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Camptothecin nano-gel

A nano-gel, camptothecin technology, applied in the directions of non-active ingredients medical preparations, organic active ingredients, skin diseases, etc., can solve problems such as clinical application limitations, and achieve prolonging action time, reducing penetration, and increasing skin retention. amount of effect

Inactive Publication Date: 2015-04-08
中国人民解放军第九八医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the limited drug loading and relative stability of these drugs limit their clinical application.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 The preparation of camptothecin nanoparticles and gel:

[0034] Preparation of blank and drug-loaded nanoparticles:

[0035]PLGA-PAMAM-OA (PPO) nanoparticles are prepared by emulsified solvent evaporation method, get 10mgPLGA dissolved in 1.5ml methylene chloride solution obtained as the organic phase, the organic phase is added to 14.5ml 0.1% (W / V) PVA 1. In the mixed solution of 4ml 0.5% PAMAM and 1.5ml Tween 80, stir at a constant speed to form a coarse emulsion, then stir with an ultrafine homogenizer for 15min (35000rpm) to form a nanoemulsion. Evaporate the organic phase, add 100 μl 1% (W / V) sodium triphosphate (TPP) for cross-linking, then stir at 300 rpm for 2 h, suspend in phosphate buffer (pH 8.0), and incubate with oleic acid (OA) After 2 hours, the blank nanoparticle PPO was obtained, and the unmodified PLGA nanoparticle (PLGA-PAMAM) was prepared according to the above method.

[0036] The preparation method of camptothecin-loaded drug-loaded ...

Embodiment 2

[0042] Example 2 Preparation of blank and drug-loaded gel (PPO gel, CPT-PPO gel):

[0043] The preparation method of the gel is as follows: take camptothecin 0.01g and dissolve it in 40ml ethanol, ultrasonically dissolve it, add swollen hydroxypropyl methylcellulose (HPMC) drop by drop and constantly stir until fully forming a gel, Stable at room temperature for 24 hours for later use to obtain camptothecin gel (CPT gel).

[0044] The preparation method of nanogel refers to the preparation method of camptothecin gel, and HPMC is added dropwise to the blank and drug-loaded aqueous solution of nanoparticles until the gel is completely formed (PPO gel, CPT-PPO gel, PP gel, CPT-PP gel), stable at room temperature for 24 hours.

Embodiment 3

[0045] Example 3 In vitro release kinetics research:

[0046] A certain amount of drug-loaded nanogels CPT-PPO and CPT-PP were put into dialysis bags respectively, placed in PBS dissolution cups with pH 7.4, the temperature was controlled at 37±1°C, and the stirring speed was 300rpm. At different times (1, 2, 4, 6, 8, 12, 22, 24, 48, 72h), take 0.5ml of dialysate, constant volume with methanol, use HPLC to measure the concentration of camptothecin, and calculate the concentration of camptothecin at different times. Dissolution percentage. The results are attached image 3 as shown..

[0047] It can be seen from the figure that the in vitro drug release of the nanogel basically followed the first-order kinetic equation, and there was no significant difference in drug release between the OA-modified drug-loaded nanogel and the unmodified drug-loaded nanogel.

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Abstract

The invention discloses a nano-system which takes PLGA (polylactic-co-glycolic acid)-coated anti-psoriasis pharmaceutical camptothecin as a core of the nano-system, coats PAMAM (polyamidoamine) on the surface of PLGA as a shell of the nano-system and adopts an emulsification solvent volatilization method to prepare camptothecin, and furthermore, oleic acid (OA) is used for modification to obtain a core-shell nano-drug delivery system after surface modification. Further, hydroxypropyl methylcellulose (HPMC) is taken as a matrix to prepare camptothecin nano-gel (CPT-PPO gel). CPT-PPO gel modified by oleinic acid can significantly improve pharmaceutical skin absorption and detention without increasing skin permeation, thereby not increasing the amount of a medicament entering blood circulation, effectively reducing systemic toxicity of the medicament and being an excellent camptothecin local treatment new dosage form.

Description

technical field [0001] The invention relates to a camptothecin nanogel and a preparation method thereof, belonging to the field of pharmacy. Background technique [0002] Psoriasis (commonly known as psoriasis), is a chronic, recurrent, proliferative epidermal disease, is a recognized chronic skin disease. Camptothecin and other hormonal drugs are often used in clinical external treatment, but due to poor skin absorption and high toxicity, it often brings great inconvenience to patients and fails to achieve the desired therapeutic effect. In recent years, the development of new drug delivery systems, especially those based on nanocarriers, has provided more options and opportunities for the treatment of skin-related diseases. The drug carrier based on the nanosystem can skillfully control the slow isochronous release of the drug, and establish a skin reservoir to exert its effect on the local skin. In addition, due to the small particle size of drugs with nanometer particl...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/107A61K31/4745A61K47/12A61P17/06
Inventor 王翔陈杨张梁宇
Owner 中国人民解放军第九八医院
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