Tripterine nanostructure lipid carrier modified by lentiviral vector and appliance for preparing and treating prostatic cancer, lung cancer and breast cancer drug

Abstract

The invention discloses a tripterine nanostructure lipid carrier modified by lentiviral vector and preparation method and application thereof, wherein teh tripterine nanostructure lipid carrier modified by the lentiviral vector consists of tripterine and a lipid carrier, various components comprise 1 part by weight of tripterine, 0.5 to 10 parts by weight of lentiviral vector, 5 to 100 parts by weight of lipid blends, 0.5 to 20 parts by weight of emulsifier and 5 to 100 parts by weight of stabilizer. The tripterine nanostructure lipid carrier modified by the lentiviral vector can increase nanoparticles encapsulating rate to 78-90%. The tripterine nanostructure lipid carrier modified by the lentiviral vector uses oral administration, thereby promoting absorbing of the tripterine in a body, improving bioavailability, reducing administration dosage, reducing accumulation of the tripterine in the body at last, reducing toxic reaction by combining sustained release of a nanostructure lipid carrier, and improving clinical therapeutic effect of the tripterine at last.

Description

technical field

[0001] The invention belongs to the field of traditional Chinese medicine preparations, and relates to a nano-structure lipid carrier of tripteryglide modified by penetrating peptide, which is a nanostructure modified by penetrating peptide by loading tripteryglide, a triterpenoid monomer component of tripterygium wilfordii, on the membrane-penetrating peptide in a lipid carrier. The invention also relates to the application of the tripteryglide nanostructure lipid carrier modified by the penetrating peptide in the preparation of drugs for treating prostate cancer, lung cancer and breast cancer by oral administration. Background technique

[0002] Tripterine (Tripterine) is from Tripterygium genus Tripterygium ( Triperygium Wilfordii The compound of pentacyclic triterpene quinone structure isolated and purified in Hook f.). Molecular formula: C 29 h 38 o 4 , molecular weight: 450.61, CAS number: 34157-83-0, structural formula:

[0003]

[0004] Trip...

Examples

Embodiment 1

[0076] Preparation of tripterine nanostructured lipid carrier modified by penetrating peptide.

[0077] Prescription: tripterine 60mg, penetrating peptide SA-R 6 L 2 120mg, glyceryl distearate 720mg, isopropyl myristate 240mg, soybean lecithin 120mg, vitamin E polyethylene glycol succinate 120mg, poloxamer aqueous solution (1%, w / w) 100mL.

[0078] Preparation process: Heating and melting glyceryl distearate at 60°C, then adding isopropyl myristate, phospholipids, vitamin E polyethylene glycol succinate, penetrating peptide and tripterine, fully dissolved in Under the condition of vigorous stirring (4000r / min), disperse the molten liquid into 100mL water phase containing poloxamer (1%, w / w) at the same temperature to obtain colostrum, and emulsify the colostrum through a high-pressure homogenizer (500bar), cycle 3-6 times; then cool and solidify in the low-temperature water phase (0-2°C), and then the tripterine nanostructure lipid carrier modified by penetrating peptide ca...

Embodiment 2

[0080] Preparation of Tripteryglide Nanostructured Lipid Carrier Lyophilized Powder Modified by Penetrating Peptide

[0081]5g of mannitol was added to the penetrating peptide-modified tripterine nanostructured lipid carrier suspension prepared in Example 1 for lyophilization, and the resulting lyophilized powder had good redispersibility, and the nanoparticles after redispersion The particle size and potential are almost unchanged.

Embodiment 3

[0083] Preparation of Tripteryglide Nanostructured Lipid Carrier Tablets Modified by Penetrating Peptides (1000 Tablets)

[0084] Pass 366 g of membrane-penetrating peptide-modified tripteryglide nanostructured lipid carrier freeze-dried powder through an 80-mesh sieve, mix with 126 g of starch, add 40 g of 10% starch slurry to make a soft material, granulate with a 14-mesh sieve, and place After drying at 55°C, sieve through a 12-mesh sieve, add 40g of dry starch and 4g of magnesium stearate, mix well, and press into tablets to obtain the product. Each tablet contains tripterine 3 mg.

technical field

[0001] The invention belongs to the field of traditional Chinese medicine preparations, and relates to a nano-structure lipid carrier of tripteryglide modified by penetrating peptide, which is a nanostructure modified by penetrating peptide by loading tripteryglide, a triterpenoid monomer component of tripterygium wilfordii, on the membrane-penetrating peptide in a lipid carrier. The invention also relates to the application of the tripteryglide nanostructure lipid carrier modified by the penetrating peptide in the preparation of drugs for treating prostate cancer, lung cancer and breast cancer by oral administration. Background technique

[0002] Tripterine (Tripterine) is from Tripterygium genus Tripterygium ( Triperygium Wilfordii The compound of pentacyclic triterpene quinone structure isolated and purified in Hook f.). Molecular formula: C 29 h 38 o 4 , molecular weight: 450.61, CAS number: 34157-83-0, structural formula:

[0003]

[0004] Trip...

Examples

Embodiment 1

[0076] Preparation of tripterine nanostructured lipid carrier modified by penetrating peptide.

[0077] Prescription: tripterine 60mg, penetrating peptide SA-R 6 L 2 120mg, glyceryl distearate 720mg, isopropyl myristate 240mg, soybean lecithin 120mg, vitamin E polyethylene glycol succinate 120mg, poloxamer aqueous solution (1%, w / w) 100mL.

[0078] Preparation process: Heating and melting glyceryl distearate at 60°C, then adding isopropyl myristate, phospholipids, vitamin E polyethylene glycol succinate, penetrating peptide and tripterine, fully dissolved in Under the condition of vigorous stirring (4000r / min), disperse the molten liquid into 100mL water phase containing poloxamer (1%, w / w) at the same temperature to obtain colostrum, and emulsify the colostrum through a high-pressure homogenizer (500bar), cycle 3-6 times; then cool and solidify in the low-temperature water phase (0-2°C), and then the tripterine nanostructure lipid carrier modified by penetrating peptide ca...

Embodiment 2

[0080] Preparation of Tripteryglide Nanostructured Lipid Carrier Lyophilized Powder Modified by Penetrating Peptide

[0081]5g of mannitol was added to the penetrating peptide-modified tripterine nanostructured lipid carrier suspension prepared in Example 1 for lyophilization, and the resulting lyophilized powder had good redispersibility, and the nanoparticles after redispersion The particle size and potential are almost unchanged.

Embodiment 3

[0083] Preparation of Tripteryglide Nanostructured Lipid Carrier Tablets Modified by Penetrating Peptides (1000 Tablets)

[0084] Pass 366 g of membrane-penetrating peptide-modified tripteryglide nanostructured lipid carrier freeze-dried powder through an 80-mesh sieve, mix with 126 g of starch, add 40 g of 10% starch slurry to make a soft material, granulate with a 14-mesh sieve, and place After drying at 55°C, sieve through a 12-mesh sieve, add 40g of dry starch and 4g of magnesium stearate, mix well, and press into tablets to obtain the product. Each tablet contains tripterine 3 mg.

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