Preparation and Performance Investigation of Phase-transition Microneedles Loaded with Insulin Aspart via Diffusion Method
Polyvinyl alcohol(PVA)-based phase-transition microneedles can be utilized to load drugs through pores formed by swelling,and are highly promising for biomolecular drug delivery.However,due to the drug distribution at the root and center of drug-loaded microneedles prepared by the conventional premixing method,the diffusion distance during drug release is large and penetration through the hydrogel network matrix is difficult,which limit the bioavailability of the drug.Therefore,the diffusion method was used for protein drug-loading and the mass ratio of PVA solution to excipient(sodium carboxymethylcellulose and dextran)solution was optimized to improve the drug loading,drug release rate,and epidermal permeability.The results showed that when the mass ratio of PVA solution to excipient solution was 3∶1 and the solid content was 17.8％,the microneedles had high swelling properties and strong mechanical properties,and could effectively deliver the drug to the dermis.Using insulin aspart as a model drug,compared with the traditional premixing method(the transdermal delivery rate was less than 25％),the transdermal delivery rate of drug-loaded microneedles prepared by the diffusion method could reach 31.0％-34.6％,and the in vitro release rate was up to 93％.The drug-loaded microneedles prepared by the diffusion method can improve the release rate and bioavailability of hydrophilic macromolecules,providing a new strategy for the development of transdermal drug delivery systems.
万方数据
维普
