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Non-spherical drug-loaded particles and controlled release preparation of lactyl polymer and preparation methods thereof

A drug-loaded particle, non-spherical technology, applied in the direction of active ingredients of hydroxyl compounds, pharmaceutical formulations, anti-tumor drugs, etc., to achieve the effects of good reproducibility, no immunogenicity, and uniform particle size distribution

Inactive Publication Date: 2012-07-04
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has not been reported that PLGA non-spherical drug carrier is prepared by emulsion-solvent evaporation method and used in the study of ATRA sustained-release preparations under the regulation of sodium polyphosphate small molecules.

Method used

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  • Non-spherical drug-loaded particles and controlled release preparation of lactyl polymer and preparation methods thereof
  • Non-spherical drug-loaded particles and controlled release preparation of lactyl polymer and preparation methods thereof
  • Non-spherical drug-loaded particles and controlled release preparation of lactyl polymer and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Weigh 150 mg of polylactic-co-glycolic acid (PLGA) (molecular weight: 10,000) and add it to 15 mL of dichloromethane, stir until dissolved at room temperature; 5 P 3 o 10 , content 90-95%) was added to 0.5% PVA (polymerization degree 550-650, alcoholysis degree 88%) solution and stirred until dissolved. Mix 15mL PLGA dichloromethane solution with 100mL PVA solution containing STP, stir at 1200rpm for 2 hours, centrifuge at 10000rpm, wash off the surfactant with deionized water, and freeze-dry at -30°C to obtain a white powder. The yield was 97%. The SEM pictures of the particles are shown in figure 1 , the shape is rod-like, the length is 6-9 μm, the diameter is 0.5-1.6 μm, the aspect ratio is 5-12, the physical and chemical properties of the particles are stable, and the reproducibility is good.

Embodiment 2

[0033] Weigh 100 mg of polylactic-co-glycolic acid (PLGA) (molecular weight: 50,000) and add it to 10 mL of dichloromethane, stir until dissolved at room temperature; add 0.735 g of sodium polyphosphate (STP) to 0.4% PVA (polymerized degree 550~650, degree of alcoholysis 88%) and stirred in the solution until dissolved. Mix 10mL PLGA dichloromethane solution with 100mL PVA solution containing STP, stir at 1200rpm for 2 hours, centrifuge at 10000rpm, wash the surfactant with deionized water, and freeze-dry at -30°C to obtain a white powder. The yield was 86%. The SEM pictures of the particles are shown in figure 2 , the shape is fibrous, the length is 18-50 μm, the diameter is 0.4-5 μm, the aspect ratio is 6-14, the physical and chemical properties of the particles are stable, and the reproducibility is good.

Embodiment 3

[0035] Weigh 100 mg of PLGA (molecular weight 5000) and 20 mg of all-trans retinoic acid (ATRA) into 10 mL of dichloromethane, stir at room temperature until dissolved; add 1.84 g of sodium polyphosphate (STP) to 0.5% PVA (Polymerization degree 550-650, alcoholysis degree 88%) Stir in the solution until dissolved. Mix 10 mL of dichloromethane solution containing ATRA and PLGA with 100 mL of PVA solution containing STP, stir at 800 rpm for 2 hours, centrifuge at 10,000 rpm, wash the surfactant with deionized water, and freeze-dry at -30°C to obtain a light yellow powder. The shape of drug-loaded particles is fibrous, see attached image 3 . Such as Figure 4 Curve d shows a slow release over a period of 4 weeks with a cumulative release rate of 7.5%. Compared with the ATRA microspheres prepared without adding small molecule excipients under the same conditions, the drug loading and encapsulation efficiency increased from 8.83%, 48.4% to 17.9% and 89.9%, respectively. Figur...

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Abstract

The invention relates to non-spherical drug-loaded particles and a controlled release preparation of a lactyl polymer and preparation methods thereof. The non-spherical particles of polylactic-co-glycolic acid (PLGA) are prepared by using an emulsion-solvent volatilization method assisted by small molecule materials. The PLGA is used as raw material coated with at least one of the following hydrophobic drugs: all-trans retinoic acid, paclitaxel, epirubicin, camptothecin or roxithromycin, wherein the mass ratio of the hydrophobic drug to a lactyl polymer high polymer material is 1:4-40. The drug-loaded particles of the all-trans retinoic acid are prepared and subjected to in vitro drug release evaluation. The results show that the preparation method has the advantages of simple preparationprocess, good reproducibility, significantly increased drug loading amount and encapsulation efficiency relative to spherical particles, very good controlled-release effect, no hemolysis initiation and safety use. The novel carrier and preparation have a potential industrial production value in the field of long-circulating controlled release of the hydrophobic drugs.

Description

technical field [0001] The invention relates to a lactic acid-based polymer non-spherical drug-loaded particle, a sustained-release preparation and a preparation method thereof, in particular to a preparation method of a lactic acid-based polymer non-spherical drug-loaded particle loaded with hydrophobic drugs, and polylactic acid-glycolic acid Copolymer (PLGA) non-spherical microparticles as the carrier of all-trans retinoic acid long-circulation sustained-release preparations. Background technique: [0002] Although spherical carriers such as polymer microspheres or nanospheres have been intensively studied in drug delivery systems, spherical carriers are easily cleared by the mononuclear phagocyte system (MPS) after intravenous injection into animals, making them in the long-term Use in circulatory sustained-release formulations is limited. In 2006, Mitragotri used the membrane stretching method to prepare polystyrene particles of different shapes, and clarified that mac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/14A61K47/34A61K31/203A61P35/00
Inventor 张其清李瑞丰周志敏熊青青
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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