Innovative Long-Acting Bisoprolol Patch: Synergistic Ion-Pair Skin Adsorption for Drug Delivery Control Coupled with Dynamic Modulation of Penetration Enhancers DOI
Yu Pang,

Wenxuan Jia,

Liuyang Wang

et al.

Molecular Pharmaceutics, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 29, 2024

This study aims to develop a sustained release patch for bisoprolol (BSP) address the issue of blood pressure fluctuations caused by traditional dosing methods, ensuring continuous drug and efficient utilization. Long-chain saturated fatty acids (C6–C12) were chosen as counterions precisely control BSP's permeation rate in formulation, ion-pairing strategy's mechanism delivery was thoroughly investigated. Molecular docking results revealed significant differences adsorption capacities different ion pairs stratum corneum (SC) epidermis, directly influencing their residence times thereby regulating passive diffusion rate. Particularly, BSP-C10 pair successfully reduced one-third its baseline. To enhance efficiency reduce costs, chemical enhancers (CPEs) are typically added patches. In contrast static analyses based on cumulative permeation, this utilized ATR-FTIR dynamic detection isopropyl myristate (IPM) preferred enhancer, studying disruptive effects skin barrier during delivery. The observed that delivery, interaction between IPM lipids follows U-shaped trend: initially increasing, then decreasing, with peak occurring at 10 h. Similarly, displays comparable pattern. addition CPE increased utilization from 39.8 ± 4.31 79.8 7.27%. strategy rapidly initial phase subsequent weakening disruption, allowing dominate maintain stable long-term therapeutic effects. Pharmacokinetic studies demonstrated newly developed BSP maintains concentrations, reduces burst effects, increases bioavailability 84.679%, doubles MRT0–t, halves Cmax, significantly occurrence fluctuations.

Language: Английский

Transdermal patch based on pressure-sensitive adhesive: the importance of adhesion for efficient drug delivery DOI
Liuyang Wang,

Junyao Ma,

Jiaxin Li

et al.

Expert Opinion on Drug Delivery, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 29, 2025

Transdermal patches offer a unique advantage by providing extended therapeutic benefits while maintaining stable plasma drug concentration. The efficacy and safety of depend significantly on their ability to adhere the skin, feature influenced various external internal factors. review primarily focuses fundamental aspects adhesion in transdermal patches, including basic information about underlying principles adhesion, delivery, characteristics pressure sensitive adhesives (PSAs), issues, impact factors, strategies improve patch relevant molecular mechanisms. development with sufficient for consistent delivery remains challenging task. Challenges stem from complex interplay among PSAs, permeation enhancers, active pharmaceutical ingredients (APIs), other excipients current compositions, further complicated variations arising dermatological These intricacies impede effectiveness patches. Progress exploration new PSA polymers, conjunction innovative is crucial establishing an optimal equilibrium between utilization rate, drug-loading, release, thus effectively addressing challenges related adhesion.

Language: Английский

Citations

0
Combining ion-pair strategy and chemical enhancers to develop mirtazapine long-acting transdermal patches for depression treatment DOI
Shuhan Liu, Hui Li, Yang Zhang

et al.

Journal of Drug Delivery Science and Technology, Journal Year: 2024, Volume and Issue: unknown, P. 106435 - 106435

Published: Nov. 1, 2024

Language: Английский

Citations

2
Innovative Long-Acting Bisoprolol Patch: Synergistic Ion-Pair Skin Adsorption for Drug Delivery Control Coupled with Dynamic Modulation of Penetration Enhancers DOI
Yu Pang,

Wenxuan Jia,

Liuyang Wang

et al.

Molecular Pharmaceutics, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 29, 2024

This study aims to develop a sustained release patch for bisoprolol (BSP) address the issue of blood pressure fluctuations caused by traditional dosing methods, ensuring continuous drug and efficient utilization. Long-chain saturated fatty acids (C6–C12) were chosen as counterions precisely control BSP's permeation rate in formulation, ion-pairing strategy's mechanism delivery was thoroughly investigated. Molecular docking results revealed significant differences adsorption capacities different ion pairs stratum corneum (SC) epidermis, directly influencing their residence times thereby regulating passive diffusion rate. Particularly, BSP-C10 pair successfully reduced one-third its baseline. To enhance efficiency reduce costs, chemical enhancers (CPEs) are typically added patches. In contrast static analyses based on cumulative permeation, this utilized ATR-FTIR dynamic detection isopropyl myristate (IPM) preferred enhancer, studying disruptive effects skin barrier during delivery. The observed that delivery, interaction between IPM lipids follows U-shaped trend: initially increasing, then decreasing, with peak occurring at 10 h. Similarly, displays comparable pattern. addition CPE increased utilization from 39.8 ± 4.31 79.8 7.27%. strategy rapidly initial phase subsequent weakening disruption, allowing dominate maintain stable long-term therapeutic effects. Pharmacokinetic studies demonstrated newly developed BSP maintains concentrations, reduces burst effects, increases bioavailability 84.679%, doubles MRT0–t, halves Cmax, significantly occurrence fluctuations.

Language: Английский

Citations

0