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Evaluation of the Structural Modification of Ibuprofen on the Penetration Release of Ibuprofen from a Drug-in-Adhesive Matrix Type Transdermal Patch.

ABSTRACT: This study aimed to evaluate the effect of chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU] from the acrylic pressure-sensitive adhesive used as a drug-in-adhesives matrix type transdermal patch. The active substances tested were ibuprofen salts obtained by pairing the ibuprofen anion with organic cations, such as amino acid isopropyl esters. The structural modification of ibuprofen tested were Ibuprofen sodium salt, [GlyOiPr][IBU], [AlaOiPr][IBU], [ValOiPr][IBU], [SerOiPr][IBU], [ThrOiPr][IBU], [(AspOiPr)₂][IBU], [LysOiPr][IBU], [LysOiPr][IBU]₂, [PheOiPr][IBU], and [ProOiPr][IBU]. For comparison, the penetration of unmodified ibuprofen and commercially available patches was also investigated. Thus, twelve transdermal patches with new drug modifications have been developed whose adhesive carrier is an acrylate copolymer. The obtained patches were characterized for their adhesive properties and tested for permeability of the active substance. Our results show that the obtained ibuprofen patches demonstrate similar permeability to commercial patches compared to those with structural modifications of ibuprofen. However, these modified patches show an increased drug permeability of 2.3 to even 6.4 times greater than unmodified ibuprofen. Increasing the permeability of the active substance and properties such as adhesion, cohesion, and tack make the obtained patches an excellent alternative to commercial patches containing ibuprofen.

SUBMITTER: Ossowicz-Rupniewska P

PROVIDER: S-EPMC9320482 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Purpose:The main objective of this present study was the investigation of potential novel transdermal patch technology (TEPI®) delivering ibuprofen as the active pharmaceutical ingredient (API) using a novel poly(ether-urethane)-silicone crosslinked pressure-sensitive adhesive (PSA) as the drug reservoir in a solvent-free manufacturing process. Methods:The patch was synthesized utilizing the hot-melt crosslinking technique without the addition of solvents at 80 °C in 100% relative humidity. Dissolution and permeation studies performed utilizing diffusion cells and subsequently HPLC validated methods were employed to determine the API content in the acceptor solution. Accelerated stability studies were also performed at 40 °C and 70% relative humidity. The adhesive performance of the fabricated patch was evaluated utilizing loop tack adhesion tests. Results:In vitro permeation experiments across both Strat-M® and human skin demonstrated that ibuprofen can easily be released from the adhesive matrix and penetrate through the studied membrane. A comparison on the permeation rates of the API across the two membranes indicated that there is not a strong correlation between the obtained data. The presence of chemical enhancers facilitated an increased flux of the API higher than observed in the basic formulation. Initial stability studies of the optimized formulation showed no degradation with respect to the drug content. Adhesion studies were also performed indicating higher values when compared with commercially available products. Conclusions:The present study demonstrated the fabrication of an ibuprofen patch utilizing a versatile, solvent-free drug delivery platform. Upon optimization of the final system, the resulting patch offers many advantages compared to commercially available formulations including high drug loading (up to 25 wt%), good adhesion, and painless removal leaving no residues on the skin. This PSA offers many advantages over existing adhesive technology. Graphical Abstract?.

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Evaluation of the Structural Modification of Ibuprofen on the Penetration Release of Ibuprofen from a Drug-in-Adhesive Matrix Type Transdermal Patch.

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