Polymer-made-micel contained administration system through skin or mucosa

A drug delivery system and polymer glue technology, which are applied in the directions of drug devices, drug delivery, and pharmaceutical formulations, to achieve the effects of simple preparation method, easy realization, and promotion of transmission and absorption.

Inactive Publication Date: 2005-02-16
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The above literatures all use homopolymer nanoparticles to encapsulate or adsorb drugs to prepare transdermal drug delivery systems. There is no research on using block or graft copolymers to assemble micelles or nanoparticles to encapsulate or adsorb drugs for transdermal or mucosal drug delivery. and patent reports

Method used

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  • Polymer-made-micel contained administration system through skin or mucosa
  • Polymer-made-micel contained administration system through skin or mucosa
  • Polymer-made-micel contained administration system through skin or mucosa

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1 (preparation of polymer assembly micelles):

[0025] Dissolve 95mg of polyethylene glycol monomethyl ether-b-poly(D,L-lactic acid) block copolymer (block ratio 2000 / 1500) and 5mg of paclitaxel in 2mL of acetone, and heat to 60°C under nitrogen protection Evaporate for 2 hours to obtain the drug / copolymer solid mixture, dry it in vacuum at room temperature, preheat the drug / copolymer solid mixture in a constant temperature water bath at 60°C until it becomes a transparent gel, add 60°C double distilled water or phosphate buffer under stirring (PBS, pH 7.6) 10mL to form a transparent micellar solution, centrifuged, and freeze-dried to obtain paclitaxel-loaded polymer micelles (PMT) lyophilized powder. The drug loading of PMT measured by high pressure liquid phase method is 4.9%.

[0026] The same method was used to prepare PMTs with different drug loadings, and the results are listed in Table 1.

[0027] Theoretical drug loading

[0028] Note: The...

Embodiment 2

[0030] Take by weighing 0.1g of the PMT (drug loading 4.9%) lyophilized powder prepared by the method of Example 1, disperse it into 1mL distilled water to form the aqueous solution of PMT, and carry out the transdermal release experiment with the Franz diffusion cell in vitro, using a depilated large Rat abdominal skin (0.7cm 2 ), the receiving solution is a phosphate buffer solution with pH=7.4. In the same way, 1 mL of PMT aqueous solution containing the same amount of paclitaxel was prepared with PMT with a drug loading of 3.4% and 8.8%, and the percutaneous release experiment was carried out. The paclitaxel in the receiving solution was detected by HPLC. The result is as figure 1 shown.

[0031] During the transdermal release test of PMT aqueous solution, the receiving solution did not change significantly within the first 12 hours, and the receiving solution turned milky white after 24 hours. The transmission electron microscope photos of the PMT solution before relea...

Embodiment 3

[0036] The device and operation are the same as in Example 2, mix 4g of PEG3350 and 6g of PEG400 to form an ointment, and weigh 0.1g of PMT freeze-dried powder with a drug loading of 4.9% prepared in Example 1 and mix it with 1g of the ointment, and then apply it on Transdermal release experiments were performed on mouse skin. The result is as Figure 4 shown.

[0037] Figure 4 The result of curve A shows that PMT in ointment can also penetrate the skin, and the penetration amount is slightly lower than the aqueous solution of PMT.

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Abstract

The invention relates to a medicine supplying system through skin or mucous which containing polymer assembled glue beam, and which is made up of at least polymer assembled glue beam whose particle size is less than 500nm or hydrophilic or water ground substance, it includes pasting agent, soft plaster, gel agent, emulsification agent, water liquid agent, or suspending agent. The merits lie in: it uses polymer assembled glue beam technology to overcome obstacle of skin or mucous, advances the transmission and absorption of medicine through skin or mucous. The medicine supplying system is specially applied to medicine, multi-peptide, ion type medicine, polarized medicine, hydrophobic medicine, metal compound medicine and medicine with high molecular, protein, gene type biology high molecular medicine supplying.

Description

technical field [0001] The invention relates to a transdermal or mucous membrane drug delivery system containing polymer assembled micelles, which is a drug delivery technology through the skin or mucous membranes by using polymer assembled micelles. Background technique [0002] The transdermal drug delivery system allows the drug to enter the body circulation through the skin at a constant rate and for a long time, avoiding the "first-pass effect" of the drug, improving the bioavailability of the drug and reducing the damage to the stomach and liver of the drug. Explanation, easy to use and so on. However, due to the limitations of skin barriers, only a few transdermal drug delivery systems have been applied. Penetration enhancers, iontophoresis and other methods can overcome skin barriers to a certain extent, but these technologies are only suitable for some small molecule drugs, and long-term use will cause toxic and side effects. Liposome ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/10A61K47/34A61M37/00
Inventor 董岸杰邓联东李军
Owner TIANJIN UNIV
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