Hydrogel-forming microarray patch mediated transdermal delivery of tetracycline hydrochloride

Antibiotic resistance is one of the most serious health problems today and is expected to worsen in the coming decades. It has been suggested that antibiotic administration routes that bypass the human gut could potentially tackle this problem. In this work, an antibiotic hydrogel-forming microarray patch (HF-MAP) system, which can be used as an alternative antibiotic delivery technology, has been fabricated. Specifically, poly(vinyl alcohol)/poly(vinylpyrrolidone) (PVA/PVP) microarray showed excellent swelling properties with >600% swelling in PBS over 24 h. The tips on the HF-MAP were proven to be able to penetrate a skin model which is thicker than stratum corneum. The antibiotic (tetracycline hydrochloride) drug reservoir was mechanically robust and dissolved completely in an aqueous medium within a few minutes.

In vivo animal studies using a Sprague Dawley rat model showed antibiotic administration using HF-MAP achieved a sustained release profile, in comparison with animals receiving oral gavage and intravenous (IV) injection, with a transdermal bioavailability of 19.1% and an oral bioavailability of 33.5%. The maximum drug plasma concentration for HF-MAP group reached 7.40 ± 4.74 μg/mL at 24 h, whereas the drug plasma concentration for both oral (5.86 ± 1.48 μg/mL) and IV (8.86 ± 4.19 μg/mL) groups peaked soon after drug administration and had decreased to below the limit of detection at 24 h. The results demonstrated that antibiotics can be delivered by HF-MAP in a sustained manner.

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Materials

Acetonitrile, citric acid, triethylamine, phosphate-buffered saline (PBS), potassium phosphate monobasic, and poly(vinyl alcohol) (PVA) (Mw = 85–124 kDa) 87–89% hydrolyzed were all purchased from Sigma-Aldrich, Steinheim, Germany. Croscarmellose sodium (CCS), marketed as ac-di-sol was acquired from FMC Health and Nutrition Ltd. (Philadelphia, USA). Poly(vinylpyrrolidone) (PVP) K29–32 (Mw = 58 kDa) was kindly provided by Ashland, Kidderminster, UK. Tetracycline hydrochloride (TC HCL) was kindly donated by Suzhou Zhuoqun Pharmaceutical Technology Ltd., Suzhou, Jiangsu Province, China. PEARLITOL® in the form of Pearlitol 50C, and phosphoric acid were purchased from Roquette (Lestrem, France) and Fluorochem Ltd. (Hadfield, UK), respectively. Stillborn piglets were sourced from local farms in Northern Ireland and were stored in freezer at −20 °C before further use. Parafilm® was purchased from Bemis Company, Inc.

Li Zhao, Lalitkumar K. Vora, Stephen A. Kelly, Linlin Li, Eneko Larrañeta, Helen O. McCarthy, Ryan F. Donnelly, Hydrogel-forming microarray patch mediated transdermal delivery of tetracycline hydrochloride, Journal of Controlled Release, Volume 356, 2023, Pages 196-204, ISSN 0168-3659, https://doi.org/10.1016/j.jconrel.2023.02.031.