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Buffered Nanoemulsion for Nose to Brain Delivery of Ziprasidone Hydrochloride: Preformulation and Pharmacodynamic Evaluation
Abstract
The study was undertaken to develop buffered nanoemulsion of ziprasidone hydrochloride (fifth generation antipshychotic) and evaluate its potential for efficacious nose to brain delivery drug delivery in animal models. Homogeneous buffered ziprasidone nanoemulsions (BZNE) were prepared by aqueous (phosphate buffer, pH 8.0) titration method using capmul MCM, labrasol and transcutol as oil, surfactant and cosurfactant respectively. The NEs (F1-F7) were characterized for pharmaceutical characteristics (% transmittance, PDI value, Zeta potential, globule size, viscosity and diffusion coefficient) and F6 with mean globule size of 145.24 ± 4.75nm (PDI = 0.186 ± 0.40) and diffusion coefficient of 0.1901± 0.04cm2/min was thermodynamically stable and was developed as buffered mucoadhesive nanoemulsions. The buffered mucoadhesive NE (βmax = 0.57) that contained 0.5% by weight of chitosan (BZMNE) exhibited 1.79 times higher diffusion coefficient (0.3418 ± 0.03) than BZNE. Pharmacodynamic study confirmed the superiority of BZMNE over BZNE in locomotor activity test (p < 0.05) and paw test (p < 0.05). Nasal ciliotoxicity study revealed the optimized BZMNE to be free from acute toxicity. Conclusively, a stable and efficacious buffered mucoadhesive NE of ziprasidone hydrochloride, that can be safely administered by intranasal route was developed.
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“Nasal ciliotoxicity studies revealed that the formulations containing ziprasidone were free from acute toxicity, and pharmacodynamic studies showed good results in locomotor activity tests and paw tests.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [53]
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Cited by
Sosnik, A., das Neves, J., & Sarmento, B. F. C. C. (2014) · Progress in Polymer Science · doi:10.1016/j.progpolymsci.2014.07.010 · Cited by 499
Chitosan in nasal delivery systems for therapeutic drugs
Casettari, L., & Illum, L. (2014) · Journal of Controlled Release · doi:10.1016/j.jconrel.2014.05.003 · Cited by 444
Nanoemulsions for “Nose-to-Brain” Drug Delivery
Bonferoni, M. C., Rossi, S., Sandri, G., Ferrari, F., Gavini, E., Rassu, G., & Giunchedi, P. (2019) · Pharmaceutics · doi:10.3390/pharmaceutics11020084 · Cited by 269
“prepared NEs loaded with ziprasidone hydrochloride, an antipsychotic drug [53].”
MethodJeong, S., Jang, J.-H., & Lee, Y. (2022) · Journal of Pharmaceutical Investigation · doi:10.1007/s40005-022-00589-5 · Cited by 293
“2017; Bahadur and Pathak 2012; Boche and Pokharkar 2017; Espinoza et al.”
BackgroundMultiple Roles of Chitosan in Mucosal Drug Delivery: An Updated Review
Mura, P., Maestrelli, F., Cirri, M., & Mennini, N. (2022) · Marine Drugs · doi:10.3390/md20050335 · Cited by 279
“…hydrochloride and evaluated their potential for an effective nose to brain delivery: NEs containing 0.5% CS showed an about two-times higher diffusion coefficient and a significantly superior efficacy in both paw test and locomotor activity test, compared with the corresponding NEs without CS [166].”
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Metadata
- Authors
- Bahadur, S., & Pathak, K.
- Venue
- Current Drug Delivery
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2012-10-01
- Volume
- 9
- Issue
- 6
- Pages
- 596-607
- ISSN
- 1567-2018 (ISSN-L)
- OpenAlex
- W1994990539
- Cited by
- 46
- References
- 0
- Citations by year
- 2026: 4 · 2025: 5 · 2024: 3 · 2023: 3 · 2022: 7 · 2021: 4 · 2020: 5 · 2019: 2 · 2017: 2 · 2016: 1 · 2015: 3 · 2014: 6 · 2013: 1
- FWCI
- 1.98
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Current Drug Delivery (publishedVersion)
- PubMed (publishedVersion)
- Funders
- U.S. Food and Drug Administration
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Keywords
- nose-to-brain delivery, intranasal drug delivery, chitosan, antipsychotic drugs, diffusion coefficient, globule size, pharmacodynamic evaluation, locomotor activity, preformulation
- MeSH terms
- Acrylates, Administration, Intranasal, Animals, Behavior, Animal, Brain, Drug Compounding, Emulsions, Motor Activity, Nasal Mucosa, Piperazines, Sheep, Thiazoles, Antipsychotic Agents, Drug Delivery Systems, Chitosan, Mice, Rats, Nanoparticles
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- CoChat. (2026). Citation check: Buffered Nanoemulsion for Nose to Brain Delivery of Ziprasidone Hydrochloride: Preformulation and Pharmacodynamic Evaluation. https://app.cochat.ai/papers/10.2174/156720112803529792
- The paper
- Bahadur, S., & Pathak, K. (2012). Buffered Nanoemulsion for Nose to Brain Delivery of Ziprasidone Hydrochloride: Preformulation and Pharmacodynamic Evaluation. Current Drug Delivery. https://doi.org/10.2174/156720112803529792
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
