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Colloids and Surfaces. B, Biointerfaces Sep 2020Emulsion formulations of essential oils are of major interest due to their relative biosafety, biocompatibility and good pharmacological potential. Their structural...
Emulsion formulations of essential oils are of major interest due to their relative biosafety, biocompatibility and good pharmacological potential. Their structural constituents (oil and water phase) facilitate ready solubilization of incorporated hydrophilic/lipophilic actives for their targeted delivery. In the present study, m5S cells were tested for their viability at various concentrations of clove oil and an alkyl polyglucoside emulsifier, viz., Montanov 202™. Thereafter, good cell viable concentrations of oil (10 %) and emulsifier (4%) were used at their optimised ratio (1:0.4) to formulate an oil in water emulsion using phase inversion technique followed by ultrasonication for particle size reduction. Gas chromatography-mass spectrometry (GC-MS) analysis of clove oil revealed eugenol (76.11 %) and eugenyl acetate (12.41 %) as major constituents. The formulated clove oil emulsion was then characterised with respect to its size, zeta potential, microscopic and thermal analysis and the presence of liquid crystals were observed in the same. It was further studied for its anti-inflammatory potential in female Wistar rats wherein topical treatment with the emulsion inhibited paw swelling induced by carrageenan model by 40-60% over 30-180 min compared to untreated animals. Similarly, the emulsion's wound healing potential was also significant with respect to wounds induced by both incision (wound breaking strength of 338.91 ± 5.02 g) and excision (95 % wound contraction by 16th day) model in these animals, with a re-epithelization period of 10.67 ± 1.67 days and results being comparable with diclofenac gel and neomycin cream (positive controls). Histopathology of the skin sections showed accelerated healing with early granular tissue and collagen formation in emulsion treated animals. It is hence envisaged that this clove oil emulsion can substitute chemical based topical products for anti-inflammatory and wound healing applications due to its biological constituents as well as because of the presence of liquid crystals in its formulation.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Cell Proliferation; Cell Survival; Cells, Cultured; Clove Oil; Edema; Emulsions; Female; Mice; Oxidative Stress; Particle Size; Rats; Rats, Wistar; Surface Properties; Wound Healing
PubMed: 32442923
DOI: 10.1016/j.colsurfb.2020.111102 -
Sensors (Basel, Switzerland) Jul 2022In this work, we investigated a platform for real-time emulsion droplet detection and size measurement in optofluidic platforms. An 8.2 µm core diameter input optical...
In this work, we investigated a platform for real-time emulsion droplet detection and size measurement in optofluidic platforms. An 8.2 µm core diameter input optical fiber and a multi-mode Gradient Refractive Index (GRIN) output fiber were integrated into an acrylic microfluidic channel platform consisting of three layers. Water-in-oil emulsions were investigated, since relevant applications have emerged in the recent past for these types of emulsions, such as drug encapsulation as well as droplet-based Polymerase Chain Reaction (PCR) amplification of DNA, among others. The main contribution of this work is in understanding the main physical phenomena (i.e., total internal reflection, refraction, and interference) behind the complex transmittance pattern obtained for these droplets. For this purpose, a frequency domain electromagnetic wave propagation modelling of the structure using the Finite Element Method (FEM) was used along with experimental measurements.
Topics: Emulsions; Microfluidics; Particle Size; Polymerase Chain Reaction; Water
PubMed: 35808495
DOI: 10.3390/s22134999 -
Drug Delivery Jun 2016Based on its antioxidant activity, melatonin was recently found to have a protection effect against photocarcinogenesis.
CONTEXT
Based on its antioxidant activity, melatonin was recently found to have a protection effect against photocarcinogenesis.
OBJECTIVE
This work aimed to develop an innovative sunscreen formulation based on the Pickering emulsions concept, stabilized by physical UV filters, modified starch and natural oils associated to melatonin as a key strategy for prevention against UV-induced skin damage.
MATERIALS AND METHODS
For this purpose, melatonin was incorporated in Pickering emulsions that were characterized using physicochemical, in vitro and in vivo testing. Physicochemical studies included physical and chemical stability by a thorough pharmaceutical control. The possible protective effects of melatonin against UV-induced cell damage in HaCaT cell lines were investigated in vitro. The safety assessment and the in vivo biological properties of the final formulations, including Human Repeat Insult Patch Test and sunscreen water resistance tests were also evaluated.
