Development and Evaluation of Novel Water-Based Drug-in-Adhesive Patches for the Transdermal Delivery of Ketoprofen.

Kwanputtha Arunprasert,Chaiyakarn Pornpitchanarong,Porawan Aumklad,Tanasait Ngawhirunpat,Prasopchai Patrojanasophon,Theerasak Rojanarata,Praneet Opanasopit

doi:10.3390/pharmaceutics13060789

Kwanputtha Arunprasert, Chaiyakarn Pornpitchanarong + Show 5 more

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https://doi.org/10.3390/pharmaceutics13060789

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Journal: Pharmaceutics	Publication Date: May 25, 2021
Citations: 9	License type: CC BY 4.0

Affiliation: Silpakorn University

Abstract

The objective of this study was to develop novel water-based drug-in-adhesive pressure-sensitive adhesives (PSAs) patches for the transdermal delivery of ketoprofen, employing poly(N-vinylpyrrolidone-co-acrylic acid) copolymer (PVPAA) and poly(methyl vinyl ether-alt-maleic anhydride) (PMVEMA) as the main components. The polymers were crosslinked with tartaric acid and dihydroxyaluminium aminoacetate using various polymer ratios. Ketoprofen was incorporated into the PVPAA/PMVEMA PSAs during the patch preparation. The physicochemical properties, adhesive properties, drug content, release profile, and skin permeation of the patches were examined. Moreover, the in vivo skin irritation and skin adhesion performance in human volunteers were evaluated. The patches prepared at a weight ratio of PVPAA/PMVEMA of 1:1 presented the highest tacking strength, with desirable peeling characteristics. The ketoprofen-loaded PVPAA/PMVEMA patches exhibited superior adhesive properties, compared to the commercial patches, because the former showed an appropriate crosslinking and hydrating status with the aid of a metal coordination complex. Besides, the permeated flux of ketoprofen through the porcine skin of the ketoprofen-loaded PVPAA/PMVEMA patches (4.77 ± 1.00 µg/cm2/h) was comparable to that of the commercial patch (4.33 ± 0.80 µg/cm2/h). In human studies, the PVPAA/PMVEMA patches exhibited a better skin adhesion performance, compared with the commercial patches, without skin irritation. In addition, the patches were stable for 6 months. Therefore, these novel water-based PSAs may be a potential adhesive for preparing drug-in-adhesive patches.

Highlights

Introduction published maps and institutional affilCurrently, transdermal drug delivery systems (TDDS) are an attractive alternative drug delivery pathway for oral administration and hypodermic injection, as they are painless, convenient, and may increase the bioavailability of the drugs [1]
poly(Nvinylpyrrolidone-co-acrylic acid) copolymer (PVPAA) copolymer was synthesized by a polymerization reaction between NVP and acrylic acid (AA) at a monomer molar ratio of 1:3
The results indicated that there was no significant difference in the physical appearance, tacking strength, peeling strength, and drug content of the ketoprofen-loaded PVPAA/poly(methyl vinyl ether-alt-maleic anhydride) (PMVEMA) patches determined at the beginning and at 3 and 6 months of the accelerated and long-term stability studies

Summary

Introduction

Transdermal drug delivery systems (TDDS) are an attractive alternative drug delivery pathway for oral administration and hypodermic injection, as they are painless, convenient, and may increase the bioavailability of the drugs [1]. TDDS may provide the controlled delivery of a drug through the stratum corneum for local or systemic approaches [2]. Drug-in-adhesive patches take advantage of close contact by the attachment of the patches and the stratum corneum, the barrier to drug transportation through the skin, to deliver the drugs into the skin or the blood circulation [4]. Pressure-sensitive adhesives (PSAs) are one of the most significant components in a transdermal system.

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