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International Journal of Biological... Jul 2023Pickering emulsions represent a promising avenue in the field of controlled drug delivery systems. Recently, cellulose nanofibers (CNFs) and chitosan nanofibers (ChNFs)...
Pickering emulsions represent a promising avenue in the field of controlled drug delivery systems. Recently, cellulose nanofibers (CNFs) and chitosan nanofibers (ChNFs) have gained interest as eco-friendly stabilizers for Pickering emulsions, yet their application in pH-responsive drug delivery systems remains unexplored. However, the potential of these biopolymer complexes in formulating stable, pH-responsive emulsions for controlled drug release is of significant interest. Here, we show the development of a highly stable, pH-responsive fish oil-in-water Pickering emulsion stabilized by ChNF/CNF complexes, with optimal stability achieved at a 0.2 wt% ChNF concentration and an average emulsion particle size of approximately 4 μm. Our results demonstrate long-term stability (16 days of storage) for ChNF/CNF-stabilized emulsions, with the interfacial membrane's pH modulation facilitating controlled, sustained ibuprofen (IBU) release. Furthermore, we observed a remarkable release of approximately 95 % of the embedded IBU within the pH range of 5-9, while the drug loading and encapsulation efficiency of the drug-loaded microspheres reached their peak at a 1 % IBU dosage, with values of 1 % and 87 %, respectively. This study highlights the potential of using ChNF/CNF complexes in designing versatile, stable, and entirely renewable Pickering systems for controlled drug delivery, with potential applications in food and eco-friendly products.
Topics: Cellulose; Emulsions; Ibuprofen; Water; Hydrogen-Ion Concentration; Particle Size
PubMed: 37210059
DOI: 10.1016/j.ijbiomac.2023.124942 -
Journal of Colloid and Interface Science Mar 2016Because the size, size distribution, and concentration of emulsions play an important role in most of the applications, controlled emulsion generation and effective...
Because the size, size distribution, and concentration of emulsions play an important role in most of the applications, controlled emulsion generation and effective concentration are of great interest in fundamental and applied studies. While microfluidics has been demonstrated to be able to produce emulsion drops with controlled size, size distribution, and hierarchical structures, progress of controlled generation of concentrated emulsions is limited. Here, we present an effective microfluidic emulsion generation system integrated with an orifice structure to separate aqueous droplets from the continuous oil phase, resulting in concentrated emulsion drops in situ. Both experimental and simulation results show that the efficiency of separation is determined by a balance between pressure drop and droplet accumulation near the orifice. By manipulating this balance via changing flow rates and microfluidic geometry, we can achieve monodisperse droplets on chip that have a concentration as high as 80,000 drops per microliter (volume fraction of 66%). The present approach thus provides insights to the design of microfluidic device that can be used to concentrate emulsions (drops and bubbles), colloidal particles (drug delivery polymer particles), and biological particles (cells and bacteria) when volume fractions as high as 66% are necessary.
Topics: Emulsions; Microfluidic Analytical Techniques; Oils; Particle Size; Surface Properties; Water
PubMed: 26722797
DOI: 10.1016/j.jcis.2015.12.032 -
AAPS PharmSciTech Apr 2022Lovastatin (Lov) is a lipid-lowering agent, with 5% bioavailability (BA) due to extensive first pass metabolism and poor solubility. To enhance dissolution and in vivo...
Design and Development of Solid SMEDDS and Liquisolid Formulations of Lovastatin, for Improved Drug Dissolution and In vivo Effects-a Pharmacokinetic and Pharmacodynamic Assessment.
Lovastatin (Lov) is a lipid-lowering agent, with 5% bioavailability (BA) due to extensive first pass metabolism and poor solubility. To enhance dissolution and in vivo effects, Lov solid self microemulsifying drug delivery system (SMEDDS) and liquisolid systems were developed and evaluated to select superior one. Solubilities were determined in oils, surfactants, and cosurfactants. Ternary phase diagrams were constructed and selected the one which showed maximum emulsion zone. In vitro dissolution, DSC, SEM and PXRD studies were used to characterize the developed formulations. In vivo studies were conducted on optimal formulations in wistar rats. Based on solubilities, Capmul PG8 and Capmul MCM were preferred as oils, Labrasol and Transcutol P as surfactant and cosurfactant. Here, Syloid XDP carrier showed better adsorption capacity among others, hence was used in optimal solid SMEDDS (SX) and liquisolid (LS) formulations. Dissolution study results showed significant improvement in release when compared to pure drug. DSC, SEM, and PXRD results indicated the loss of drug crystallinity in optimal formulations. In pharmacokinetic (PK) study, SX and LS showed 2.57 and 1.43 fold improvements in AUC, when compared to that of coarse suspension (CS). In pharmacodynamic (PD) study, hyperlipidemia was induced by Triton X-100. CS and LS treatments showed a decline in hyperlipidemic levels at 4 h. But, SX-treated group showed early onset of decline at 2 h. Further, the duration of anti-hyperlipidemia was at least 12 h extra when compared to CS and LS. This study confirmed the superiority of SX over LS in PK and PD effects.
