Development of Solid Lipid-polymer Hybrid Nanoparticles as Potential Oral Delivery Systems for Lipophilic Bioactive Compounds

Development of Solid Lipid-polymer Hybrid Nanoparticles as Potential Oral Delivery Systems for Lipophilic Bioactive Compounds PDF Author: Taoran Wang
Publisher:
ISBN:
Category : Electronic dissertations
Languages : en
Pages :

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Book Description
Solid lipid-polymer hybrid nanoparticles (SLPN) are nanocarriers made from a combination of polymers and lipids. By integrating the advantages of biocompatible lipid-based nanoparticles and gastrointestinal (GI)-stable polymeric nanoparticles, SLPN are the ideal delivery system for delivering lipophilic compounds orally. In this project, two novel preparation strategies were proposed to fabricate GI-stable SLPN: 1) Bovine serum albumin (BSA) and dextran were first conjugated through Maillard reaction and the conjugates were exploited as macromolecular emulsifier and surface coating layer to prepare SLPN by a solvent diffusion and sonication method. In this approach, the multilayer structure was formed by self-assembly of BSA-dextran micelles to envelope solid lipid via a pH- and heating-induced facile process with simultaneous surface deposition of pectin; 2) Dextran was first oxidized and functionalized with more surface aldehyde groups, and then the SLPN was fabricated through in situ conjugation between oxidized dextran and BSA-emulsified solid lipid. Both types of SLPN were applied to encapsulate lipophilic bioactive compounds, including curcumin and astaxanthin (ASTN). The major objectives of this dissertation were to 1) systematically study the fabrication parameters in two preparation strategies to prepare SLPN; 2) comprehensively characterize the structural and colloidal properties of as-prepared two types of SLPN; 3) explore and compare the encapsulation and delivery applications of SLPN for lipophilic bioactive compounds, including curcumin and ASTN. In summary, the surface-functionalized SLPN could significantly improve the physicochemical properties of lipid nanoparticles and expand their potential as oral delivery systems for lipophilic bioactive compounds.

Development of Solid Lipid-polymer Hybrid Nanoparticles as Potential Oral Delivery Systems for Lipophilic Bioactive Compounds

Development of Solid Lipid-polymer Hybrid Nanoparticles as Potential Oral Delivery Systems for Lipophilic Bioactive Compounds PDF Author: Taoran Wang
Publisher:
ISBN:
Category : Electronic dissertations
Languages : en
Pages :

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Book Description
Solid lipid-polymer hybrid nanoparticles (SLPN) are nanocarriers made from a combination of polymers and lipids. By integrating the advantages of biocompatible lipid-based nanoparticles and gastrointestinal (GI)-stable polymeric nanoparticles, SLPN are the ideal delivery system for delivering lipophilic compounds orally. In this project, two novel preparation strategies were proposed to fabricate GI-stable SLPN: 1) Bovine serum albumin (BSA) and dextran were first conjugated through Maillard reaction and the conjugates were exploited as macromolecular emulsifier and surface coating layer to prepare SLPN by a solvent diffusion and sonication method. In this approach, the multilayer structure was formed by self-assembly of BSA-dextran micelles to envelope solid lipid via a pH- and heating-induced facile process with simultaneous surface deposition of pectin; 2) Dextran was first oxidized and functionalized with more surface aldehyde groups, and then the SLPN was fabricated through in situ conjugation between oxidized dextran and BSA-emulsified solid lipid. Both types of SLPN were applied to encapsulate lipophilic bioactive compounds, including curcumin and astaxanthin (ASTN). The major objectives of this dissertation were to 1) systematically study the fabrication parameters in two preparation strategies to prepare SLPN; 2) comprehensively characterize the structural and colloidal properties of as-prepared two types of SLPN; 3) explore and compare the encapsulation and delivery applications of SLPN for lipophilic bioactive compounds, including curcumin and ASTN. In summary, the surface-functionalized SLPN could significantly improve the physicochemical properties of lipid nanoparticles and expand their potential as oral delivery systems for lipophilic bioactive compounds.

