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Nanoemulsion-based transdermal delivery of third-generation steroidal and non-steroidal aromatase inhibitors in
Lanyang Gao1,2, Lin Gao1, Shiyao Huang1
1Metabolic Hepatobiliary and Pancreatic Diseases Key Laboratory of Luzhou City, Academician (Expert) Workstation of Sichuan Province, Department of General Surgery (Hepatopancreatobiliary Surgery), Fundamental and Clinical Research on Mental Disorders Key Laboratory of Luzhou, The Affiliated Hospital Southwest Medical University, Luzhou, China.
Abstract:
Aromatase inhibitors are effective in treating hormone receptor-positive breast cancer, particularly in postmenopausal women. However, the challenges of inconsistent dissolution, variable absorption and side effects with oral administration persist. To address these issues, transdermal delivery has emerged as a viable alternative. In our study, we have developed nanoemulsion-based transdermal creams containing third-generation aromatase inhibitors Exemestane (EXE) or Letrozole (LE) and evaluated their toxicity, anti-tumour effects and androgenic potency using preclinical models including Bama minipigs, DMBA-induced breast cancer rats and orchidectomized male rats. The results of our study are significant, suggesting that both creams effectively penetrated the skin, demonstrating an impressive anti-breast cancer effect. Importantly, EXE cream had no organ toxicity at the tested dose, providing a reassuring safety profile for its use. In contrast, LE cream displayed reversible toxicity from drug molecule itself in animals at the given dose, dissipating after 3 weeks of withdrawal and recovery. This study establishes a solid foundation for the safe clinical use of third-generation aromatase inhibitors. It highlights transdermal creams as a promising drug delivery carrier for administering them.
Insights
Transdermal creams with aromatase inhibitors show promise for breast cancer treatment. Exemestane cream demonstrated efficacy and safety, while Letrozole cream showed reversible toxicity in preclinical models.
Area of Science:
- Pharmacology
- Oncology
- Drug Delivery Systems
Background:
- Aromatase inhibitors are crucial for hormone receptor-positive breast cancer, but oral formulations face challenges like poor absorption and side effects.
- Transdermal delivery offers a potential solution to overcome oral administration limitations.
Purpose of the Study:
- To develop and evaluate nanoemulsion-based transdermal creams containing third-generation aromatase inhibitors Exemestane (EXE) and Letrozole (LE).
- To assess the toxicity, anti-tumour efficacy, and androgenic potency of these transdermal formulations in preclinical models.
Main Methods:
- Development of nanoemulsion-based transdermal creams with Exemestane and Letrozole.
- Evaluation of skin penetration, anti-tumour effects, and toxicity in Bama minipigs, DMBA-induced breast cancer rats, and orchidectomized male rats.
Main Results:
- Both Exemestane and Letrozole transdermal creams demonstrated effective skin penetration and significant anti-breast cancer effects.
- Exemestane cream exhibited no organ toxicity at the tested dose, indicating a favorable safety profile.
- Letrozole cream showed reversible toxicity, which resolved after drug withdrawal.
Conclusions:
- Transdermal creams are a promising drug delivery system for third-generation aromatase inhibitors.
- Exemestane transdermal cream presents a safe and effective option for breast cancer treatment, warranting further clinical investigation.
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