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Investigation and optimization of hydrogel microneedles for transdermal delivery of caffeine


Citation

Chandran, Rubhan and Mohd Tohit, Eusni Rahayu and Stanslas, Johnson and Salim, Norazlinaliza and Tuan Mahmood, Tuan Mazlelaa (2022) Investigation and optimization of hydrogel microneedles for transdermal delivery of caffeine. Tissue Engineering, Part C: Methods, 28 (10). pp. 545-556. ISSN 1937-3384; ESSN: 1937-3392

Abstract

Caffeine is therapeutically effective for treating apnea, cellulite formation, and pain management. It also exhibits neuroprotective and antioxidant activities in different models of Parkinson's disease and Alzheimer's disease. However, caffeine administration in a minimally invasive and sustainable manner through the transdermal route is challenging owing to its hydrophilic nature. Therefore, this study demonstrated a transdermal delivery approach for caffeine by utilizing hydrogel microneedle (MN) as a permeation enhancer. The influence of formulation parameters such as molecular weight (MW) of PMVE/MA (polymethyl vinyl ether/maleic anhydride) copolymer and sodium bicarbonate (NaHCO3) concentration on the swelling kinetics and mechanical integrity of the hydrogel MNs was investigated. In addition, the effect of different MN application methods and needle densities of hydrogel MN on the skin insertion efficiency and penetration depth was also evaluated. The swelling degree at equilibrium percentage (% Seq) recorded for hydrogels fabricated with Gantrez S-97 (MW = 1,500,000 Da) was significantly higher than formulation with Gantrez AN-139 (MW = 1,080,000 Da). Increasing the concentration of NaHCO3 also significantly increased the % Seq. Moreover, a 100% penetration was recorded for both the applicator and combination of applicator and thumb pressure compared with only 11% for thumb pressure alone. The average diameter of micropores created by the applicator method was 62.94 μm, which was significantly lower than the combination of both applicator and thumb pressure MN application (100.53 μm). Based on histological imaging, the penetration depth of hydrogel MN increased as the MN density per array decreased. The hydrogel MN with the optimized formulation and skin insertion parameters was tested for caffeine delivery in an in vitro Franz diffusion cell setup. Approximately 2.9 mg of caffeine was delivered within 24 h, and the drug release profile was best fitted to the Korsmeyer–Peppas model, displaying Super Case II kinetics. In conclusion, a combination of thumb and impact application methods and reduced needle density improved the skin penetration efficiency of hydrogel MNs. The results also show that hydrogel MNs fabricated from 3% w/w NaHCO3 and high MW of copolymer exhibit optimum physical and swelling properties for enhanced transdermal delivery.


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Additional Metadata

Item Type: Article
Divisions: Faculty of Medicine and Health Science
Faculty of Science
DOI Number: https://doi.org/10.1089/ten.tec.2022.0045
Publisher: Mary Ann Liebert
Keywords: Drug delivery system; Formulation; Hydrogel; In vitro model; Microneedle; Permeation enhancer; Polymeric drug delivery system; Skin; Transdermal
Depositing User: Ms. Zaimah Saiful Yazan
Date Deposited: 15 Mar 2024 04:23
Last Modified: 15 Mar 2024 04:23
Altmetrics: http://www.altmetric.com/details.php?domain=psasir.upm.edu.my&doi=10.1089/ten.tec.2022.0045
URI: http://psasir.upm.edu.my/id/eprint/101986
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