Dataset Information

Chitosan/?-glycerophosphate in situ gelling mucoadhesive systems for intravesical delivery of mitomycin-C.

ABSTRACT: The development of mucoadhesive in situ gelling formulations for intravesical application may improve the therapeutic outcomes of bladder cancer patients. In this work, chitosan/?-glycerophosphate (CHIGP) thermosensitive formulations have been prepared using three different chitosan grades (62, 124 and 370?kDa). Their ability to form in situ gelling systems triggered by changes in temperature upon administration to urinary bladder were evaluated using vial inversion and rheological methods. Texture analysis was used to study their mucoadhesive properties as well as syringeability through the urethral catheter. The retention of CHIGP formulations, with fluorescein sodium as the model drug, was studied on porcine urinary bladder mucosa ex vivo using the flow-through technique and fluorescent microscopy. CHIGP formulations containing mitomycin-C were prepared and drug release was studied using in vitro dialysis method. It was established that the molecular weight of chitosan influenced the thermogelling, mucoadhesive and drug release behaviour of the in situ gelling delivery systems. Formulations prepared from chitosan with greatest molecular weight (370?kDa) were found to be the most promising for intravesical application due to their superior gelling properties and in vitro retention in the bladder.

SUBMITTER: Kolawole OM

PROVIDER: S-EPMC6733296 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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Publications

Chitosan/β-glycerophosphate in situ gelling mucoadhesive systems for intravesical delivery of mitomycin-C.

Kolawole Oluwadamilola M OM Lau Wing Man WM Khutoryanskiy Vitaliy V VV

International journal of pharmaceutics: X 20190222

The development of mucoadhesive in situ gelling formulations for intravesical application may improve the therapeutic outcomes of bladder cancer patients. In this work, chitosan/β-glycerophosphate (CHIGP) thermosensitive formulations have been prepared using three different chitosan grades (62, 124 and 370 kDa). Their ability to form in situ gelling systems triggered by changes in temperature upon administration to urinary bladder were evaluated using vial inversion and rheological ...[more]

PMID: 31517272

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Project description:Pharmaceutical approaches based on nanotechnologies and the development of eye drops composed of the mucoadhesive polymers chitosan and hyaluronic acid are emerging strategies for the efficient treatment of ocular diseases. These innovative nanoparticulate systems aim to increase drugs' bioavailability at the ocular surface. For the successful development of these systems, the evaluation of mucoahesiveness (the interaction between the ocular delivery system and mucins present on the eye) is of utmost importance. In this context, the aim of the present work was to investigate the mucoadhesivity of a novel nanoparticle eye drop formulation containing an antibiotic (ceftazidime) intended to treat eye infections. Eye drop formulations comprised a polymer (hydroxypropyl) methyl cellulose (HPMC) 0.75% (w/v) in an isotonic solution incorporating chitosan/sodium tripolyphosphate (TPP)-hyaluronic acid-based nanoparticles containing ceftazidime. The viscosity of the nanoparticles, and the gels incorporating the nanoparticles were characterized in contact with mucin at different mass ratios, allowing the calculation of the rheological synergism parameter (??). Results showed that at different nanoparticle eye formulation:mucin weight ratios, a minimum in viscosity occurred which resulted in a negative rheological synergism. Additionally, the results highlighted the mucoadhesivity of the novel ocular formulation and its ability to interact with the ocular surface, thus increasing the drug residence time in the eye. Moreover, the in vitro release and permeation studies showed a prolonged drug release profile from the chitosan/TPP-hyaluronic acid nanoparticles gel formulation. Furthermore, the gel formulations were not cytotoxic on ARPE-19 and HEK293T cell lines, evaluated by the metabolic and membrane integrity tests. The formulation was stable and the drug active, as shown by microbiological studies. In conclusion, chitosan/TPP-hyaluronic acid nanoparticle eye drop formulations are a promising platform for ocular drug delivery with enhanced mucoadhesive properties.

Dataset Information

Chitosan/?-glycerophosphate in situ gelling mucoadhesive systems for intravesical delivery of mitomycin-C.

Publications

Chitosan/β-glycerophosphate <i>in situ</i> gelling mucoadhesive systems for intravesical delivery of mitomycin-C.

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