Polymer nanoparticles for loading alkaline antitumor drugs

Abstract

The invention relates to polymer nano-particles for loading alkaline antitumor drugs. A polymer material forming the nanoparticles has biological compatibility and biodegradability, and the polymer material loads the alkaline antitumor drugs; and the polymer material comprises liposome, polylactic acid, polylactic acid-glycolic acid copolymer, polycaprolactone, chitosan, albumin and cyclodextrin; and the alkaline antitumor drug is a micromolecule antitumor drug with pKa being more than 7.4 and comprises adriamycin, pharmorubicin, taxol, docetaxel, vinblastine, vincristine, topotecan and alkaloid Chinese medicine monomers. The polymer nano-particles solve the defects that the pH dependence and physiological drug fastness cannot be reversed. The polymer nano-particles are free from introducing additional drugs, so that the influence on the internal environment of an organism is small, the pH dependence physiological drug fastness is reversed through the polymer nano-particles, not only is the effect realized, but also since no influence is caused for the internal environment of the organism, the polymer nano-particles are safe to use, little in side effect, and wide in application range.

Description

technical field [0001] The present invention relates to macromolecular nano antitumor drugs, in particular to macromolecular nano particles loaded with basic antitumor drugs. Background technique [0002] The pH-dependent physiological drug resistance of malignant tumors has been discovered, but it has not been paid attention to and used. Its production mechanism is as described in the instructions figure 1 As shown, the brief description is as follows: [0003] The pH value of cells is divided into two parts: intracellular pH (pHi) and extracellular pH (pHe). The extracellular pH of normal tissue cells is generally around 7.4, and pHi is similar to or slightly lower than pHe. Due to the metabolic characteristics of malignant tumors, in tumor cells, pHe<pHi, the intracellular-extracellular pH gradient is opposite to that of normal tissues. For weakly basic drugs, when the pH value of the environment is lower than the pKa value of the drug, the [OH - ] are neutralized...

AI Technical Summary

Problems solved by technology

But existing these two kinds of methods all have the following common defects: 1, for the regulation of intracellular and extracellular pH value nonspecificity (both changing the pH value of tumor tissue, also changing the pH value of non-tumor tissue), this has caused in In animal experiments, both methods have side effects that cannot be ignored. The occurrence of side effects is related to the lack of specificity of the above-mentioned drugs and interference with the internal environment of the organism; according to the relevant research of the applicant, the change of the internal environment of the organism may even be caused by The disorder interferes with the normal metabolism and immune function of the organism, but reduces the effect of anti-tumor drugs; 2. The drug doses in animal experiments are converted to humans, which are significantly higher than the commonly used clinical doses (tens to hundreds of times)

For reversing pH-dependent physiological drug resistance, it can be said that there is no satisfactory method and effect so far

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