Composition, preparation method and application for mediating transdermal absorption of biological macromolecules

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and discloses a composition capable of mediating the transdermal absorption of biomacromolecules, a preparation method and an application thereof. Skin agent; epidermis denaturing dissolving agent is composed of 2% alginic acid and protein denaturing dissolving agent. The protein denaturing dissolving agent is composed of sodium alginate and high-concentration urea in water. The mass volume ratio of sodium alginate is 2%. The transdermal agent is a certain concentration lauryl azone emulsion. The present invention reduces the thickness of the surface layer and makes the inner epidermis in a semi-dissolved state, and uses a transdermal agent to expand the intercellular space and increase the fluidity of the cell membrane. At this time, the application of protein, polypeptide or other drug macromolecules to the skin can be efficiently absorbed by the skin dermis. layers of cell absorption. The denaturing effect of the protein denaturant adopted in the invention on the epidermis is reversible, and the protein is automatically refolded after the water washing concentration is reduced, and the inner epidermis can be restored.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a composition capable of mediating transdermal absorption of biomacromolecules, a preparation method and an application. Background technique [0002] At present, the skin's absorption efficiency of active substances directly determines the therapeutic or skin care effects of ointment drugs and beauty products. Promoting the skin absorption efficiency of active ingredients is a key research direction in the field of skin drug delivery. The barriers for drug absorption through the skin include the outermost epidermis composed of dead epidermal cells, the inner epidermis composed of semikeratinized epidermal cells, the subepidermal dermal cells, and the tight anchor links between cells. The delivery of drug molecules needs to pass through these three barriers to enter the dermal cells and deep tissues. [0003] Traditional plaster formulations usua...

AI Technical Summary

Problems solved by technology

Third, the operation is difficult: the operation is generally to manually press the skin with the microneedle array to create a wound, and it is difficult to control the force. If the force is too high, the microneedle will damage the dermal tissue, which may cause tissue fluid to leak out and even cause bleeding; If it is too small, it will not be able to completely pierce the epidermis, and it will not be able to promote the absorption of macromolecules

Fourth, the production is difficult and the cost is high: there are certain difficulties in the length control and precise arrangement of the microneedles. On the one hand, it produces high manufacturing costs. On the other hand, there are differences in the thickness of the epidermis of different human skin , the length of the microneedle is difficult to achieve personalized design

However, the existing non-invasive transdermal technology can only achieve skin absorption of small molecules and some fat-soluble molecules, and cannot achieve skin absorption of biological macromolecules such as proteins and peptides without destroying the structure and barrier function of the skin.

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