Thiolated particles as effective intravesical drug delivery systems for treatment of bladder-related diseases.
OBJECTIVE
To prove in vivo mucoadhesiveness of thiolated and well-established polymeric microparticles and nanoparticles (NPs) as a promising nanomedical tool for the treatment of bladder-related diseases.


METHODS
Spray drying and ionic gelation were used in order to generate microparticles and NPs. For particle detection, the fluorescent marker, fluorescein diacetate, was incorporated in microparticles and NPs, respectively. Mucoadhesive properties of the particles were pre-evaluated via rheological measurements and ex vivo in the porcine urinary bladder model to identify the most appropriate particles for in vivo application in female Sprague Dawley rats.


RESULTS
Pretrials indicated that particles based on chitosan were most suitable as an intravesical drug delivery system for in vivo application. The retention time of thiolated chitosan NPs on the rat urinary bladder mucosa was approximately 170-fold higher in comparison with the pure fluorescent marker, fluorescein diacetate, having being applied as aqueous suspension without polymeric excipients.


CONCLUSIONS
This advanced nanomedical tool based on thiolated chitosan seems to be a promising approach for the treatment of bladder-related diseases.
Pharmaceutical Technology, Center for Molecular Biosciences, Leopold-Franzens-University Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.
Jan
J
Barthelmes
Sarah
S
Dünnhaupt
Sibylle
S
Unterhofer
Glen
G
Perera
Wolfgang
W
Schlocker
Andreas
A
Bernkop-Schnürch
D000818:Animals; D016503:Drug Delivery Systems; D005260:Female; D005456:Fluorescent Dyes; D051381:Rats; D017207:Rats, Sprague-Dawley; D013438:Sulfhydryl Compounds / Q000737:chemistry*; D001745:Urinary Bladder Diseases / Q000188:drug therapy*
D005456:Fluorescent Dyes; D013438:Sulfhydryl Compounds