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      • Record: found
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      Optimization of LDL targeted nanostructured lipid carriers of 5-FU by a full factorial design

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          Abstract

          Background:

          Nanostructured lipid carriers (NLC) are a mixture of solid and liquid lipids or oils as colloidal carrier systems that lead to an imperfect matrix structure with high ability for loading water soluble drugs. The aim of this study was to find the best proportion of liquid and solid lipids of different types for optimization of the production of LDL targeted NLCs used in carrying 5-Fu by the emulsification-solvent evaporation method.

          Materials and Methods:

          The influence of the lipid type, cholesterol or cholesteryl stearate for targeting LDL receptors, oil type (oleic acid or octanol), lipid and oil% on particle size, surface charge, drug loading efficiency, and drug released percent from the NLCs were studied by a full factorial design.

          Results:

          The NLCs prepared by 54.5% cholesterol and 25% of oleic acid, showed optimum results with particle size of 105.8 nm, relatively high zeta potential of –25 mV, drug loading efficiency of 38% and release efficiency of about 40%. Scanning electron microscopy of nanoparticles confirmed the results of dynamic light scattering method used in measuring the particle size of NLCs.

          Conclusions:

          The optimization method by a full factorial statistical design is a useful optimization method for production of nanostructured lipid carriers.

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          Most cited references13

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          Nanostructured lipid matrices for improved microencapsulation of drugs.

          R.H Müller, M. Radtke, S.A. Wissing (2002)
          At the beginning of the nineties solid lipid nanoparticles (SLN) have been introduced as a novel nanoparticulate delivery system produced from solid lipids. Potential problems associated with SLN such as limited drug loading capacity, adjustment of drug release profile and potential drug expulsion during storage are avoided or minimised by the new generation, the nanostructured lipid carriers (NLC). NLC are produced by mixing solid lipids with spatially incompatible lipids leading to special structures of the lipid matrix, i.e. three types of NLC: (I) the imperfect structured type, (II) the structureless type and (III) the multiple type. A special preparation process-applicable to NLC but also SLN-allows the production of highly concentrated particle dispersions (>30-95%). Potential applications as drug delivery system are described.
          Article 0 comments Cited 222 times – based on 0 reviews     Review now
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            Preparation and characterization of stearic acid nanostructured lipid carriers by solvent diffusion method in an aqueous system.

            Qing Ye, Hong Yuan, Qiang Hu … (2005)
            Nanostuctured lipid carriers (NLC) based on mixture of solid lipids with spatially incompatible liquid lipids are a new type of lipid nanoparticles, which offer the advantage of improved drug loading capacity and release properties. In present study, stearic acid (SA) nanostuctured lipid carriers with various oleic acid (OA) content were successfully prepared by solvent diffusion method in an aqueous system. The size and surface morphology of nanoparticles were significantly influenced by OA content. As OA content increased up to 30wt%, the obtained particles showed pronounced smaller size and more regular morphology in spherical shape with smooth surface. Compared with solid lipid nanoparticles (SLN), NLC exhibited improved drug loading capacity, and the drug loading capacity increased with increasing OA content. These results were explained by differential scanning calorimetry (DSC) investigations. The addition of OA to nanoparticles formulation resulted in massive crystal order disturbance and less ordered matrix of NLC, and hence, increased the drug loading capacity. The drug in vitro release behavior from NLC displayed biphasic drug release pattern with burst release at the initial stage and prolonged release afterwards, and the successful control of release rate at the initial stage can be achieved by controlling OA content.
            Article 0 comments Cited 84 times – based on 0 reviews     Review now
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              Solid lipid nanoparticles and nanostructured lipid carriers--innovative generations of solid lipid carriers.

              S Shidhaye, Reshma Vaidya, Sagar Sutar … (2008)
              The first generation of solid lipid carrier systems in nanometer range, Solid Lipid Nanoparticles (SLN), was introduced as an alternative to liposomes. SLN are aqueous colloidal dispersions, the matrix of which comprises of solid biodegradable lipids. SLN are manufactured by techniques like high pressure homogenization, solvent diffusion method etc. They exhibit major advantages such as modulated release, improved bioavailability, protection of chemically labile molecules like retinol, peptides from degradation, cost effective excipients, improved drug incorporation and wide application spectrum. However there are certain limitations associated with SLN, like limited drug loading capacity and drug expulsion during storage, which can be minimized by the next generation of solid lipids, Nanostructured lipid carriers (NLC). NLC are lipid particles with a controlled nanostructure that improves drug loading and firmly incorporates the drug during storage. Owing to their properties and advantages, SLN and NLC may find extensive application in topical drug delivery, oral and parenteral administration of cosmetic and pharmaceutical actives. Cosmeceuticals is emerging as the biggest application target of these carriers. Carrier systems like SLN and NLC were developed with a perspective to meet industrial needs like scale up, qualification and validation, simple technology, low cost etc. This paper reviews present status of SLN and NLC as carrier systems with special emphasis on their application in Cosmeceuticals; it also gives an overview about various manufacturing techniques of SLN and NLC.
              Article 0 comments Cited 34 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Adv Biomed Res
                Journal ID (iso-abbrev): Adv Biomed Res
                Journal ID (publisher-id): ABR
                Title: Advanced Biomedical Research
                Publisher: Medknow Publications & Media Pvt Ltd (India )
                ISSN (Electronic): 2277-9175
                Publication date Collection: 2012
                Publication date (Electronic): 28 August 2012
                Volume: 1
                Electronic Location Identifier: 45
                Affiliations
                [1]Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, India
                [1 ]Department of Medicinal Chemistry, Faculty of Pharmacy and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan, India
                Author notes
                Address for correspondence: Prof. Jaleh Varshosaz, Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, India. E-mail: varshosaz@ 123456pharm.mui.ac.ir
                Article
                Publisher ID: ABR-1-45
                DOI: 10.4103/2277-9175.100147
                PMC ID: 3544134
                PubMed ID: 23326776
                SO-VID: 45e920ae-1f5a-4ec5-8083-3ebd8f863593
                Copyright © Copyright: © 2012 Andalib
                License:

                This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

                History
                Date received : 12 March 2012
                Date accepted : 10 May 2012
                Categories
                Subject: Original Article

                ScienceOpen disciplines: Molecular medicine
                Keywords: 5-fu,ldl targeted nanostructured lipid carriers,optimization,structural parameters
                Data availability:
                ScienceOpen disciplines: Molecular medicine
                Keywords: 5-fu, ldl targeted nanostructured lipid carriers, optimization, structural parameters

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