Topics: Administration, Oral; Animals; Biological Availability; Drug Delivery Systems; Drug Liberation; Emulsions; Excipients; Lovastatin; Oils; Rats; Solubility; Surface-Active Agents; Suspensions
PubMed: 35460060
DOI: 10.1208/s12249-022-02272-2 -
International Journal of Biological... Jul 2023Although various researches evaluated the stability and drug loading efficiency of chitosan Pickering emulsion, few studies assessed the role and mechanism of emulsions...
Pickering emulsion stabilized by parasin I and chitosan nanoparticles enhances protection against intestinal microbiota homeostasis by reducing inflammation in peritonitis mice.
Although various researches evaluated the stability and drug loading efficiency of chitosan Pickering emulsion, few studies assessed the role and mechanism of emulsions in gut flora homeostasis. Thus, in the basics of our previously published natural and antimicrobial Pickering emulsions, the function of emulsion on the intestinal microbiota and inflammation response was explored in Kunming mice with peritonitis. The results showed that lipid/peptide nanoparticles emulsion (LPNE) and the chitosan peptide-embedded nanoparticles emulsion (CPENE) presented less collagen fiber than parasin I in peritoneal tissue, and CPENE could reduce peritoneal inflammation by decreasing the expression of NOD-, LRR- and pyrin domain-containing protein 3 (NLRP3). The CPENE showed better histological morphology with a smaller fibrosis area in the spleen. Moreover, CPENE, LPNE, and parasin I-conjugated chitosan nanoparticle emulsion (PCNE) groups can increase the abundance of ABC transporters, DNA repair, and recombination proteins, and improve gut microbial. Furthermore, the Pickering emulsion showed a better protection effect on the composition and function of intestinal microbiota by decreasing interleukin-1β secretion and assembly of the inflammasome of NLRP3. These results could provide evidence for intestinal microbiota homeostasis of chitosan Pickering emulsion in inflammation-related diseases.
Topics: Mice; Animals; Emulsions; Gastrointestinal Microbiome; Chitosan; NLR Family, Pyrin Domain-Containing 3 Protein; Mice, Inbred NOD; Peritonitis; Inflammation; Nanoparticles; Particle Size
PubMed: 37263085
DOI: 10.1016/j.ijbiomac.2023.125016 -
AAPS PharmSciTech Apr 2020In the presented study, insight into the development and optimisation of the dry emulsion formulation and spray drying process is provided. The aim was to facilitate the...
In the presented study, insight into the development and optimisation of the dry emulsion formulation and spray drying process is provided. The aim was to facilitate the dissolution of the poorly soluble, highly lipophilic drug, simvastatin, by forming spray-dried dry emulsion particles having adequate powder flow properties, while assuring sufficient drug content. Simvastatin and a mixture of caprylic, capric triglyceride and 1-oleoyl-rac-glycerol were employed as a model drug and solubilising oils, respectively. A matrix of the dry emulsions was composed at a fixed ratio mixture of mannitol and HPMC. Tween 20 was used in low amounts as the primary emulsion stabiliser. To facilitate process optimisation, a DoE surface response design was used to study the influence of formulation and process parameters on the particle size distribution, powder bulk properties, emulsion reconstitution ability, drug stability and process yield of spray-dried products. Two-fluid nozzle geometry was identified, studied and confirmed to be important for most product critical quality attributes. Models obtained after the study showed acceptable coefficients of determination and provided good insight in the relationship governing the process and product characteristics. Five model optimised products showed adequate process yield, suitable particle size distribution, good reconstitution ability and improved dissolution profile, when compared to a non-lipid-based tablet and the pure drug. However, the obtained dry emulsion powders exhibited poor flow character according to the Carr index. The optimised product was further analysed with NMR during lipolysis to gain insight into the species formed during digestion and the kinetics of their formation.
