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Published on: February 9, 2019
Phosphate decorated lipid-based nanocarriers providing a prolonged mucosal residence time
Nuri Ari Efiana1, Andrea Fürst2, Ahmad Saleh3
1Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria; Department of Pharmaceutical Technology, Faculty of Pharmacy, Universitas Ahmad Dahlan, Jl. Prof. Dr. Soepomo, S.H., Janturan, Warungboto, Umbulharjo, Yogyakarta 55164, Indonesia.
Phosphate-decorated lipid nanocarriers, including self-emulsifying drug delivery systems (SEDDS), solid lipid nanoparticles (SLN), and nanostructured lipid carriers (NLC), significantly prolonged intestinal residence time. These enhanced nanocarriers demonstrated improved mucosal adhesion and payload delivery potential.
Area of Science:
- Nanotechnology
- Drug Delivery Systems
- Biomaterials Science
Background:
- Conventional nanocarriers often have limited residence time in the gastrointestinal tract, hindering effective drug absorption.
- Surface modification of nanocarriers is a key strategy to improve their interaction with mucosal surfaces.
Purpose of the Study:
- To develop phosphate-decorated lipid-based nanocarriers (SEDDS, SLN, NLC) to enhance mucosal residence time.
- To investigate the surface charge conversion and release properties of these modified nanocarriers.
Main Methods:
- Lipid nanocarriers (SEDDS, SLN, NLC) were decorated with tetradecyltrimethylammonium bromide (TTAB) and polyoxyethylene (9) nonylphenol monophosphate ester (PNPP).
- Zeta potential, cytotoxicity, charge conversion using intestinal alkaline phosphatase (IAP), and phosphate release studies were conducted.
- Nanocarrier residence time was evaluated on porcine intestinal mucosa.
Main Results:
- Surface decoration induced significant zeta potential shifts, particularly for NLC$_{TTAB-PNPP}$ (Δ22 mV).
- Lipid-based nanocarriers showed no toxicity up to 0.3% concentration.
- Phosphate release was rapid for all decorated nanocarriers (SEDDS$_{TTAB-PNPP}$, SLN$_{TTAB-PNPP}$, NLC$_{TTAB-PNPP}$).
- SLN$_{TTAB-PNPP}$ and NLC$_{TTAB-PNPP}$ exhibited a 4-fold increase in mucosal residence time compared to blank formulations.
Conclusions:
- Phosphate modification of lipid-based nanocarriers effectively prolongs their intestinal residence time.
- These modified nanocarriers hold promise for improving drug delivery and therapeutic efficacy through enhanced mucosal interaction.
