Thiolated particles as effective intravesical drug delivery systems for treatment of bladder-related diseases

• Published in: Nanomedicine (London, England) Vol. 8; no. 1; pp. 65 - 75
• Main Authors: Barthelmes, Jan, Dünnhaupt, Sarah, Unterhofer, Sibylle, Perera, Glen, Schlocker, Wolfgang, Bernkop-Schnürch, Andreas
• Format: Journal Article
• Language: English
• Published: London Future Medicine Ltd 01.01.2013; Future Medicine
• Subjects: Animals; Biological and medical sciences; Bladder diseases; Care and treatment; Drug Delivery Systems; Drugs; Female; Fluorescent Dyes; General pharmacology; Health aspects; intravesical drug delivery system; Medical sciences; microparticle; mucoadhesion; nanoparticle; Nanoparticles; Nephrology. Urinary tract diseases; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Rats; Rats, Sprague-Dawley; Sulfhydryl Compounds - chemistry; Thiols; urinary bladder; Urinary Bladder Diseases - drug therapy; Urinary system; Urinary system involvement in other diseases. Miscellaneous; Urinary tract. Prostate gland; Vehicles; intravesical drug delivery system; Bioadhesion; Urinary system disease; Pharmaceutical technology; Nanoparticle; Control release polymer; Mucosa; Thiolate; Drug carrier; Urinary tract disease; Urinary system; Urinary bladder; Microparticle; Bladder disease; mucoadhesion nanoparticle; Intravesical administration; Nanomedicine
• ISSN: 1743-5889; 1748-6963
• DOI: 10.2217/nnm.12.76

To prove mucoadhesiveness of thiolated and well-established polymeric microparticles and nanoparticles (NPs) as a promising nanomedical tool for the treatment of bladder-related diseases. 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 in the porcine urinary bladder model to identify the most appropriate particles for application in female Sprague Dawley rats. Pretrials indicated that particles based on chitosan were most suitable as an intravesical drug delivery system for 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. This advanced nanomedical tool based on thiolated chitosan seems to be a promising approach for the treatment of bladder-related diseases. Original submitted 20 January 2012; Revised submitted 20 April 2012; Published online 20 July 2012