Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs.
Summary of "Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs."
The aim of this study was to develop tocol derivatives of chitosan able (i) to self-assemble in the gastrointestinal tract and (ii) to enhance the solubility of poorly soluble drugs. Among the derivatives synthesized, tocopherol succinate glycol chitosan (GC-TOS) conjugates spontaneously formed micelles in aqueous solution with a critical micelle concentration of 2μgmL(-1). AFM and TEM analysis showed that spherical micelles were formed. The GC-TOS increased water solubility of 2 model class II drugs. GC-TOS loading efficiency was 2.4% (w/w) for ketoconazole and 0.14% (w/w) for itraconazole, respectively. GC-TOS was non-cytotoxic at concentrations up to 10mgmL(-1). A 3.4-fold increase of the apparent permeation coefficient of ketoconazole across a Caco-2 cell monolayer was demonstrated. Tocol polymer conjugates may be promising vehicles for the oral delivery of poorly soluble drugs.
Affiliation
Université catholique de Louvain, Louvain Drug Research Institute, Pharmaceutics and Drug Delivery, Avenue Mounier, 73, B1.73.12, 1200 Brussels, Belgium.
Journal Details
This article was published in the following journal.
Name: International journal of pharmaceutics
ISSN: 1873-3476
Pages: 452-60
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/22212463
- DOI: http://dx.doi.org/10.1016/j.ijpharm.2011.12.010
Medical and Biotech [MESH] Definitions
Ethylene Glycol
A colorless, odorless, viscous dihydroxy alcohol. It has a sweet taste, but is poisonous if ingested. Ethylene glycol is the most important glycol commercially available and is manufactured on a large scale in the United States. It is used as an antifreeze and coolant, in hydraulic fluids, and in the manufacture of low-freezing dynamites and resins.
Drug Carriers
Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.
Food, Genetically Modified
Food derived from genetically modified organisms (ORGANISMS, GENETICALLY MODIFIED).
Capsules
Hard or soft soluble containers used for the oral administration of medicine.
Streptococcus Gordonii
A species of gram-positive, facultatively anaerobic bacteria in the family STREPTOCOCCACEAE. It is a normal inhabitant of the human oral cavity, and causes DENTAL PLAQUE and ENDOCARDITIS. It is being investigated as a vehicle for vaccine delivery.
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