Microneedles containing cross-linked hyaluronic acid particulates for control of degradation and swelling behaviour after administration into skin

Abstract

Microneedles (MN) containing cross-linked hyaluronic acid (X-linked HA) particulates were prepared to control the degradation and swelling behaviour after transdermal drug delivery. The X-linked HA particulates were prepared by cross-linking HA chains and then passing the particulates through a sieve. Then, microneedles were prepared by micromolding method. The rheological properties of X-linked HA were studied. The penetration success rate, mechanical failure and dissolution rate of microneedles containing only hyaluronic acid (HA MN) and microneedles containing X-linked HA were compared. The delivery of fluorescein into the skin with X-linked HA MN was also observed using a confocal microscope. The size of the pulverised particulates in water ranged between 29 and 82 μm in diameter. The HA MN and X-linked HA MN were 270 μm in length. X-linked HA MN with fluorescein was inserted to a depth of 90% of the microneedle length successfully. There was no decrease in the penetration success rate for MN with up to 20% content of X-linked HA particulates. X-linked HA MN with up to 20% of particulate content did not change the dissolution time. Delay in degradation of HA, sustained drug release, and swelling behaviour of the skin layer can be obtained by X-linked HA MN.

A systematic review of carbohydrate-based microneedles: current status and future prospects

“…Cross-linking of HA may cause swelling and tailor the degradation or drug delivery [ 59 , 71 ]. Zhang et al [ 59 ] designed cross-linked HA MNs with 1,4-butanediol diglycidyl ether, enhancing the mechanical strength of MNs and lowering degradation of the matrix, thus, an excellent prospect for prolonged drug delivery.…”

“…Cross-linking of HA may cause swelling and tailor the degradation or drug delivery [59,71]. Zhang et al [59] In vivo studies revealed that the release of the drug was achieved within 5 mins after insertion, and microarrays were completely dissolved within 15 mins in the skin [79].…”

The most promising microneedle device: present and future of hyaluronic acid microneedle patch

“…compared the penetration success, mechanical strength, and dissolution rate of pure HA MNP and x-HA MNP. The latter was found to degrade more slowly than the former, but completely within 200 hours (Choi et al., 2018b ). And the addition of cross-linking agent resulted in a strong elastic behavior of the skin after drug administration.…”

Transdermal patches fabricated from hyaluronic acid for the enhanced skin penetration of therapeutic entities

“…Choi et al fabricated microneedles comprising cross-linked HA by micromolding strategy 30 . HA was cross-linked using 1,4butanediol diglycidylether.…”