Solid lipid nanometer particle in-situ gel rubber preparations of biological adherent cyclosporine A and preparation method thereof

Abstract

The invention pertains to the field of medical technology, which discloses a biological adhesive cyclosporine A solid lipid nanoparticle in situ gel preparation and the preparation method thereof. The preparation includes the treatment effective amount of cyclosporin A, emulsifier, lipid material, charge controlling agent/coating material and so on, and each 1000ml preparation contains: 0.05g to 5.0g of cyclosporin A, 0.0g to 50g of lipid material, 0.5 to 60g of emulsifier, 0.1g to 30g of coating material, 200.0g to 500.0g of gel matrix, and the purified water is added to 1000ml. Positive charge material is firstly coated on the nanoparticle surface and then is prepared into in situ gel preparation. The particle size of the nanoparticle which is prepared by the invention is less than 200nm, the envelope rate is higher, the performance is more than the zeta potential of plus23mv and is increased along with the consumption of charge controlling agent/coating material, and the potential is improved. The preparation of the invention shows better adhesion of the dual-mucosa, which can be used in local drug delivery; as the retention time on the drug delivery part is prolonged, the action time of the drug is long, the bioavailability and the treatment index of the drug can be improved, and the dosage, toxicity and side effects can be reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a bioadhesive cyclosporine A solid lipid nanoparticle in-situ gel preparation and a preparation method thereof, more specifically, to a solid coated with a positively charged material Lipid nanoparticle in situ gel preparation and preparation method thereof. Background technique [0002] Cyclosporine A is a fat-soluble, cyclic polypeptide compound composed of 11 amino acids. In 1983, the U.S. Food and Drug Administration approved the official registration and marketing of cyclosporine A, which is mainly used for the prevention and treatment of rejection after organ or tissue transplantation and the treatment of autoimmune diseases. Systemic application of cyclosporine preparations has low bioavailability and large individual differences, which can easily cause side effects such as nephrotoxicity, liver toxicity, central nervous system toxicity, and gastrointestinal reactions. Top...

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Problems solved by technology

(2) The in situ gel of lipid nanoparticles stays in the eye for a long time, that is, the adhesion of the gel and the adhesion of the nanoparticles play a dual role. The mucous membrane has an adhesive effect, which fully prolongs the action time of the drug, while the ordinary gel only increases the residence time of the eye through the physical adhesion of the gel. After the gel is eroded, the drug will flow out with tears, and the action time is relatively short

(3) The in-situ gel has low viscosity and good fluidity at room temperature, which is beneficial for ocular administration. The drug forms a gel in the eye to prolong the residence time, while ordinary gels have high viscosity at room temperature and poor fluidity. inconvenient

(4) The in-situ gel has a small viscosity at room temperature, which is conducive to the preparation of cans, while the ordinary gel has a high viscosity, and it is easy to generate a large number of air bubbles during preparation, which is inconvenient for industrial production and filling.

(5) The low viscosity of the in-situ gel is conducive to uniform distribution in the eye during eye drops, and then forms a gel. However, ordinary gel has a high viscosity, and the drug is not easy to distribute evenly on the surface of the cornea and conjunctiva, so it can only be used by blinking. Uniform coating

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