Slow-release soluble microneedle delivery system for mite-allergen-loaded microspheres

Abstract

The invention discloses a slow-release soluble microneedle delivery system for mite-allergen-loaded microspheres. The system comprises a needle body and a backing, wherein the needle body comprises the mite allergen microspheres and a matrix material, the matrix material is a mixture of a methyl vinyl ether-maleic anhydride copolymer and polyethylene glycol, and the content ratio of the methyl vinyl ether-maleic anhydride copolymer to the polyethylene glycol is (2:1)-(1:1). According to the system, the specific component types and content ratio of the mite allergen microspheres are selected, so that the prepared mite allergen slow-release microspheres are excellent in performance and can well load mite allergen; and the specific component types and content ratio of the matrix material and the specific drug loading ratio are selected, so that the prepared mite allergen slow-release soluble microneedle is excellent in formability, mechanical strength and other performance, the release time of the drug is greatly prolonged, the treatment effect is superior to that of a non-slow-release mite allergen soluble microneedle, the administration frequency of the mite allergen can be reduced, and the compliance of a patient can be improved.

Description

technical field [0001] The invention relates to the technical field of administration of mite allergens, in particular to a slow-release soluble microneedle delivery system loaded with mite allergen microspheres. Background technique [0002] Mites are an important source of allergens that induce allergic diseases such as asthma, allergic rhinitis, and eczema. In recent years, investigations and studies in many countries such as the United States, New Zealand, and Australia have successively confirmed that the close relationship between mite-derived allergens and allergic diseases is the cause of allergic diseases such as allergic asthma; desensitization treatment has become the most effective treatment for such diseases. treatment method. However, mite allergens are currently mostly administered in the form of injections, and long-term injections lead to poor patient compliance. Therefore, a new dosage form for the delivery of mite allergens is urgently needed. [0003] A...

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Problems solved by technology

[0005] By consulting the literature and patents at home and abroad, there are literature and patent reports that mite allergens are directly loaded into soluble microneedles: for example, Kim et al. prepared soluble microneedles with hyaluronic acid to deliver mite allergens (Kim J H, Shin J U, Kim et al. S H, etal.Successful transdermal allergen delivery and allergen-specificimmunotherapy using biodegradable microneedle patches[J].Biomaterials,2018,150:38-48); such as the Japanese patent with publication number JP2014156433A and the Chinese patent with publication number CN109715075A, which describe Material selection when soluble microneedles are directly loaded with allergens, but none of them involve the related content of mite allergen slow-release microneedles

[0006] In addition, there is no mite allergen microsphere delivery at present, although there are microsphere delivery of pollen allergen and bee venom allergen (AProtective Allergy Vaccine Based on CpG-and Protamine-Containing PLGA Microparticles[J].Pharmaceutical Research, 2007 , 24(10):1927-1935.), but there are compositional differences between the protein components of mite allergen vaccines and pollen allergens, bee venom allergens, etc., how to have a good loading effect on mite allergens still remains Uncertain

[0007] In addition, although some researchers have prepared soluble microneedles loaded with microspheres, they have not passed the corresponding formulation screening to achieve better mechanical properties (Ke C J, Lin Y J, Hu Y C, et al. Multidrug release based on microneedle arrays filled with pH-responsive PLGA hollow microspheres.[J].Biomaterials,2012,33(20):5156-5165; DeMuth P C,Garcia-Beltran W F,Ai-Ling ML,et al.Composite dissolving microneedles for coordinated control of antigen and adjuvant delivery kinetics in transcutaneous vaccination[J].Advanced functional materials,2013,23(2):161-172), at the same time, the loaded drug is different, the construction material of the microspheres will also change, according to the literature (Zhang Jie, Ma Fengsen, Zhan Haohui et al., Matrix materials and their composite materials used to construct dissolvable microneedles[J]. Combination will lead to differences in the mechanical properties of soluble microneedles; according to the literature (Park J H, Allen M G, PrausnitzM R. Polymer microneedles for controlled-release drug delivery [J]. Pharmaceutical Research, 2006,23(5):1008-19) It can be seen that as the content of drugs in the microneedle formulation increases, the mechanical properties of the microneedle will decrease.

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