Tri-block polymer and preparation method thereof

A polymer and tri-block technology, applied in the direction of drug combinations, pharmaceutical formulations, genetic material components, etc., can solve the problems of high cytotoxicity, difficult to degrade, etc., and achieve the effect of enhanced penetration and retention effects, and excellent tissue permeability

Active Publication Date: 2014-10-15
SUZHOU UNIV
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

However, this type of polymer is difficult to degrade in cells and has high cytotoxicity, which limits its application to a certain extent.

Method used

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  • Tri-block polymer and preparation method thereof
  • Tri-block polymer and preparation method thereof
  • Tri-block polymer and preparation method thereof

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Embodiment 1

[0031] This embodiment provides a kind of N-succinyl chitosan-poly-L-lysine-soft fatty acid triblock polymer, refer to the attached figure 1 , which is a schematic diagram of the synthetic route of the N-succinyl chitosan-poly-L-lysine-soft fatty acid triblock polymer provided by the present invention. In this embodiment, the specific synthesis method includes the following steps:

[0032] 1. Synthesis of N-succinyl chitosan-poly-L-lysine (NSC-PLL)

[0033] Dissolve 0.4 g of NSC in 25 mL of distilled water and stir to form a solution. Put 0.32 g PLL, 0.192 g EDC·HCl and 0.057 g NHS into the above reaction solution respectively, 1.1 mol.L -1 Adjust pH to 5.6 with HcL, magnetically stir the reaction liquid, react at room temperature for 7 2 h, place in a dialysis bag (MWCO=3 500), dialyze with distilled water for 3 days, filter and freeze-dry to obtain NSC-PLL.

[0034] 2. Activation of palmitic acid (PA)

[0035] 0.128 g of soft fatty acid was added to 25 ml of dry dichlor...

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Abstract

The invention discloses a tri-block polymer and a preparation method thereof. The tri-block polymer takes fatty acid as a core, takes poly-L-lysine as a middle layer and takes N-succinyl chitosan as a casing to be self-assembled into a micelle in an aqueous solution. The hydrophobic core is used for entrapping hydrophobic anti-cancer drugs, such as Adriamycin, Taxol and the like; the middle layer carrying positive charges is used for adsorbing genes, such as DNA, siRNA and the like, and the prepared micelle can release the supported genes after being degraded; the hydrophilic casing can reduce the toxicity of the poly-L-lysine and prolong the blood circulation time of the poly-L-lysine after system administration. According to the tri-block polymer, the genes are adsorbed after particles are formed, so that the control on sizes of the micelle particles and large-scale preparation of the micelle particles are facilitated; the tri-block polymer can also being used for transfecting the genes to enter target cells and regulate expression of interest protein in the presence of serum and has the good biocompatibility, and a novel supporter and a novel preparation form are provided for the establishment of a targeted anti-tumor drug delivery system.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an N-succinyl chitosan (NSC)-poly-L-lysine (PLL)-fatty acid (FA) triblock polymer and a preparation method thereof. Background technique [0002] At present, the treatment of tumors has become a global problem that needs to be solved urgently. In the treatment of tumor diseases, the effect of drug therapy is not good, most chemotherapy drugs have poor water solubility and lack of selectivity for tumor sites (Cheong I, Huang X, Bettegowda C, Diaz LAJ, Kinzler KW, Zhou SB, et al. A bacterial protein enhances the release and efficacy of liposomal cancer drugs. Science.2006; 314:1308–1311), and with the widespread use of antineoplastic drugs, most tumor cells develop multidrug resistance, which has become one of the key factors for the failure of tumor chemotherapy One (Gullotti E, Yeo Y. Extracellular activated nanocarriers: a new paradigm of tumor targeted drug delivery. M...

Claims

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Application Information

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IPC IPC(8): C08G81/00C08B37/08A61K47/36A61K48/00A61P35/00
Inventor 张学农张春歌
Owner SUZHOU UNIV
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