Preparation method and application of a sarcosine-based pH-responsive polyamino acid drug-loaded nanoparticle

By using sarcosine-based pH-responsive polyamino acid drug-loaded nanoparticles, the problems of toxicity and low delivery efficiency of chemotherapy drugs have been solved, enabling precise drug release and efficient treatment in the tumor microenvironment.

CN122167727APending Publication Date: 2026-06-09NINGDE NORMAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
NINGDE NORMAL UNIV
Filing Date
2026-01-30
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

Existing chemotherapy drugs such as doxorubicin have serious problems of cardiotoxicity, bone marrow suppression and rapid systemic clearance in clinical applications. In addition, traditional polyethylene glycol as a carrier material has problems of immunogenicity, non-degradability and affecting cell uptake, resulting in low drug delivery efficiency and drug resistance in the tumor microenvironment.

Method used

Using sarcosine-based pH-responsive polyamino acid drug-loaded nanoparticles, through block copolymer synthesis, protecting group removal, and drug-loaded nanoparticle preparation, spherical nanomicelles with a core-shell structure are formed. By utilizing the hydrophilicity of the sarcosine segment and the hydrophobicity of the phenylalanine segment, combined with the pH responsiveness of the lysine segment, the precise release of drugs in the tumor microenvironment can be achieved.

Benefits of technology

It achieves precise drug release in the tumor microenvironment, reduces systemic toxicity, improves drug delivery efficiency and anti-tumor effect, prolongs blood circulation time, avoids burst release, enhances tumor cell killing effect and reduces systemic toxicity.

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Abstract

This application provides a method for preparing pH-responsive polyamino acid drug-loaded nanoparticles based on sarcosine and their application. Sar-NNCA, L-lysine-NCA, and L-phenylalanine-NCA are dissolved in anhydrous DMF and polymerized under argon protection with a hexamethyldisilazine initiator to obtain a polyamino acid block copolymer Sar-NNCA. 80 -Lys(Cbz) n -Phe 10 The crude product was deprotected under HBr / acetic acid and loaded with DOX to obtain Sar. 80 -Lys n -Phe 10 -DOX. This application describes the preparation of a pH-responsive polymer nanoplatform, Sar, by encapsulating doxorubicin in polysarcosine-polylysine-polyphenylalanine nanoparticles via Schiff base bonds. 80 -Lys n -Phe 10 -DOX is used for tumor treatment. These polyamino acid nanoparticles are spherical with an average particle size of approximately 200 nanometers, exhibiting pH-responsive properties, excellent cellular uptake capacity, and anti-tumor effects. In vitro experiments show that Sar... 80 -Lys n -Phe 10 The carrier material exhibits excellent biocompatibility. The newly synthesized Sar... 80 -Lys n -Phe 10 -DOX nanomicelles show promise as a drug delivery system for cancer treatment.
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