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Microencapsulation of DEET in Solid Lipid Microparticles: production, characterization and safety evaluation
Paula A Santos1, Márcio R M DA Silva1, Melanie Tavares1
1Universidade Federal do Rio de Janeiro (UFRJ), Laboratório de Desenvolvimento Galênico, Faculdade de Farmácia, Avenida Carlos Chagas Filho, 373, 21941-901 Rio de Janeiro, RJ, Brazil.
Anais Da Academia Brasileira De Ciencias
|September 8, 2022
Summary
Solid Lipid Microparticles (SLM) effectively reduced skin permeation of DEET, enhancing safety and potentially prolonging insect repellent action. This formulation shows promise for insect bite prevention.
Area of Science:
- Dermatology
- Materials Science
- Pharmacology
Background:
- DEET is a highly effective insect repellent but exhibits significant skin permeation.
- High skin permeation of DEET raises safety concerns and may limit its duration of action.
Purpose of the Study:
- To encapsulate DEET within Solid Lipid Microparticles (SLM).
- To evaluate the safety and efficacy of SLM for topical application.
- To assess the impact of SLM on DEET skin permeation and retention.
Main Methods:
- DEET was encapsulated in SLM and characterized for morphology and particle size.
- An analytical method for DEET quantification using High-Performance Liquid Chromatography (HPLC) was developed and validated.
- Cytotoxicity was assessed in vitro using keratinocytes, fibroblasts, and macrophages.
- Ex vivo skin permeation and retention studies were conducted.
Main Results:
- SLM exhibited micrometric size and spherical morphology.
- The HPLC method was validated as selective, linear, precise, accurate, and robust.
- The SLM formulation demonstrated no cytotoxicity.
- SLM significantly reduced DEET skin permeation compared to free DEET in ethanol, enhancing safety.
- Increased DEET skin retention was observed with SLM, suggesting prolonged efficacy.
Conclusions:
- Solid Lipid Microparticles provide a safe topical formulation for DEET.
- SLM can mitigate DEET skin permeation, improving its safety profile.
- The enhanced skin retention of DEET by SLM may extend its insect repellent effect, offering a promising approach for insect bite prevention.