Lipid Nanoparticles: Production, Characterization and Stability

Lipid Nanoparticles: Production, Characterization and Stability PDF Author: Rohan Shah
Publisher: Springer
ISBN: 3319107119
Category : Medical
Languages : en
Pages : 105

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Book Description
​What are lipid nanoparticles? How are they structured? How are they formed? What techniques are best to characterize them? How great is their potential as drug delivery systems? These questions and more are answered in this comprehensive and highly readable work on lipid nanoparticles. This work sets out to provide the reader with a clear and understandable understanding of the current practices in formulation, characterization and drug delivery of lipid nanoparticles. A comprehensive description of the current understanding of synthesis, characterization, stability optimization and drug incorporation of solid lipid nanoparticles is provided. Nanoparticles have attracted great interest over the past few decades with almost exponential growth in their research and application. Their small particle size and subsequent high surface area make them ideal in many uses, but particularly as drug carrier systems. Nanoparticles made from lipids are especially attractive because of their enhanced biocompatibility imparted by the lipid. The work provides a detailed description of the types of lipid nanoparticles available (e.g. SLN, NLC, LDC, PLN) and how they range from imperfect crystalline to amorphous in structure. Current thoughts on where drugs are situated (e.g. in the core, or at the interface) and how this can be manipulated are discussed. The many techniques for production, including the author’s own variant of microwave heating, are fully discussed. Techniques for measuring arguably the most important characteristics of particle size and polydispersity are discussed, along with techniques to measure crystallinity, shape and drug capacity. Finally, a full chapter on techniques for measuring stability, both in the absence and presence of drugs, is discussed, along with suggestions on how to optimize that stability. This work appeals to students of colloid science, practitioners of research into drug delivery and academics alike.

Lipid Polymer Hybrid Nanoparticles

Lipid Polymer Hybrid Nanoparticles PDF Author: Nayab Tahir
Publisher:
ISBN:
Category : Medical
Languages : en
Pages : 0

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Book Description
Applications of nanotechnology and material sciences emerge in the development of various novel drug delivery systems that have been proven as promising clinically. Among these, liposomes, noisome, polymeric carriers and lipid-based delivery system were extensively explored and enter into clinical trials and clinical applications. However, each system has its own pros and cons in term of different physicochemical, pharmacokinetics and therapeutics aspects. Lipid-polymer hybrid carriers merge the potential benefit of these structural components and can be prepared by different approaches to improve the therapeutic outcomes. In this chapter, we provide the useful insight about the lipid-polymer hybrid nanoparticles (LPHNPs) that can be prepared by using the different structural components including the synthetic and natural polymers and lipids. Among these, we also explain the various methods to prepare the LPHNPs with various desired characteristics. Finally, the various therapeutic and clinical applications have been presented briefly.

Bioactive Delivery Systems for Lipophilic Nutraceuticals

Bioactive Delivery Systems for Lipophilic Nutraceuticals PDF Author: Ming Miao
Publisher: Royal Society of Chemistry
ISBN: 183916557X
Category : Technology & Engineering
Languages : en
Pages : 464

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Book Description
There is growing interest in the food, supplements, cosmetics, and pharmaceutical industries in improving the healthiness of their products by incorporating lipophilic bioactive substances like oil-soluble vitamins (A, D and E), omega-3 fatty acids, and nutraceuticals (carotenoids, curcuminoids and flavonoids). However, there are many challenges that need to be overcome due to their poor water-solubility, chemical stability, and bioavailability. For this reason, there is interest in the development of effective encapsulation technologies to increase the efficacy of lipophilic bioactives. This book reviews the encapsulation systems currently available for delivering lipophilic bioactives, including their preparation, functionality, and application range, including nanoemulsions, emulsions, Pickering emulsions, HIPEs, microgels, organogels and liposomes. Chapters 1-2 review the biological activity of delivery systems and lipophilic bioactives. Chapters 3-5 describe the materials and preparation methods used to assemble delivery systems. Chapters 6-17 focus on the formation and application of different kinds of delivery systems. Chapter 18 discusses future trends in the development of bioactive delivery systems. Edited and authored by world renowned scholars, the book provides a state-of-the-art overview of the design, fabrication, and utilization of delivery systems for bioactives that will be useful for academic, government, and industrial scientists in fields such as pharmaceuticals, cosmetics, agriculture, chemical engineering, nutrition, and foods.

