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SHR Neuro Cancer Cardio Lipid Metab Microb
Gradauer, K; Vonach, C; Leitinger, G; Kolb, D; Fröhlich, E; Roblegg, E; Bernkop-Schnürch, A; Prassl, R.
Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties.
Int J Nanomedicine. 2012; 7(8):2523-2534
Doi: 10.2147/IJN.S29980
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- Leading authors Med Uni Graz
- Gradauer Kerstin
- Prassl Ruth
- Co-authors Med Uni Graz
- Fröhlich Eleonore
- Kolb Dagmar
- Leitinger Gerd
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- Abstract:
- Aim: To develop mucoadhesive liposomes by anchoring the polymer chitosan-thioglycolic acid (chitosan-TGA) to the liposomal surface to target intestinal mucosal membranes. Methods: Liposomes consisting of phosphatidylcholine (POPC) and a maleimide-functionalized lipid were incubated with chitosan-TGA, leading to the formation of a thioether bond between free SH-groups of the polymer and maleimide groups of the liposome. Uncoated and newly generated thiomer-coated liposomes were characterized according to their size, zeta potential, and morphology using photon correlation spectroscopy and transmission electron microscopy. The release behavior of calcitonin and the fluorophore/quencher-couple ANTS/DPX (8-aminonaphthalene-1,3,6-trisulfonic acid/p-xylene-bis-pyridinium bromide) from coated and uncoated liposomes, was investigated over 24 hours in simulated gastric and intestinal fluids. To test the mucoadhesive properties of thiomer-coated and uncoated liposomes in-vitro, we used freshly excised porcine small intestine. Results: Liposomes showed a concentration-dependent increase in size - from approximately 167 nm for uncoated liposomes to 439 nm for the highest thiomer concentration used in this study. Likewise, their zeta potentials gradually increased from about-38 mV to +20 mV, clearly indicating an effective coupling of chitosan-TGA to the surface of liposomes. As a result of mucoadhesion tests, we found an almost two-fold increase in the mucoadhesion of coupled liposomes relative to uncoupled ones. With fluorescence microscopy, we saw a tight adherence of coated particles to the intestinal mucus. Conclusion: Taken together, our current results indicate that thiomer-coated liposomes possess a high potential to be used as an oral drug-delivery system.
- Find related publications in this database (using NLM MeSH Indexing)
- Adhesiveness - drug effects
- Animals -
- Cell Line, Tumor -
- Cell Survival - drug effects
- Chitosan - administration and dosage Chitosan - chemistry
- Histocytochemistry -
- Intestinal Mucosa - drug effects Intestinal Mucosa - metabolism
- Intestine, Small - cytology Intestine, Small - metabolism
- Liposomes - administration and dosage Liposomes - chemistry
- Maleimides - chemistry
- Microscopy, Fluorescence -
- Naphthalenes - chemistry
- Particle Size -
- Phosphatidylcholines - chemistry
- Pyridinium Compounds - chemistry
- Sulfhydryl Compounds - chemistry
- Swine -
- Thioglycolates - chemistry
- Find related publications in this database (Keywords)
- thiomer
- liposome
- mucoadhesion
- chitosan-thioglycolic acid
- oral drug delivery