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Nanometer granule prepn of bufanin albumin and its prepn process

A technology of albumin nanoparticles and bufalin, which is applied in the field of medicine, can solve the problems of organic solvent residues, limited reliability, and difficult purification of nanoparticles, and achieve less organic solvent residues, lower toxic and side effects, and strong operability Effect

Active Publication Date: 2006-05-17
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some existing methods for preparing albumin nanoparticles often have disadvantages such as difficulty in controlling the particle size, large residual or unstable surfactants, etc. For example, if the thermal denaturation emulsification method is used, an organic solvent needs to be used to remove the oily residue and the surface. Active agents not only easily cause the residue of organic solvents, which brings difficulties to the purification of nanoparticles, but also the particle size is difficult to control, and it is also unfavorable for thermally unstable drugs.
If the pH-aggregation method is used, the particle size of albumin nanoparticles is also difficult to control, and the pH value needs to be adjusted under salt-free conditions. However, in the presence of high concentrations of protein, the reliability of measuring the pH value with a glass electrode is limited.
In view of the above reasons, there have been no reports of bufalin albumin nanoparticle preparations so far

Method used

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  • Nanometer granule prepn of bufanin albumin and its prepn process
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  • Nanometer granule prepn of bufanin albumin and its prepn process

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Embodiment 1

[0031] Embodiment 1. Preparation of bufolin albumin nanoparticle preparation

[0032] Dissolve 50mg of albumin in 2ml of water, dissolve 5mg of bufalin in 1ml of ethanol, add bufalin alcohol solution into the albumin aqueous solution, control the pH value between 5-7, stir at 0.5ml / Continue to add 3ml of ethanol at a speed of min until an emulsion colloidal suspension is formed. Add 27μl of cross-linking agent glutaraldehyde under stirring, and stir continuously for 24 hours to promote the cross-linking and solidification of nanoparticles. Gently heat and evaporate under reduced pressure to remove organic solvents such as ethanol. Freeze-dry to obtain the bufalin nanoparticle preparation of the present invention.

Embodiment 2

[0033] Example 2 Preparation of bufolin albumin nanoparticle preparation

[0034] Dissolve 100mg of albumin in 4ml of water, dissolve 20mg of bufalin in 2ml of ethanol solution, add bufalin alcohol solution into the albumin aqueous solution, control the pH value between 5-7, and continuously add an appropriate amount of dehydrating agent under stirring Acetone, to form a milky colloidal suspension, add an appropriate amount of cross-linking agent methyl polyethylene-dextran under stirring to form a milky white opaque liquid, stir continuously for 26 hours to promote cross-linking and solidification of nanoparticles, evaporate under slight heat and decompression, remove organic solvents such as ethanol and acetone, and freeze-dried to obtain the bufalin nanoparticle preparation of the present invention.

[0035] Observation of appearance and morphology: adopt tungsten phosphate negative staining method, observe the appearance and morphology of bufalin nanoparticles prepared by ...

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Abstract

The present invention relates to medicine technology, and is nanometer granular bufalin-albumin preparation as one new preparation form of bufalin and its preparation process. Bufalin has excellent effects of treating tumor, reversing chemotherapeutic drug resistance, inhibiting hepatitis B virus copying, etc. but high toxicity and short intracorporeal half life, forming no medicine preparation up to now. The nanometer granular bufalin-albumin preparation of the present invention has round shape of nanometer grains, narrow grain size distribution in the range of 50-250 nm, average grain size of 102 nm, liver targeting and delayed releasing, so that it has increased concentration in target organ for long time action, raised curative effect and lowered toxic side effect and may be used in preparing medicine for treating liver cancer and hepatitis B.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a bufalin albumin nanoparticle preparation and a preparation method thereof. Background technique [0002] Bufalin is a component in animal toads, and its chemical structure is as follows: [0003] [0004] In vitro experiments have confirmed that it has good anti-tumor effects, reversing chemotherapy resistance, improving immunity and inhibiting hepatitis B virus replication. Experiments have also confirmed that its killing and inhibiting effects on tumors within a certain concentration range are positively correlated with the time of action. (Su Yonghua, Yin Xicai, Xie Juemin, et al. "In vitro tumor inhibitory effect of cinobufacin combined with mitomycin". Journal of Anhui University of Traditional Chinese Medicine. 2003, 22(3). 45-48 / Su Yonghua, Yin Xicai, Xie Juemin, et al. "Three Inhibitory effect of a toad toxin monomer on the growth of SMM...

Claims

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Application Information

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IPC IPC(8): A61K38/38A61K31/26A61P1/16A61P31/20A61P35/00
Inventor 苏永华凌昌全
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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