Lipid Nanoparticulate Drug Delivery Systems

Lipid Nanoparticulate Drug Delivery Systems PDF Author: Sudarshan Kumar Singh
Publisher:
ISBN:
Category : Medical
Languages : en
Pages : 0

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Book Description
Hybrid lipid polymers significantly changed the postulation of low or less bioavailability of conventional drug delivery systems. Several drug delivery systems already exist for the encapsulation and subsequent release of lipophilic drugs with enhanced therapeutic efficacy and are well described in the scientific literature. Among these, lipid polymer-based nanoparticles have specifically come up for dermal, transdermal, mucosal, intramuscular, and ocular drug administration routes in the last 20 years. Moreover, lipid nanoparticles showed potential for active targeting of anticancer therapy, delivery of DNA or RNA materials, and use as a diagnostic imaging agent. Therefore, the multifarious nanostructured lipid carriers can reduce the undesired effects with maximum utilization of active moiety. In this, chapter a brief discussion is presented on the source of synthetic and natural lipid polymers with the use of surfactants. Moreover, a summary on formulation and pharmaceutical characterization of nanostructured lipid carriers considering solid lipid nanoparticles and vesicular drug delivery systems has been taken into consideration. In addition, a light on bioactive fortified with lipid nanoparticles was reviewed for maximizing its therapeutic efficacy. Furthermore, this chapter,Äôs focus to bring out the latest applications via recent scientific publications from the Scopus database on nanostructure carriers that showed promising application for the treatments of potentially life-threatening diseases has been summarized.

Biocompatible Polymeric Nanoparticles with Innovative Structural Design for Oral Delivery of Lipophilic Bioactives

Biocompatible Polymeric Nanoparticles with Innovative Structural Design for Oral Delivery of Lipophilic Bioactives PDF Author: Qiaobin Hu
Publisher:
ISBN:
Category : Electronic dissertations
Languages : en
Pages :

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Book Description


Polymeric Nanomaterials in Nanotherapeutics

Polymeric Nanomaterials in Nanotherapeutics PDF Author:
Publisher: Elsevier
ISBN: 0128139331
Category : Science
Languages : en
Pages : 558

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Book Description
Polymeric Nanomaterials in Nanotherapeutics describes how polymeric nanosensors and nanorobotics are used for biomedical instrumentation, surgery, diagnosis and targeted drug delivery for cancer, pharmacokinetics, monitoring of diabetes and healthcare. Key areas of coverage include drug administration and formulations for targeted delivery and release of active agents (drug molecules) to non-healthy tissues and cells. The book demonstrates how these are applied to dental work, wound healing, cancer, cardiovascular diseases, neurodegenerative disorders, infectious diseases, chronic inflammatory diseases, metabolic diseases, and more. Methods of administration discussed include oral, dental, topical and transdermal, pulmonary and nasal, ocular, vaginal, and brain drug delivery and targeting. Drug delivery topics treated in several subchapters includes materials for active targeting and cases study of polymeric nanomaterials in clinical trials. The toxicity and regulatory status of therapeutic polymeric nanomaterials are also examined. The book gives a broad perspective on the topic for researchers, postgraduate students and professionals in the biomaterials, biotechnology, and biomedical fields. Shows how the properties of polymeric nanomaterials can be used to create more efficient medical treatments/therapies Demonstrates the potential and range of applications of polymeric nanomaterials in disease prevention, diagnosis, drug development, and for improving treatment outcomes Accurately explains how nanotherapeutics can help in solving problems in the field through the latest technologies and formulations

Development, Characterization and Evaluation of Solid Lipid Nanoparticles as a Potential Anticancer Drug Delivery System

Development, Characterization and Evaluation of Solid Lipid Nanoparticles as a Potential Anticancer Drug Delivery System PDF Author: Meghavi Patel
Publisher:
ISBN:
Category :
Languages : en
Pages : 83

