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International Journal of Molecular... Jan 2021(1) Background: Chiral nanoparticular systems have recently emerged as a compelling platform for investigating stereospecific behavior at the nanoscopic level. We...
(1) Background: Chiral nanoparticular systems have recently emerged as a compelling platform for investigating stereospecific behavior at the nanoscopic level. We describe chiroselective supramolecular interactions that occur between DNA oligonucleotides and chiral polyurea nanocapsules. (2) Methods: We employ interfacial polyaddition reactions between toluene 2,4-diisocyanate and lysine enantiomers that occur in volatile oil-in-water nanoemulsions to synthesize hollow, solvent-free capsules with average sizes of approximately 300 nm and neutral surface potential. (3) Results: The resultant nanocapsules exhibit chiroptical activity and interact differentially with single stranded DNA oligonucleotides despite the lack of surface charge and, thus, the absence of significant electrostatic interactions. Preferential binding of DNA on D-polyurea nanocapsules compared to their L-counterparts is demonstrated by a fourfold increase in capsule size, a 50% higher rise in the absolute value of negative zeta potential (ζ-potential), and a three times lower free DNA concentration after equilibration with the excess of DNA. (4) Conclusions: We infer that the chirality of the novel polymeric nanocapsules affects their supramolecular interactions with DNA, possibly through modification of the surface morphology. These interactions can be exploited when developing carriers for gene therapy and theranostics. The resultant constructs are expected to be highly biocompatible due to their neutral potential and biodegradability of polyurea shells.
Topics: Aptamers, Nucleotide; DNA; Drug Carriers; Emulsions; Humans; Nanocapsules; Oligonucleotides; Particle Size; Polymers
PubMed: 33430158
DOI: 10.3390/ijms22020584 -
BMC Pregnancy and Childbirth Feb 2024Local anaesthetic systemic toxicity (LAST) is a rare but life-threatening complication that can occur after local anaesthetic administration. Various clinical guidelines... (Review)
Review
BACKGROUND
Local anaesthetic systemic toxicity (LAST) is a rare but life-threatening complication that can occur after local anaesthetic administration. Various clinical guidelines recommend an intravenous lipid emulsion as a treatment for local anaesthetic-induced cardiac arrest. However, its therapeutic application in pregnant patients has not yet been established. This scoping review aims to systematically identify and map the evidence on the efficacy and safety of intravenous lipid emulsion for treating LAST during pregnancy.
METHOD
We searched electronic databases (Medline, Embase and Cochrane Central Register Controlled Trials) and a clinical registry (lipidrescue.org) from inception to Sep 30, 2022. No restriction was placed on the year of publication or the language. We included any study design containing primary data on obstetric patients with signs and symptoms of LAST.
RESULTS
After eliminating duplicates, we screened 8,370 titles and abstracts, retrieving 41 full-text articles. We identified 22 women who developed LAST during pregnancy and childbirth, all presented as case reports or series. The most frequent causes of LAST were drug overdose and intravascular migration of the epidural catheter followed by wrong-route drug errors (i.e. intravenous anaesthetic administration). Of the 15 women who received lipid emulsions, all survived and none sustained lasting neurological or cardiovascular damage related to LAST. No adverse events or side effects following intravenous lipid emulsion administration were reported in mothers or neonates. Five of the seven women who did not receive lipid emulsions survived; however, the other two died.
CONCLUSION
Studies on the efficacy and safety of lipids in pregnancy are scarce. Further studies with appropriate comparison groups are needed to provide more robust evidence. It will also be necessary to accumulate data-including adverse events-to enable clinicians to conduct risk-benefit analyses of lipids and to facilitate evidence-based decision-making for clinical practice.
Topics: Infant, Newborn; Female; Humans; Pregnancy; Anesthetics, Local; Fat Emulsions, Intravenous; Pregnant Women; Parturition; Lipids
PubMed: 38355477
DOI: 10.1186/s12884-024-06309-1 -
Nutrients Feb 2024The milk fat globule membrane (MFGM) is a thin film that exists within the milk emulsion, suspended on the surface of milk fat globules, and comprises a diverse array of... (Review)
Review
BACKGROUND
The milk fat globule membrane (MFGM) is a thin film that exists within the milk emulsion, suspended on the surface of milk fat globules, and comprises a diverse array of bioactive components. Recent advancements in MFGM research have sparked a growing interest in its biological characteristics and health-related functions. Thorough exploration and utilization of MFGM as a significant bioactive constituent in milk emulsion can profoundly impact human health in a positive manner. Scope and approach: This review comprehensively examines the current progress in understanding the structure, composition, physicochemical properties, methods of separation and purification, and biological activity of MFGM. Additionally, it underscores the vast potential of MFGM in the development of additives and drug delivery systems, with a particular focus on harnessing the surface activity and stability of proteins and phospholipids present on the MFGM for the production of natural emulsifiers and drug encapsulation materials.
