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Low molecular weight chitosan modified liposomes and preparation method thereof

A technology of low molecular weight and chitosan, which is applied in the direction of liposome delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of being insoluble in water, and achieve convenient preparation methods and improved Bioavailability, effect of prolonging action time

Inactive Publication Date: 2009-04-15
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But the disadvantage is that it is insoluble in water under physiological conditions

Method used

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  • Low molecular weight chitosan modified liposomes and preparation method thereof
  • Low molecular weight chitosan modified liposomes and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Phospholipids 500mg

[0042] Cholesterol 100mg

[0043] Phosphatidylserine 25mg

[0044] Low molecular weight chitosan (molecular weight 150mg

[0045] 5000)

[0046] Calcitonin 50mg

[0047] water 25mL

[0048] Glucose 400mg

[0049]Mannitol 1000mg

[0050] Alpha-Tocopherol 10mg

[0051] Preparation method: Dissolve the prescription amount of phospholipids, cholesterol, phosphatidylserine, calcitonin and α-tocopherol in an appropriate amount of ethanol, put it in a round bottom flask, rotatively evaporate the ethanol to completely evaporate, and vacuum dry for 12 hours to form a film; Dissolve glucose and mannitol in 25mL water to obtain the water phase; take 20mL of the water phase and place it in a round-bottomed flask with phospholipid film formation, shake it sufficiently to disperse the film into a liposome suspension, put it in a high-pressure milk homogenizer, and Cycle 8 times under 600Bar pressure; dissolve the prescribed amount of low-molecular-weight...

Embodiment 2

[0053] Phospholipids 900mg

[0054] Low molecular weight chitosan (molecular weight 10mg

[0055] 4000)

[0056] Topotecan 10mg

[0057] Sucrose 80mg

[0058] Preparation method: Prescribed amount of phospholipids, topotecan and 10 mL of water were emulsified in a high-shear emulsifier for 7 minutes to obtain colostrum; dissolved sucrose in 5 mL of water, added the above-mentioned colostrum and mixed evenly, and placed in a high-pressure milk homogenizer. Circulate 8 times under 600Bar pressure to obtain liposome suspension; dissolve the prescribed amount of low molecular weight chitosan in 1mL deionized water, slowly add it to the above liposome under stirring, stir at room temperature for 20min, freeze-dry to remove water , that is.

Embodiment 3

[0060] Phospholipids 240mg

[0061] Cholesterol 650mg

[0062] Docetaxel 20mg

[0063] Low molecular weight chitosan (molecular weight 10mg

[0064] 4000)

[0065] Sucrose 80mg

[0066] Preparation method: Dissolve the prescribed amount of phospholipids, cholesterol and docetaxel in an appropriate amount of ethanol, put it in a round-bottomed flask, evaporate the ethanol completely by rotary evaporation, and dry it in vacuum for 12 hours to form a film; dissolve the prescribed amount of glucose and mannitol in 25mL Water to obtain the aqueous phase; take 20mL of the aqueous phase and place it in a round-bottomed flask with phospholipid film formation, shake it sufficiently to disperse the film into a liposome suspension, place it in a high-pressure milk homogenizer, and circulate it 8 times under a pressure of 600 Bar; Dissolve low-molecular-weight chitosan in 5 mL of water, slowly add it into the liposome under stirring, stir at room temperature for 20 minutes, freeze-dry...

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Abstract

The invention relates to the field of pharmaceutical preparation, and particularly discloses a novel medicinal carrier, namely a low molecular weight chitosan modified liposome and a preparation method thereof. The low molecular weight chitosan modified liposome consists of phospholipid, cholesterol, low molecular weight chitosan, a medicine and other additives. The carrier can be combined with the medicine so as to form pharmaceutical preparations for clinic application. Compared with the prior liposome, the low molecular weight chitosan modified liposome has the advantages that the low molecular weight chitosan modified liposome has unique characteristics, can improve the absorption and transportation of the medicine, the bioavailability, the slow-releasing and long-acting action, can realize the targeted administration action, reduce the toxic and side effects of the medicine, decrease the administration frequency, improve the compliance of a patient and facilitate the administration. In addition, the preparation method has the advantages that the preparation method is convenient and is suitable for industrialized production, and has extremely high application value in the field of pharmaceutical preparation.

Description

Technical field: [0001] The invention relates to the field of pharmaceutical preparations, in particular to liposomes modified with low molecular weight chitosan and a preparation method thereof. Background technique: [0002] Chitosan is the only positively charged polysaccharide of natural origin, which has excellent biological properties, such as: biofilm adhesion, promotion of drug absorption, good biocompatibility, antibacterial activity, etc. But the disadvantage is that it is insoluble in water under physiological conditions. In order to improve its water solubility, a lot of research has been done to modify it, mainly including quaternization, carboxymethylation and sulfated derivatives. A large number of hydroxyl groups and amino groups on chitosan molecules will form intermolecular and intramolecular hydrogen bonds. When chitosan is degraded, the molecular weight decreases, the hydrogen bond in the molecule weakens, it is easy to interact with solvent molecules, ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/36A61K45/00
Inventor 潘卫三李宁聂淑芳关津庄春阳
Owner SHENYANG PHARMA UNIVERSITY
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