Preparation method of supermolecule globular micelle based on antidepressant medicament chlorpromazine
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A technology of spherical micelles and supramolecules, which is applied in the field of preparation of supramolecular spherical micelles, can solve the problems of low drug loading rate and lack of self-assembly characteristics, and achieve low raw material consumption, low cost and excellent preparation methods. easy effect
Inactive Publication Date: 2014-02-05
NANKAI UNIV
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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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[0017] A preparation method of supramolecular spherical micelles based on the antidepressant drug chlorpromazine, dissolving SC4AH and CPZ in water, and uniformly mixing to obtain supramolecular micelles, the concentrations of SC4AH and CPZ in the supramolecular micelles solution are respectively 25 μM and 75 μM.
[0018] figure 1 Schematic diagram for the construction of supramolecular spherical micelles by non-covalent co-assembly.
[0019] Both SC4AH and CPZ are amphipathic, as figure 2 As shown, the critical aggregation concentration of SC4AH is 210 μM; image 3 As shown, the critical aggregation concentration of CPZ is 140 μM; Figure 4 As shown, the critical aggregation concentration of SC4AH+CPZ was 12 μM when the molar ratio of SC4AH and CPZ was fixed at 1:3.
[0020]The particle size and morphology of the supramolecular micelles were characterized by dynamic light scattering and high-resolution transmission electron microscopy, respectively. Figure 5 Dynamic li...
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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...
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