Novel formulations for topical delivery of tranexamic acid: assessing the need of epidermal targeting for hyperpigmentation disorders

ABSTRACT

Introduction

Tranexamic acid is used for the treatment of hyperpigmentation, and the topical route is the most favorable route for its administration. Tranexamic acid lowers plasmin and tyrosinase, which reduces melanin and skin hyperpigmentation. Low penetration through the outer layer of skin and low availability at target melanocyte cells limit tranexamic acid topical administration. Different novel delivery systems like liposomes, microneedles, topical beads, and microparticles can help in overcoming these limitations.

Areas covered

The mechanism of action of tranexamic acid and novel delivery systems for its topical delivery have been discussed. Further, patents related to the topical delivery of tranexamic acid and clinical trials undertaken to analyze their potential have been discussed.

Expert opinion

Targeting tranexamic acid in the epidermal layer makes more amount of drug available for action on melanocytes, the target site for tranexamic acid. Novel drug delivery formulations like liposomes, solid lipid nanoparticles, nano-lipidic carriers, and topical beads have the potential of achieving epidermal targeting. Epidermal targeting of tranexamic acid can help in the superior delivery of the drug, making its topical treatment more efficient.

KEYWORDS:

• Epidermal targeting
• hyperpigmentation disorders
• melasma
• nano drug delivery systems
• topical drug delivery
• tranexamic acid

Article highlights

• Topical delivery of tranexamic acid is limited by less availability at the target site.

• Novel drug delivery systems can significantly improve the delivery of tranexamic acid via topical route.

• Entrapment of tranexamic acid in lipid-based carrier systems is a challenge.

• Clinical trials have shown the advantages of novel delivery systems in delivering tranexamic acid in comparison to conventional systems.

• Increasing permeation through stratum corneum and reducing diffusion to systemic circulation can enhance the efficacy.

• Epidermal targeting technique can improve therapy of hyperpigmentation by tranexamic acid.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.