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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 -
Current Drug Delivery 2023Nanotechnology has attracted researchers around the globe owing to the small size and targeting properties of the drug delivery vectors. The interest in... (Review)
Review
Nanotechnology has attracted researchers around the globe owing to the small size and targeting properties of the drug delivery vectors. The interest in self-nanoemulsifying drug delivery systems (SNEDDS) has shown an exponential increase from the formulator's point of view. SNEDDS have shown wide applicability in terms of controlled and targeted delivery of various types of drugs. They chemically consist of oil, surfactants and co-surfactants that decrease the emulsion particle size to the range of <100 nm. However, stability issues such as drug precipitation during storage, incompatibility of ingredients in shell, decrease their application for the long run and these issues have been highlighted in this paper. The current review throws limelight on the biological aspects and process parameters. In addition, the process of absorption from GI is also discussed in detail. SNEDDS have been utilized as a treatment option for various diseases like cancer, diabetes, and ocular and pulmonary diseases. Along with this, the authors highlight the advances involving in vivo and in vitro lipolysis studies on SNEDDS, also highlighting recent innovations in this field, such as novel combinations of drug-free solid SNEDDS + solid dispersions, lipid-modified chitosan containing mucoadhesive SNEDDS, pHsensitive SNEDDS and several others.
Topics: Drug Delivery Systems; Surface-Active Agents; Emulsions; Nanotechnology; Particle Size; Nanoparticles; Solubility; Biological Availability; Administration, Oral
PubMed: 35598245
DOI: 10.2174/1567201819666220519125003 -
Journal of Colloid and Interface Science Jan 2023Encapsulation of sensitive water-soluble bioactive materials such as fragrances, polyphenols and enzymes poses an immense challenge with capsules templated from...
HYPOTHESIS
Encapsulation of sensitive water-soluble bioactive materials such as fragrances, polyphenols and enzymes poses an immense challenge with capsules templated from water-in-oil (w/o) emulsions. Generation of radicals, heating, and extreme pH that are necessary for shell formation through interfacial reactions may have undesired influences on the active ingredients and thus lower their activity.
EXPERIMENTS
To overcome these limitations, we present a method to encapsulate sensitive ingredients, whereby capsules are templated from a w/o Pickering emulsion stabilized by binary particles of different hydrophilicity levels; the particles assembled at the water/oil interface are then crosslinked by polydiisocyanate (PHDI) at room temperature and neutral pH. Zein and casein nanoparticles were used as hydrophilic stabilizers and lipase was chosen as a model sensitive biomolecule that was encapsulated in the water core.
FINDINGS
Our results indicated that the enzymes encapsulated in colloid capsules had higher activity than those encapsulated in traditional w/o Pickering emulsion without shell crosslinking. The capsule structure effectively protected enzymes from the outer environment. This method is well suited for the encapsulation and protection of sensitive ingredients and shows great application in food, drug, and cosmetic industries.
Topics: Emulsions; Water; Polyphenols; Nanoparticles; Lipase; Particle Size
PubMed: 36179576
DOI: 10.1016/j.jcis.2022.09.106 -
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 -
Drug Development and Industrial Pharmacy Aug 2021The aim of this study was to develop a pediatric oral preparation for ibuprofen.
OBJECTIVE
The aim of this study was to develop a pediatric oral preparation for ibuprofen.
SIGNIFICANCE
Ibuprofen is widely used for defervescence in children, but medication compliance is poor due to its bitter taste. Dry emulsions possess good stability and can be transported and stored in solid form; they can be dispersed into liquid emulsions with water and easily administered to children.
METHODS
In this study, a dry emulsion excipient was prepared by spray drying: a mixture of orange peel and corn oils (3:7, w/w) was used as the oil phase and solvent for ibuprofen; gum arabic and gum tragacanth were chosen as emulsifiers; and maltodextrin was used as a solid carrier.
RESULTS
The particle sizes of the liquid and reconstituted emulsions were 5.75 µm and 6.11 µm, respectively; the average particle size distribution of the dry emulsion powder was 8.13 µm; scanning electron microscopy showed that the dry emulsion powder was composed of evenly distributed smooth spheres. At a drug loading of 36.52 ± 1.15 mg/g, 90% of ibuprofen was released from the dry emulsion excipient within 30 min. Sensory evaluations using human volunteers, rats, and an electronic tongue demonstrated that the emulsion had a taste-masking effect on ibuprofen. It was further corroborated by studies using a rat model that highlighted a 1.76-fold increase in ibuprofen absorption when the drug was administered as an emulsion compared with granules.
CONCLUSIONS
These results indicate that the dry emulsion for taste-masking is promising and valuable in the development of ibuprofen for pediatrics.
