Preparation of Solid Lipid Nanoparticle-Containing Ovalbumin Based Reverse Micelle-Double Emulsion Technique (original) (raw)
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International Journal of Pharmaceutics, 2010
Phase inversion temperature PIT method Low-energy method Hydrophilic material a b s t r a c t This study presents novel, recently patented technology for encapsulating hydrophilic species in lipid nano-emulsions. The method is based on the phase-inversion temperature method (the so-called PIT method), which follows a low-energy and solvent-free process. The nano-emulsions formed are stable for months, and exhibit droplet sizes ranging from 10 to 200 nm. Hydrophilic model molecules of fluorescein sodium salt are encapsulated in the oily core of these nano-emulsion droplets through their solubilisation in the reverse micellar system. As a result, original, multi-scaled nano-objects are generated with a 'hydrophilic molecule in a reverse-micelles-in-oil-in-water' structure. Once fluorescein has been encapsulated it remains stable, for thermodynamic reasons, and the encapsulation yields can reach 90%. The reason why such complex objects can be formed is due to the soft method used (PIT method) which allows the conservation of the structure of the reverse micelles throughout the formulation process, up to their entrapment in the nano-emulsion droplets. In this study, we focus the investigation on the process itself, revealing its potential and limits. Since the formulation of nanocarriers for the encapsulation of hydrophilic substances still remains a challenge, this study may constitute a significant advance in this field.
Protein entrapment in PEGylated lipid nanoparticles
International journal of pharmaceutics, 2013
Defining appropriate delivery strategies of therapeutic proteins, based on lipid nanoparticulate carriers, requires knowledge of the nanoscale organization that determines the loading and release properties of the nanostructured particles. Nanoencapsulation of three cationic proteins (human brain-derived neurotrophic factor (BDNF), α-chymotrypsinogen A, and histone H3) was investigated using anionic nanoparticle (NP) carriers. PEGylated lipid NPs were prepared from self-assembled liquid crystalline phases involving monoolein and eicosapentaenoic acid. Inclusion of the antioxidant α-tocopherol favoured the preparation of stealth hexosome carriers. The purpose of the present work is to reveal the structural features of the protein-loaded lipid nanocarriers by means of high resolution small-angle X-ray scattering (SAXS) and cryogenic transmission electron microscopy (cryo-TEM). The obtained results indicate that protein entrapment is concentration-dependent and may significantly modify...
Bulletin of University of Agricultural Sciences and Veterinary Medicine Cluj-Napoca. Food Science and Technology
Lipid nanoparticles are getting a growing scientific and technological interest, worldwide. Either Solid Lipid Nanoparticles (SLNs), Nanostructured Lipid Carriers (NLCs), Lipid Drug Conjugates (LDCs) or Polymer-Lipid Nanoparticles (PLNs) have been produced and investigated last years, being reccomended as emerging carrier systems for many food and biomedical applications. An overview of the last publications, mainly since 2017 is presented, underlying the most important methods and techniques used for their preparation (e.g. high shear homogenization in hot and cold conditions, ultrasound assisted melt emulsification) as well techniques applied for measuring the size, calorimetric properties, zeta-potential, etc. Most relevant data related to the use of food-grade ingredients and designed lipid nanoparticles as delivery systems for organic and inorganic bioactive molecules in food or packaging’s are presented. The major reason for this trend in food science is the aim to overcome pr...
Development of double emulsion nanoparticles for the encapsulation of bovine serum albumin
Colloids and surfaces. B, Biointerfaces, 2017
In the present work, a double emulsion was developed for the encapsulation of Bovine Serum Albumin (BSA) as a model protein for the future encapsulation of viral proteins. The first emulsion polydispersity index (PDI) was studied with increasing concentrations of poly (ε-caprolactone) (PCL) as stabilizer (from 16% w/v to 5% w/v) and polyvinyl alcohol (PVA) as the surfactant in the second emulsion at 1.5% w/v. Results suggest that at decreasing concentrations of PCL the PDI of the emulsion also decrease, indicating that viscosity of the emulsion is crucial in the homogeneity of the resultant size distribution of the nanoparticles. When PVA concentration in the second emulsion was increased from 1.5% w/v to 2.5% w/v the PDI also increased. To study the relationship between the structure of the surfactant in the second emulsion and the resultant BSA encapsulation, emulsions were prepared with Pluronic F68 and PVA both at 1.5% w/v and PCL in the first emulsion at 5% w/v. Results indicat...
