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Layered microneedle, layered microneedle contraceptive system and preparation method and application of layered microneedle contraceptive system

A micro-needle and needle-tip technology, which is applied in the field of pharmaceutical preparations, can solve problems such as contraceptive failure, physical injury to users, and limited release rate, and achieve the effects of avoiding drug waste, meeting the needs of contraceptive duration, and avoiding discomfort

Pending Publication Date: 2022-04-05
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the elimination half-life of LNG in the blood is only 8.8 ～ 11 hours. During oral administration, the user needs to take the medicine regularly and quantitatively to achieve the purpose of long-term contraception. Missing or taking the wrong dose will lead to contraceptive failure
In addition, patients often experience nausea, vomiting and other uncomfortable symptoms after taking LNG, resulting in lower medication compliance
When LNG is used for long-acting drug delivery, it has been developed as a long-acting contraceptive product such as Norplant, which is a safe and effective contraceptive implant, but the implant requires professional medical personnel to implant into the human body, and surgery is required after use Taking it out will not only cause physical harm to the user but also increase the economic burden
Although in the prior art (Long-acting reversible contraception by effervescent microneedlepatch.Sci.Adv.2019,5(11):eaaw8145.) microneedles are used to deliver contraceptive drugs, the method of use is usually to simply physically mix the drug with the matrix, The release rate of the drug is controlled by the dissolution rate of the matrix, resulting in the release rate of the drug being limited by the properties of the material, which cannot achieve a regular and quantitative release

Method used

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  • Layered microneedle, layered microneedle contraceptive system and preparation method and application of layered microneedle contraceptive system
  • Layered microneedle, layered microneedle contraceptive system and preparation method and application of layered microneedle contraceptive system
  • Layered microneedle, layered microneedle contraceptive system and preparation method and application of layered microneedle contraceptive system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Preparation of layered microneedles:

[0046] (1) A layered microneedle patch was prepared using a polydimethylsiloxane (PDMS) mold with a conical hole array (Taizhou Microchip Pharmaceutical Technology Co., Ltd.). All arrays on the mold contain 10×10 needles, the array area is 8mm×8mm, the conical hole array contains 10×10 needles, the center-to-center spacing of each needle tip is 650 μm, and the height of each needle is 800 μm.

[0047] (2) Prepare a PVP (90k molecular weight) aqueous solution with a concentration of 300mg / ml to form a needlepoint pouring fluid.

[0048] (3) Use a straw to draw 200 μL of the prepared needle tip pouring solution and apply it on the PDMS mold, and centrifuge at 4000 rpm for 20 minutes to fill the microcavity of the PDMS mold and remove excess solution remaining on the surface of the mold.

[0049] (4) Weigh 300 mg of PS particles and dissolve in 1 mL of dioxazole solution (1,4-dioxane) to obtain a PS (molecular weight of 260k) dioxazo...

Embodiment 2

[0053] Fabrication of fluorescent layered microneedles

[0054] Weigh 1 μg of rhodamine B (R-B) powder and dissolve it in 2 mL of 300 mg / mL PVP aqueous solution to form a needle tip pouring solution, weigh 1 μg of coumarin 6 (C-6) powder and dissolve it in 2 mL of 300 mg / mL PS In the bisoxazole solution as the base pouring liquid, other preparation steps are the same as in Example 1.

[0055] like figure 2 The MC shown in (A) is a bright-field photo of fluorescent layered microneedles. figure 2 R-B shown in (B) is the fluorescence photo of the needle tip, figure 2 C-6 shown in (C) is the fluorescent photo of the substrate, figure 2 The Merge shown in (D) is the merged result of the R-B needle tip and the C-6 substrate. From the results of these four fluorescent photos, it can be known that the double-layer microneedle was successfully prepared.

Embodiment 3

[0057] Preparation steps of LNG@PCL nanospheres

[0058] (1) Weigh 50 mg of polycaprolactone (PCL) and 10 mg of levonorgestrel LNG, mix and dissolve in 3 mL of dichloromethane (DCM) to obtain a DCM mixed solution.

[0059] (2) Add the DCM mixed solution obtained in step (1) into 15 mL of PVA aqueous solution with a concentration of 50 mg / ml, and ultrasonically break in an ice bath for 30 minutes to form an O / W emulsion.

[0060] (3) The O / W emulsion obtained in the stirring step (2) was removed by volatilization to remove the DCM in the emulsion, and the stirring time was 24 hours.

[0061] (4) After removing DCM, the prepared LNG@PCL nanosphere precipitate was collected by centrifugation at 1000 rpm for 10 minutes, and washed 3 times with distilled water.

[0062] (5) Resuspend the washed LNG@PCL nanospheres in 20mg / mL aqueous mannitol solution, freeze-dry the resuspension, as image 3 As shown in (A), smooth and round LNG@PCL nanospheres are generated.

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Abstract

The invention discloses a layered microneedle, a layered microneedle contraception system and a preparation method and application of the layered microneedle, the layered microneedle comprises a polystyrene (PS) layer and a polyvinylpyrrolidone (PVP) layer, a needle body of the layered microneedle contraception system comprises nanospheres LNG (at) PCL / F68 and free levonorgestrel (LNG), and the nanospheres LNG (at) PCL / F68 are prepared by mixing the levonorgestrel (LNG), polycaprolactone (PCL) and poloxamer 188 (F68). A certain amount of medicine can be continuously and stably released by adjusting the dosage of F68 or the input amount of medicine LNG, and the requirements of different crowds for contraception duration are met. Meanwhile, due to the removable design of the layered microneedle substrate, the discomfort caused by the fact that other percutaneous preparations such as dressings stay on the skin surface for a long time is avoided, and the embarrassment that a patient uses contraceptive products is avoided.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a layered microneedle, a layered microneedle contraceptive system and a preparation method and application thereof. Background technique [0002] Unplanned pregnancy has always been one of the problems plaguing all mankind. Although there are many contraceptive methods, such as physical contraception and hormonal contraception, there are problems such as side effects and missed doses. Implantable long-acting contraceptives such as subcutaneous implants can continue to prevent pregnancy for several years. At the same time, the drug enters the blood circulation through local capillaries, which can effectively avoid the gastrointestinal absorption of traditional oral preparations. Professional training, limited use. According to (Lack of pain associated with microfabricated microneedles. Anesth Analg. 2001,92 (2): 502-504.) report, the transdermal patch of co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00
Inventor 鞠艳敏戴建君邓舒月
Owner CHINA PHARM UNIV
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