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Multi-core co-shell compound drug-carrying microsphere, and preparation method and application thereof

A drug-loaded microsphere and multi-core technology, which is applied in the fields of application, pharmaceutical formulation, and drug combination, can solve the problems of drug burst release and drug loading rate reduction, and achieve improved utilization, good biocompatibility, and reduced burst release effect of effect

Active Publication Date: 2019-10-15
EZHOU INST OF IND TECH HUAZHONG UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it is a hydrophilic polymer, and FNS is relatively hydrophobic. Direct drug loading will inevitably lead to a decrease in the drug loading rate, and there will inevitably be drug burst release.

Method used

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  • Multi-core co-shell compound drug-carrying microsphere, and preparation method and application thereof
  • Multi-core co-shell compound drug-carrying microsphere, and preparation method and application thereof
  • Multi-core co-shell compound drug-carrying microsphere, and preparation method and application thereof

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preparation example Construction

[0042] The second aspect of the present invention provides a method for preparing the above-mentioned multi-core co-shell composite drug-loaded microspheres, the steps comprising:

[0043] S1. Heat and dissolve the oil-soluble PHBV in an organic solvent, and then add FNS sonication to dissolve it in the organic solvent to obtain a drug-loaded PHBV solution;

[0044] S2. Add the drug-loaded PHBV solution obtained in step S1 into the polyvinyl alcohol solution, and stir to form an O / W emulsion;

[0045] S3. Add the O / W emulsion obtained in step S2 dropwise into the polyvinyl alcohol solution, stir until the organic solvent volatilizes to obtain the drug-loaded microspheres, and freeze-dry them after washing;

[0046] S4. Add the FNS / PHBV microspheres obtained in step S3 to the PVA / CS mixed solution containing Tween80, stir and sonicate to form a S / W mixed phase;

[0047] S5. Add the S / W mixed phase obtained in step S4 into the pre-emulsified oil phase, stir to form a S / W / O emul...

Embodiment 1

[0066] Weigh 160mg PHBV (PHV is 12mol%) in the mixed organic solvent that is equipped with 4mL dichloromethane / ethyl acetate (dichloromethane / ethyl acetate=70:30, v / v), the water bath is heated to 40 ℃ fully Dissolve, add 80mg FNS immediately after cooling, and dissolve the drug by ultrasonication for 8min. Add the above FNS / PHBV solution into a glass sample bottle containing 16mL 1wt% PVA1788, use a high-speed homogenizer to homogeneously stir at 8000rpm for 2min to form an O / W emulsion, and then add it to a three-necked flask containing 160mLPVA1788 after standing for 5min , stirred mechanically at 480 rpm for 5 h at room temperature, collected the drug-loaded microspheres by centrifugation, washed three times with deionized water, and stored after freeze-drying. The morphology and structure of the drug-loaded microspheres were observed and analyzed by field emission scanning electron microscopy (FESEM). attached by figure 1 It can be seen that the drug-loaded microspheres...

Embodiment 2

[0069] Weigh 0.8g of PVA124 and add 5.85mL of deionized water in a water bath to heat to dissolve, meanwhile weigh 0.04210g of CS (molecular weight is 110kDa) and dissolve in 5mL of 1wt% acetic acid solution. The two were mixed under magnetic stirring, and then a certain volume of Tween80 was added into the PVA / CS mixed solution to make the final concentration 0.5 wt%, and the magnetic stirring was continued for 20 min. Disperse the FNS / PHBV microspheres prepared in Example 1 in 3.5mL of 1wt% polyvinyl alcohol 1788 solution, then add the PVA / CS mixed solution dropwise under magnetic stirring, and then perform ultrasonication for 30min after magnetic stirring for 20min to form a uniform S / W mixed phase. The S / W mixed phase was slowly added dropwise to 72 mL of n-heptane with a mass fraction of 2.43% Span80 (pre-emulsified for 30 min), magnetically stirred at 350 rpm at room temperature for 30 min to form a S / W / O emulsion, and 25 wt. % glutaraldehyde solution (ether: 4.15 mL, g...

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Abstract

The invention discloses a multi-core co-shell compound drug-carrying microsphere, and a preparation method and application thereof. Firstly, through an emulsified solvent evaporation method, an FNS (Finasteride) / PHBV (Poly(3-hydroxybutyrate-3-hydroxyvalerate)) microsphere is prepared, the FNS / PHBV microsphere is coated to a PVA (Polyvinyl alcohol) / CS (Chitosan) hydrophilic polymer matrix through an inverse suspension crosslinking method, a hydrophobic drug is efficiently and artfully coated to the hydrophilic polymer, and the load rate of a hydrophilic drug is improved. The particle size of the prepared FNS / PHBV@PVA / CS drug-carrying microsphere meets the treatment requirement of a prostate targeted embolism. From a drug release curve, a whole drug release process is free from burst release, and sustained release is realized. An in-vitro cell experiment and a hemolytic experiment prove that the microsphere exhibits good cellular compatibility and blood compatibility. A rabbit ear embolism experiment preliminarily indicates that the microsphere has a good embolism effect and good histocompatibility. In addition, the microsphere has the advantages of simple preparation technology andcontrollable particle size and is suitable for industrial batch production. The physical embolism performance and the drug slow release performance of the compound drug-carrying microsphere can be effectively combined, and the microsphere has a potential application prospect in BPH (Benign Prostate Hyperplasia) embolism treatment.

Description

technical field [0001] The invention belongs to the technical field of prostate interventional medicine, and in particular relates to a multi-core co-shell composite drug-loaded microsphere and its preparation method and application. Background technique [0002] Benign prostatic hyperplasia (BPH) is one of the common urinary system diseases in middle-aged and elderly men, mainly manifested as lower urinary tract symptoms such as frequent urination, dysuria, and urinary hesitancy. For mild patients, drug treatment is generally used to relieve symptoms, but it cannot be completely eradicated. The method of surgical treatment brings greater trauma to the patient and is prone to complications. Clinically, transurethral prostatectomy is considered to be the "gold standard" in the treatment of BPH, but the disadvantage of this method is that the prostate gland cannot be completely separated and removed from the surrounding capsule, and the remaining prostate gland will lead to p...

Claims

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Application Information

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IPC IPC(8): A61K9/62A61K47/34A61K47/32A61K47/36A61K31/58A61P13/08A61L24/08A61L24/06A61L24/04A61L24/00
CPCA61K9/5026A61K9/5031A61K9/5036A61K9/5073A61K9/5089A61K31/58A61L24/001A61L24/0015A61L24/046A61L24/06A61L24/08A61L2300/204A61L2300/602A61P13/08C08L5/08C08L29/04C08L67/04
Inventor 杨光李晓宏纪雄发肖骏曹佳梦尹雅琪
Owner EZHOU INST OF IND TECH HUAZHONG UNIV OF SCI & TECH
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