KEY FINDINGS AND CONCLUSIONS
MFGM harbors numerous active substances that possess diverse physiological functions, including the promotion of digestion, maintenance of the intestinal mucosal barrier, and facilitation of nerve development. Typically employed as a dietary supplement in infant formula, MFGM's exceptional surface activity has propelled its advancement toward becoming a natural emulsifier or encapsulation material. This surface activity is primarily derived from the amphiphilicity of polar lipids and the stability exhibited by highly glycosylated proteins.
Topics: Infant; Humans; Emulsions; Glycolipids; Glycoproteins; Milk Proteins; Lipid Droplets; Emulsifying Agents
PubMed: 38474716
DOI: 10.3390/nu16050587 -
Human & Experimental Toxicology 2022The aim of this study was to examine the effects of lipid emulsions on carnitine palmitoyltransferase I (CPT-I), carnitine acylcarnitine translocase (CACT), carnitine...
The aim of this study was to examine the effects of lipid emulsions on carnitine palmitoyltransferase I (CPT-I), carnitine acylcarnitine translocase (CACT), carnitine palmitoyltransferase II (CPT-II), and the mitochondrial dysfunctions induced by toxic doses of local anesthetics in H9c2 rat cardiomyoblasts. The effects of local anesthetics and lipid emulsions on the activities of CPT-I, CACT, and CPT-II, and concentrations of local anesthetics were examined. The effects of lipid emulsions, N-acetyl-L-cysteine (NAC), and mitotempo on the bupivacaine-induced changes in cell viability, reactive oxygen species (ROS) levels, mitochondrial membrane potential (MMP), and intracellular calcium levels were examined. CACT, without significantly altering CPT-I and CPT-II, was inhibited by toxic concentration of local anesthetics. The levobupivacaine- and bupivacaine-induced inhibition of CACT was attenuated by all concentrations of lipid emulsion, whereas the ropivacaine-induced inhibition of CACT was attenuated by medium and high concentrations of lipid emulsion. The concentration of levobupivacaine was slightly attenuated by lipid emulsion. The bupivacaine-induced increase of ROS and calcium and the bupivacaine-induced decrease of MMP were attenuated by ROS scavengers NAC and mitotempo, and the lipid emulsion. Collectively, these results suggested that the lipid emulsion attenuated the levobupivacaine-induced inhibition of CACT, probably through the lipid emulsion-mediated sequestration of levobupivacaine.
Topics: Anesthetics, Local; Animals; Bupivacaine; Carnitine Acyltransferases; Emulsions; Enzyme Inhibitors; Levobupivacaine; Male; Myoblasts, Cardiac; Rats; Ropivacaine
PubMed: 35135371
DOI: 10.1177/09603271211065978 -
Food & Function Apr 2021In this study, β-carotene loaded oil-in-water emulsions were stabilized by complex interfaces composed of propylene glycol alginate (PGA), rhamnolipids (Rha), and zein...
In this study, β-carotene loaded oil-in-water emulsions were stabilized by complex interfaces composed of propylene glycol alginate (PGA), rhamnolipids (Rha), and zein colloidal particles (ZCPs). The influence of mixed biopolymer-surfactant, biopolymer-particle, surfactant-particle and biopolymer-surfactant-particle interfaces on the performance of the emulsions was investigated. The stability, microstructure, rheological properties, and in vitro gastrointestinal digestion of the emulsions were controlled by regulating the adding sequence and mass ratio of the multiple stabilizers. The droplet size of the emulsion was in the range of 14-77 μm. After encapsulation into the emulsions stabilized by the complex interfaces, the photothermal stability of β-carotene were increased by 41.53% and 21.52%, respectively. The co-existence of particles, biopolymers, and surfactants could induce competitive displacement, multilayer deposition and an interparticle network at the interface. Compared with a single PGA- or Rha-stabilized emulsion, the complex interface-stabilized emulsion reduced the release of FFA by 28.06% and 26.16%, respectively. The interfacial composition of the emulsion and the delayed lipid digestion further affected the bioaccessibility of β-carotene in the gastrointestinal tract (GIT). The mixed biopolymer-particle-surfactant interface-stabilized emulsion could be incorporated in foods, pharmaceuticals and cosmetics for excellent stability, targeted nutrient delivery and controlled lipolysis.
