Ternary composite nano system based on methoxy polyethylene glycol-polylactic acid and application of ternary composite nano system

A technology of methoxy polyethylene glycol and polyethylene glycol, applied in the field of pharmaceutical preparations, can solve systemic toxicity, poor immediate release targeting, low drug loading and encapsulation efficiency, and inability to effectively encapsulate drugs and other problems to achieve the effect of increasing the efficacy of the drug, prolonging the circulation time in the body, and increasing the bioavailability

Inactive Publication Date: 2018-05-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the binary composite nanosystem based on MPP has the following limitations: (1) the particle size is too large
In the MPP binary system, because the interaction between MPP and another polymer is often weak, the nanosystem is relatively loose, and the drug in the carrier is easy to release during the preparation process and blood circulation, which is not conducive to its reaching the lesion. play a therapeutic role
(3) Drug loading and encapsulation efficiency are not high
In the MPP binary system, the weak force between MPP and another polymer makes the nanosystem relatively loose. At the same t

Method used

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  • Ternary composite nano system based on methoxy polyethylene glycol-polylactic acid and application of ternary composite nano system
  • Ternary composite nano system based on methoxy polyethylene glycol-polylactic acid and application of ternary composite nano system
  • Ternary composite nano system based on methoxy polyethylene glycol-polylactic acid and application of ternary composite nano system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: Preparation of MPP / TPGS / POL124 ternary composite nanosystem

[0046]Process I: Weigh an appropriate amount of MPP, TPGS, and POL124 and dissolve them in water respectively. The ratio of the total weight of MPP, TPGS, and POL124 to the weight of water is 3:1000, and the weight ratio of MPP, TPGS, and POL124 is 2:1:1, and stir for 1 hour , ultrasonication for 30min, dialysis for 24h, and 0.8μm microporous membrane filtration to obtain a ternary composite nanosystem based on MPP / TPGS / POL124.

[0047] Process II: Weigh an appropriate amount of MPP, TPGS, and POL124 and dissolve them in acetone, methanol, and methanol respectively. The weight ratio of MPP to acetone is 6:1000, the weight ratio of TPGS to methanol is 3:1000, and the weight ratio of POL124 to methanol is 3 : 1000, the weight ratio of MPP, TPGS and POL124 is 2:1:1, acetone and methanol are removed by rotary evaporation, vacuum dried for 12 hours after film formation, vigorously stirred with water ...

Embodiment 2

[0048] Example 2: Preparation of MPP / 4-arm-PEG-TPGS / POL185 ternary composite nanosystem loaded with indomethacin

[0049] Process I: Weigh an appropriate amount of MPP, 4-arm-PEG-TPGS, and POL185 and dissolve them in water respectively. The ratio of the total weight of MPP, 4-arm-PEG-TPGS, and POL185 to the weight of water is 30:1000. MPP, 4-arm -The weight ratio of PEG-TPGS to POL185 is 5:2:1. Weigh an appropriate amount of indomethacin and dissolve it in ethanol. The weight ratio of indomethacin to ethanol is 15:1000. Indomethacin and MPP / 4- The weight ratio of arm-PEG-TPGS / POL185 is 3:20, slowly add the indomethacin solution dropwise into the MPP / 4-arm-PEG-TPGS / POL185 solution, stir at room temperature for 2h, ultrasonic for 30min, dialyze for 24h, 0.8 The MPP / 4-arm-PEG-TPGS / POL185 ternary composite nanosystem loaded with indomethacin was obtained by filtering with a microporous membrane of μm.

[0050] Process II: Weigh an appropriate amount of MPP, 4-arm-PEG-TPGS, and PO...

Embodiment 3

[0051] Example 3: Preparation of MPP / TLA / POL238 ternary composite nanosystem loaded with lansoprazole and octreotide

[0052] Process I: Weigh an appropriate amount of MPP, TLA, and POL238 and dissolve them in water respectively. The ratio of the total weight of MPP, TLA, and POL238 to the weight of water is 50:1000, and the weight ratio of MPP, TLA, and POL238 is 10:3:4. A suitable amount of lansoprazole is dissolved in dimethylformamide, and an appropriate amount of octreotide is taken and dissolved in water. The weight ratio of lansoprazole and dimethylformamide is 20: 1000, and the weight ratio of octreotide and water is 15: 1000. The weight ratio of lansoprazole and octreotide is 1: 1, and the weight ratio of the total weight of lansoprazole and octreotide to MPP / TLA / POL238 is 1: 3, and the solution of lansoprazole and octreotide is slowly added dropwise to MPP / TLA / POL238 solution, stirred at room temperature for 2 hours, ultrasonicated for 40 minutes, dialyzed for 12 ho...

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Abstract

The invention relates to a ternary composite nano system based on methoxy polyethylene glycol-polylactic acid/polyethylene glycol vitamin E succinate and a derivative thereof/poloxamer . The ternary composite nano system has a diversified structure and is used for carrying out single loading or multidrug co-loading on various types of hydrophobic and hydrophilic drugs, the particle size is 50 to 100 nm, and the drug loading capacity and the encapsulation efficiency are high. The ternary composite nano system can be swallowed into cells through passive targeting of EPR (Enhanced Permeability and Retention Effect), excretion of MDR (Multidrug Resistance) protein on drugs can be avoided, and meanwhile, the polyethylene glycol vitamin E succinate and the derivative thereof have different-mechanism anti-MDR function with the poloxamer, so that the ternary composite nano system is capable of realizing mutual supplementation of multiple different anti-MDR mechanisms, and has a better anti-MDReffect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a ternary composite nano system based on methoxypolyethylene glycol-polylactic acid and its application. Background technique [0002] Multidrug resistance (MDR) refers to the long-term exposure of tumor cells to a certain chemotherapeutic drug, which not only produces resistance to this chemotherapeutic drug, but also produces cross-resistance to other chemotherapeutic drugs with different structures and functions. . At present, the occurrence of multidrug resistance is not limited to tumor chemotherapy drugs, anti-infective drugs and a variety of oral drugs also have MDR phenomenon, which greatly reduces the efficacy of drugs. The causes of MDR are extremely complex, and the overexpression of the ABC (Adenosinetriphosphate-binding cassette, ABC) membrane transport pump is the most important reason for the generation of MDR. The ABC family related to MDR has 48 members....

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/22A61K47/10A61K9/107
Inventor 姚静张萍苏纳特刘腾飞徐程熊慧
Owner CHINA PHARM UNIV
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