Lipogels for Encapsulation of Hydrophilic Proteins and Hydrophobic Small Molecules
Biomacromolecules, 2018
Lipid-polymer hybrid materials have the potential to exhibit enhanced stability and loading capabilities in comparison to parent liposome or polymer materials. However, complexities lie in formulating and characterizing such complex nanomaterials. Here we describe a lipid-coated polymer gel (lipogel) formulated using a single-pot methodology, where self-assembling liposomes template a UV-curable polymer gel core. Using fluorescently labeled lipids, protein, and hydrophobic molecules, we characterized their formation, purification, stability, and encapsulation efficiency via common instrumentation methods such as dynamic light scattering (DLS), matrix-assisted laser desorption ionization-mass spectrometry (MALDI-MS), UV-vis spectroscopy, fluorescence spectroscopy, and single-particle total internal reflection fluorescence (TIRF) microscopy. In addition, we confirmed that these dual-guest-loaded lipogels are stable in solution for several months. The simplicity of this complete aqueou...
Procedia Food Science, 2011
Eight oil-in-water emulsions were prepared using melt high-pressure homogenisation (HPH) at 300 or 1200 Bar. The emulsions produced from lipid phase (20%) were composed by palm oil alone or in mixture with α-tocopherol at 4:1 weight ratio, and an aqueous phase containing whey proteins alone or in mixture with phospholipids. The resulting nanoemulsions (fat droplet size ranging from 200-500 nm) presented different stability against aggregation and coalescence, fat crystallinity and polymorphisms in relation to different degrees of α-tocopherol encapsulation and protection against chemical degradation. Protein stabilised emulsions were monomodal, while emulsions stabilised by proteins and lecithins were slightly bimodal. Application of an isothermal treatment (4°C for 2 hours) to these emulsions showed crystallization peaks located at longer time values in smaller particle size emulsions, while in the presence of added α-tocopherol average particle size values were higher and crystallization was not observed in 2 hours storage. Study of fat polymorphisms performed after 12 hours storage at 4°C revealed the formation of 2L structures with coexistence of α, β' and β forms in all of the emulsions. Increasing HPH from 300 to 1200 Bar favoured development of β structure (4.5 A -1 ) in α-tocopherol added emulsions, with the presence of one extra peak β structure evolved at 3.9 A -1 only in emulsions containing lecithins. α-tocopherol addition decreased in 2L structures (by approx. 40-50 %). The formation of lipid nanoparticles with decreasing size values (increasing HPH parameters) was accompanied by increased long-term stability against aggregation and coalescence, but increased vitamin degradation (up to 15 wt% for 1200 bar). Degradation of α-tocopherol after 2 months storage at 4°C was lower for nanoparticles stabilised by whey proteins alone (21 and 33%, respectively) than for nanoparticles stabilised by whey proteins in mixture with phospholipids and presenting higher size values (44 and 52 %, respectively), where β polymorphs were more evolved.
