Oligopeptide-based pH-sensitive amphoteric ion and application thereof in medicament

Abstract

The invention relates to the field of accessories and preparations with medicinal functions, in particular to a kind of oligopeptide-based pH-sensitive amphoteric ion lipid (I) or (II). In the invention, the derivatives of the oligopeptide amphoteric ion lipid have different surface charges under different pH conditions and can take relatively strong negative charges in a physiological environment with pH near neutrality so that the lipid has good blood compatibility; when the lipid reaches a tumor part, the surface charges of the oligopeptide amphoteric ion lipid are reversed in an acidulous tumor environment, so that the original electronegativity is reversed into electropositivity; and a carrier with positive charges is easily combined with the surface of a tumor cell, and the tumor cell targeting can be effectively realized through an endocytosis path. In lysosome, a cationic carrier continuously realizes a function of proton sponge or a function of splitting lysosome membranes, and the two functions can ensure the integrity of the carrier, so that the carrier can safely escape to cytoplast or other organelles.

Description

technical field

[0001] The invention relates to the field of pharmaceutical functional excipients and preparations. It specifically relates to a class of oligopeptide pH-sensitive zwitterionic lipids and a preparation method thereof, and also relates to its application in preparations as a drug carrier such as being assembled into a liposome or as a coating material for a cationic carrier. Background technique

[0002] As a drug carrier, liposome has the advantages of targeting the drug to the reticuloendothelial system, prolonging drug efficacy, reducing drug toxicity, improving curative effect, avoiding tolerance, and changing the route of administration. However, as a drug carrier, liposomes still have disadvantages such as unsatisfactory targeting characteristics for some diseases, poor in vivo stability and storage stability, which limit the clinical application and industrial production of liposomes. In recent years, people have developed new liposomes such as long-ci...

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