Artículo
Radiolabeled Risperidone microSPECT/CT Imaging for Intranasal Implant Studies Development
Autor/es | Simón, Jon Ander
Utomo, Emilia Pareja, Félix Collantes, María Quincoces, Gemma Otero, Aarón Ecay, Margarita Domínguez Robles, Juan Larrañeta, Eneko Peñuelas, Iván |
Departamento | Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica |
Fecha de publicación | 2023 |
Fecha de depósito | 2024-03-04 |
Publicado en |
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Resumen | The use of intranasal implantable drug delivery systems has many potential advantages for the treatment of different diseases, as they can provide sustained drug delivery, improving patient compliance. We describe a novel ... The use of intranasal implantable drug delivery systems has many potential advantages for the treatment of different diseases, as they can provide sustained drug delivery, improving patient compliance. We describe a novel proof-of-concept methodological study using intranasal implants with radiolabeled risperidone (RISP) as a model molecule. This novel approach could provide very valuable data for the design and optimization of intranasal implants for sustained drug delivery. RISP was radiolabeled with 125I by solid supported direct halogen electrophilic substitution and added to a poly(lactide-co-glycolide) (PLGA; 75/25 D,L-Lactide/glycolide ratio) solution that was casted on top of 3D-printed silicone molds adapted for intranasal administration to laboratory animals. Implants were intranasally administered to rats, and radiolabeled RISP release followed for 4 weeks by in vivo non-invasive quantitative microSPECT/CT imaging. Percentage release data were compared with in vitro ones using radiolabeled implants containing either 125I-RISP or [125I]INa and also by HPLC measurement of drug release. Implants remained in the nasal cavity for up to a month and were slowly and steadily dissolved. All methods showed a fast release of the lipophilic drug in the first days with a steadier increase to reach a plateau after approximately 5 days. The release of [125I]I− took place at a much slower rate. We herein demonstrate the feasibility of this experimental approach to obtain high-resolution, non-invasive quantitative images of the release of the radiolabeled drug, providing valuable information for improved pharmaceutical development of intranasal implants. |
Agencias financiadoras | Academy of Medical Sciences Ministerio de Ciencia e Innovación (MICIN). España |
Identificador del proyecto | SBF005\1011
RYC-2021-034357-I |
Cita | Simón, J.A., Utomo, E., Pareja, F., Collantes, M., Quincoces, G., Otero, A.,...,Peñuelas, I. (2023). Radiolabeled Risperidone microSPECT/CT Imaging for Intranasal Implant Studies Development. Pharmaceutics, 15 (3), 843. https://doi.org/10.3390/pharmaceutics15030843. |
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Radiolabeled Risperidone.pdf | 2.900Mb | [PDF] | Ver/ | |