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To determine the main components of Astragalus membranaceus (Fisch.) Bge (A. membranaceus, Huang Qi), Astragaloside Ⅳ (AⅣ) and Astragalus polysaccharides (AP), to characterize their properties, evaluate their in vivo efficacy, and to analyze drug diffusion using dissolving microneedle (DMN) technology in vivo.
Respectively, AⅣ- and AP-loaded DMNs comprising chitosan (CTS) and polyvinyl alcohol (PVA) were prepared via dual-mold forming. Their morphology, mechanical properties, in vivo solubility, and skin irritation characteristics were tested. In vivo efficacy was assessed in cyclophosphamide-induced immunosuppressed mice, in vivo diffusion of AⅣ and AP by DMNs and conventional methods was compared, and the rheological properties of AⅣ-CTS-PVA and AP-CTS-PVA mixtures were measured.
Subcutaneous dissolution and absorption of AⅣ-CTS-PVA and AP-CTS-PVA microneedles (MNs) at low doses (50%–17% of intraperitoneal AⅣ injection and 12%–4% of intravenous AP injection) reduced the spleen index and acid phosphatase activity in immunosuppressed mouse models, increased the thymus index, and achieved equivalent or better systemic therapeutic effects. Compared with injections, AⅣ and AP achieved controllable solid-liquid conversion through delivery with CTS-PVA MNs, resulting in highly localized aggregation within 48 h, reducing the initial explosive effect of the drug, and achieving stable and slow drug release.
The present study enhances our understanding of the efficacy and remote effects of drug-loaded DMNs from a traditional Chinese medicine (TCM) perspective, thereby promoting the development of precise and efficient delivery of TCM and further expanding the drug-loading range and application scenarios for DMNs.
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This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
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