State of the Art in Constructing Gas-Propelled Dissolving Microneedles for Significantly Enhanced Drug-Loading and Delivery Efficiency

Dissolving microneedles (MNs) have emerged as a promising transdermal delivery system, as they integrate the advantages of both injection and transdermal preparations. However, the low drug-loading and limited transdermal delivery efficiency of MNs severely hinder their clinical applications. Microp...

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Bibliographic Details
Main Authors: Minmin Zhang, Beibei Yang, Xuanyu Luan, Ling Jiang, Chao Lu, Chuanbin Wu, Xin Pan, Tingting Peng
Format: Article
Language:English
Published: MDPI AG 2023-03-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/15/4/1059
Description
Summary:Dissolving microneedles (MNs) have emerged as a promising transdermal delivery system, as they integrate the advantages of both injection and transdermal preparations. However, the low drug-loading and limited transdermal delivery efficiency of MNs severely hinder their clinical applications. Microparticle-embedded gas-propelled MNs were developed to simultaneously improve drug-loading and transdermal delivery efficiency. The effects of mold production technologies, micromolding technologies, and formulation parameters on the quality of gas-propelled MNs were systematically studied. Three-dimensional printing technology was found to prepare male mold with the highest accuracy, while female mold made from the silica gel with smaller Shore hardness could obtain a higher demolding needle percentage (<i>DNP</i>). Vacuum micromolding with optimized pressure was superior to centrifugation micromolding in preparing gas-propelled MNs with significantly improved <i>DNP</i> and morphology. Moreover, the gas-propelled MNs could achieve the highest <i>DNP</i> and intact needles by selecting polyvinylpyrrolidone K30 (PVP K30), polyvinyl alcohol (PVA), and potassium carbonate (K<sub>2</sub>CO<sub>3</sub>): citric acid (CA) = 0.15:0.15 (<i>w</i>/<i>w</i>) as the needle skeleton material, drug particle carrier, and pneumatic initiators, respectively. Moreover, the gas-propelled MNs showed a 1.35-fold drug loading of the free drug-loaded MNs and 1.19-fold cumulative transdermal permeability of the passive MNs. Therefore, this study provides detailed guidance for preparing MNs with high productivity, drug loading, and delivery efficiency.
ISSN:1999-4923