Preparation method of supermolecule globular micelle based on antidepressant medicament chlorpromazine

Abstract

The invention discloses a preparation method of a supermolecule globular micelle based on an antidepressant medicament chlorpromazine. The method comprises the following steps: constructing a medicament carrier through the supermolecule interaction of amphiphilic sulfonated calix [4] arene and an antidepressant medicament chlorpromazine hydrochloride, dissolving the amphiphilic sulfonated calix [4] arene and the antidepressant medicament chlorpromazine hydrochloride in water, and uniformly mixing to obtain a nano supermolecule globular micelle solution; and non-covalently modifying a targeting agent trimethyl chitosan through a bonding site of the calix arene on the surface of the micelle to obtain the supermolecule micelle loaded with trimethyl chitosan on the surface. The preparation method has the advantages that the preparation method is simple and convenient, and fewer subjective and objective raw materials are used; the medicament load rate is high since the medicament molecules are the constructing units of the medicament carrier and the medicament molecules are immobilized; the micelle can be used for non-covalently modifying the targeting agent trimethyl chitosan through the bonding site of the surface calix arene so that the micelle has a wide application prospect in the field of targeted medicament delivery.

Description

【Technical field】 [0001] The invention belongs to the preparation of nano-supramolecular drug carriers, in particular to a preparation method of supramolecular spherical micelles based on the antidepressant drug chlorpromazine. 【Background technique】 [0002] Self-assembled nanocarriers are widely used in many fields, especially drug delivery. A variety of assemblies have been used as drug carriers, such as phospholipids, polymers, dendrimers and inorganic nanoparticles, etc., see: 1) Vladimir, P.T.Nat.Rev.Drug Discovery2005, 4, 145-160; 2) Vasant, V.R.J.Clin .Pharmacol.1990,30,10-23; 3)Samad,A.;Alam,M.I.;Saxena,K.Curr.Pharm.Des.2009,15,2958-2969;4)Liong,M.;Lu,J .; Kovochich, M.; Xia, T.; Ruehm, S.G.; Nel, A.E.; Tamanoi, F.; Zink, J.I. ACS Nano 2008, 2, 889-896. A commonly used drug carrier is to form an assembly from nanomaterials, and then encapsulate drug molecules in it, see: Mary, E.C.; William, B.L.; Nicholas, A.P.Acc.Chem.Res. 2011, 44, 1061-1070. But the disadvant...

AI Technical Summary

Problems solved by technology

But the disadvantage of this method is that the loading rate of the drug is not high (not higher than 10%)

However, there are still few reports on this aspect, mainly because most drug molecules do not have the characteristics of self-assembly

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