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Book Description
Solid lipid nanoparticles (SLNs) consist of spherical solid lipid particles in the nanometer size range, which are dispersed in water or in an aqueous surfactant solution. SLN technology represents a promising new approach to deliver hydrophilic as well as lipophilic drugs. The commercialization of SLN technology remains limited despite numerous efforts from researchers. The purpose of this research was to advance SLN preparation methodology by investigating the feasibility of preparing glyceryl monostearate (GMS) nanoparticles by using three preparation methods namely microemulsion technique, magnetic stirring technique and temperature modulated solidification technique of which the latter two were developed in our laboratory. An anticancer drug 5-fluorouracil was incorporated in the SLNs prepared via the temperature modulated solidification process. Optimization of the magnetic stirring process was performed to evaluate how the physicochemical properties of the SLN was influenced by systematically varying process parameters including concentration of the lipid, concentration of the surfactant, type of surfactant, time of stirring and temperature of storage. The results demonstrated 1:2 GMS to tween 80 ratio, 150 ml dispersion medium and 45 min stirring at 4000 RPM speed provided an optimum formulation via the temperature modulated solidification process. SLN dispersions were lyophilized to stabilize the solid lipid nanoparticles and the lyophilizates exhibited good redispersibility. The SLNs were characterized by particle size analysis via dynamic light scattering (DLS), zeta potential, transmission electron microscopy (TEM), differential scanning calorimetry (DSC), drug encapsulation efficiency and in vitro drug release studies. Particle size of SLN dispersion prepared via the three preparation techniques was approximately 66 nm and that of redispersed lyophilizates was below 500 nm. TEM images showed spherical to oval particles that were less dense in the core with a well-defined shell and the particle size was in agreement with the particle size analysis data obtained by DLS. DSC thermograms of the lyophilized SLNs indicate a reduction in the crystallinity order of GMS particles. The drug encapsulation efficiency was found to be approximately 30%. In vitro drug release studies from redispersed lyophilized SLNs showed that 17 % of the encapsulated drug was released within 2 h. The SLNs prepared in our lab demonstrated characteristics that can potentially be utilized in an anticancer drug delivery system. Future in vitro cell culture and in vivo animal model studies will delineate compatibility and utility of these formulations in biological systems.

ROLE OF LIPID-BASED DELIVERY SYSTEMS IN THE BIOLOGICAL FATE OF LIPOPHILIC NUTRACEUTICALS AND INORGANIC NANO-PARTICLES IN THE GASTROINTESTINAL TRACT.

ROLE OF LIPID-BASED DELIVERY SYSTEMS IN THE BIOLOGICAL FATE OF LIPOPHILIC NUTRACEUTICALS AND INORGANIC NANO-PARTICLES IN THE GASTROINTESTINAL TRACT. PDF Author: Mingfei Yao
Publisher:
ISBN:
Category :
Languages : en
Pages :