Topics: Biological Availability; Biopolymers; Digestion; Drug Stability; Elasticity; Emulsions; Gastrointestinal Tract; Microscopy, Electron, Scanning; Particle Size; Pepsin A; Surface-Active Agents; Viscosity; Zein; beta Carotene
PubMed: 33877248
DOI: 10.1039/d0fo02975k -
Journal of Colloid and Interface Science Nov 2023Pharmaceutical formulation of oral dosage forms is continuously challenged by the low solubility of new drug candidates. Pickering emulsions, emulsions stabilized with...
Pharmaceutical formulation of oral dosage forms is continuously challenged by the low solubility of new drug candidates. Pickering emulsions, emulsions stabilized with solid particles, are a promising alternative to surfactants for developing long-term stable emulsions that can be tailored for controlled release of lipophilic drugs. In this work, a non-emulsifying lipid-based formulation (LBF) loaded with fenofibrate was formulated into an oil-in-water (O/W) emulsion synergistically stabilized by stearic acid and silica (SiO) nanoparticles. The emulsion had a droplet size of 341 nm with SiO particles partially covering the oil-water interface. In vitro lipid digestion was faster for the emulsion compared to the corresponding LBF due to the larger total surface area available for digestion. Cellulose biopolymers were added to the emulsion to produce a gel for semi-solid extrusion (SSE) 3D printing into tablets. The emulsion gel showed suitable rheological attributes for SSE, with a trend of higher viscosity, yield stress, and storage modulus (G'), compared to a conventional self-emulsifying lipid-based emulsion gel. The developed emulsion gel allows for a non-emulsifying LBF to be transformed into solid dosage forms for rapid lipid digestion and drug release of a poorly water-soluble drug in the small intestine.
Topics: Surface-Active Agents; Emulsions; Silicon Dioxide; Lipids; Nanoparticles; Water
PubMed: 37478742
DOI: 10.1016/j.jcis.2023.07.055 -
European Journal of Pharmaceutics and... Jan 2022Core-shell microspheres hold great promise as a drug delivery system because they offer several benefits over monolithic microspheres in terms of release kinetics, for... (Review)
Review
Core-shell microspheres hold great promise as a drug delivery system because they offer several benefits over monolithic microspheres in terms of release kinetics, for instance a reduced initial burst release, the possibility of delayed (pulsatile) release, and the possibility of dual-drug release. Also, the encapsulation efficiency can significantly be improved. Various methods have proven to be successful in producing these core-shell microspheres, both the conventional bulk emulsion solvent evaporation method and methods in which the microspheres are produced drop by drop. The latter have become increasingly popular because they provide improved control over the particle characteristics. This review assesses various production methods for core-shell microspheres and summarizes the characteristics of formulations prepared by the different methods, with a focus on their release kinetics.
Topics: Delayed-Action Preparations; Drug Compounding; Drug Delivery Systems; Drug Liberation; Emulsions; Kinetics; Microspheres; Particle Size; Polymers
PubMed: 34861359
DOI: 10.1016/j.ejpb.2021.11.007 -
Ultrasonics Sonochemistry Mar 2023A lysozyme-oregano essential oil (Lys-OEO) antibacterial emulsion was developed via ultrasonic treatment. Based on the general emulsion materials of ovalbumin (OVA) and...
A lysozyme-oregano essential oil (Lys-OEO) antibacterial emulsion was developed via ultrasonic treatment. Based on the general emulsion materials of ovalbumin (OVA) and inulin (IN), the addition of Lys and OEO successfully inhibited the growth of E. coli and S. aureus, two representatives of which were Gram-negative and Gram-positive bacteria respectively. The emulsion system in this study was designed to compensate for the limitation that Lys could only act on Gram-positive bacteria, and the stability of the emulsion was improved using ultrasonic treatment. The optimal amounts among OVA, Lys and OEO were found to be the mass ratio of 1:1 (Lys to OVA) and 20% (w/w) OEO. The ultrasonic treatment at the power of 200, 400, 600, and 800 W and time length of 10 min improved the stability of emulsion, in which the surface tension was below 6.04 mN/m and the Turbiscan stability index (TSI) did not exceed 10. The multiple light scattering showed that sonicated emulsions were less prone to delamination; salt stability and pH stability of emulsions were improved, CLSM image showed emulsion as oil-in-water type. In the meantime, the particles of the emulsions were found to become smaller and more uniform with ultrasonic treatment. The best dispersion and stability of the emulsion were both achieved at 600 W with a zeta potential of 7.7 mV, the smallest particle size and the most uniform particle distribution.
