Nanocrystalline of hydrophobic drug, as well as preparation and application methods of nanocrystalline
A technology of hydrophobic drugs and nanocrystals, which is applied in the field of insoluble hydrophobic drug nanocrystals and insoluble hydrophobic drug nanocrystals, can solve the problems of decomposition loss of effective components of drugs, drug pollution, and hydrophobic and insoluble drugs, and achieves good general applicability. high drug loading, narrow particle size distribution
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[0059] Example 1
[0060] A paclitaxel nanocrystal preparation is prepared by the following method:
[0061] (1) Dissolve 20 mg of paclitaxel in 100 μL of dichloromethane and mix with 10 mL of 0.1 wt% poloxamer The aqueous solution of F127 was mixed; the emulsification treatment was carried out by ultrasonic with a power of 20W to obtain an O / W emulsion with paclitaxel dissolved in the oil phase;
[0062] (2) soak the O / W emulsion obtained in step (1) in liquid nitrogen to solidify, then immediately transfer it to a freeze dryer for drying for 48 hours, remove the solvent molecules therein, and obtain a crude paclitaxel nanocrystal, which is then subjected to repeated Resuspension-centrifugation-resuspension for purification to obtain paclitaxel nanocrystal products, which are recorded as NPs;
[0063] figure 1 It is a transmission electron microscope (TEM) photograph of the paclitaxel nanocrystals (NPs) in Example 1; the prepared paclitaxel nanocrystals have an average pa...
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[0064] Example 2
[0065] A nanocrystal of iRGD functionalized paclitaxel, the difference between its preparation method and Example 1 is only: Full or partial replacement of F127 with iRGD-modified poloxamers F127, the obtained iRGD functionalized paclitaxel nanocrystals were denoted as iNPs.
[0066] figure 2 This is the TEM image of the iRGD functionalized paclitaxel nanocrystals (iNPs) in Example 2; the prepared iRGD functionalized paclitaxel nanocrystals have an average particle size of 71.3 nm and a drug loading of 94.33 wt% respectively.
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[0067] Example 3
[0068] A paclitaxel nanocrystal preparation is prepared by the following method:
[0069] (1) 1 mg of paclitaxel was dissolved in 1 mL of dichloromethane, and mixed with 1 mL of 2.0 wt% poloxamer The aqueous solution of F127 was mixed and emulsified by ultrasonic with a power of 100W to obtain an O / W emulsion with paclitaxel dissolved in the oil phase;
[0070] (2) soak the O / W emulsion obtained in step (1) in liquid nitrogen to solidify, then immediately transfer it to a freeze dryer for drying for 48 hours, remove the solvent molecules therein, and obtain a crude paclitaxel nanocrystal, which is then subjected to repeated Resuspension-centrifugation-resuspension for purification to obtain paclitaxel nanocrystal products, which are recorded as NDs;
[0071] image 3 It is the TEM image of the paclitaxel nanocrystals (NDs) in Example 3; the prepared paclitaxel nanocrystals have an average particle size of 8.6 nm and a drug loading of 80.57 wt% respective...
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