Abstract
The development of dissolving microneedles (DMN) is one of the advanced technologies in transdermal drug delivery systems, which precisely deliver the drugs through a rapid dissolution of polymers after insertion into the skin. In this study, we fabricated nanoemulsion-loaded dissolving microneedle (DMN) arrays for intradermal and transdermal drug delivery. For this task, model drug (amphotericin B, AmB)-loaded nanoemulsion (NE) were prepared by the probe-sonication method. AmB-loaded-NE was prepared using Capmul MCM C-8 EP/NF, Tween® 80, poly(vinyl alcohol) (PVA-10 kDa), and poly (vinyl pyrrolidone) (PVP-360 kDa or K29/32) by using SpeedMixer™, followed by probe-sonication and evaluated for particle size and polydispersity index (PDI). Transmission electron microscopy (TEM) was also used to assess the particle size before and after DMN casting. AmB-NE embedded DMN arrays were found to be strong enough, revealed efficient skin insertion, and penetrated down to the fourth layer (depth ≈ 508 μm) of Parafilm M® (validated skin model). Ex vivo skin deposition experiments in full-thickness neonatal porcine demonstrated that after 24 h, AmB-NE-DMN arrays were able to deposit 111.05 ± 48.4 µg/patch AmB into the skin. At the same time, transdermal porcine skin permeation studies showed significantly higher permeability of AmB (29.60 ± 8.23 μg/patch) from AmB-NE-DMN compared to MN-free AmB-NE patches (5.0 ± 6.15 μg/patch) over 24 h. Antifungal studies of optimized AmB-NE-DMN, AmB-loaded discs and drug-free DMN against Candida albicans, confirmed the synergistic activity of Campul-MCM C-8, used in the nanoemulsion formulation. This study establishes that nanoemulsion based dissolving microneedle may serve as an efficient system for intradermal as well as transdermal drug delivery.Graphical abstract
Highlights
Transdermal drug delivery is beneficial for the administration of therapeutic molecules, as it bypasses the first-pass metabolism associated with oral administration [1], depending upon the size of molecules [2]
dissolving microneedles (DMN) patches were designed with drug-lipidic nanosystem-loaded arrays in order to deliver the drug transdermally as well as intradermally
DMN serves as drug reservoirs and is self-implanted subcutaneously to release antifungal drugs locally and sustainably without producing systemic side effects
Summary
Transdermal drug delivery is beneficial for the administration of therapeutic molecules, as it bypasses the first-pass metabolism associated with oral administration [1], depending upon the size of molecules [2]. DMN formulation from lipophilic drugs causes a drug loading and content uniformity problem, which may be overcome by using organic solvents to improve the solubilization. Lipophilic drugs are more potential candidates for developing topical formulations because of their significant benefits, such as high permeability across the cellular lipid membrane, enhanced absorption, and metabolism, and greater therapeutic achievement over hydrophilic drugs [12–14]. Another fascinating system explained formerly in the literature was nanoemulsion (NE). Various oils have been used in NE, like, isopropyl myristate, castor oil, triacetin, soybean oil, sesame oil, coconut oil, Capmul PG8, triacylglycerides, vitamin E, and clove oil [17, 18]
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