Development and evaluation of rivastigmine loaded chitosan nanoparticles for brain targeting

Fazil, Mohammad; Shadab,; Haque, Syed Ehtaishamul; Kumar, Manish; Baboota, Sanjula; Sahni, Jasjeet Kaur; Ali, Javed

doi:10.1016/j.ejps.2012.04.013

Cited by 302 publications

(153 citation statements)

References 33 publications

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“…Zetasizer tends to measure the apparent diameter of the particles, including the hydrodynamic layers surrounding the particles, resulting in an overestimated particle size [35]. Figure 2 illustrates the infrared spectra of naproxen, GMS, Nap-SLN6 and physical mixture (with the same composition).…”

Section: Tem Analysismentioning

confidence: 99%

The design of naproxen solid lipid nanoparticles to target skin layers

Âkbari

Saeedi

Morteza‐Semnani

et al. 2016

Colloids and Surfaces B: Biointerfaces

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(2016) The design of naproxen solid lipid nanoparticles to target skin layers. Colloids and Surfaces B: Biointerfaces, This version is available from Sussex Research Online: http://sro.sussex.ac.uk/67745/ This document is made available in accordance with publisher policies and may differ from the published version or from the version of record. If you wish to cite this item you are advised to consult the publisher's version. Please see the URL above for details on accessing the published version. Copyright and reuse:Sussex Research Online is a digital repository of the research output of the University.Copyright and all moral rights to the version of the paper presented here belong to the individual author(s) and/or other copyright owners. To the extent reasonable and practicable, the material made available in SRO has been checked for eligibility before being made available.Copies of full text items generally can be reproduced, displayed or performed and given to third parties in any format or medium for personal research or study, educational, or not-for-profit purposes without prior permission or charge, provided that the authors, title and full bibliographic details are credited, a hyperlink and/or URL is given for the original metadata page and the content is not changed in any way. This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. Graphical Abstract Highlights  Naproxen solid lipid nanoparticles (Nap-SLN) can successfully be prepared by ultrasonication  Properties of these nanoparticles can be optimized by lipid concentrations  HLB of the surfactants played a crucial effect on properties of solid lipid nanoparticles  Nap-SLN increased the drug concentration in skin layer rather than systemic absorption Accepted Manuscript AbstractThe aim of the current investigation was to produce naproxen solid lipid nanoparticles (Nap-SLNs) by the ultrasonication method to improve its skin permeation and also to investigate the influence of Hydrophilic-lipophilic balance (HLB) changes on nanoparticles properties. The properties of obtained SLNs loaded with naproxen were characterized by photon correlation spectroscopy (PCS), transmission electron microscopy (TEM) and differential scanning calorimetry (DSC). FT-IR was also used to investigate any interaction between naproxen and the excipients used at the molecular level during the preparation of the SLNs. The performance of the formulations was investigated in terms of skin permeation and also the retention of the drug by the skin. It was found that generally, with increasing the lipid concentration, the average particle size and polydispersity index (PDI) ...

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Section: Tem Analysismentioning

confidence: 99%

The design of naproxen solid lipid nanoparticles to target skin layers

Âkbari

Saeedi

Morteza‐Semnani

et al. 2016

Colloids and Surfaces B: Biointerfaces

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“…delivery has come to the forefront as an alternative to invasive delivery methods to bypass the BBB and target drugs directly to the brain. This may provide significant advantages such as non-invasiveness, bypassing BBB and decreasing systemic drug exposition, thereby reducing systemic side effects as compared to current conventional strategies [6,7]. The drug may be transported directly into the brain tissue (i.e., olfactory bulb) or the cerebrospinal fluid through the olfactory region of the nasal cavity [7,8].…”

Section: Introductionmentioning

confidence: 99%

“…This may provide significant advantages such as non-invasiveness, bypassing BBB and decreasing systemic drug exposition, thereby reducing systemic side effects as compared to current conventional strategies [6,7]. The drug may be transported directly into the brain tissue (i.e., olfactory bulb) or the cerebrospinal fluid through the olfactory region of the nasal cavity [7,8]. The strategy to achieve improved delivery to the brain would be a combination of a system that specifically targets the olfactory region and bioadhesive characteristic that retains the formulation at the absorption site for prolonged period of time and improves drug delivery [9].…”

