Niclosamide nanocrystalline temperature-sensitive gel as well as preparation method and application thereof
A technology of niclosamide and temperature-sensitive gel, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., can solve problems such as limitation, hemolysis and allergy, and achieve system toxicity The effect of high drug loading and simple preparation method
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Embodiment 1
[0044] 150 mg of niclosamide was dissolved in 4 ml of ethanol / acetone (50 / 50, v / v) mixed solvent, and 50 mg of poloxamer 188 was dissolved in 50 ml of deionized water. The aforementioned niclosamide solution was slowly added dropwise into the poloxamer 188 solution under magnetic stirring, and the organic solvent was removed by rotary evaporation to obtain a coarse suspension of niclosamide. Finally, the crude suspension of niclosamide was homogenized under high pressure for 20 times under a pressure of 1000 bar to obtain a nanocrystal suspension of niclosamide. Weigh about 0.25g of temperature-sensitive gel matrix, add 1ml of the niclosamide nanocrystal suspension prepared above, and magnetically stir overnight in an ice bath to obtain a niclosamide nanocrystal gel with a gel concentration of 20%. . The actual measured concentration of niclosamide is 2.558mg / ml, the particle size is 172nm, the PDI is 0.191, and the gel phase transition temperature is about 35°C.
Embodiment 2
[0046] 150 mg of niclosamide was dissolved in 4 ml of ethanol / acetone (50 / 50, v / v) mixed solvent, and 75 mg of poloxamer 188 was dissolved in 50 ml of deionized water. The aforementioned niclosamide solution was slowly added dropwise into the poloxamer 188 solution under magnetic stirring, and the organic solvent was removed by rotary evaporation to obtain a coarse suspension of niclosamide. Finally, the crude suspension of niclosamide was homogenized under high pressure for 20 times under a pressure of 1000 bar to obtain a nanocrystal suspension of niclosamide. Weigh about 0.25g of temperature-sensitive gel matrix, add 1ml of the niclosamide nanocrystal suspension prepared above, and magnetically stir overnight in an ice bath to obtain a niclosamide nanocrystal gel with a gel concentration of 20%. . The actual measured concentration of niclosamide is 2.417mg / ml, the particle size is 178nm, the PDI is 0.187, and the gel phase transition temperature is about 35°C.
Embodiment 3
[0048] 150 mg of niclosamide was dissolved in 4 ml of ethanol / acetone (50 / 50, v / v) mixed solvent, and 150 mg of poloxamer 188 was dissolved in 50 ml of deionized water. The aforementioned niclosamide solution was slowly added dropwise into the poloxamer 188 solution under magnetic stirring, and the organic solvent was removed by rotary evaporation to obtain a coarse suspension of niclosamide. Finally, the crude suspension of niclosamide was homogenized under high pressure for 20 times under a pressure of 1000 bar to obtain a nanocrystal suspension of niclosamide. Weigh about 0.25g of temperature-sensitive gel matrix, add 1ml of the niclosamide nanocrystal suspension prepared above, and magnetically stir overnight in an ice bath to obtain a niclosamide nanocrystal gel with a gel concentration of 20%. . The actual measured concentration of niclosamide is 2.397mg / ml, the particle size is 194nm, the PDI is 0.215, and the gel phase transition temperature is about 35°C.
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Abstract
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