Formulation optimization and in vitro skin penetration of spironolactone loaded solid lipid nanoparticles

Kelidari, Hamid Reza; Saeedi, Majid; Âkbari, Jafar; Morteza‐Semnani, Katayoun; Gill, Pooria; Valizadeh, Hadi; Nokhodchi, Ali

doi:10.1016/j.colsurfb.2015.02.046

Cited by 86 publications

(51 citation statements)

References 21 publications

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“…Increasing lipid level but decreasing both the surfactant and phospholipid concentrations seems to increase the EE. This finding is in line with previous reports (Priyanka & Hasan, 2012;Kelidari & Saeedi, 2015) and can be justified by the fact that higher lipid concentration will provide more space to increase lipid content and reduce the tendency of drug to escape to the external phase.…”

Section: Response Surface Explorationsupporting

confidence: 93%

“…As the level of the lipid increases, the small PS is maintained only if the level of the surfactant is increased correspondingly. This observation was reported elsewhere (Kelidari et al, 2015) and was attributed to the ability to effectively reduce the interfacial tension between aqueous and lipid phases, which subsequently would lead to the formation of smaller droplets. Higher surfactant concentration effectively stabilizes the particles by forming a steric barrier on the particle surface, and thereby protect smaller particles and prevent their coalescence into bigger ones (Rahman & Zidan, 2010).…”

Section: Response Surface Explorationsupporting

confidence: 74%

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Topical ketoprofen nanogel: artificial neural network optimization, clustered bootstrap validation, and in vivo activity evaluation based on longitudinal dose response modeling

et al. 2016

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Objectives: This work aimed at investigating the potential of solid lipid nanoparticles (SLN) as carriers for topical delivery of Ketoprofen (KP); evaluating a novel technique incorporating Artificial Neural Network (ANN) and clustered bootstrap for optimization of KP-loaded SLN (KP-SLN); and demonstrating a longitudinal dose response (LDR) modeling-based approach to compare the activity of topical non-steroidal anti-inflammatory drug formulations. Methods: KP-SLN was fabricated by a modified emulsion/solvent evaporation method. BoxBehnken design was implemented to study the influence of glycerylpalmitostearate-to-KP ratio, Tween 80, and lecithin concentrations on particle size, entrapment efficiency, and amount of drug permeated through rat skin in 24 hours. Following clustered bootstrap ANN optimization, the optimized KP-SLN was incorporated into an aqueous gel and evaluated for rheology, in vitro release, permeability, skin irritation and in vivo activity using carrageenan-induced rat paw edema model and LDR mathematical model to analyze the time course of anti-inflammatory effect at various application durations. Results: Lipid-to-drug ratio of 7.85 ], Tween 80 of 1.27% [bootstrap 95%CI: 0.601-2.40%], and Lecithin of 0.263% [bootstrap 95%CI: 0.263-0.328%] were predicted to produce optimal characteristics. Compared with profenid Õ gel, the optimized KP-SLN gel exhibited slower release, faster permeability, better texture properties, greater efficacy, and similar potency. Conclusions: SLNs are safe and effective permeation enhancers. ANN coupled with clustered bootstrap is a useful method for finding optimal solutions and estimating uncertainty associated with them. LDR models allow mechanistic understanding of comparative in vivo performances of different topical formulations, and help design efficient dermatological bioequivalence assessment methods.

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Section: Response Surface Explorationsupporting

confidence: 93%

Section: Response Surface Explorationsupporting

confidence: 74%

Topical ketoprofen nanogel: artificial neural network optimization, clustered bootstrap validation, and in vivo activity evaluation based on longitudinal dose response modeling

et al. 2016

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“…A system employing three improved Franz diffusion cells was used for permeation studies. The excised rat skin was set in place with the stratum corneum facing the donor compartment and the dermis facing the receptor [27]. The receiver compartment was filled with 5.5 ml of 50:50 ethanol/water mixture.…”

Section: In Vitro Skin Permeation Studymentioning

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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“…Thus, the solubility enhancement of poorly watersoluble SP is one of the key challenges in pharmaceutical research (7). Various techniques have been reported to increase the dissolution rate of poorly water-soluble SP, such as cyclodextrin complexation approach, freeze-drying or lyophilisation, solid dispersion strategy, liposomal formulations and solid lipid nanoparticles (SLNs) approach (2)(3)(4)8). Bourezg et al prepared a SP-loaded SLN formulation and reported as one of the efficient ways to enhance the dissolution of water-insoluble drugs (6).…”

Section: Introductionmentioning

confidence: 99%

Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability

et al. 2016

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Abstract.Stable solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) formulations to enhance the dissolution rates of poorly soluble drug spironolactone (SP) were being developed. Probe ultra-sonication method was used to prepare SLNs and NLCs. All NLCs contained stearic acid (solid lipid carrier) and oleic acid (liquid lipid content), whereas, SLNs were prepared and optimised by using the solid lipid only. The particles were characterised in terms of particle size analysis, thermal behaviour, morphology, stability and in vitro release. The zeta sizer data revealed that the increase in the concentration of oleic acid in the formulations reduced the mean particle size and the zeta potential. The increase in concentration of oleic acid from 0 to 30% (w/w) resulted in a higher entrapment efficiency. All nanoparticles were almost spherically shaped with an average particle size of about ∼170 nm. The DSC traces revealed that the presence of oleic acid in the NLC formulations resulted in a shift in the melting endotherms to a higher temperature. This could be attributed to a good long-term stability of the nanoparticles. The stability results showed that the particle size remained smaller in NLC compared to that of SLN formulations after 6 months at various temperatures. The dissolution study showed about a 5.1-to 7.2-fold increase in the release of the drug in 2 h compared to the raw drug. Comparing all nanoparticle formulations indicated that the NLC composition with a ratio of 70:30 (solid:liquid lipid) is the most suitable formulation with desired drug dissolution rates, entrapment efficiency and physical stability.

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Formulation optimization and in vitro skin penetration of spironolactone loaded solid lipid nanoparticles

Cited by 86 publications

References 21 publications

Topical ketoprofen nanogel: artificial neural network optimization, clustered bootstrap validation, and in vivo activity evaluation based on longitudinal dose response modeling

Topical ketoprofen nanogel: artificial neural network optimization, clustered bootstrap validation, and in vivo activity evaluation based on longitudinal dose response modeling

The design of naproxen solid lipid nanoparticles to target skin layers

Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability

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