RESULTS AND DISCUSSION
These studies demonstrated that melatonin sunscreen Pickering emulsion was beneficial and presented a powerful protection against UVB-induced damage in HaCat cells, including inhibition of apoptosis. The inclusion of zinc oxide, titanium dioxide, green coffee oil and starch ensured a high SPF (50+) against UVA and UVB.
CONCLUSION
The combination of melatonin, multifunctional solid particles and green coffee oil, contributed to achieve a stable, effective and innovative sunscreen with a meaningful synergistic protection against oxidative stress.
Topics: Emulsions; Humans; Melatonin; Oils; Oxidative Stress; Skin; Starch; Sunscreening Agents; Titanium; Ultraviolet Rays; Zinc Oxide
PubMed: 26755411
DOI: 10.3109/10717544.2015.1128496 -
Molecular Pharmaceutics Oct 2021Nanoemulsions are considered as the most promising solution to improve the delivery of ophthalmic drugs. The design of ophthalmic nanoemulsions requires an extensive... (Review)
Review
Nanoemulsions are considered as the most promising solution to improve the delivery of ophthalmic drugs. The design of ophthalmic nanoemulsions requires an extensive understanding of pharmaceutical as well as technological aspects related to the selection of excipients and formulation processes. This Review aims at providing the readers with a comprehensive summary of possible compositions of nanoemulsions, methods for their formulation (both laboratory and industrial), and differences between technological approaches, along with an extensive outline of the research methods enabling the confirmation of properties, pharmaceutical performance, and biological activity of the obtained product. The composition of the formulation has a major influence on the properties of the final product obtained with low-energy emulsification methods. Increasing interest in high-energy emulsification methods is a consequence of their scalability important from the industrial perspective. Considering the high-energy emulsification methods, both the composition and conditions of the process (e.g., device power level, pressure, temperature, homogenization time, or number of cycles) are important for the properties and stability of nanoemulsions. It is advisible to determine the effect of each parameter on the quality of the product to establish the optimal process parameters' range which, in turn, results in a more reproducible and efficient production.
Topics: Administration, Ophthalmic; Emulsions; Eye Diseases; Humans; Nanoparticle Drug Delivery System; Quality Control
PubMed: 34533317
DOI: 10.1021/acs.molpharmaceut.1c00650 -
Therapeutic Delivery Jul 2021The present study focused on the development of a dry emulsion tablet of raloxifene hydrochloride (RXF) using a solid carrier adsorption technique to enhance oral...
The present study focused on the development of a dry emulsion tablet of raloxifene hydrochloride (RXF) using a solid carrier adsorption technique to enhance oral bioavailability. An oil-in-water emulsion was formulated and converted into dry powder using HPMC K4M plus Aerosil 200, then compressed into tablets. The prepared emulsion was evaluated for globule size, drug content and zeta potential. release study revealed significantly higher release from emulsion. The prepared tablets possessed acceptable hardness, friability, weight variation, disintegration time, thickness, etc. pharmacokinetic studies indicated a more than sevenfold increase in oral bioavailability. Stability studies indicated good physical and chemical stability of the developed formulation. The authors successfully formulated dry emulsion tablets with enhanced oral bioavailability.
Topics: Adsorption; Biological Availability; Emulsions; Raloxifene Hydrochloride; Solubility; Tablets
PubMed: 34165001
DOI: 10.4155/tde-2021-0025 -
Folia Medica Dec 2021Lipid emulsions are increasingly used as an antidote to lipophilic drug intoxications. The dose recommended by the American Society of Regional Anesthesia is used...
INTRODUCTION
Lipid emulsions are increasingly used as an antidote to lipophilic drug intoxications. The dose recommended by the American Society of Regional Anesthesia is used primarily for the treatment of local anesthetic systemic toxicity. There is insufficient information about what the dose of lipid emulsions (LE) should be in other intoxications depending on their severity.
AIM
To determine the LE dose in a shock or haemodynamic instability in patients with acute exogenous intoxications treated with LE.
MATERIALS AND METHODS
Forty-nine patients with acute lipophilic drug intoxications were treated with LE in the Clinic of Toxicology at the Naval Hospital in Varna.Statistical analysis was performed using the statistical functions of Excel 2016 and the Statistica 7.0 software package.
