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Enhanced skin permeation using polyarginine modified nanostructured lipid carriers
Punit P Shah1, Pinaki R Desai, Debra Channer
1College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA.
Summary
Surface modification of nanostructured lipid carriers (NLCs) with an 11-arginine peptide (R11) significantly enhanced topical drug delivery into deeper skin layers. This improved delivery reduced inflammation in an allergic contact dermatitis model.
Area of Science:
- Nanotechnology in drug delivery
- Dermal and transdermal drug transport
- Biomaterials and surface modification
Background:
- Effective topical delivery of drugs to deeper skin layers remains a challenge.
- Nanostructured lipid carriers (NLCs) offer potential for enhanced drug encapsulation and delivery.
- Surface modification of NLCs with cell-penetrating peptides (CPPs) can improve skin permeation.
Purpose of the Study:
- To investigate the impact of polyarginine chain length on the topical delivery efficacy of surface-modified NLCs.
- To optimize the number of arginines in CPPs for enhanced drug penetration into deeper skin layers.
- To evaluate the combined delivery of Spantide II (SP) and ketoprofen (KP) for treating allergic contact dermatitis (ACD).
Main Methods:
- NLCs were prepared using a hot-melt technique and surface-modified with CPPs (polyarginines or YKA).
- In vivo confocal and Raman spectroscopy were used to assess skin permeation of fluorescent dye-loaded NLCs.
- In vitro skin permeation, drug release studies (Franz diffusion cells), and an ACD mouse model were employed.
Main Results:
- Surface modification with an 11-arginine peptide (R11) significantly enhanced NLC skin permeation compared to other polyarginines and TAT peptides.
- NLC-R11 demonstrated higher retention of SP and KP in the dermis after 24 hours compared to solution and unmodified NLCs.
- SP+KP-NLC-R11 significantly reduced ear thickness in an ACD mouse model (p<0.05) compared to controls.
Conclusions:
- Surface modification of NLCs with R11 is a promising strategy for improving the topical delivery of drugs like SP and KP.
- Enhanced transport across deeper skin layers by NLC-R11 leads to effective reduction of ACD-associated inflammation.
- Polyarginine chain length is a critical factor in optimizing CPP-mediated enhancement of NLC topical delivery.
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