Sustained-release microneedle patch and preparation method thereof

Abstract

The invention discloses a sustained-release microneedle patch and a preparation method thereof, and relates to the technical field of medicines. The microneedle patch comprises a needle body and a needle tip on the needle body, and at least the needle tip part comprises a part which is prepared from needle tip preparation liquid and can realize gelation in the drying process of the microneedle patch; and solutes of the needle tip preparation liquid comprise glycerophosphate compounds and nonionic cellulose ether compounds. The glycerophosphate and the cellulose ether compound can compete for water molecules, so that the cloud point of the cellulose ether compound is changed, the microneedle is gelatinized in the drying process, the gel microneedle with a good skin puncture effect is prepared, and in-vivo slow release of entrapped drugs is realized.

Description

technical field [0001] The invention relates to the technical field of medicine. More specifically, it relates to a slow-release microneedle patch and a preparation method thereof. Background technique [0002] Sustained-release microneedle is a new type of transdermal drug delivery preparation that can achieve continuous and gentle delivery of drugs after acting in the skin. It is suitable for the use of drugs that require long-term drug administration and narrow therapeutic windows. The advantages of safety and convenience have greatly improved the medication compliance of patients, and they occupy an important position in the research of new microneedle drug delivery preparations. Existing sustained-release microneedles are mainly based on (1) sustained-release systems such as microspheres, liposomes, and solid dispersions; (2) degradable polymer materials such as polylactic acid-glycolic acid copolymers and chitosan; (3) Sol-gel phase transition materials were designed...

AI Technical Summary

Problems solved by technology

[0004] Chinese patent CN102202720A discloses a method for preparing phase-inversion polymer microneedles by using cross-linked polyvinyl alcohol. Through repeated operations of freezing at -20°C and thawing at 4°C, water-soluble polyvinyl alcohol can be formed through microcrystal construction in aqueous solution. Gel, so as to realize the sustained release delivery of drugs, but the preparation process is cumbersome and time-consuming, which is not suitable for mass industrial production of sustained-release microneedles; and phase-change microneedles made of PLGA-PEG-PLGA triblock copolymer , the raw material synthesis process is complicated, and the material has poor water solubility, and organic reagents need to be introduced, which has potential safety hazards (Marc Pearton, Chris Allender, Keith Brain, et al. Gene Delivery to the Epidermal Cells of Human Skin Explants Using Microfabricated Microneedles and Hydrogel Formulations. Pharmaceutical Research. 2008,25(2):407-416.); Both carbomer and poloxamer gel are widely used as carriers of local therapeutic drugs in the pharmaceutical industry because of their good temperature-sensitive characteristics, acting on mucous membranes or skin, etc. Sustained release of drugs can be achieved in the affected area, but these two materials have extremely poor mechanical strength and cannot be made into skin-piercing microneedles. Existing studies have first used metal microneedles or polymer microneedles with sufficient mechanical strength. The skin is pretreated with needles, and the microchannel is opened, and then the drug-loaded carbomer or poloxamer solution is applied to the surface of the skin treated with microneedles, and a sol-gel phase transition process occurs by using its temperature-sensitive properties , forming a drug reservoir to achieve slow drug release

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