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Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers

The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be appropriate. This study investigates the feasibility of developing a buccal film impregnated with paliperidone-loaded nanostructured...

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Autores principales: AlMulhim, Fahad Mohammed, Nair, Anroop B., Aldhubiab, Bandar, Shah, Hiral, Shah, Jigar, Mewada, Vivek, Sreeharsha, Nagaraja, Jacob, Shery
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10674218/
https://www.ncbi.nlm.nih.gov/pubmed/38004510
http://dx.doi.org/10.3390/pharmaceutics15112530
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author AlMulhim, Fahad Mohammed
Nair, Anroop B.
Aldhubiab, Bandar
Shah, Hiral
Shah, Jigar
Mewada, Vivek
Sreeharsha, Nagaraja
Jacob, Shery
author_facet AlMulhim, Fahad Mohammed
Nair, Anroop B.
Aldhubiab, Bandar
Shah, Hiral
Shah, Jigar
Mewada, Vivek
Sreeharsha, Nagaraja
Jacob, Shery
author_sort AlMulhim, Fahad Mohammed
collection PubMed
description The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be appropriate. This study investigates the feasibility of developing a buccal film impregnated with paliperidone-loaded nanostructured lipid carriers (NLCs) and assesses the potential to enhance its bioavailability. Box–Behnken-based design optimization of NLCs was performed by examining the particles’ physical characteristics. The polymeric film was used to load optimized NLCs, which were then assessed for their pharmaceutical properties, permeability, and pharmacokinetics. The optimization outcomes indicated that selected formulation variables had a considerable (p < 0.05) impact on responses such as particle size, entrapment efficiency, and % drug release. Desired characteristics such as a negative charge, higher entrapment efficiency, and nanoparticles with ideal size distribution were shown by optimized NLC dispersions. The developed film demonstrated excellent physico-mechanical properties, appropriate texture, good drug excipient compatibility (chemically stable formulation), and amorphous drug nature. A sustained Weibull model drug release (p < 0.0005) and superior flux (~5-fold higher, p < 0.005) were seen in NLC-loaded film compared to plain-drug-loaded film. The pharmacokinetics profile in rabbits supports the goal of buccal therapy as evidenced by significantly higher AUC(0–12) (p < 0.0001) and greater relative bioavailability (236%) than the control. These results support the conclusion that paliperidone-loaded NLC buccal film has the potential to be an alternate therapy for its effective administration in the treatment of schizophrenia.
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spelling pubmed-106742182023-10-25 Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers AlMulhim, Fahad Mohammed Nair, Anroop B. Aldhubiab, Bandar Shah, Hiral Shah, Jigar Mewada, Vivek Sreeharsha, Nagaraja Jacob, Shery Pharmaceutics Article The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be appropriate. This study investigates the feasibility of developing a buccal film impregnated with paliperidone-loaded nanostructured lipid carriers (NLCs) and assesses the potential to enhance its bioavailability. Box–Behnken-based design optimization of NLCs was performed by examining the particles’ physical characteristics. The polymeric film was used to load optimized NLCs, which were then assessed for their pharmaceutical properties, permeability, and pharmacokinetics. The optimization outcomes indicated that selected formulation variables had a considerable (p < 0.05) impact on responses such as particle size, entrapment efficiency, and % drug release. Desired characteristics such as a negative charge, higher entrapment efficiency, and nanoparticles with ideal size distribution were shown by optimized NLC dispersions. The developed film demonstrated excellent physico-mechanical properties, appropriate texture, good drug excipient compatibility (chemically stable formulation), and amorphous drug nature. A sustained Weibull model drug release (p < 0.0005) and superior flux (~5-fold higher, p < 0.005) were seen in NLC-loaded film compared to plain-drug-loaded film. The pharmacokinetics profile in rabbits supports the goal of buccal therapy as evidenced by significantly higher AUC(0–12) (p < 0.0001) and greater relative bioavailability (236%) than the control. These results support the conclusion that paliperidone-loaded NLC buccal film has the potential to be an alternate therapy for its effective administration in the treatment of schizophrenia. MDPI 2023-10-25 /pmc/articles/PMC10674218/ /pubmed/38004510 http://dx.doi.org/10.3390/pharmaceutics15112530 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
AlMulhim, Fahad Mohammed
Nair, Anroop B.
Aldhubiab, Bandar
Shah, Hiral
Shah, Jigar
Mewada, Vivek
Sreeharsha, Nagaraja
Jacob, Shery
Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers
title Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers
title_full Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers
title_fullStr Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers
title_full_unstemmed Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers
title_short Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers
title_sort design, development, evaluation, and in vivo performance of buccal films embedded with paliperidone-loaded nanostructured lipid carriers
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10674218/
https://www.ncbi.nlm.nih.gov/pubmed/38004510
http://dx.doi.org/10.3390/pharmaceutics15112530
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