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- Title
State of the Art in Constructing Gas-Propelled Dissolving Microneedles for Significantly Enhanced Drug-Loading and Delivery Efficiency.
- Authors
Zhang, Minmin; Yang, Beibei; Luan, Xuanyu; Jiang, Ling; Lu, Chao; Wu, Chuanbin; Pan, Xin; Peng, Tingting
- Abstract
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 (DNP). Vacuum micromolding with optimized pressure was superior to centrifugation micromolding in preparing gas-propelled MNs with significantly improved DNP and morphology. Moreover, the gas-propelled MNs could achieve the highest DNP and intact needles by selecting polyvinylpyrrolidone K30 (PVP K30), polyvinyl alcohol (PVA), and potassium carbonate (K2CO3): citric acid (CA) = 0.15:0.15 (w/w) 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.
- Subjects
SILICA gel; THREE-dimensional printing; POLYVINYL alcohol; POTASSIUM carbonate; MOLDS (Casts &; casting); DRUG carriers
- Publication
Pharmaceutics, 2023, Vol 15, Issue 4, p1059
- ISSN
1999-4923
- Publication type
Article
- DOI
10.3390/pharmaceutics15041059