Fabrication and Characterization of Thiolated Chitosan Microneedle Patch for Transdermal Delivery of Tacrolimus

Abstract

Microneedle patch is a prominent strategy with minimal invasion and painless application to improve skin penetration of drug molecules. Herein, we report microneedle patch (MNP) as an alternative to the oral route for the systemic delivery of tacrolimus (TM), an immunosuppressant drug. Thiolated chitosan (TCS) based microneedle patch was fabricated and characterized in vitro and in vivo for its mechanical strength, skin penetration, drug release, and skin irritation. The MNP having 225 needles with 575 μm showed good mechanical properties in terms of tensile strength and percentage elongation. The skin penetration showed 84% penetration with no breakage. Histology of the mice skin after insertion showed the penetration of needles into the dermis. In vitro release and ex vivo permeation studies through Franz diffusion cell showed the sustained release (82.5%) of TM from the MNP with significantly higher (p < 0.05) skin permeation as compared with controls, respectively. Moreover, in vivo biocompatibility in rats showed the safety of the material and patch. Thus, the TCS microneedle patch has the potential to be developed as a transdermal delivery system for tacrolimus with improved bioavailability and sustained release over a longer period.

Polymeric microneedle‐mediated sustained release systems: Design strategies and promising applications for drug delivery

“…Chemotherapy is one of the most important arsenals to kill tumors [69] . Various versatile carriers greatly improve the anti-tumor effect of chemotherapy drugs [ 70 , 71 ].For chemotherapy, MN@SRS have been employed for delivery of doxorubicin (Dox), dacarbazine, and other drugs for chemotherapy [72] , [73] , [74] . Typically, Kim et al reported a design of a biodegradable MN patch based on porous silicon ( p -Si) with a novel water-soluble backing ( Fig.…”

Microneedle-Based Natural Polysaccharide for Drug Delivery Systems (DDS): Progress and Challenges

“…Nevertheless, the microneedles were able to penetrate the tumor-mimicking agarose gel and promote layerbased drug release [129]. It is reported that the addition of the thiol group improves the mechanical properties of chitosan, and hence, thiolated MNs are prepared with optimum mechanical strength and sharpness [130].…”

Microneedles for painless transdermal immunotherapeutic applications

“…In 2020, Ahmad et al fabricated thiolated chitosan (TCS)-based MN patch containing tacrolimus (TM), an immunosuppressant agent for the treatment of autoimmune disorders, by a mold casting method. The TCS-based MN patch was able to improve the drug bioavailability through circumvention of the hepatic first-pass metabolism and intestinal P-gp efflux and deliver the drug in a more sustained manner than oral administration [136]. Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) analysis demonstrated that characteristic peaks of TM were retained in MN patches, suggesting the stability of TM during the preparation process of the patches.…”