Abstract
To date, only approximately 20 drugs synthesized with small molecules have been approved by the FDA for use in traditional transdermal patches (TTP) owing to the extremely low permeation rate of the skin barrier for macromolecular drugs. A novel touch-actuated microneedle array patch (TMAP) was developed for transdermal delivery of liquid macromolecular drugs. TMAP is a combination of a typical TTP and a solid microneedle array (MA). High doses of liquid drug formulations, especially heat-sensitive compounds can be easily filled and stored in the drug reservoir of TMAPs. TMAP can easily penetrate the skin and automatically retract from it to create microchannels through the stratum corneum (SC) layer using touch-actuated ‘press and release’ actions for passive permeation of liquid drugs. Comparison of subcutaneous injection, TTP, solid MA, and dissolvable MA, indicated that insulin-loaded TMAP exhibited the best hypoglycemic effect on type 1 diabetic rats. A ‘closed-loop’ permeation control was also provided for on-demand insulin delivery based on feedback of blood glucose levels (BGLs). Twenty IU-insulin-loaded TMAP maintained the type 1 diabetic rats in a normoglycemic state for approximately 11.63 h, the longest therapeutic duration among all previously reported results on microneedle-based transdermal patches. TMAP possesses excellent transdermal drug delivery capabilities.
Highlights
The transdermal drug delivery system (TDDS) describes the system that releases a drug from a specially designed device that diffuses through various layers of skin and into the systemic circulation to exert its therapeutic effects (Prausnitz and Langer, 2008; Han and Das, 2015; Ma and Wu, 2017)
We present a novel MA transdermal patch named touch-actuated microneedle array patch (TMAP) for ondemand dosage delivery of liquid macromolecular drugs
This study developed a novel microneedle-based transdermal patch referred to as TMAP for long-term delivery of liquid macromolecular drugs
Summary
The transdermal drug delivery system (TDDS) describes the system that releases a drug from a specially designed device that diffuses through various layers of skin and into the systemic circulation to exert its therapeutic effects (Prausnitz and Langer, 2008; Han and Das, 2015; Ma and Wu, 2017). Approximately five basic types of MA have been developed for transdermal drug delivery, named porous MA, solid MA, coated MA, dissolvable/degradable MA (DMA), and hollow MA (van der Maaden et al, 2012; Tuan-Mahmood et al, 2013; van der Maaden et al, 2015; Larran~eta et al, 2016). These MAs have key features, yet they have some limitations, which prevent their market spreading. The development of an MA transdermal patch with increased mechanical strength, that is self-administered, has low cost, and is capable of delivering large doses of liquid macromolecular drugs, is still a challenge.
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