Nano-micro drug delivery system and preparation method of 10-hydroxyl camptothecin

A hydroxycamptothecin system technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of repeated droplet breakage, low drug loading, and uncontrollable , to achieve the effect of increasing the embedding rate, improving the drug effect, and stabilizing the dispersion

Inactive Publication Date: 2012-02-15
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] In the above literature, the preparation methods of nano-micro-carriers are mechanical stirring method, homogeneous emulsification method or ultrasonic emulsification method, etc. The emulsion preparation process will generate high shear force, and its dispersion...

Method used

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  • Nano-micro drug delivery system and preparation method of 10-hydroxyl camptothecin
  • Nano-micro drug delivery system and preparation method of 10-hydroxyl camptothecin
  • Nano-micro drug delivery system and preparation method of 10-hydroxyl camptothecin

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Effect test

Embodiment 1

[0059] In the experiment, a microporous membrane with a pore size of 2.8 μm was used to prepare drug-loaded gel microspheres. The specific implementation was as follows: the hydrophobic membrane with a pore size of 2.8 μm was soaked in a lipophilic substance, so that the porous membrane was fully wetted to ensure the drug-loaded gel microspheres on the membrane. The hydrophobic chain is completely stretched, and the NaOH solution with a pH value of 8 is selected to prepare the aqueous phase solution in the experiment. 10-Hydroxycamptothecin is used as the water phase, and the oil phase is a mixture of liquid paraffin and sherwood oil with a volume ratio of 1: 2, and contains 4.0wt% emulsifier PO-500, wherein the volume ratio of the oil phase to the water phase is 30:1, take 2 mL of the water phase with a pH value of 8 and 60 mL of the oil phase to mix the pre-emulsion; then press the pre-emulsion repeatedly through the membrane pores under a pressure of 0.280 MPa until a W / O em...

Embodiment 2

[0063] In the experiment, a microporous membrane with a pore size of 2.8 μm was used to prepare drug-loaded gel microspheres. The specific implementation was as follows: the hydrophobic membrane with a pore size of 2.8 μm was soaked in a lipophilic substance, so that the porous membrane was fully wetted to ensure the drug-loaded gel microspheres on the membrane. The hydrophobic chain is completely stretched, and the NaOH solution with a pH value of 10 is used to prepare the aqueous phase solution in the experiment, as follows: a 1.0wt% alginate aqueous solution is prepared with a NaOH solution with a pH value of 10, and the concentration is 1mg / mL 10-Hydroxycamptothecin is used as the water phase, wherein the oil phase (O) is olive oil, and contains 2.0wt% emulsifier Arlacel83, and the volume ratio of the oil phase to the water phase is 40: 1; get the water phase with a pH value of 10 2mL was mixed with 80mL oil phase to prepare a pre-emulsion; then the pre-emulsion was repeate...

Embodiment 3

[0067]In the experiment, a microporous membrane with a pore size of 2.8 μm was used to prepare drug-loaded gel microspheres. The specific implementation was as follows: the hydrophobic membrane with a pore size of 2.8 μm was soaked in a lipophilic substance, so that the porous membrane was fully wetted to ensure the drug-loaded gel microspheres on the membrane. The hydrophobic chains are fully stretched. Prepare 0.5wt% alginate aqueous solution with pH=8 NaOH solution, and contain 10-hydroxycamptothecin at a concentration of 1mg / mL as the water phase, and the oil phase (O) is cottonseed oil, and contains 7.0wt% The emulsifier PO-310, the volume ratio of oil phase (O) and water phase (W) is 30: 1, get 2mL concentration and be that the alginate aqueous solution of 0.5wt% is mixed with 60mL oil phase to prepare pre-emulsion, then pre-emulsion The emulsion is repeatedly pressed through the membrane pores under a pressure of 0.300MPa until a W / O emulsion with uniform particle size ...

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Abstract

The invention relates to a nano-micro drug delivery system and a preparation method of a slightly soluble drug of 10-hydroxyl camptothecin (HCPT). The invention makes use of alginate to dissolve HCPT under alkalic condition; then acidic calcium chloride miniemulsion is added to the prepared uniform HCPT-containing emulsion to have crosslinking and curing reactions; at the time when the emulation droplets cure, the HCPT constellation is partially transformed, so that the HCPT crystallize; and then, an acidic chitosan solution or an acidic chitosan derivative is used for secondly curing so as to let the HCPT to crystallize further more. The product prepared through the method is a composite alginate chitosan microsphere or a micro-capsule drug delivery system loaded with HCPT with uniform size and stable dispersion. The nano microspheres of the system have uniform grain size and stable dispersion and the drugs in the nano microspheres exist in the form of closed-loop medicinal nanocrystalline. The invention can realize the increase of solubility of indissolvable drugs and the improvement of bioavailability and effectively improves the encapsulation rate of the indissolvable drugs.

Description

technical field [0001] The invention relates to a nano-micro drug delivery system and a preparation method thereof, in particular to a nano-micro drug delivery system of an insoluble drug 10-hydroxycamptothecin (HCPT) and a preparation method thereof. Background technique [0002] With the development of high-throughput drug screening technology, a large number of active compounds used in the treatment of major diseases have been screened out, but most of them cannot be used in clinical applications due to their high molecular weight and strong hydrophobicity resulting in poor solubility. Therefore, improving the solubility and bioavailability of poorly soluble drugs has always been a hot spot in pharmaceutical research. Currently commonly used methods include liposome embeddings, solid dispersions, and cyclodextrin inclusion complexes. However, these methods have problems such as low drug loading, complicated preparation process, poor stability, and slow drug release rate....

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/50A61K31/4745A61K47/36A61K47/44A61P35/00
Inventor 王连艳马光辉杨娟娟张岳玲杨婷媛周炜清
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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