the mixture was heated at 80° C. for about 30 minutes. After allowing the mixture to cool to room temperature, the state of b...
Embodiment 2
[0207] Example 2: Non-aqueous liquid agent composition (mixed ionic liquid) of NF-κB decoy
[0208] Since the transdermal absorbability of external preparations is affected by drug concentration and drug environment (whether near saturation, etc.), NF-κB decoy liquid formulations mainly based on mixed ionic liquid solutions of levulinic acid were prepared as described below. And, the solubility of NF-κB decoy in the mixed ionic liquid was also determined.
[0209] (1) Solubility (i) of NF-κB decoy in levulinic acid mixed ionic liquid:
[0210] A mixed ionic liquid is prepared, wherein triisopropanolamine levulinate is added in a weight ratio of 1 to 9 relative to the amount of triethanolamine levulinate as 1. The solubility of NF-κB decoy in these mixed ionic liquids was determined according to the method of Example 1. The results are shown in Tables 3-1 and 3-2 below.
[0211] [Table 3-1]
[0212]
[0213] [Note]
[0214] ● trietha: Triethanolamine
[0215] ●triiso...
Embodiment 3
[0254] Example 3: Ointment formulations of NF-κB decoys
[0255] The ionic liquid solution in which the bait was dissolved was mixed with the base of the external preparation to study the preparation of various external preparation compositions. First, the bait was mixed with an ointment base to create an ointment formulation of the bait, and the effect of the ionic liquid on the skin permeability of the bait was examined.
[0256] (1) The role of levulinic acid-based ionic liquids in ointment preparations:
[0257] Weigh out levulinic acid and triethanolamine and mix together in equimolar proportions. An appropriate amount of propyl gallate was added thereto, and the mixture was warmed at 80°C for 20 minutes. The viscous solution obtained was weighed at room temperature, and the NF-κB decoy shown in SEQ ID NO: 1 was added thereto, and the bait was thermally dissolved at 40° C. for 2 days to produce levulinic acid dissolved in the NF-κB decoy Ionic liquid solution of trieth...
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