Target temperature control type polysaccharide-supporting long-circulating liposome-microbubble compound drug delivery system and preparation method thereof

A long-circulating liposome and drug delivery system technology, applied in liposome delivery, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of low coupling efficiency, low drug loading, poor stability, etc. The effect of drug dosage, good efficacy, and improved encapsulation efficiency

Active Publication Date: 2019-04-09
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of this system for polysaccharide antineoplastic drugs (especially water-soluble drug active ingredients) has the following problems: low coup

Method used

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  • Target temperature control type polysaccharide-supporting long-circulating liposome-microbubble compound drug delivery system and preparation method thereof
  • Target temperature control type polysaccharide-supporting long-circulating liposome-microbubble compound drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 1) Preparation of polysaccharide-loaded thermosensitive liposomes

[0037]Weigh 32mg dipalmitoylphosphatidylcholine (DPPC), 5mg monopalmitoylphosphatidylcholine (MPPC), 3mg distearoylphosphatidylethanolamine-polyethylene glycol (DSPE-mPEG2000) and 3mg distearyl Acylphosphatidylethanolamine-polyethylene glycol-biotin (DSPE-mPEG2000-biotin) was dissolved in 2 mL of chloroform previously added to a 50 mL centrifuge tube, and 4 mg of polysaccharide was weighed and dissolved in 1 mL of distilled water to obtain polysaccharide aqueous solution , the aqueous solution of polysaccharide polysaccharide is added to the chloroform that dissolves the phospholipid material (that is, the above-mentioned DPPC, MPPC, DSPE-mPEG2000 and DSPE-mPEG2000-biotin), and is ultrasonically emulsified with a probe for 2min under ice-bath conditions to form milky white W 1 / O type colostrum (that is, emulsion), the colostrum was added to 5mL distilled water, and ultrasonically emulsified for 3min un...

Embodiment 2

[0043] 1) Preparation of polysaccharide-loaded thermosensitive liposomes

[0044] Weigh 35mg dipalmitoylphosphatidylcholine (DPPC), 5mg monopalmitoylphosphatidylcholine (MPPC), 3mg distearoylphosphatidylethanolamine-polyethylene glycol (DSPE-mPEG2000) and 3mg distearyl Acylphosphatidylethanolamine-polyethylene glycol-biotin (DSPE-mPEG2000-biotin) was dissolved in 2 mL of chloroform previously added to a 50 mL centrifuge tube, and 5 mg of polysaccharide was weighed and dissolved in 1 mL of distilled water to obtain polysaccharide aqueous solution. Add the aqueous solution of polysaccharide polysaccharide to the chloroform in which the phospholipid materials (i.e. the above-mentioned DPPC, MPPC, DSPE-mPEG2000 and DSPE-mPEG2000-biotin) are dissolved, and ultrasonically emulsify with a probe for 3 minutes under ice bath conditions to form a milky white W 1 / O type colostrum (that is, emulsion), the colostrum is added to 5mL distilled water, and ultrasonically emulsified for 5min u...

Embodiment 3

[0050] 1) Preparation of polysaccharide-loaded thermosensitive liposomes

[0051] Weigh 30mg dipalmitoylphosphatidylcholine (DPPC), 5mg monopalmitoylphosphatidylcholine (MPPC), 4mg distearoylphosphatidylethanolamine-polyethylene glycol (DSPE-mPEG2000) and 4mg distearyl Acylphosphatidylethanolamine-polyethylene glycol-biotin (DSPE-mPEG2000-biotin) was dissolved in 2 mL of chloroform previously added to a 50 mL centrifuge tube, and 4 mg of polysaccharide was weighed and dissolved in 1 mL of distilled water to obtain polysaccharide aqueous solution. Add the aqueous solution of polysaccharide polysaccharide to the chloroform in which the phospholipid materials (i.e. the above-mentioned DPPC, MPPC, DSPE-mPEG2000 and DSPE-mPEG2000-biotin) are dissolved, and ultrasonically emulsify with a probe for 3 minutes under ice bath conditions to form a milky white W 1 / O type colostrum (that is, emulsion), the colostrum was added to 5mL distilled water, and ultrasonically emulsified for 3min ...

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Abstract

The invention discloses a target temperature control type polysaccharide-supporting long-circulating liposome-microbubble compound drug delivery system and a preparation method thereof. Ganoderma applanatum polysaccharide-supporting thermosensitive liposome prepared with a compound emulsified solvent evaporation method and perfluoropropane microbubbles prepared with a film dispersion method are taken as examples, liposome and microbubbles are connected with a biotin-avidin coupling method, and a ganoderma applanatum polysaccharide-supporting thermosensitive liposome-microbubble compound is prepared. The compound is used as the drug delivery system, efficient release of drugs in sub-high-temperature field local tissue can be realized by use of targeted blasting of microbubbles and local temperature control effects, the bioavailability of drugs can be improved, and residues of thermal ablated tumor are reduced.

Description

technical field [0001] The invention relates to a temperature-controlled liposome substance that can be used for drug delivery, in particular to a targeted temperature-controlled long-circulation thermosensitive liposome-microbubble complex. Background technique [0002] Tongue polysaccharide is an active ingredient extracted from the dry fruiting body of Tongue, which has been proven to have good anti-tumor activity and enhance the immune function of the body. Studies have shown that polysaccharides can regulate the activity of T cells, stimulate the autoimmune response in vivo, stimulate the secretion of IFN-γ and IL-2, or inhibit the production of TGF-β1, IL-10 and VEGF, thereby preventing the growth and development of tumors. However, there is still the problem of low oral drug availability. [0003] As a drug carrier, liposome has attracted much attention in recent years. Liposome encapsulates the drug in a bimolecular layer similar to the biological membrane structur...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/715A61K41/00A61K47/66A61P35/00A61P37/04
CPCA61K41/00A61K47/665A61K47/6911A61P35/00A61P37/04A61K31/715A61K2300/00
Inventor 袁佳妮罗文张云飞杨晓刘海静
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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