# Discovery of epidermal/dermal targeting formulations for cutaneous squamous cell carcinoma

> **NIH NIH R43** · VIA THERAPEUTICS, LLC · 2021 · $251,917

## Abstract

The incidence and mortality rates of cutaneous squamous cell carcinoma (cSCC) and skin cancer
continues to increase. It is expected that 1 in 5 Americans will develop skin cancer in their lifetime.
Although surgical excision is typically indicated and effective, surgery is not always appropriate or
possible. Efforts to treat and/or prevent using pharmacological agents are limited by poor delivery to
the site of action (the skin epidermis and dermis) and majority of the pharmacological therapy involves
systemic administration with few topical agents available. Existing drugs and combinations of natural
compounds with potential to be used against skin cancer, including cSCC, have <1% bioavailability
when administered orally, which means that they are ineffective in reaching the site of action and thus
produce an inadequate pharmacological response, while when administered intravenously can lead to
aggressive adverse side-effects. Although the skin is an accessible organ, topical treatment of skin
cancers and precancerous lesions has been limited by either insufficient drug permeation through the
stratum corneum or too much drug permeation into the systemic circulation and off-targeting. We seek
to overcome these opposing barriers to drug delivery utilizing a high-throughput screening method we
have developed including formulation libraries which allow the discovery of viable epidermal/dermal
targeted drug delivery systems. Skin irritation potential utilizing reconstructed human skin and efficacy
testing based on UV-induced photocarcinogenesis in SKH-1 mice will also be performed. The overall
goal of this proposal is to develop drug formulations for the prevention, treatment, and the avoidance of
progression of cSCC that would be able to deliver the drug inside the skin and be maintained in the skin
for a period of time by avoiding or minimizing systemic absorption and off-target effects while
potentiating therapeutic efficacy. Based on strong preliminary data, we hypothesize that the delivery of
drugs with reduction and prevention of tumor progression properties are able to be developed in a
topical formulation that delivers the drug inside the skin while minimizing systemic absorption and
adverse effects. This type of therapy is more convenient to the patient and can lead to better patient
compliance and therapeutic efficacy by increasing the drug's bioavailability at the site of action.

## Key facts

- **NIH application ID:** 10259286
- **Project number:** 1R43CA257783-01A1
- **Recipient organization:** VIA THERAPEUTICS, LLC
- **Principal Investigator:** John Joseph Koleng
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $251,917
- **Award type:** 1
- **Project period:** 2021-07-12 → 2024-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10259286

## Citation

> US National Institutes of Health, RePORTER application 10259286, Discovery of epidermal/dermal targeting formulations for cutaneous squamous cell carcinoma (1R43CA257783-01A1). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10259286. Licensed CC0.

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