Fabrication, Physicochemical Characterization, and Performance Evaluation of Biodegradable Polymeric Microneedle Patch System for Enhanced Transcutaneous Flux of High Molecular Weight Therapeutics

Abstract

A revolutionary paradigm shift is being observed currently, towards the use of therapeutic biologics for disease management. The present research was focused on designing an efficient dosage form for transdermal delivery of α-choriogonadotropin (high molecular weight biologic), through biodegradable polymeric microneedles. Polyvinylpyrrolidone-based biodegradable microneedle arrays loaded with high molecular weight polypeptide, α-choriogonadotropin, were fabricated for its systemic delivery via transdermal route. Varied process and formulation parameters were optimized for fabricating microneedle array, which in turn was expected to temporally rupture the stratum corneum layer of the skin, acting as a major barrier to drug delivery through transdermal route. The developed polymeric microneedles were optimized on the basis of quality attributes like mechanical strength, axial strength, insertion ratio, and insertion force analysis. The optimized polymeric microneedle arrays were characterized for in vitro drug release studies, ex vivo drug permeation studies, skin resealing studies, and in vivo pharmacokinetic studies. Results depicted that fabricated polymeric microneedle arrays with mechanical strength of above 5 N and good insertion ratio exhibited similar systemic bioavailability of α-choriogonadotropin in comparison to marketed subcutaneous injection formulation of α-choriogonadotropin. Thus, it was ultimately concluded that the designed drug delivery system can serve as an efficient tool for systemic delivery of therapeutic biologics, with an added benefit of overcoming the limitations of parenteral delivery, achieving better patient acceptability and compliance.

Noninvasive vaccination against infectious diseases

“… 157 Several materials, including polymers, colloidal silica, ceramics, steel, glass, sugar, hydrogel, and alumina, are used for microneedle fabrication. 158-164 Each type of microneedle employs different mechanisms for vaccine delivery. Solid microneedles are generally made of stainless steel with a diameter of 500 μm, which directly generates skin pores and allows the penetration of topical vaccine through the surface of the pretreated skin into the body, 165 while drug-coated microneedles are used to release the drug slowly into the skin.…”

Translation of Polymeric Microneedles for Treatment of Human Diseases: Recent Trends, Progress, and Challenges

“…A closer look at the MN patches reveals high-resolution architecture with fine and sharp tips [181,[183][184][185][186].…”

“…The images of coated MNs are captured digitally from a fixed working distance using different magnifications (e.g., 30, 80, 110, or 120×) [ 2 , 164 ]. A closer look at the MN patches reveals high-resolution architecture with fine and sharp tips [ 181 , 183 , 184 , 185 , 186 ].…”

Multifunctional Graphene-Oxide-Reinforced Dissolvable Polymeric Microneedles for Transdermal Drug Delivery

“…Sufficient GO loading is critical in preventing microbial contamination, which is consistent with established knowledge of the antibacterial and antifungal effect of GO, resulting from the mechanical damage of cell membranes by basal plane contact and oxidative chemical species generated at GO edges. 38−40 This mechanism has two S11), so GO-DPMNs can prevent microbial infections until complete healing of the insertion sites over 6−24 h. 12,41 Unlike small antibiotic molecules or dissolved silver ions, GO does not diffuse quickly or decompose within the insertion pores in the skin tissue, enabling their long-acting effect. Second, the combined antibacterial mechanism, that is, mechanical and chemical, makes it extremely difficult for microbes to evolve GO-resistant strains because microbes must use phospholipidbased cell membranes, which are susceptible to both mechanical damage and chemical oxidation.…”