RESULTS
The percentage of patients receiving a low dose of LE of 0.3 ml/kg (93.87%) was significantly higher than the percentage of patients treated with a medium (2.04%) and a high dose (4.08%) of LF. The high dose of LE of 1.5 ml/kg recommended by the American Society of Regional Anesthesia was administered to two patients (4.08%). In severe intoxications with exotoxic shock, the rate of LE administration varies from 20 ml/h to 40 ml/h.
CONCLUSIONS
In severe intoxications with cardiotoxic syndrome and haemodynamic instability, LE should be used in the dose as suggested by the American Society of Regional Anesthesia. It is possible to use lower doses of LE in the range of 0.3-0.6 ml/kg in all moderate poisonings administered by continuous intravenous infusion for 12-24-48 hours. No side effects were observed at these doses.
Topics: Acute Disease; Antidotes; Drug-Related Side Effects and Adverse Reactions; Emulsions; Fat Emulsions, Intravenous; Humans; Lipids
PubMed: 35851238
DOI: 10.3897/folmed.63.e59216 -
Physical Chemistry Chemical Physics :... Aug 2023Multicompartment structures have the potential for biomedical applications because they can act as multifunctional systems and provide simultaneous delivery of drugs and... (Review)
Review
Multicompartment structures have the potential for biomedical applications because they can act as multifunctional systems and provide simultaneous delivery of drugs and diagnostics agents of different types. Moreover, some of them mimic biological cells to some extent with organelles as separate sub-compartments. This article analyses multicompartment colloidal structures with smaller sub-units covered with lipid or polymer membranes that provide additional protection for the encapsulated substances. Vesosomes with small vesicles encapsulated in the inner pools of larger liposomes are the most studied systems to date. Dendrimer molecules are enclosed by a lipid bilayer shell in dendrosomes. Capsosomes, polymersomes-in-polymer capsules, and cubosomes-in-polymer capsules are composed of sub-compartments encapsulated within closed multilayer polymer membranes. Janus or Cerberus emulsions contain droplets composed of two or three phases: immiscible oils in O/W emulsions and aqueous polymer or salt solutions that are separated into two or three phases and form connected droplets in W/O emulsions. In more cases, the external surface of engulfed droplets in Janus or Cerberus emulsions is covered with a lipid or polymer monolayer. eLiposomes with emulsion droplets encapsulated into a bilayer shell have been given little attention so far, but they have very great prospects. In addition to nanoemulsion droplets, solid lipid nanoparticles, nanostructured lipid carriers and inorganic nanoparticles can be loaded into eLiposomes. Molecular engineering of the external membrane allows the creation of ligand-targeted and stimuli-responsive multifunctional systems. As a result, the efficacy of drug delivery can be significantly enhanced.
Topics: Polymers; Emulsions; Capsules; Drug Delivery Systems; Lipid Bilayers
PubMed: 37565484
DOI: 10.1039/d3cp01984e -
Small (Weinheim An Der Bergstrasse,... May 2019Microcapsules with molecule-selective permeation are appealing as microreactors, capsule-type sensors, drug and cell carriers, and artificial cells. To accomplish...
Microcapsules with molecule-selective permeation are appealing as microreactors, capsule-type sensors, drug and cell carriers, and artificial cells. To accomplish molecular size- and charge-selective permeation, regular size of pores and surface charges have been formed in the membranes. However, it remains an important challenge to provide advanced regulation of transmembrane transport. Here, smart microcapsules are designed that provide molecular polarity- and temperature-dependent permeability. With capillary microfluidic devices, water-in-oil-in-water (W/O/W) double-emulsion drops are prepared, which serve as templates to produce microcapsules. The oil shell is composed of two monomers and dodecanol, which turns to a polymeric framework whose continuous voids are filled with dodecanol upon photopolymerization. One of the monomers provides mechanical stability of the framework, whereas the other serves as a compatibilizer between growing polymer and dodecanol, preventing macrophase separation. Above melting point of dodecanol, molecules that are soluble in the molten dodecanol are selectively allowed to diffuse across the shell, where the rate of transmembrane transport is strongly influenced by partition coefficient. The rate is drastically lowered for temperatures below the melting point. This molecular polarity- and temperature-dependent permeability renders the microcapsules potentially useful as drug carriers for triggered release and contamination-free microreactors and microsensors.
