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Expanding Transdermal Delivery with Lipid Nanoparticles: A New Drug-in-NLC-in-Adhesive Design
M Mendes1,2, S C C Nunes3, J J Sousa1,2
1Faculty of Pharmacy, University of Coimbra , Coimbra, Portugal.
Molecular Pharmaceutics
|May 6, 2017
Summary
This study developed a novel transdermal patch for co-delivering olanzapine and simvastatin using nanostructured lipid carriers (NLC) and propylene glycol enhancer. The optimized patch demonstrated enhanced drug permeation and reduced cytotoxicity, paving the way for future in vivo studies.
Area of Science:
- Pharmaceutics
- Drug Delivery
- Materials Science
Background:
- Transdermal drug delivery systems offer advantages for systemic drug administration.
- Co-delivery of multiple drugs presents challenges in achieving optimal release and permeation profiles.
- Nanostructured lipid carriers (NLC) show potential for enhancing drug solubility and skin penetration.
Purpose of the Study:
- To develop and optimize a monolithic transdermal patch for the co-delivery of olanzapine (OL) and simvastatin (SV).
- To investigate the role of NLC, chemical enhancers, and skin pretreatment on drug permeation and patch properties.
- To evaluate the cytotoxicity of the developed transdermal system.
Main Methods:
- Quality by Design (QbD) approach for formulation optimization.
- Incorporation of NLC for drug encapsulation and enhanced permeation.
- Evaluation of propylene glycol as a chemical enhancer.
- Assessment of Dermaroller pretreatment as an active permeation strategy.
- In vitro skin permeation studies and molecular dynamics simulations.
- Adhesion property testing and cytotoxicity assays.
Main Results:
- Propylene glycol significantly enhanced the permeation of both OL and SV, with enhancement ratios of 8.1 and 12.9, respectively.
- The type of adhesive and the presence of an enhancer played crucial roles in skin permeation.
- Dermaroller pretreatment did not yield significant improvements in drug permeation.
- NLC demonstrated a capacity to reduce the cytotoxicity of the drugs, particularly simvastatin.
- Molecular dynamics simulations provided mechanistic insights into the observed permeation enhancement.
Conclusions:
- The combination of NLC and a chemical enhancer (propylene glycol) is the primary driver for enhanced transdermal permeation in this system.
- The developed transdermal patch offers a promising platform for the co-delivery of olanzapine and simvastatin.
- The NLC formulation contributes to reduced drug-induced cytotoxicity.
- Further in vivo studies are warranted to validate the potential of this transdermal patch.
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