Core-Shell Arginine-Containing Chitosan Microparticles for Enhanced Transcorneal Permeation of Drugs

Giulia Di Prima, Paola Varvara', Mariano Licciardi, Nicolò Mauro, Gaetano Giammona, Gennara Cavallaro, Mariano Licciardi, Nicolò Mauro, Gaetano Giammona

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1 Citazione (Scopus)

Abstract

Chitosan oligosaccharide (C) was functionalized with L-arginine (A) and short hydrocarbon chains (C8) to design an amphiphilic copolymer, henceforth CAC8, leading to microparticles (MPs) consisting of an arginine-decorated hydrophilic shell and inner hydrophobic domains allowing the encapsulation of high amount hydrophobic drugs such as sorafenib tosylate (>10% w/w). L-arginine side chains were selected in order to impart the final MPs enhanced transcorneal penetration properties, thus overcoming the typical biological barriers which hamper the absorption of drugs upon topical ocular administration. The mucoadhesive properties and drug release profile of the CAC8 MPs (CAC8-MPs) were studied, showing that CAC8-MPs can strongly interact with mucin, and thus gradually release their payload in situ to potentially improve the bioavailability of the drug after topical administration. In vitro transcorneal studies also showed that CAC8-MPs are endowed with effective permeation enhancer ability combined with negligible toxicity.
Lingua originaleEnglish
pagine (da-a)960-969
Numero di pagine10
RivistaJournal of Pharmaceutical Sciences
Volume108
Stato di pubblicazionePublished - 2019

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Chitosan
Arginine
Topical Administration
Ophthalmic Administration
Pharmaceutical Preparations
Mucins
Hydrocarbons
Oligosaccharides
Biological Availability

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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title = "Core-Shell Arginine-Containing Chitosan Microparticles for Enhanced Transcorneal Permeation of Drugs",
abstract = "Chitosan oligosaccharide (C) was functionalized with L-arginine (A) and short hydrocarbon chains (C8) to design an amphiphilic copolymer, henceforth CAC8, leading to microparticles (MPs) consisting of an arginine-decorated hydrophilic shell and inner hydrophobic domains allowing the encapsulation of high amount hydrophobic drugs such as sorafenib tosylate (>10{\%} w/w). L-arginine side chains were selected in order to impart the final MPs enhanced transcorneal penetration properties, thus overcoming the typical biological barriers which hamper the absorption of drugs upon topical ocular administration. The mucoadhesive properties and drug release profile of the CAC8 MPs (CAC8-MPs) were studied, showing that CAC8-MPs can strongly interact with mucin, and thus gradually release their payload in situ to potentially improve the bioavailability of the drug after topical administration. In vitro transcorneal studies also showed that CAC8-MPs are endowed with effective permeation enhancer ability combined with negligible toxicity.",
author = "{Di Prima}, Giulia and Paola Varvara' and Mariano Licciardi and Nicol{\`o} Mauro and Gaetano Giammona and Gennara Cavallaro and Mariano Licciardi and Nicol{\`o} Mauro and Gaetano Giammona",
year = "2019",
language = "English",
volume = "108",
pages = "960--969",
journal = "Journal of Pharmaceutical Sciences",
issn = "0022-3549",
publisher = "John Wiley and Sons Inc.",

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TY - JOUR

T1 - Core-Shell Arginine-Containing Chitosan Microparticles for Enhanced Transcorneal Permeation of Drugs

AU - Di Prima, Giulia

AU - Varvara', Paola

AU - Licciardi, Mariano

AU - Mauro, Nicolò

AU - Giammona, Gaetano

AU - Cavallaro, Gennara

AU - Licciardi, Mariano

AU - Mauro, Nicolò

AU - Giammona, Gaetano

PY - 2019

Y1 - 2019

N2 - Chitosan oligosaccharide (C) was functionalized with L-arginine (A) and short hydrocarbon chains (C8) to design an amphiphilic copolymer, henceforth CAC8, leading to microparticles (MPs) consisting of an arginine-decorated hydrophilic shell and inner hydrophobic domains allowing the encapsulation of high amount hydrophobic drugs such as sorafenib tosylate (>10% w/w). L-arginine side chains were selected in order to impart the final MPs enhanced transcorneal penetration properties, thus overcoming the typical biological barriers which hamper the absorption of drugs upon topical ocular administration. The mucoadhesive properties and drug release profile of the CAC8 MPs (CAC8-MPs) were studied, showing that CAC8-MPs can strongly interact with mucin, and thus gradually release their payload in situ to potentially improve the bioavailability of the drug after topical administration. In vitro transcorneal studies also showed that CAC8-MPs are endowed with effective permeation enhancer ability combined with negligible toxicity.

AB - Chitosan oligosaccharide (C) was functionalized with L-arginine (A) and short hydrocarbon chains (C8) to design an amphiphilic copolymer, henceforth CAC8, leading to microparticles (MPs) consisting of an arginine-decorated hydrophilic shell and inner hydrophobic domains allowing the encapsulation of high amount hydrophobic drugs such as sorafenib tosylate (>10% w/w). L-arginine side chains were selected in order to impart the final MPs enhanced transcorneal penetration properties, thus overcoming the typical biological barriers which hamper the absorption of drugs upon topical ocular administration. The mucoadhesive properties and drug release profile of the CAC8 MPs (CAC8-MPs) were studied, showing that CAC8-MPs can strongly interact with mucin, and thus gradually release their payload in situ to potentially improve the bioavailability of the drug after topical administration. In vitro transcorneal studies also showed that CAC8-MPs are endowed with effective permeation enhancer ability combined with negligible toxicity.

UR - http://hdl.handle.net/10447/340021

UR - http://www.interscience.wiley.com/jpages/0022-3549

M3 - Article

VL - 108

SP - 960

EP - 969

JO - Journal of Pharmaceutical Sciences

JF - Journal of Pharmaceutical Sciences

SN - 0022-3549

ER -