Section: Introductionmentioning

confidence: 99%

Optimised nanoformulation of bromocriptine for direct nose-to-brain delivery: biodistribution, pharmacokinetic and dopamine estimation by ultra-HPLC/mass spectrometry method

Shadab

Haque

Fazil

et al. 2014

Expert Opinion on Drug Delivery

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“…Nasal route has advantages of fast absorption of drug, enhanced bioavailability even at lower doses, rapid onset of therapeutic action, circumvent liver or gastrointestinal metabolism, reduced risk of overdose, non-invasive administration, convenient, self-medication and better patient compliance (Li et al, 2002;Vyas et al, 2006;Jogani et al, 2008;Kaur & Kim, 2008;Elshafeey et al, 2009;Patel et al, 2013b). Scientists are making many attempts to find efficient and new ways to prevent extensive first pass metabolism and target the drug to the receptor site in brain for treating brain disorders (Wolfgang & Heidrun, 2005;Porecha et al, 2009;Fazil et al, 2012;Md et al, 2013;Mahajan et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

“…The intranasal administration of drug can be increased by coadministering a permeation enhancer (Patel et al, 2013b). ME have been thoroughly studied as a drug carrier due to their special features, such as ease of preparation due to spontaneous formation, thermodynamic stability, high-solublization capacity for the hydrophilic and lipophilic drugs, transparent and elegant appearance, enhanced penetration through the biological membranes, increased bioavailability, and less inter-and intra-individual variability in drug pharmacokinetics (Li et al, 2002;Zhang et al, 2004;Wolfgang & Heidrun, 2005;Kaur & Kim, 2008;Elshafeey et al, 2009;Porecha et al, 2009;Shinde et al, 2011;Fazil et al, 2012;Md et al, 2013;Mahajan et al, 2014). …”

Section: Introductionmentioning

confidence: 99%

Paliperidone microemulsion for nose-to-brain targeted drug delivery system: pharmacodynamic and pharmacokinetic evaluation

Patel¹,

Patel²,

Bhatt³

et al. 2014

Drug Delivery

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Objective: The objective of present study was to develop and evaluate paliperidone (PALI) loaded microemulsion (PALI-ME) for intranasal delivery in the treatment of schizophrenia. Material and methods: The PALI-ME was formulated by the spontaneous microemulsification method and characterized for physicochemical parameters. Pharmacodynamic assessments (apomorphine-induced compulsive behavior and spontaneous motor activity) were performed using mice. All formulations were tagged with 99m Tc (technetium). Pharmacokinetic evaluation of PALI in the brain was investigated using Swiss albino rats. Brain scintigraphy imaging was performed in rabbits. Results and discussion: PALI-ME was found stable with average droplet size of 20.01 ± 1.28 nm. In pharmacodynamic studies, significant (p50.05) deference in parameters estimated, were found between the treated and control groups. Tc-tagged PALI solution (PALI-SOL)/ PALI-ME/PALI muco-adhesive ME (PALI-MME) was found to be stable and suitable for in vivo studies. Brain-to-blood ratio at all sampling points up to 8 h following intranasal administration of PALI-MME compared to intravenous PALI-ME was found to be 6-8 times higher signifying greater extent of distribution of the PALI in brain. Rabbit brain scintigraphy demonstrated higher intranasal uptake of the PALI into the brain. Conclusion: This investigation demonstrates a prompt and larger extent of transport of PALI into the brain through intranasal PALI-MME, which may prove beneficial for treatment of schizophrenia.

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Development and evaluation of rivastigmine loaded chitosan nanoparticles for brain targeting

Cited by 302 publications

References 33 publications

The design of naproxen solid lipid nanoparticles to target skin layers

The design of naproxen solid lipid nanoparticles to target skin layers

Optimised nanoformulation of bromocriptine for direct nose-to-brain delivery: biodistribution, pharmacokinetic and dopamine estimation by ultra-HPLC/mass spectrometry method

Paliperidone microemulsion for nose-to-brain targeted drug delivery system: pharmacodynamic and pharmacokinetic evaluation

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