Abstract
Dissolving microneedle (DMN) patches were developed as efficient and patient-friendly transdermal delivery systems for biopharmaceuticals. However, recent studies have confirmed that the efficiency of DMNs to deliver biopharmaceuticals is highly reduced because of incomplete insertion caused by the stiffness and elastic properties of the skin. Therefore, micropillar integrated DMNs were developed to overcome the insertion limitations of DMN patches. Although micropillars were designed as integrated applicators to implant DMNs across the skin, they can also become inserted into the skin, leading to skin injury and inflammation. Herein, we have developed a separable micropillar integrated DMN (SPDMN) capable of inserting DMNs across the skin with high efficiency while minimizing skin injury risk through the introduction of a safety ring feature. Unlike previously developed systems, the SPDMN does not require continuous skin attachment and can be detached immediately post-application, leaving DMNs implanted inside the skin. Altogether, the findings of this study lead to the development of a quick, safe, and efficient DMN-based drug delivery platform.
Highlights
Skin, the largest organ of the human body, is a potential target for the delivery of biopharmaceuticals [1]
The results suggest that the risk of skin injury is minimized in separable micropillar integrated dissolving microneedles (DMNs) (SPDMN) fabricated with a micropillar diameter of 500 μm in comparison to micropillars with a smaller diameter and those without a safety ring or curved edge
To ensure that only DMNs and not micropillars were inserted into the skin, the base diameter of the DMNs was fabricated at 300 ± 21 μm, which was approximately 200 μm smaller than the base diameter of the 500 μm micropillars
Summary
The largest organ of the human body, is a potential target for the delivery of biopharmaceuticals [1]. Due to the barrier properties of the stratum corneum of the skin, the transdermal delivery of biopharmaceuticals is limited to low molecular weight lipophilic compounds [2,3]. The oral administration of biopharmaceuticals is patient-friendly, there is a risk of drug activity reduction due to the first pass metabolism effect of the gastrointestinal tract and gastric acids [4,5]. To address the above-mentioned limitations, various transdermal delivery systems have been developed to improve the low transdermal permeation properties of the delivery systems [7] Among these systems, dissolving microneedles (DMNs) have been introduced as patient-friendly systems that enable the successful delivery of the encapsulated biopharmaceuticals, regardless of their molecular weight, across the skin barrier [8,9]. DMNs are micro-dimensioned needles composed of a biodegradable polymeric matrix backbone and are capable of piercing the stratum corneum and undergoing dissolution in a minimally invasive manner [10,11]
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