Journal of Nanomedicine & Nanotechnology, 2015
Hydrophobic ion-pairing (HIP) complexation-based approach has been employed to reduce aqueous solubilities of peptide and protein drugs. The solubility of a protein molecule is due to presence of charged amino acids present on the surface. HIP complexation is a technique to complex ionizable functional groups of protein and peptide molecules with oppositely charged functional groups of a complex forming agent. The main objective of this study was to formulate and evaluate HIP complexes of lysozyme with sodium dodecyl sulfate (SDS) as an ion paring agent. Results of % binding effciency shown that the formation of HIP complexes were dependent on pH of lysozyme solution and molar ratio of lysozyme to SDS. Aqueous solubilities of HIP complexes were very low compared to lysozyme alone. The e¬ffect of HIP complexation on enzymatic activity of lysozyme was also studied. Further, lipid-polymer hybrid nanoparticles (LPNs) loaded with lysozyme and lysozyme:SDS HIP complex were prepared by using a solid-in-oil-in-water (s/o/w) emulsion solvent evaporation method and characterised with respect to morphology, size and encapsulation efficiency. We observed significant improvement in encapsulation efficiency for lysozyme:SDS HIP complex-loaded LPNs. This study demonstrates a novel approach of formulating protein-loaded nanoparticles which can also be employed for delivery of proteins.
Preparation of a novel lipid-core micelle using a low-energy emulsification method
Drug delivery and translational research, 2018
High-energy methods for the manufacturing of nanomedicines are widely used; however, interest in low-energy methods is increasing due to their simplicity, better control over the process, and energy-saving characteristics during upscaling. Here, we developed a novel lipid-core micelle (LCM) as a nanocarrier to encapsulate a poorly water-soluble drug, nifedipine (NFD), by hot-melt emulsification, a low-energy method. LCMs are self-assembling colloidal particles composed of a hydrophobic core and a hydrophilic shell. Hybrid materials, such as Gelucire 44/14, are thus excellent candidates for their preparation. We characterized the obtained nanocarriers for their colloidal properties, drug loading and encapsulation efficiency, liquid state, stability, and drug release. The low-energy method hot-melt emulsification was successfully adapted for the manufacturing of small and narrowly dispersed LCMs. The obtained LCMs had a small average size of ~ 11 nm and a narrow polydispersity index (...
Solid Lipid Nanoparticles – a Brief Review
Nanotechnology opens up new vistas of research in the development of novel drug delivery systems. These colloidal nanoparticles based on biodegradable and biocompatible polymeric systems have largely influenced the controlled and targeted drug delivery aspects. Nanoparticles loaded bioactive not only deliver the drugs to the specific organs within the body but the delivery rate in addition can be controlled as being bystanders, burst controlled, pulsatile and modulated. Many leading small molecule drugs are lipophilic. Lipophiles, or poorly water soluble molecules, play a very important, beneficial role in numerous biological processes. A novel pharmaceutical, applications of lipophilic compounds have been demonstrated by scientists and, more research effort is focused to develop novel approaches that utilize Lipophiles to overcome most challenging pharmaceutical issues as they increasingly discover Lipophiles' diverse capabilities in biological processes. Lipophilic delivery is a challenging in a venue of the pharmaceutical sciences. Upon introduction to aqueous biological environments, lipophilic molecules exhibit instability, food interactions, reduced bioavailability, non-specific targeting, and toxic effects that produce undesired immunogenic responses and reduced efficacy, So the Lipophiles must be formulated and delivered in a safe, efficacious, and cost effective manner. 40% of all poorly water soluble drug candidates and are abandoned due to solubility, stability, and delivery issues.
Formulation of solid lipid nanoparticles and their applications.
Solid lipid nanoparticles (SLN) introduced in 1991 represent an alternative carrier system to traditional colloidal carriers, such as emulsions, liposomes and polymeric micro-and nanoparticles. 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. SLN combine advantages of the traditional systems but avoid some of their major disadvantages. 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. Due to their unique size-dependent properties, lipid nanoparticles offer the possibility to develop new therapeutics. 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. The ability to incorporate drugs into nanocarriers offers a new prototype in drug delivery that could be used for secondary and tertiary levels of drug targeting. This review mainly focuses on the advantages and limitations of the solid lipid nanoparticles over other colloidal carriers and different techniques available for the formulation of SLNs and their applications in therapeutics.