Preparation and preliminary investigation of hyaluronic acid microneedle patches loaded with rapamycin nanocrystals
Objective Biodegradable drug loaded microneedles can achieve sustained,safe,and painless local drug release,while microneedle drug delivery systems used in the cardiovascular field can maximize the local anticoagulation of drugs,inhibit endometrial hyperplasia,and reduce the toxic side effects of systemic drug administration.For this purpose,this article prepared a hyaluronic acid microneedle patch loaded with rapamycin nanocrystals,and evaluated its preliminary physicochemical properties,in vitro simulated drug release performance evaluation,and analysis and evaluation of its puncture performance into the great saphenous vein.Methods Firstly,the aqueous rapamycin nanoparticles(RAP-NPs)doped with 1.5 million molecular weight hyaluronic acid(HA)as the base material are used to form drug evenly dispersed hydrogels.Then the water-soluble hyaluronic acid microneedle patches(HA-RAP-MN)of rapamycin aqueous nanocrystalline suspensions are prepared by the polydimethylsiloxane(PDMS)template method.Finally,preliminary physicochemical properties and in vitro simulated drug release performance analysis and evaluation are conducted on this drug loaded microneedle.Results RAP NPs aqueous suspension can form a mixed mixture with HA hydrogel,which enables drugs to be evenly dispersed in microneedles and continuously release drugs,and solves the technical bottleneck that insoluble drug molecules cannot be evenly dispersed in HA hydrogel.Drug simulation release experiments show that rapamycin can release more than 70%of drugs within 8 hours,achieving sustained release effect.Immunofluorescence application testing can prove that rapamycin is uniformly distributed in the venous media and intima.Conclusions The hyaluronic acid microneedle patch HA-RAP-MN,a water-soluble rapamycin nanocrystal suspension,has promising potential for local reduction of intimal hyperplasia after coronary artery bypass grafting.
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