Topics: Chemical Phenomena; Desiccation; Drug Delivery Systems; Drug Stability; Emulsions; Glycerides; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Particle Size; Polysorbates; Simvastatin; Solubility; Tablets; Technology, Pharmaceutical
PubMed: 32318974
DOI: 10.1208/s12249-020-01651-x -
AAPS PharmSciTech Dec 2022Essential oils consist of oxygenated structures of secondary metabolites of aromatic plants with anti-psoriatic activities. Tea tree oil (TTO) is an essential oil with...
Essential oils consist of oxygenated structures of secondary metabolites of aromatic plants with anti-psoriatic activities. Tea tree oil (TTO) is an essential oil with good anti-microbial and anti-inflammatory properties, exhibiting reduced levels of IL-1, IL-8, and PGE 2. Thymoquinone (TMQ) is popular herb in traditional medicine with known therapeutic benefits in several diseases and ailments. The ternary phase diagram was prepared with the weight ratio of S (Tween® 80:Labrasol®): oil:water ratio for o/w emulsion preparation. The globule size was 16.54 ± 0.13 nm, and PDI around 0.22 ± 0.01 of the TTO-TMQ emulsion and found thermodynamically stable. The percentage drug content was found in the range of 98.97 ± 0.62 to 99.45 ± 0.17% with uniformity of the ThymoGel using Carbopol®. The extensive physicochemical properties were studied using different analytical techniques, and in vitro drug release was performed using Franz-diffusion apparatus. Anti-psoriatic activity of the formulations was studied using Imiquimod-induced psoriasis-like inflammation model in male Balb/c mice and parameters like PASI score, ear thickness, and spleen to body weight index were determined as well as histological staining, ELISA, skin compliance, and safety evaluation of TTO were performed. The combination of essential oils with TMQ shows synergistic activity and efficiently reduces the psoriasis disease condition.
Topics: Mice; Animals; Oils, Volatile; Emulsions; Skin; Psoriasis; Tea Tree Oil
PubMed: 36550259
DOI: 10.1208/s12249-022-02482-8 -
Current Drug Delivery 2016Colloidal systems are most prominent delivery systems mainly used as vehicles for the transportation, targeting the various types of biomolecules, proteins, peptides,... (Review)
Review
BACKGROUND
Colloidal systems are most prominent delivery systems mainly used as vehicles for the transportation, targeting the various types of biomolecules, proteins, peptides, synthetic medicinal agents.
OBJECTIVE
To provide concise information on patents that are directly or indirectly related to the nanoemulsions.
METHODS
The ample of research work going on with such system, in which small insoluble particle/droplets are dispersed within the immiscible secondary liquid referred to as continuous phase, is enormous. A highly praised colloidal system is nanoemulsion which possesses 'nano' sized droplets of one phase dispersed within second continuous phase.
RESULTS
The characteristic features of nanoemulsion are their optical clarity, clear or bluish tint appearance and small globule size (20-200 nm) which makes them insensitive to gravitational instability, dilution and temperature. Above of all, achieving said properties using lower surfactant concentration and by supplying external energy differentiate them from microemulsion, which uses higher amount of surfactant thereby making them toxic for human body. Due to such variable advantages, researchers are engaged in going for the protecting their ideas in nanoemulsions by filling various patents.
CONCLUSION
Patents in this review, covers various areas (types of drug delivery and applications) where nanoemulsion are used. Literature revealed that filing of patents on nanoemulsion increased tremendously during last 5 years and will increase in upcoming time as 21st century will be called as the century of nanomedicine.
Topics: Cosmetics; Drug Administration Routes; Drug Delivery Systems; Drug Stability; Emulsions; Humans; Nanoparticles; Patents as Topic
PubMed: 26324230
DOI: 10.2174/1567201812666150901111930 -
International Journal of Pharmaceutics Jan 2023Drug-loaded emulsions for spray drying should be optimised for their rheological behaviour and stability under operating conditions, as this is essential for achieving...