Topics: Oils, Volatile; Emulsions; Origanum; Muramidase; Escherichia coli; Staphylococcus aureus; Particle Size; Anti-Bacterial Agents; Water
PubMed: 36871524
DOI: 10.1016/j.ultsonch.2023.106348 -
European Journal of Pharmaceutical... Aug 2022Intranasally administered non-steroidal anti-inflammatory drugs (NSAIDs) offer an innovative opportunity in the field of pain management. Combination of the nasal...
Intranasally administered non-steroidal anti-inflammatory drugs (NSAIDs) offer an innovative opportunity in the field of pain management. Combination of the nasal physiological advantages such as the rich vascularization and large absorption area along with novel nanomedical formulations can fulfill all the necessary criteria of an advanced drug delivery system. Nanoemulsions represent a versatile formulation approach suitable for nasal drug delivery by increasing the absorption and the bioavailability of many drugs for systemic and nose-to-brain delivery due to their stability, small droplet size and optimal solubilization properties. In this study we aimed to develop meloxicam (MX)-loaded mucoadhesive nanoemulsions and to investigate the nasal applicability of the optimized formulations. Our results indicated the optimized nanoemulsion formulation (MX-NE3) had a droplet size of 158.5 nm in monodisperse droplet size distribution (polydispersity index of 0.211). The surface charge was -11.2 mV, which helped with the colloidal stability upon dilution at simulated nasal conditions and storage. The high encapsulation efficiency (79.2%) mediated a 15-fold drug release and a 3-fold permeability increase at nasal conditions compared to the initial MX. Proper wetting properties associated with high mucoadhesion prosper the increased residence time on the surface of the nasal mucosa. No cytotoxic effect of the formulations was observed on NIH/3T3 mouse embryonic fibroblast cell lines, which supports the safe nasal applicability.
Topics: Administration, Intranasal; Animals; Drug Delivery Systems; Emulsions; Fibroblasts; Meloxicam; Mice; Nasal Mucosa; Particle Size
PubMed: 35662634
DOI: 10.1016/j.ejps.2022.106229 -
Journal of Ocular Pharmacology and... May 2023Prostaglandin analogue topical medications are one of the most effective therapeutic approaches for the chronic management of glaucoma and ocular hypertension, through... (Review)
Review
Prostaglandin analogue topical medications are one of the most effective therapeutic approaches for the chronic management of glaucoma and ocular hypertension, through the reduction of elevated intra ocular pressure (IOP). While many of the first generations of anti-glaucoma eye drops were preserved with benzalkonium chloride, their repeated use may induce chronic ocular surface toxicity that leads to ocular surface disease (OSD) signs and symptoms. As a result, soft-preservatives and preservative-free formulations have been developed with the goal to avoid the long-term iatrogenic toxicity of the preservative agents. In addition, it has been suggested that OSD and its associated inflammation may negatively impact the efficacy of the IOP-lowering medications, including treatment adherence and compliance. Hence, it may be particularly interesting that glaucoma medications can concomitantly protect and "heal" the ocular surface and its environment while lowering elevated IOP, for the greater benefit of glaucoma patients. The objective of the present review is to briefly present the preclinical data of the cationic oil-in-water emulsion of latanoprost (latanoprost-CE) to shed some light on its mechanisms of action. It overall supports the following hypothesis: the restoration of a healthy ocular surface environment and treatment of the OSD signs and symptoms will allow for an improved elevated IOP reduction and glaucoma management. This would be achieved with a once daily dosing regimen to preserve glaucoma patients' vision, ocular surface, and quality-of-life and wellness.
Topics: Humans; Latanoprost; Glaucoma, Open-Angle; Emulsions; Intraocular Pressure; Prostaglandins F, Synthetic; Antihypertensive Agents; Glaucoma; Ocular Hypertension; Ophthalmic Solutions; Preservatives, Pharmaceutical
PubMed: 37015075
DOI: 10.1089/jop.2022.0155