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Radiolabeled Risperidone microSPECT/CT Imaging for Intranasal Implant Studies Development.
Jon Ander Simón1, Emilia Utomo2, Félix Pareja1
1Radiopharmacy Unit, Department of Nuclear Medicine, Clinica Universidad de Navarra, University of Navarra, IdiSNA, 31008 Pamplona, Spain.
Pharmaceutics
|March 29, 2023
Summary
This study demonstrates a new method using radiolabeled risperidone (RISP) in intranasal implants for sustained drug delivery. The technique allows non-invasive imaging to track drug release, aiding in the development of better nasal drug delivery systems.
Area of Science:
- Pharmaceutical Sciences
- Biomedical Engineering
- Radiochemistry
Background:
- Intranasal implantable drug delivery systems offer sustained release and improved patient compliance.
- Developing effective intranasal implants requires precise methods to study drug release kinetics.
Purpose of the Study:
- To establish a proof-of-concept methodology for evaluating intranasal implants using radiolabeled risperidone (RISP).
- To provide valuable data for the design and optimization of sustained-release intranasal implants.
Main Methods:
- Radiolabeling of RISP with 125I and incorporation into poly(lactide-co-glycolide) (PLGA) implants.
- Intranasal administration of implants to rats and in vivo non-invasive quantitative microSPECT/CT imaging over 4 weeks.
- Comparison of in vivo release data with in vitro release studies (HPLC and radiolabeled implants).
Main Results:
- Intranasal implants remained in place for up to a month, dissolving slowly and steadily.
- All methods indicated a rapid initial release of the lipophilic drug, reaching a plateau around 5 days.
- In vivo imaging provided high-resolution, quantitative data on radiolabeled drug release.
Conclusions:
- The developed experimental approach is feasible for high-resolution, non-invasive imaging of drug release from intranasal implants.
- This method offers valuable insights for the pharmaceutical development of advanced intranasal drug delivery systems.
- The study highlights the potential of sustained drug delivery via intranasal implants for improved therapeutic outcomes.

