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Drug delivery platform using w/o/w-type triolein emulsion promotive of blood-brain barrier opening

A technology of triolein and drugs, which is applied in the field of drug delivery platform using W/O/W triolein emulsion to promote the opening of the blood-brain barrier, and can solve problems such as drug delivery obstacles for brain diseases

Active Publication Date: 2021-08-17
PUSAN NAT UNIV IND UNIV COOPERATION FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the BBB, tight junctions are formed between cells, so fat-soluble substances can pass through the BBB, but water-soluble substances or polymer substances have difficulty passing through the BBB, which is an obstacle for drug delivery for treating brain diseases

Method used

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  • Drug delivery platform using w/o/w-type triolein emulsion promotive of blood-brain barrier opening
  • Drug delivery platform using w/o/w-type triolein emulsion promotive of blood-brain barrier opening
  • Drug delivery platform using w/o/w-type triolein emulsion promotive of blood-brain barrier opening

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The preparation of the triolein emulsion of W / O / W bilayer structure

[0049] Such as figure 1 As shown in the schematic diagram of , in order to prepare a triolein emulsion (right) with a W / O / W double-layer structure that is more stable than the conventional triolein emulsion (left), firstly, Span 80 (as a surface active ) and Congo red (as a water-soluble pigment) were mixed with triolein (Sigma Aldrich) and red water droplets in the triolein solution were emulsified by a sonicator to prepare the first emulsion.

[0050] At this time, as a result of observing the emulsion by using an optical microscope, as figure 2 As shown in A, it was confirmed that the red water-soluble pigment was located inside the triolein in the form of droplets.

[0051] Then, a certain amount of water containing 1% polyvinyl alcohol was added to the first emulsion, and mixed using a syringe as a power source to prepare a triolein emulsion with a W / O / W structure, which contained water drople...

Embodiment 2

[0053] Measurement of the average particle size distribution of the triolein emulsion of W / O / W bilayer structure

[0054] Using an optical microscope, 200 or more particles of the triolein emulsion of the W / O / W bilayer structure prepared according to the method disclosed in Example 1 above were randomly sampled according to their average particle size, and passed Particle diameters were measured and statistically processed using the Image J program with a scale bar versus length comparison.

[0055] As a result, such as image 3 As shown in and , the triolein emulsion mainly exhibited an average particle diameter of 5 μm-20 μm, and the average value was about 7.58 μm. At this time, it is estimated that particles with an average particle diameter of 5 μm–20 μm are involved in temporary BBB opening, and safety may be greatly affected when an emulsion containing a large number of particles larger than 20 μm is used.

[0056] [Table 1]

[0057]

Embodiment 3

[0058] Confirmation of the drug delivery effect of the triolein emulsion of the W / O / W bilayer structure to the brain

[0059] (1) Confirmation of BBB opening activity of triolein emulsion

[0060] First, a triolein emulsion was prepared according to the method performed in Example 1, and the average diameter was set to 7 μm, and the emulsion concentration was adjusted to 2%. The microcatheter was injected into the femoral artery of rabbits (1.7 Kg, male) sold separately by Semtako, and the needle tip was placed in one carotid artery, and 7 mL of the above-prepared emulsion was injected per rabbit. Subsequently, 3 mL of trypan blue was injected into the rabbit immediately, and 2 hours later, the brain of the rabbit was excised and the blue stained area was observed. At this time, the following principle was used: when the BBB is open, the open area is stained blue.

[0061] As a result, such as Figure 4 As shown, it was found that the BBB open area of ​​right brain tissue ...

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Abstract

The present invention relates to a composition comprising, as an active ingredient for drug delivery into a tissue having a tight junction, a triolein emulsion in an internal water phase / oil phase / external water phase (water / oil / water; W / O / W)-type structure in which an oil droplet includes triolein and a water droplet is enclosed inside the oil droplet, and to a preparation method therefor. The triolein emulsion in the W / O / W-type structure according to the present invention has water-phase droplets enclosed inside oil-phase droplets while exhibiting that the triolein retains the activity of opening BBB. In addition, the emulsion includes a surfactant and thus has excellent safety. Allowing a liposoluble drug to be further enclosed in the oil-phase droplets, the emulsion can used as a composite formulation and thus more effectively deliver the drug into tissues having tight junctions such as the brain, the testis, the retina, and the like.

Description

technical field [0001] The present invention relates to a composition for drug delivery and a preparation method thereof. The composition for drug delivery contains, as an active ingredient, triolein having an inner water phase / oil phase / outer water phase structure. ) lotion. Background technique [0002] For the treatment of CNS-related diseases, various types of therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, tumor suppressors, antibiotics and their prodrugs, precursors, derivatives and intermediates have been developed . Furthermore, the many known neuroactive peptides offer additional possibilities as useful therapeutic agents. Since neuroactive peptides play important biochemical roles in the CNS, such as neurotransmitters and / or neuromodulators, the delivery of such peptides of different sequences to the CNS may provide many opportunities for therapeutic benefit. Delivery of endogenous and synthetic opioid peptides such as ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/113A61K9/00A61K31/573A61K45/06
CPCA61K9/113A61K31/704A61K9/0085A61P35/00A61K31/573A61K47/14
Inventor 金鹤镇金哲民田炳学俞振旭李柱昊
Owner PUSAN NAT UNIV IND UNIV COOPERATION FOUND
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