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.
Université catholique de Louvain, Louvain Drug Research Institute, Pharmaceutics and Drug Delivery, Avenue Mounier, 73, B1.73.12, 1200 Brussels, Belgium.
This article was published in the following journal.
Name: International journal of pharmaceutics
- 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
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.
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).
Hard or soft soluble containers used for the oral administration of medicine.
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.
Chitosan (CS) grafted with β-cyclodextrin (CD-g-CS) nanoparticles as a new carrier for poorly water-soluble drugs has been developed. The CD-g-CS polymer is readily synthesized from chitosan and mono...
Chitosan-based nanoparticles have been widely used as a carrier for gene delivery due to their low toxicity and the positively charged amino groups in chitosan. In this study, we hypothesized that int...
The condensed version: Thiolated glycol chitosan can form stable nanoparticles with polymerized siRNAs through charge-charge interactions and self-cross-linking. This poly-siRNA/glycol chitosan nanopa...
The aim of this study was to develop a novel nanoparticulate formulation and test its potential for oral peptide drug delivery. Chitosan-6-mercaptonicotinic acid is a novel thiolated chitosan with str...
The limited solubility and dissolution rate exhibited by poorly soluble drugs is major challenges in the pharmaceutical process. Following oral administration, the poorly soluble drugs generally show...
Chitosan is a natural product that is produced commercially through the deacetylation of chitin, which is found in the exoskeleton of crustaceans. It has been suggested that chitosan has a...
The "dry eye syndrome" DES is a highly prevalent ocular disease, in particular in the elderly population. One mainstay of therapy for patients suffering from DES is the use of topically ad...
The purpose of this study is to explore the protective effect and safety of soluble beta-1,3/1,6-glucan compared to placebo in oral mucositis in head and neck patients receiving radiothera...
Purpose: This study is aimed to be a prospective clinical trial to investigate the efficacy of a chitosan-coated nasal packing (ChitoFlex® used in conjunction with the HemCon Nasal Plug)...
The purpose of this study is to determine if the use of HemCon chitosan-based dressings is effective to facilitate safe, effective debridement of chronic wounds in the operating room and i...