Solid lipid nanoparticles (SLN) for controlled drug delivery - a review of the state of the art.
03 Jul 2000-European Journal of Pharmaceutics and Biopharmaceutics (Elsevier)-Vol. 50, Iss: 1, pp 161-177
TL;DR: Relevant issues for the introduction of SLN to the pharmaceutical market, such as status of excipients, toxicity/tolerability aspects and sterilization and long-term stability including industrial large scale production are discussed.
About: This article is published in European Journal of Pharmaceutics and Biopharmaceutics.The article was published on 2000-07-03. It has received 3260 citations till now. The article focuses on the topics: Drug carrier & Solid lipid nanoparticle.
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TL;DR: Electrospinning is a highly versatile method to process solutions or melts, mainly of polymers, into continuous fibers with diameters ranging from a few micrometers to a few nanometers, applicable to virtually every soluble or fusible polymer.
Abstract: Electrospinning is a highly versatile method to process solutions or melts, mainly of polymers, into continuous fibers with diameters ranging from a few micrometers to a few nanometers. This technique is applicable to virtually every soluble or fusible polymer. The polymers can be chemically modified and can also be tailored with additives ranging from simple carbon-black particles to complex species such as enzymes, viruses, and bacteria. Electrospinning appears to be straightforward, but is a rather intricate process that depends on a multitude of molecular, process, and technical parameters. The method provides access to entirely new materials, which may have complex chemical structures. Electrospinning is not only a focus of intense academic investigation; the technique is already being applied in many technological areas.
3,833 citations
TL;DR: An overview on some of the currently used systems for drug delivery, varying from biological substances like albumin, gelatine and phospholipids for liposomes, and more substances of a chemical nature like various polymers and solid metal containing nanoparticles is provided.
Abstract: The use of nanotechnology in medicine and more specifically drug delivery is set to spread rapidly. Currently many substances are under investigation for drug delivery and more specifically for cancer therapy. Interestingly pharmaceutical sciences are using nanoparticles to reduce toxicity and side effects of drugs and up to recently did not realize that carrier systems themselves may impose risks to the patient. The kind of hazards that are introduced by using nanoparticles for drug delivery are beyond that posed by conventional hazards imposed by chemicals in classical delivery matrices. For nanoparticles the knowledge on particle toxicity as obtained in inhalation toxicity shows the way how to investigate the potential hazards of nanoparticles. The toxicology of particulate matter differs from toxicology of substances as the composing chemical(s) may or may not be soluble in biological matrices, thus influencing greatly the potential exposure of various internal organs. This may vary from a rather high local exposure in the lungs and a low or neglectable exposure for other organ systems after inhalation. However, absorbed species may also influence the potential toxicity of the inhaled particles. For nanoparticles the situation is different as their size opens the potential for crossing the various biological barriers within the body. From a positive viewpoint, especially the potential to cross the blood brain barrier may open new ways for drug delivery into the brain. In addition, the nanosize also allows for access into the cell and various cellular compartments including the nucleus. A multitude of substances are currently under investigation for the preparation of nanoparticles for drug delivery, varying from biological substances like albumin, gelatine and phospholipids for liposomes, and more substances of a chemical nature like various polymers and solid metal containing nanoparticles. It is obvious that the potential interaction with tissues and cells, and the potential toxicity, greatly depends on the actual composition of the nanoparticle formulation. This paper provides an overview on some of the currently used systems for drug delivery. Besides the potential beneficial use also attention is drawn to the questions how we should proceed with the safety evaluation of the nanoparticle formulations for drug delivery. For such testing the lessons learned from particle toxicity as applied in inhalation toxicology may be of use. Although for pharmaceutical use the current requirements seem to be adequate to detect most of the adverse effects of nanoparticle formulations, it can not be expected that all aspects of nanoparticle toxicology will be detected. So, probably additional more specific testing would be needed.
3,140 citations
Cites background from "Solid lipid nanoparticles (SLN) for..."
