Abstract

AbstractPoorly soluble drugs constitute more than 60% of currently marketed pharmaceuticals with over two‐thirds of promising new chemical entities failing to enter a clinical setting due to solubility issues. Although oral formulations have made some impact, alternative enhancement strategies for administration of such molecules are actively sought. Over the last decade, innovation on a global scale has enabled the expansion of the frontiers of microarray patches (MAPs) further than ever before. Initially designed to load low doses of hydrophilic and potent therapeutic agents, MAPs are now becoming a viable strategy for the immediate and long‐acting delivery of poorly soluble drugs through the skin. This together with the advantages of transdermal administration over the oral and parenteral routes, make of MAPs an appealing platform for the development of products with increased patient compliance. Undoubtedly, MAPs will soon become a readily available therapeutic alternative, and experts from academia, industry and regulatory bodies are working together aiming to facilitate the progression of MAPs toward safe and effective clinical use. This review aims to highlight the ability of MAPs to deliver poorly soluble actives, discuss the mechanisms behind in‐skin drug absorption, and evaluate the future direction of the field.

Highlights

  • Soluble drugs constitute more than 60% of currently marketed entities being poorly soluble in water and pharmaceuticals with over two-thirds of promising new chemical entities

  • Alternative work reported by Lin et al, encompassed the use of dissolving microarray patches (MAPs) composed of hyaluronic acid (HA) and HP-β-CD to deliver the hydrophobic drug triamcinolone acetonide in an animal model.[108]

  • The work discussed here serves to reveal the benefits of the addition of CDs to the formulation of MAPs that are intended to be used for the intradermal delivery of hydrophobic drugs

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Summary

Intradermal Administration of Hydrophobic Drugs

An increasingly wide range of studies has explored the challenging field of delivering poorly soluble drugs intradermally via MAPs. Some researchers chose model drugs such as Nile Red (NR) for formulation purposes only; without specifying explicit therapeutic targets. While most studies have explored the intradermal delivery of hydrophobic drugs using dissolving MAPs as aforementioned, the possibility of using other types of MAPs such as coated or hydrogel-forming MAPs was investigated. Some studies investigated the intradermal delivery of the coarse drug only without processing prior to delivery. All these strategies share the same aim of increasing the in-skin absorption of poorly soluble drugs.

Nanoparticle-Based Microarray Patches
Lipid-Based Nanoparticles
Polymeric Nanoparticles
Microparticle-Based Formulations
Solid Dispersions
Drug Solutions for Microneedle Coating
MAPs Loaded with Coarse Drug Particles
Delivery of Drugs Using Cosolvency
Cyclodextrin Inclusion Complexes
In-Skin Dissolution and Absorption of Drug Micro- and Nanocrystals
Targeting the Lymphatic System with Nanoparticle-Based MAPs
Conclusion and Future Outlook
Findings
Conflict of Interest
Full Text
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