A kind of intestinal administration carrier thiolated calcium alginate microspheres and preparation method thereof

Abstract

The invention relates to sulfhydrylation calcium alginate microspheres as an intestinal drug delivery carrier and a preparation method of the sulfhydrylation calcium alginate microsphere. The method comprises the following steps: mixing sodium alginate with sulfhydrylation calcium alginate according to the mass ratio of (1 to 8) to 1 and preparing a solution with the mass concentration of 0.5 to 5percent, then adding an oil phase containing a surfactant and emulsifying at room temperature at 200 to 900 rpm for 45 minutes, adding CaCl2 powder and continuously stirring at 100 to 400 rpm for 0.5to 3 hours to realize cross-linking and solidifying of the microspheres, carrying out centrifugal demulsification, washing and then screening the microspheres to obtain the sulfhydrylation calcium alginate microspheres. The sulfhydrylation calcium alginate microspheres prepared with an emulsification method disclosed by the invention have uniform and controllable particle size and good monodispersity. The prepared sulfhydrylation calcium alginate microspheres have strong mucosal adhesion properties in small intestine and can prolong the residence time of the microspheres in the intestine, sothat the long-acting administration effect is achieved. Therefore, the sulfhydrylation calcium alginate microspheres prepared with the preparation method disclosed by the invention have potential market application prospects in the fields of a drug delivery system for bioactive drugs such as protein, polypeptide and the like as well as intestinal targeted drug delivery.

Description

technical field [0001] The invention relates to the field of biomedical materials, in particular to a thiolated calcium alginate microsphere, a carrier for intestinal drug delivery, with uniform and controllable particle size, good monodispersity, and good intestinal adhesion and pH responsiveness. its preparation method. Background technique [0002] With the rapid development of biomedical technology, bioactive macromolecular drugs such as proteins, peptides and enzymes are used for the diagnosis or treatment of cancer, cardiovascular and other diseases. Macromolecular drugs often enter the human body through intravenous injection, which can cause physical pain and psychological panic to patients. Non-intravenous injections such as oral administration will reduce the bioavailability of drugs, because protein or polypeptide drugs will be degraded by pepsin and trypsin in the gastrointestinal tract and lose their activity after oral administration, so they cannot reach the ...

AI Technical Summary

Problems solved by technology

However, when used as a drug carrier, the sudden release of sodium alginate is too obvious. Calcium alginate microspheres prepared by the traditional emulsification method usually release 80% of the drug within 20 minutes, resulting in high drug concentration and even harm to patient health

In addition, the P-gp transporter widely present on the cells of the gastrointestinal tract is a drug efflux transporter, which allows the drugs that have entered the cells to be effluxed out, thus limiting the oral absorption of many exogenous drugs and reducing the drug bioavailability

[0004] Sodium alginate adheres to the small intestinal mucosa through non-covalent bonds such as van der Waals force, hydrogen bond and electrostatic attraction, so its adhesion is not strong compared with covalent bonds