Drug-loaded emulsions for spray drying should be optimised for their rheological behaviour and stability under operating conditions, as this is essential for achieving the desired physicochemical properties of the final dry product. Our aim was therefore to investigate the structure and stability of a water-in-oil (W/O) emulsion containing vancomycin hydrochloride as the active ingredient in the aqueous phase, poly(d,l-lactide-co-glycolide) as the structural polymer in the dichloromethane-based organic phase, and various stabilisers using low-field nuclear magnetic resonance (LF NMR) and rheological characterisation. Four emulsions were tested, namely-one without stabiliser, one with Poloxamer® 407, one with chitosan and Span™ 80 and one with chitosan only. The theoretical interpretation of the rheological data allowed the determination of the velocity and the shear rate/stress profiles inside the feed path of the W/O emulsion, aspects that are critical for the industrial scale-up of the emulsion drying process. In addition, LF NMR demonstrated that shaking was sufficient to restore the original emulsion structure and that the droplet size of all emulsions was in the range of 1-10 μm, although the emulsion with chitosan had the narrowest droplet size distribution and the higher zero shear viscosity, which accounts for the increased long-term stability due to impeded droplets movement.
Topics: Water; Polylactic Acid-Polyglycolic Acid Copolymer; Emulsions; Spray Drying; Chitosan; Magnetic Resonance Spectroscopy; Rheology; Particle Size
PubMed: 36509222
DOI: 10.1016/j.ijpharm.2022.122471 -
International Journal of Pharmaceutics Mar 2015Pain accompanying intravenous injections of propofol is a major problem in anesthesia. Pain is ascribed to the interaction of propofol with the local vasculature and...
PURPOSE
Pain accompanying intravenous injections of propofol is a major problem in anesthesia. Pain is ascribed to the interaction of propofol with the local vasculature and could be impacted by rapid dissolution of the emulsion formulation to release the drug. In this paper, we measure the dissolution of propofol emulsions including the commercial formulation Diprivan(®).
METHODS
We image the turbidity of blood protein sink solutions after emulsions are injected. The images are digitized, and the drug release times are estimated from the pixel intensity data for a range of starting emulsion droplet size. Drug release times are compared to a mechanistic model.
RESULTS
After injection, pixel intensity or turbidity decreases due to reductions in emulsion droplet size. Drug release times can still be measured even if the emulsion does not completely dissolve such as with Diprivan(®). Both pure propofol emulsions and Diprivan(®) release drug very rapidly (under five seconds). Reducing emulsion droplet size significantly increases the drug release rate. Drug release times observed are slightly longer than the model prediction likely due to imperfect mixing.
CONCLUSIONS
Drug release from emulsions occurs very rapidly after injection. This could be a contributing factor to pain on injection of propofol emulsions.
Topics: Drug Liberation; Emulsions; Injections, Intravenous; Models, Theoretical; Propofol; Serum Albumin, Bovine; Solubility
PubMed: 25636303
DOI: 10.1016/j.ijpharm.2015.01.045 -
Biomaterials Science Feb 2021Emulsion electrospinning is a versatile technique used to create fibrous meshes for applications in drug delivery and tissue engineering. In this study, the effects of...
Emulsion electrospinning is a versatile technique used to create fibrous meshes for applications in drug delivery and tissue engineering. In this study, the effects of surfactant and increasing internal phase volume fraction on emulsion electrospun fiber morphology were investigated. The fiber diameter, surface topography, internal architecture, mesh hydrophobicity, and fiber volume fraction were all characterized and the resulting effects on model drug release and cell response were determined. Surfactant relocation to the fiber surface resulted in alterations to fiber surface topography and internal morphology, increased rate of water adsorption into the mesh, and reduced burst effects of drug release. Increasing the internal phase volume fraction within the emulsion resulted in minimal change to fiber diameter, surface morphology, fiber volume fraction, and rate of water adsorption illustrating the ability to increase drug loading without affecting fiber properties. Lastly, all meshes promoted cell adhesion and good viability with a trend of increased MTT absorbance from cells on the surfactant and emulsion fibers possibly suggesting that an increase in surface area via smaller fiber diameter and fiber volume fraction increases metabolic activity. Overall, these studies indicate that fiber morphology and mesh hydrophobicity can be tuned by controlling surfactant location within fibers and internal phase volume fraction. Modulating fiber properties within the emulsion electrospun mesh is important to achieve controlled drug release and cell response for tissue engineering applications.
Topics: Cell Adhesion; Drug Liberation; Emulsions; Surface-Active Agents; Tissue Engineering
PubMed: 33393536
DOI: 10.1039/d0bm01751e