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Pyramidal microneedles with enhanced drug loading capacity and method for manufacturing

A pyramid-shaped, micro-needle technology, which is applied in the direction of drug devices, micro-needles, drug delivery, etc., can solve the problems of lengthy, impractical large-scale production, etc.

Inactive Publication Date: 2019-11-19
林治远
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method is lengthy as it involves several cycles of casting and drying, which may be impractical for mass production

Method used

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  • Pyramidal microneedles with enhanced drug loading capacity and method for manufacturing
  • Pyramidal microneedles with enhanced drug loading capacity and method for manufacturing
  • Pyramidal microneedles with enhanced drug loading capacity and method for manufacturing

Examples

Experimental program
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Effect test

example 1

[0043] Two types of microneedle templates were prepared, one was a common type with patch size 8 mm × 8 mm, 14 × 14 array, height = 600 μm, base = 200 μm × 200 μm, tip-to-tip distance = 500 μm; the other had Same configuration but with "Extended Bevel Base" feature. The drug suspension is diclofenac sodium at a concentration of 2.5 mg / ml. The matrix material solution is hyaluronic acid (HA) 0.6 g / ml. First, 40 μl of diclofenac suspension (containing 0.1 mg of diclofenac sodium) was loaded on two microneedle templates. The loaded template was subjected to a centrifugation process at 5000 rpm for 5 minutes, after which the supernatant was removed from the substrate cavity of the microneedle template. Second, 60 μl of HA solution was loaded on the two microneedle templates, followed by centrifugation at 5000 rpm for 7 minutes. Finally, the microneedle template was placed in an environmental chamber at 25°C and 40% relative humidity (RH) for 8 hours at atmospheric pressure.

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example 2

[0050] This experiment was performed to investigate the importance of the order of centrifugation of drug suspensions and matrix material solutions. An "extended bevel base" microneedle template with a configuration of 10 x 10 array, height = 600 μm, base = 200 μm x 200 μm, tip-to-tip distance = 500 μm was used. The drug suspension was diclofenac sodium at a concentration of 25 mg / ml, and the matrix material solution was sodium hyaluronate (HA) at a concentration of 0.6 g / ml. There are two specimens, one is "matrix first" and the other is "drug first". For "matrix-first" specimens, 40 μl of matrix material solution was loaded onto the microneedle template, and the loaded template was subjected to a centrifugation process at 5000 rpm for 5 minutes. Subsequently, 40 μl of the drug suspension was loaded onto the HA-filled microneedle template. The microneedle template was subjected to another centrifugation process at 5000 rpm for 7 minutes. Finally, the centrifuged template w...

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Abstract

The present invention provides a solution to increase the drug loading capacity and drug delivery precision of dissolving microneedles. These solutions include: (a) increasing the base of the microneedle cavities without substantially changing the microneedle's height and geometry, (b) use of drug suspension and sedimentation of drug by centrifugation, and (c) a specific centrifugation order for filling drug and matrix material. In the first preferred embodiment, a microneedle master mould comprising a plurality of pyramidal microneedles (5100), wherein each of the pyramidal microneedles further comprising a chamfered base (5200) which extends to and adjoins with its neighbouring chamfered bases is provided. In the second preferred embodiment, a method of making dissolving microneedles isprovided, comprising (a) providing a microneedle template comprising a plurality of pyramidal microneedle cavities, wherein each of the pyramidal microneedle cavities further comprising a chamfered base which extends to and adjoins with its neighbouring chamfered bases; (b) loading a drug suspension in the substrate cavity on the microneedle template; (c) centrifuging the microneedle template which is loaded with a drug suspension, (d) loading a matrix material solution in the substrate cavity on the microneedle template; (d) centrifuging the microneedle template loaded with the drug suspension and the matrix material solution; and (e) drying the centrifuged microneedle template in a controlled environment.

Description

technical field [0001] The present invention relates to intradermal drug delivery using microneedles. More specifically, the present invention relates to methods of enhancing the drug loading capability of microneedles. Background technique [0002] Microneedles are tiny spikes with a submillimeter height of 50 μm–500 μm, usually loaded with drugs that will be delivered painlessly into the skin. When microneedles physically penetrate the skin, it is considered an intradermal route and is more effective at delivering drugs to the skin than transdermal patches that do not physically penetrate the skin. Microneedle patches are preferred in drug delivery due to several beneficial features. For example, it is painless compared to parenteral (injection with a needle) administration, so it can be self-administered by the patient. Compared with oral administration, it is delivered directly to the systemic circulation without passing through the gastrointestinal tract. This means...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61M37/00
CPCA61K9/0021A61M37/0015A61M2037/0023A61M2037/0046A61M2037/0053
Inventor 林治远
Owner 林治远
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