Topics: Capsules; Drug Carriers; Emulsions; Permeability; Polymers; Temperature
PubMed: 30997745
DOI: 10.1002/smll.201900434 -
Small (Weinheim An Der Bergstrasse,... Sep 2018Interfacial self-assembly is a powerful organizational force for fabricating functional nanomaterials, including nanocarriers, for imaging and drug delivery. Herein, the...
Interfacial self-assembly is a powerful organizational force for fabricating functional nanomaterials, including nanocarriers, for imaging and drug delivery. Herein, the interfacial self-assembly of pH-responsive metal-phenolic networks (MPNs) on the liquid-liquid interface of oil-in-water emulsions is reported. Oleic acid emulsions of 100-250 nm in diameter are generated by ultrasonication, to which poly(ethylene glycol) (PEG)-based polyphenolic ligands are assembled with simultaneous crosslinking by metal ions, thus forming an interfacial MPN. PEG provides a protective barrier on the emulsion phase and renders the emulsion low fouling. The MPN-coated emulsions have a similar size and dispersity, but an enhanced stability when compared with the uncoated emulsions, and exhibit a low cell association in vitro, a blood circulation half-life of ≈50 min in vivo, and are nontoxic to healthy mice. Furthermore, a model anticancer drug, doxorubicin, can be encapsulated within the emulsion phase at a high loading capacity (≈5 fg of doxorubicin per emulsion particle). The MPN coating imparts pH-responsiveness to the drug-loaded emulsions, leading to drug release at cell internalization pH and a potent cell cytotoxicity. The results highlight a straightforward strategy for the interfacial nanofabrication of pH-responsive emulsion-MPN systems with potential use in biomedical applications.
Topics: Animals; Doxorubicin; Drug Delivery Systems; Emulsions; Hydrogen-Ion Concentration; Mice; Nanostructures; Oleic Acid; Polyethylene Glycols
PubMed: 30156378
DOI: 10.1002/smll.201802342 -
Cardiovascular and Interventional... May 2021To examine physiochemical characteristics and drug release properties of cisplatin powder and lipiodol mixtures formed by a glass membrane emulsification device compared...
PURPOSE
To examine physiochemical characteristics and drug release properties of cisplatin powder and lipiodol mixtures formed by a glass membrane emulsification device compared with a 3-way stopcock.
MATERIALS AND METHODS
Seven different types of mixtures were evaluated: cisplatin powder and lipiodol directly mixed (suspension), complete cisplatin solution and lipiodol mixed by a 3-way stopcock or the device (emulsion), incomplete cisplatin solution and lipiodol mixed by a 3-way stopcock or the device (solid-in-water emulsion), and contrast material and cisplatin suspension mixed by a 3-way stopcock or the device (solid-in-oil emulsion).
RESULT
The percentages of water-in-oil were 98.08 ± 0.27% in the emulsion formed by the device, while 70.3 ± 4.63% in the emulsion formed by a 3-way stopcock (P = 0.037). Solid-in-water and solid-in-oil emulsions formed by the device showed 98.09 ± 0.38% and 98.70 ± 0.40% of water-in-oil, respectively, whereas both solid-in-water and solid-in-oil emulsions formed by a 3-way stopcock showed 0.00%. Homogenous droplet sizes were shown by using the device. The half release times of cisplatin in the emulsions formed by the device were 197 ± 19, 244 ± 24 and 478 ± 52 min, respectively, which were significantly longer than the emulsion formed by a 3-way stopcock of 8 ± 8 min (P = 0.046-0.050). Suspension showed the longest release time; however, the viscosity was lowest.
CONCLUSION
The glass membrane emulsification device formed almost 100% water-in-oil, whereas 3-way stopcock produced 100% oil-in-water when incomplete solution or suspension was mixed. Slower cisplatin release was shown in the emulsions formed by the device.
Topics: Antineoplastic Agents; Carcinoma, Hepatocellular; Chemoembolization, Therapeutic; Cisplatin; Drug Liberation; Emulsions; Ethiodized Oil; Humans; Liver Neoplasms
PubMed: 33415417
DOI: 10.1007/s00270-020-02757-2