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Nanostructured lipid carrier surface modified with Eudragit RS 100 and its potential ophthalmic functions
Wenji Zhang1, Xuedong Li2, Tiantian Ye3
1Department of Pharmaceutics, School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang, People's Republic of China ; Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
International Journal of Nanomedicine
|September 24, 2014
Summary
This study enhanced ocular drug delivery using Eudragit (EDU) RS 100-coated nanostructured lipid carriers (NLCs). The modified NLCs demonstrated improved stability, extended precorneal clearance, and enhanced corneal penetration for genistein delivery.
Area of Science:
- Nanotechnology
- Ocular Drug Delivery
- Materials Science
Background:
- Nanostructured lipid carriers (NLCs) offer potential for ocular drug delivery.
- Surface modification of NLCs is crucial for improving ocular performance and stability.
- Genistein is a compound with potential therapeutic applications that requires effective delivery systems.
Purpose of the Study:
- To evaluate the ocular performance of genistein-loaded NLCs coated with cationic Eudragit (EDU) RS 100.
- To assess the impact of EDU RS 100 coating on NLC stability, precorneal clearance, and corneal penetration.
- To confirm the safety and non-irritating nature of the modified NLCs for ocular application.
Main Methods:
- Genistein-loaded NLCs (GEN-NLC) were prepared using melt-emulsification followed by EDU RS 100 surface absorption.
- Surface characterization included zeta potential measurements and transmission electron microscopy (TEM).
- Ocular performance was evaluated using gamma scintigraphy for precorneal clearance and apparent permeability coefficients (Papp) for corneal penetration. Draize and cytotoxicity tests assessed safety.
Main Results:
- EDU RS 100 coating uniformly formed a spherical layer, increasing zeta potential from -7.46 mV to +13.60 mV.
- The coating significantly improved NLC stability by preventing particle size growth.
- EDU RS 100-GEN-NLC exhibited extended precorneal clearance, a 1.22-fold increase in AUC, and a 3.3-fold increase in Papp, indicating enhanced ocular bioavailability and corneal penetration.
- Draize and cytotoxicity tests confirmed the ocular tissues and corneal cells were non-irritant and non-toxic.
Conclusions:
- Surface modification of NLCs with cationic EDU RS 100 significantly enhances their physicochemical properties and ocular performance.
- The developed EDU RS 100-coated GEN-NLC shows promise as a safe and effective system for ocular drug delivery.
- This approach offers advantages for improving the therapeutic efficacy of drugs administered via the ocular route.
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