...Besides degradation physical means such as heating and light may be used to provoke the therapeutic effect Table 1 Overview of nanoparticles and their applications in Life Sciences Particle class Materials Application Natural Chitosan Drug/Gene delivery materials or Dextrane derivatives Gelatine Alginates Liposomes Starch Dendrimers Branched polymers Drug delivery Fullerenes Carbon based carriers Photodynamics Drug delivery Polymer carriers Polylactic acid Drug/gene delivery Poly(cyano)acrylates Polyethyleinemine Block copolymers Polycaprolactone Ferrofl uids SPIONS Imaging (MRI) USPIONS Quantum dots Cd/Zn-selenides Imaging In vitro diagnostics Various Silica-nanoparticles Gene delivery Mixtures of above Table 2 Chemicals under investigation for drug delivery Albumin Damascelli et al 2003 Cetyl alcohol/polysorbate Koziara et al 2004 Chitosan Dyer et al 2002; Huang et al 2004 Gelatin Cascone et al 2002 Gold Hainfi eld et al 2004; Paciotti et al 2004 Hydrogels Gupta and Gupta 2004 Magnetic iron oxide Gupta and Gupta 2005 Methoxy Kim et al 2003 poly(ethylene glycol)/poly(ε-caprolactone) Polyalkylcyanoacrylate composites Alyautdin et al 1997; Kreuter et al 2003 Poly(D,L-lactic-co-glycolic)acid (PLGA) Panyam et al 2002; Weissenbrock et al 2004 Solid lipid formulations Muller et al 2000; Wissing et al 2004 International Journal of Nanomedicine 2008:3(2)136...
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...…Ferrofl uids SPIONS Imaging (MRI) USPIONS Quantum dots Cd/Zn-selenides Imaging In vitro diagnostics Various Silica-nanoparticles Gene delivery Mixtures of above Table 2 Chemicals under investigation for drug delivery Albumin Damascelli et al 2003 Cetyl alcohol/polysorbate Koziara et al 2004…...
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...…Polyalkylcyanoacrylate composites Alyautdin et al 1997; Kreuter et al 2003 Poly(D,L-lactic-co-glycolic)acid (PLGA) Panyam et al 2002; Weissenbrock et al 2004 Solid lipid formulations Muller et al 2000; Wissing et al 2004 International Journal of Nanomedicine 2008:3(2)136...
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TL;DR: An overview about the selection of the ingredients, different ways of SLN production and SLN applications, and the in vivo fate of the carrier are presented.
2,786 citations
TL;DR: Two nonviral gene delivery systems using either biodegradable poly(D,Llactide-co-glycolide) (PLG) nanoparticles or cell penetrating peptide (CPP) complexes have been designed and studied using A549 human lung epithelial cells.
Abstract: The development of nonviral vectors for safe and efficient gene delivery has been gaining considerable attention recently. An ideal nonviral vector must protect the gene against degradation by nuclease in the extracellular matrix, internalize the plasma membrane, escape from the endosomal compartment, unpackage the gene at some point and have no detrimental effects. In comparison to viruses, nonviral vectors are relatively easy to synthesize, less immunogenic, low in cost, and have no limitation in the size of a gene that can be delivered. Significant progress has been made in the basic science and applications of various nonviral gene delivery vectors; however, the majority of nonviral approaches are still inefficient and often toxic. To this end, two nonviral gene delivery systems using either biodegradable poly(D,Llactide-co-glycolide) (PLG) nanoparticles or cell penetrating peptide (CPP) complexes have been designed and studied using A549 human lung epithelial cells. PLG nanoparticles were optimized for gene delivery by varying particle surface chemistry using different coating materials that adsorb to the particle surface during formation. A variety of cationic coating materials were studied and compared to more conventional surfactants used for PLG nanoparticle fabrication. Nanoparticles (~200 nm) efficiently encapsulated plasmids encoding for luciferase (80-90%) and slowly released the same for two weeks. After a delay, moderate levels of gene expression appeared at day 5 for certain positively charged PLG particles and gene expression was maintained for at least two weeks. In contrast, gene expression mediated by polyethyleneimine (PEI) ended at day 5. PLG particles were also significantly less
2,189 citations
TL;DR: As a novel type of lipid nanoparticles with solid matrix, the nanostructured lipid carriers (NLC) are presented and improvements discussed, for example, increase in loading capacity, physical and chemical long-term stability, triggered release and potentially supersaturated topical formulations.