Topics: Animals; Child; Emulsions; Excipients; Humans; Ibuprofen; Oils; Particle Size; Powders; Rats; Taste
PubMed: 34605349
DOI: 10.1080/03639045.2021.1989458 -
International Journal of Biological... Aug 2020In recent years, the use of food grade natural biodegradable particles as Pickering emulsion stabilizer has attracted wide attentions. In this study, chitosan/gum Arabia...
In recent years, the use of food grade natural biodegradable particles as Pickering emulsion stabilizer has attracted wide attentions. In this study, chitosan/gum Arabia (CS/GA) nanoparticles were prepared and their potential use in stabilizing Pickering emulsion and delivering curcumin were evaluated. It was found that CS and GA combined mainly through electrostatic interactions, and the obtained nanoparticles were about 100 nm of size and displayed higher surface activity than chitosan nanoparticles. Fluorescence microscopy showed that the nanoparticles accumulated at the oil-water interface. The environmental stability of Pickering emulsion got improved with the increase of nanoparticle concentration, and was sensitive to the changes of pH and ionic strength, while the emulsion remained stable under all test temperatures. The Pickering emulsion stabilized by 0.75% CS/GA nanoparticles displayed higher curcumin embedding rate of 94%, and also showed improved protection on curcumin during storage and controlled release during in vitro digestion. These results confirmed that the CS/GA nanoparticle stabilized-Pickering emulsion could be used as an effective deliver system for bioactive substances.
Topics: Chitosan; Curcumin; Drug Carriers; Drug Stability; Emulsions; Gum Arabic; Microscopy, Fluorescence; Nanoparticles; Particle Size; Surface-Active Agents
PubMed: 32344077
DOI: 10.1016/j.ijbiomac.2020.04.177 -
International Journal of Pharmaceutical... 2021Concentrated 7% w/w a-arbutin cream was formulated and evaluated using O/W and W/O emulsion bases as an extemporaneous preparation for melasma treatment. Cream bases...
Concentrated 7% w/w a-arbutin cream was formulated and evaluated using O/W and W/O emulsion bases as an extemporaneous preparation for melasma treatment. Cream bases were formulated with two pH values, 4.0 and 5.5, using a hot process. The stability of the creams was studied for 60 days under three storage conditions (i.e., 2°C to 8°C, 30°C, 40°C). Cream characteristics and all aspects of product stability including physical, chemical, and microbial were investigated. Stability was defined as no dramatic change in color, viscosity, pH, and no visible microbial growth. For stability, at least 90% of the initial a-arbutin concentration quantified by stability-indicating high-performance liquid chromatography must be obtained. It was found that pH had no influence on the a-arbutin or formulations' stability. All formulations had a-arbutin remaining higher than 90% (approximately 92%) after being stored for 60 days in all storage conditions with no significant changes in pH or viscosity. All samples complied with the microbial limits test for nonsterile pharmaceutical preparation for cutaneous products. However, a color change was detected in O/W and W/O emulsions, especially at 40°C storage condition within 28 and 14 days, respectively. Drug crystals were observed in W/O emulsion stored at 2°C to 8°C. Concerning the in vitro drug release, a-arbutin was released from O/W emulsion but not from W/O emulsion. From the above results, the O/W emulsion that was developed in this study can be used as a cream base for concentrated a-arbutin as an extemporaneous preparation. The developed a-arbutin cream prepared using O/W emulsions can be used as an extemporaneous preparation with a beyond-use date of 60 days when stored at room temperature (30°C) and in the refrigerator (2°C to 8°C).
Topics: Arbutin; Drug Stability; Emulsions; Humans; Melanosis; Temperature; Viscosity
PubMed: 33503011
DOI: No ID Found -
Current Drug Delivery 2020A novel, Supersaturable Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) has been prepared to improve the Dutasteride's poor aqueous solubility.
OBJECTIVE
A novel, Supersaturable Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) has been prepared to improve the Dutasteride's poor aqueous solubility.
METHODS
By adding Hydroxy Propyl Methyl Cellulose (HPMC) as a precipitation inhibitor to conventional SNEDDS, a supersaturable system was prepared. Firstly, the prepared SNEDDS played an important role in increasing the aqueous solubility and hence oral absorption due to nano-range size. Secondly, the S-SNEDDS found to be advantageous over SNEDDS for having a higher drug load and inhibition of dilution precipitation of Dutasteride. Formulated S-SNEDDS (F1-F9) ranged from 37.42 ± 1.02 to 68.92 ± 0.09 nm with PDI 0.219-0.34 and drug loading of over 95 percent.
RESULTS
The study of in-vitro dissolution revealed higher dissolution for S-SNEDDS compared to SNEDDS and Avodart soft gelatin capsule as a commercial product. In addition, higher absorption was observed for S-SNEDDS showing approximately 1.28 and 1.27 fold AUC (0-24h) and Cmax compared to commercial products. Therefore, S-SNEDDS has proven as a novel drug delivery system with a higher drug load, higher self-emulsification efficiency, higher stability, higher dissolution and pronounced absorption.