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Book Description
The oral bioavailability of lipophilic bioactive molecules can be greatly increased by encapsulating them within engineered lipid nanoparticles, such as micelles, microemulsions and nanoemulsions. After ingestion these engineered lipid nanoparticles are disassembled in the gastrointestinal tract (GIT), and then reassembled into biological lipid nanoparticles (mixed micelles) in the small intestine. These mixed micelles solubilize and transport lipophilic bioactive components to the epithelium cells. The mixed micelles themselves are then disassembled and reassembled into yet another form of biological lipid nanoparticle (chylomicrons, CMs) within the enterocyte cells. The CMs carry the bioactive components into the systemic (blood) circulation via the lymphatic system, thereby avoiding metabolism in the small intestine and liver. Polymethoxyflavones (PMFs) are bioactive flavonoids found in citrus fruits that have been shown to have potential health promoting properties. However, their application as nutraceuticals in functional foods and beverages is currently limited due to their low water solubility and high melting point. The oral bioavailability of lipophilic compounds can be enhanced by promoting their intestinal lymphatic transport through co-administration with digestible lipids. First, we investigated the effects of chylomicron-mediated intestinal lymphatic transport on the bioavailability of 5-hydroxy-6, 7, 8, 3', 4'-pentamethoxylflavone (5-DN), one of representative PMFs in Caco-2 cells. Our results demonstrated that oleic acid and bile acid promoted secretion of CMs in Caco-2 cells, with mean diameter ranged from 70 to 150 nm. The intracellular level of 5-DN increased 3-fold by co-incubation with the mixed micelle solution. Moreover, the basolateral level of 5-DN increased 3-fold due to enhanced chylomicron-mediated transport. Based on the above results, we then evaluate the influence of different fatty acid types on the properties of mixed micelles, cellular lipid droplets and CMs, and on the uptake of the highly lipophilic nutraceutical 5-DN. There were distinct differences in the structural properties of CMs formed depending on fatty acid unsaturation. Oleic acid (C18:1) was most effective at enhancing transport of 5-DN and led to the formation of the largest CMs. Linoleic acid (C18:2) and linolenic acid (C18:3) also promoted 5-DN incorporation into CMs, but they were less efficient than oleic acid. The metabolism of 5-DN within the epithelium cells was greatly reduced when they were incorporated into CMs, presumably because they were isolated from metabolic enzymes in the cytoplasm. These results have important implications for the design of lipid nanoparticle-based delivery systems for lipophilic drugs and nutraceuticals by targeting them to the lymphatic circulation. Fatherly, we studied the effects of triglycerides-based nanoemulsion delivery systems with different fatty acid chain lengths on the bioavailability 5-DN. 5-DN was encapsulated in medium chain triglycerides (MCT) or canola oil (long chain triglycerides, LCT) based nanoemulsion. They were subject to a simulated gastrointestinal digestion model. Finally, the mixed micelle phase was applied to Caco-2 monolayer cell model that mimics intestinal absorption. Higher bioaccessibility of 5-DN was found in MCT nanoemulsion than canola nanoemulsion, 13% vs.7% respectively. However, only 30% 5-DN crossed Caco-2 monolayer while half of them were metabolized for MCT nanoemulsion, up to 60% 5-DN and only 10% were metabolized in canola nanoemulsion. Results also demonstrated more lipid droplets and CMs were formed by canola nanoemulsion, which were responsible for transportation of 5-DN to the lymph. In conclusion, although for lipophilic components like 5-DN, relatively higher bioaccessibility can be achieved by MCT-based nanoemulsion, LCT-based emulsion was more potent in enhancing the bioavailability through increased lymphatic transport. Lipids especially the ones with polyunsaturated long chain fatty acids (PUFA) are very susceptible to oxidation. Ingestion of oxidized lipids is associated with all kinds of health risk: diabetes, tumor development and atherosclerosis. Meanwhile, the oxidation of lipids may affect the absorption of lipophilic bioactive components in foods. We compared the effect of oxidized and unoxidized PUFA, linoleic acid (LA) on the transport of the highly lipophilic compound 5-hydroxy 6,7,8,4' tetramethoxylflavone (5-DMT) by a Caco-2 cell model. Results turned out that unoxidized LA improved bioavailability of 5-DMT by stimulating CMs. Oxidized LA also showed an effect of improving transport of 5-DMT. However, it significantly affected the morphology of Caco-2 monolayer especially the tight junction. Accordingly, the transport pathway could be altered compared to the unoxidized LA, which will ultimately influence the distribution and metabolism fate of lipophilic components in the human body. Recently, the fate of inorganic nanoparticles in foods after ingestion has been attracted highly attention. Based on the above model and experimental methods, we also investigate the transport and toxicity of inorganic nanoparticle (AuNPs) on Caco-2 cell monolayer. AuNPs with different size (15nm, 50nm and 100nm) were applied. Our results demonstrated that more amount of gold was retained in the monolayer and higher toxicity was caused for larger size of AuNPs. Besides, mixed micelles greatly improve the secretion of AuNPs. The influence may be associated with formation abundant lipid droplets and CMs in the monolayer after fatty acids were taken in.

Edible Oleogels

Edible Oleogels PDF Author: Alejandro G. Marangoni
Publisher: Elsevier
ISBN: 163067009X
Category : Technology & Engineering
Languages : en
Pages : 350

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Book Description
In an effort to provide alternatives to trans and saturated fats, scientists have been busy modifying the physical properties of oils to resemble those of fats. In this fashion, many food products requiring a specific texture and rheology can be made with these novel oil-based materials without causing significant changes to final product quality. The major approach to form these materials is to incorporate specific molecules (polymers, amphiphiles, waxes) into the oil components that will alter the physical properties of the oil so that its fluidity will decrease and the rheological properties will be similar to those of fats. These new oilbased materials are referred to as oil gels, or “oleogels,“ and this emerging technology is the focus of many scientific investigations geared toward helping decrease the incidence of obesity and cardiovascular disease. Presents a novel strategy to eliminate trans fats from our diets and avoid excessive amounts of saturated fat by structuring oil to make it behave like crystalline fat Reviews recent advances in the structuring of edible oils to form new mesoscale and nanoscale structures, including nanofibers, mesophases, and functionalized crystals and crystalline particles Identifies evidence on how to develop trans fat free, low saturate functional shortenings for the food industry that could make a major impact on the health characteristics of the foods we consume