1,783 citations
References
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TL;DR: The principle suitability of SLN as a prolonged release formulation for lipophilic drugs is demonstrated and tetracaine and prednisolone loaded SLN showed a distinctly prolonged release over a monitored period of 5 weeks.
879 citations
Book•
24 Aug 2000
TL;DR: Polymers as Drug Delivery Carriers Hydrophilic Cellulose Derivatives as Drug delivery Carriers: Influence of Substitution Type on the Properties of Compressed Matrix Tablets, Carmen Ferrero Rodriguez and Nathalie Bruneau.
Abstract: Polymers as Drug Delivery Carriers Hydrophilic Cellulose Derivatives as Drug Delivery Carriers: Influence of Substitution Type on the Properties of Compressed Matrix Tablets, Carmen Ferrero Rodriguez, Nathalie Bruneau, Jerome Barra, Dorothee Alfonso, and Eric Doelker Poly(Vinyl Alcohol) as a Drug Delivery Carrier, Surya K. Mallapragada and Shannon McCarthy-Schroeder Development of Acrylate and Methacrylate Polymer Networks for Controlled Release by Photopolymerization Technology, Robert Scott, Jennifer H. Ward, and Nicholas A. Peppas Smart Polymers for Controlled Drug Delivery, Joseph Kost and Smadar A. Lapidot Complexing Polymers in Drug Delivery, Anthony M. Lowman Polylactic and Polyglycolic Acids as Drug Delivery Carriers, Lisa Brannon-Peppas and Michel Vert Use of Infrared and Raman Spectroscopy for Characterization of Controlled Release Systems, A. B. Scranton, B. Drescher, E. W. Nelson, and J. L. Jacobs Accurate Models in Controlled Drug Delivery Systems, Balaji Narasimhan Mechanism-Based Classification of Controlled Release Devices Drug Release from Swelling-Controlled Systems, Paolo Colombo, Patrizia Santi, Ruggero Bettini,Christopher S. Brazel, and Nikolaos A. Peppas Superporous Hydrogels as a Platform for Oral Controlled Drug Delivery, Haesun Park, Jun Chen, and Kinam Park Osmotic Implantable Delivery Systems, Jeremy C. Wright, Felix Theeuwes, and Cynthia L. Stevenson Bioadhesive Controlled Release Systems, Nicholas A. Peppas, Monica D. Little, and Yanbin Huang Micro- and Nanoparticulate Release Systems Microencapsulation Technology: Interfacial Polymerization Method, A. Atila Hincal and H. Suheyla Kas Nanoparticulate Controlled Release Systems for Cancer Therapy, C. Dubernet, E. Fattal, and P. Couvreur Microencapsulation Using Coacervation/Phase Separation: An Overview of the Technique and Applications, H. Suheyla Kas and Levent Oner Microsphere Preparation by Solvent Evaporation Method, A. Atila Hincal and Sema Calis Nanosuspensions-A Formulation Approach for Poorly Soluble and Poorly Bioavailable Drugs, R. H. Muller, B. H. L. Bohm, and M. J. Grau Large-Scale Production of Solid Lipid Nanoparticles (SLN) and Nanosuspensions (DissoCubes), R. H. Muller, S. Gohla, A. Dingler, and T. Schneppe Solid Lipid Nanoparticles (SLN) as a Carrier System for the Controlled Release of Drugs, R. H. Muller, A. Lippacher, and S. Gohla Stability of Encapsulated Substances in Poly(Lactide-co-Glycolide) Delivery Systems, Steven P. Schwendeman, Gaozhong Zhu, Anna Shenderova, and Wenle Jiang Development of Polysaccharides as Novel Drug Carrier Systems, C. Vauthier and P. Couvreur Classification of Controlled Release Devices According to Administration Site An Overview of Controlled Release Systems, S. Venkatraman, N. Davar, A. Chester, and L. Kleiner Research and Development Aspects of Oral Controlled-Release Dosage Forms, Yihong Qiu and Guohua Zhang A Gastrointestinal Retentive Microparticulate System to Improve Oral Drug Delivery, Y. Kawashima, H. Takeuchi, and