CONCLUSION
In conclusion, S-SNEDDS could be a newly emerging approach to enhance aqueous solubility in many folds for drugs belonging to BCS Class II and IV and thus absorption and oral bioavailability.
Topics: 5-alpha Reductase Inhibitors; Drug Carriers; Drug Delivery Systems; Dutasteride; Emulsions; Hypromellose Derivatives; Nanoparticles; Particle Size; Solubility; Surface Properties
PubMed: 31721703
DOI: 10.2174/1567201816666191112111610 -
Colloids and Surfaces. B, Biointerfaces Jan 2021Low-environmental-impact emulsion systems for transdermal drug delivery in topical treatment have gained increasing interest. However, low stability and adverse systemic...
Low-environmental-impact emulsion systems for transdermal drug delivery in topical treatment have gained increasing interest. However, low stability and adverse systemic side effects severely decrease their efficiency. This study proposed a stable oil-in-water (O/W) emulsion loaded with bifonazole (BFZ) as a lipophilic drug stabilized by poly(2-isopropoxy-2-oxo-1,3,2-dioxaphospholane)-modified cellulose nanocrystals (CNC-g-PIPP) as vehicles for topical delivery of lipophilic drugs. We fully characterized stability, BFZ-loaded particle-stabilized emulsions (PEs) for morphology, droplet size, and its distribution. In addition, we evaluated the in vitro drug-releasing capacity and in vitro skin permeation of BFZ in a porcine skin animal model using a side-bi-side® diffusion cell. An O/W BFZ-loaded emulsion stabilized with CNC-g-PIPP particles (BFZ-loaded CP-PE) with a small mean droplet size of 2.54 ± 1.39 μm was developed and was stable for > = 15 days without a significant change in droplet size. The BFZ-loading efficiency in PEs was 83.1 %. BFZ was slowly released over an extended period, and the releasing ratio from BFZ-loaded CP-PE was only 17 % after 48 h. The BFZ-loaded CP-PE showed a ∼4.4-fold increase in BFZ permeation and penetration compared to a conventional surfactant-stabilized emulsion and BFZ control solution. Fluorescence-labeling studies showed that BFZ-loaded CP-PE could well penetrate skin layers from the stratum corneum (SC) to the dermis. In addition, histopathology studies of porcine skin treated with the PE formulation showed an intact SC with unaltered adjacent structures and no observed signs of inflammation. Therefore, the proposed CP-PE shows great potential as a transdermal drug carrier for enhancing lipophilic drug permeation.
Topics: Administration, Cutaneous; Animals; Drug Carriers; Emulsions; Particle Size; Skin; Skin Absorption; Swine; Water
PubMed: 33142258
DOI: 10.1016/j.colsurfb.2020.111423 -
Clinical Toxicology (Philadelphia, Pa.) Aug 2017The Lipid Emulsion Therapy workgroup, organized by the American Academy of Clinical Toxicology, recently conducted a systematic review, which subjectively evaluated... (Meta-Analysis)
Meta-Analysis Review
INTRODUCTION
The Lipid Emulsion Therapy workgroup, organized by the American Academy of Clinical Toxicology, recently conducted a systematic review, which subjectively evaluated lipid emulsion as a treatment for local anesthetic toxicity. We re-extracted data and conducted a meta-analysis of survival in animal models.
METHODS
We extracted survival data from 26 publications and conducted a random-effect meta-analysis based on odds ratio weighted by inverse variance. We assessed the benefit of lipid emulsion as an independent variable in resuscitative models (16 studies). We measured Cochran's Q for heterogeneity and I to determine variance contributed by heterogeneity. Finally, we conducted a funnel plot analysis and Egger's test to assess for publication bias in studies.
RESULTS
Lipid emulsion reduced the odds of death in resuscitative models (OR =0.24; 95%CI: 0.1-0.56, p = .0012). Heterogeneity analysis indicated a homogenous distribution. Funnel plot analysis did not indicate publication bias in experimental models.
DISCUSSION
Meta-analysis of animal data supports the use of lipid emulsion (in combination with other resuscitative measures) for the treatment of local anesthetic toxicity, specifically from bupivacaine. Our conclusion differed from the original review. Analysis of outliers reinforced the need for good life support measures (securement of airway and chest compressions) along with prompt treatment with lipid.
Topics: Anesthetics, Local; Animals; Bupivacaine; Combined Modality Therapy; Disease Models, Animal; Dogs; Drug Compounding; Emulsions; Fat Emulsions, Intravenous; Odds Ratio; Poisoning; Rabbits; Rats; Resuscitation; Risk Assessment; Risk Factors; Swine; Time Factors
PubMed: 28346007
DOI: 10.1080/15563650.2017.1288911