Abstract
Concanavalin A (ConA)-conjugated poly(ethylene glycol)-poly(lactic acid) nanoparticles (ConA-NPs) were prepared for targeted drug delivery to the cervical lymph nodes after intranasal administration. ConA, a lectin specifically binding to α-mannose and α-glucose, was covalently conjugated on NPs without loss of its carbohydrates binding bioactivity. In vitro cellular uptake experiment demonstrated that NPs could be uptaken by Calu-3 cells in a time- and concentration-dependent manner, and conjugation of ConA on NPs could significantly increase the rate and amount of cellular uptake. ConA-NP showed no obvious toxicity to Calu-3 cells in vitro or to the nasal cilia of rats in vivo. Compared with NPs without ConA, ConA-NP is more effective in targeting drugs to the deep cervical lymph nodes, as evidenced by 1.36-2.52 times increase of targeting efficiency, demonstrating that ConA-NP is a potential carrier for targeted drug delivery to the cervical lymph nodes via nasal route.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Intranasal
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Animals
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Cell Line, Tumor
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Cervix Uteri / drug effects
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Cervix Uteri / metabolism
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Concanavalin A / chemistry*
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Concanavalin A / metabolism
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Concanavalin A / toxicity
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Coumarins / administration & dosage*
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Coumarins / blood
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Coumarins / pharmacokinetics*
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Drug Carriers / chemistry*
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Drug Carriers / metabolism
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Drug Carriers / toxicity
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Drug Delivery Systems*
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Female
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Humans
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Lactates / chemistry*
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Lactates / metabolism
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Lactates / toxicity
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Lymph Nodes / drug effects
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Lymph Nodes / metabolism*
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Male
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Nanoparticles / chemistry
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Nanoparticles / metabolism
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Nanoparticles / toxicity
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Polyethylene Glycols / chemistry*
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Polyethylene Glycols / metabolism
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Polyethylene Glycols / toxicity
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Rats
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Rats, Sprague-Dawley
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Thiazoles / administration & dosage*
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Thiazoles / blood
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Thiazoles / pharmacokinetics*
Substances
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Coumarins
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Drug Carriers
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Lactates
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Thiazoles
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coumarin 6
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poly(lactic acid-ethylene glycol)
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Concanavalin A
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Polyethylene Glycols