H. Yamamoto In Vitro-In Vivo Correlations in the Development of Solid Oral Controlled Release Dosage Forms, Yihong Qiu, Emil E. Samara, and Guoliang Cao Gamma Scintigraphy in the Analysis of the Behavior of Controlled Release Systems, C. G. Wilson and N. Washington Electrically Assisted Transdermal Delivery of Drugs, Ajay K. Banga A Novel Method Based on Artificial Neural Networks for Optimizing Transdermal Drug Delivery Systems, Kozo Takayama and Tsuneji Nagai Transdermal Drug Delivery by Skin Electroporation, Tani Chen, Robert Langer, and James C. Weaver Enhancement of Transdermal Transport Using Ultrasound in Combination with Other Enhancers, Joseph Kost, Samir Mitragotri, and Robert Langer Electrotransport Systems for Transdermal Delivery: A Practical Implementation of Iontophoresis, Erik R. Scott, J. Bradley Phipps, J. Richard Gyory, and Rama V. Padmanabhan Peptide and Protein Release Systems Controlled Release Protein Therapeutics: Effects of Process and Formulation on Stability, Paul A. Burke Solid-State Chemical Stability of Peptides and Proteins: Application to Controlled Release Formulations, Elizabeth M. Topp, Yuan Song, Ashley Wilson, Rong Li, Michael J. Hageman, and Richard L. Schowen Growth Factor Release from Biodegradable Hydrogels to Induce Neovascularization, Yoshita Ikada and Yasuhiko Tabata Biopolymers for Release of Interleukin-2 for Treatment of Cancer, Debra J. Trantolo, Joseph D. Gresser, A. Ganiyu Jimoh, Donald L. Wise,and James C. Yang Medical Applications of Drug Delivery Osmotic Drug Delivery from Asymmetric Membrane Film-Coated Dosage Forms, Mary Tanya am Ende, Scott M. Herbig, Richard W. Korsmeyer, and Mark B. Chidlaw Controlled Release Pain Management Systems, Vasif Hasirci, Dilek Sendil, Leonidas C. Goudas, Daniel B. Carr, and Donald L. Wise Biodegradable Systems for Long-Acting Nestorone, Debra J. Trantolo, Donald L. Wise, A. J. Moo-Young, Yung-Yueh Hsu, and Joseph D. Gresser Preparation and Evaluation of Buprenorphine Microspheres for Parenteral Administration, William R. Ravis, Yuh-Jing Lin, and Ram Murty Prolonged Release of Hydromorphone from a Novel Poly(Lactic-co-Glycolic) Acid Depot System: Initial In Vitro and In Vivo Observations, Leonidas C. Goudas, Daniel B. Carr, Richard M. Kream, Louis Shuster, William M. Vaughan, Joseph D. Gresser,Donald L. Wise, and Debra J. Trantolo Incorporation of an Active Agent into a Biodegradable Cement: Encapsulation of the Agent as Protection from Chemical Degradation During Cure and Effect on Release Profile, Joseph D. Gresser, Debra J. Trantolo, Pattisapu R. J. Gangadharam, Hisanori X. Nagaoka,Yung-Yueh Hsu, and Donald L. Wise The Pharmacoeconomic Value of Controlled Release Dosage Forms, Laura B. Gardner
668 citations
TL;DR: In this article, a poloxamer 188 stabilized Compritol SLN formulation was prepared and its stability was investigated as a function of storage temperature, light exposure and packing material (untreated and siliconized vials of glass quality I).
568 citations
TL;DR: In this paper, solid lipid nanoparticles (SLN) were produced by high pressure homogenization of a melted lipid (Dynasan 112) dispersed in water at increased temperature (70°C). Soy lecithin and poloxamer 188 were used as surfactants and stabilizers of the particles.
520 citations
TL;DR: Enhanced retinol palmitate uptake should derive from specific SLN effects and is not due to non-specific occlusive properties, as Transepidermal water loss (TEWL) and the influence of drug free SLN on retinyl palmitates uptake exclude pronounced Occlusive effects.
492 citations