Fascile synthesis of biocompatible polymer capsule nanoparticles for drug encapsulation

Patent metadata

Field	Value
Publication number	US-9592205-B2
Application number	US-201213624038-A
Country	US
Kind code	B2
Filing date	Sep 21, 2012
Priority date	Sep 21, 2011
Publication date	Mar 14, 2017
Grant date	Mar 14, 2017

Abstract

The present invention relates to a method for preparing a capsule nanoparticle used in encapsulating hydrophobic medicines, comprising the following steps: (A) providing a biocompatible polymer and an organic solution containing a hydrophobic medicine; (B) stirring the organic solution at 3-10° C., and titrating with an alcohol solution, so as to make the biocompatible polymer encapsulate hydrophobic medicine to form a capsule nanoparticle; (C) ultrasonic vibrating the capsule nanoparticle at 3-10° C.; (D) filtering the capsule nanoparticle to an average size controllable in the range of 60-450 nm; and (E) lyophilizing the encapsulated particles.

First claim

What is claimed is:

1. A method for preparing capsules encapsulating hydrophobic medicines, comprising the steps of:
(A) providing an organic solution having a biocompatible polymer and a hydrophobic medicine;
(B) stirring the organic solution at a low temperature of 3 to 10° C., and titrating with an alcohol solution, to make the biocompatible polymer encapsulate the hydrophobic medicine to form a capsule nanoparticle;
(C) ultrasonic vibrating the capsule nanoparticle at a low temperature of 3 to 10° C.;
(D) filtering the capsule nanoparticle, to make an average capsule nanoparticle diameter of the capsule nanoparticle at 60-450 nm; and
(E) lyophilizing the capsule nanoparticle;
Wherein the biocompatible polymer is selected from the group consisting (poly-(D,L-lactide-co-glycolide)), PLA, and PEG-PLA;
and wherein the steps (A) to (E) are performed without surfactant.

2. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein the hydrophobic medicine is an anti-cancer medicine.

3. The method for preparing capsules encapsulating hydrophobic medicines according to claim 2 , wherein, the anti-cancer is at least selected from the group consisting of: phyxol, J-30, LY 294002 and AG490.

4. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein the organic solution is acetone solution.

5. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein, step (B) is stirring the organic solution at a low temperature of 4-6° C.

6. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein the alcohol is an ethanol solution.

7. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein step (C) is ultrasonic vibrating the capsule nanoparticle at a low temperature of 4-6° C.

8. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein step (C) further comprises a step (C1):
(C1) adding the organic solution having the capsule nanoparticle into a milli Q water (M.Q water), and ultrasonic vibrating the capsule nanoparticle.

9. The method for preparing capsules encapsulating hydrophobic medicines according to claim 8 , wherein step (C) further comprises a step (C2):
(C2) eliminating the organic solution in the milli Q water.

10. The method for preparing capsules encapsulating hydrophobic medicines according to claim 9 , wherein in step (C2), remaining organic solution in the milli Q water is eliminated through dialysis.

11. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein, an average capsule nanoparticle diameter of the capsule nanoparticle is 150-250 nm.

12. The method for preparing capsules encapsulating hydrophobic medicines according to claim 9 , step (E) further comprises a step (E1):
(E1) replacing the milli Q water having the capsule nanoparticle with a milli Q water having sucrose and the capsule nanoparticle.

13. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein, an encapsulation rate for the biocompatible polymer encapsulating the hydrophobic medicine is 10-90%.

Assignees

• Shieh Dar-Bin
• Univ Nat Cheng Kung

Inventors

• Shieh Dar-Bin

Classifications

• A61K9/5153

  Polyesters, e.g. poly(lactide-co-glycolide) · CPC title

• Y10S977/915

  Therapeutic or pharmaceutical composition · CPC title

• A61K31/337

  having four-membered rings, e.g. taxol · CPC title

• Y10S977/788

  Of specified organic or carbon-based composition · CPC title

• A61K9/5192 Primary

  Processes · CPC title