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

AI Technical Summary

Problems solved by technology

However, it is a hydrophilic polymer, and FNS is relatively hydrophobic. Direct drug loading will ine

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

Examples

Experimental program
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Example Embodiment

[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 include:

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

[0044] S2. The drug-loaded PHBV solution obtained in step S1 is added to the polyvinyl alcohol solution and stirred to form an O / W emulsion;

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

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

[0047] S5. Add the S / W mixed phase obtained in step S4 to the pre-emulsified oil phase, stir to form an S / W / O emulsion, add ether-sat...

Example Embodiment

[0065] Example 1

[0066] Weigh 160 mg of PHBV (PHV is 12 mol%) in a mixed organic solvent of 4 mL of dichloromethane / ethyl acetate (dichloromethane / ethyl acetate=70:30, v / v), and heat it to 40℃ fully in a water bath Dissolve, add 80mg FNS immediately after cooling, and ultrasonic for 8min to dissolve the drug. Add the above FNS / PHBV solution to a glass sample bottle containing 16mL of 1wt% PVA1788, use a high-speed homogenizer to homogenize and stir at 8000rpm for 2min to form an O / W emulsion. After standing for 5min, add it to a three-necked flask containing 160mLPVA1788 In, mechanical stirring at 480 rpm at room temperature for 5 hours, centrifugation to collect the drug-loaded microspheres, centrifugal cleaning with deionized water 3 times, freeze-drying and storage. The morphological structure of drug-loaded microspheres was observed and analyzed by field emission scanning electron microscope (FESEM). By the attachment figure 1 It can be seen that the drug-loaded microsphe...

Example Embodiment

[0068] Example 2

[0069] Weigh 0.8g PVA124 into 5.85mL deionized water bath and heat to dissolve, meanwhile weigh 0.04210g CS (molecular weight 110kDa) and dissolve it in 5mL 1wt% acetic acid solution. The two were mixed under magnetic stirring, then a certain volume of Tween80 was added to the PVA / CS mixed solution to make the final concentration 0.5wt%, and the magnetic stirring was continued for 20 minutes. The FNS / PHBV microspheres prepared in Example 1 were dispersed in 3.5 mL of 1wt% polyvinyl alcohol 1788 solution, and then the PVA / CS mixed solution was added dropwise under magnetic stirring. After magnetic stirring for 20 minutes, it was ultrasonicated for 30 minutes 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-emulsification for 30 minutes), and magnetically stirred at 350 rpm for 30 minutes at room temperature to form an S / W / O emulsion. Add 25wt saturated ether % Gluta...

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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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