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Molecules (Basel, Switzerland) Nov 2022Pickering emulsions are emulsion systems stabilized by solid particles at the interface of oil and water. Pickering emulsions are considered to be natural,... (Review)
Review
Pickering emulsions are emulsion systems stabilized by solid particles at the interface of oil and water. Pickering emulsions are considered to be natural, biodegradable, and safe, so their applications in various fields-such as food, cosmetics, biomedicine, etc.-are very promising, including as a vehicle for essential oils (EOs). These oils contain volatile and aromatic compounds and have excellent properties, such as antifungal, antibacterial, antiviral, and antioxidant activities. Despite their superior properties, EOs are prone to evaporation, decompose when exposed to light and oxygen, and have low solubility, limiting their industrial applications. Several studies have shown that EOs in Pickering emulsions displays less sensitivity to evaporation and oxidation, stronger antibacterial activity, and increased solubility. In brief, the application of Pickering emulsions for EOs is interesting to explore. This review discusses recent progress in the application of Pickering emulsions, particularly as EO carriers, drug carriers, antioxidant and antimicrobial carriers, and in active packaging.
Topics: Emulsions; Oils, Volatile; Antioxidants; Excipients; Anti-Bacterial Agents
PubMed: 36431978
DOI: 10.3390/molecules27227872 -
Scientific Reports Sep 2023Neuroblastoma, the most common type of pediatric extracranial solid tumor, causes 10% of childhood cancer deaths. Despite intensive multimodal treatment, the outcomes of...
Neuroblastoma, the most common type of pediatric extracranial solid tumor, causes 10% of childhood cancer deaths. Despite intensive multimodal treatment, the outcomes of high-risk neuroblastoma remain poor. We urgently need to develop new therapies with safe long-term toxicity profiles for rapid testing in clinical trials. Drug repurposing is a promising approach to meet these needs. Here, we investigated disulfiram, a safe and successful chronic alcoholism treatment with known anticancer and epigenetic effects. Disulfiram efficiently induced cell cycle arrest and decreased the viability of six human neuroblastoma cell lines at half-maximal inhibitory concentrations up to 20 times lower than its peak clinical plasma level in patients treated for chronic alcoholism. Disulfiram shifted neuroblastoma transcriptome, decreasing MYCN levels and activating neuronal differentiation. Consistently, disulfiram significantly reduced the protein level of lysine acetyltransferase 2A (KAT2A), drastically reducing acetylation of its target residues on histone H3. To investigate disulfiram's anticancer effects in an in vivo model of high-risk neuroblastoma, we developed a disulfiram-loaded emulsion to deliver the highly liposoluble drug. Treatment with the emulsion significantly delayed neuroblastoma progression in mice. These results identify KAT2A as a novel target of disulfiram, which directly impacts neuroblastoma epigenetics and is a promising candidate for repurposing to treat pediatric neuroblastoma.
Topics: Animals; Child; Humans; Mice; Alcohol Deterrents; Cell Line, Tumor; Disulfiram; Down-Regulation; Drug Repositioning; Emulsions; Histone Acetyltransferases; Neuroblastoma
PubMed: 37777587
DOI: 10.1038/s41598-023-43219-2 -
Colloids and Surfaces. B, Biointerfaces Jul 2021Nanoemulsions are kinetically stabilized emulsions with droplet sizes in the nanometer scale. These nanodroplets are able to confine spaces in which reactions of... (Review)
Review
Nanoemulsions are kinetically stabilized emulsions with droplet sizes in the nanometer scale. These nanodroplets are able to confine spaces in which reactions of polymerization or precipitation can take place, leading to the formation of particles and capsules that can act as nanocarriers for biomedical applications. This review discusses the different possibilities of using nanoemulsions for preparing biomedical nanocarriers. According to the chemical nature, nanocarriers prepared in nanoemulsions are classified in polymeric, inorganic, or hybrid. The main synthetic strategies for each type are revised, including miniemulsion polymerization, nanoemulsion-solvent evaporation, spontaneous emulsification, sol-gel processes, and combination of different techniques to form multicomponent materials.
Topics: Emulsions; Polymers; Solvents
PubMed: 33892282
DOI: 10.1016/j.colsurfb.2021.111764 -
AAPS PharmSciTech Dec 2010Injectable lipid emulsions, for decades, have been clinically used as an energy source for hospitalized patients by providing essential fatty acids and vitamins. Recent... (Review)
Review
Injectable lipid emulsions, for decades, have been clinically used as an energy source for hospitalized patients by providing essential fatty acids and vitamins. Recent interest in utilizing lipid emulsions for delivering lipid soluble therapeutic agents, intravenously, has been continuously growing due to the biocompatible nature of the lipid-based delivery systems. Advancements in the area of novel lipids (olive oil and fish oil) have opened a new area for future clinical application of lipid-based injectable delivery systems that may provide a better safety profile over traditionally used long- and medium-chain triglycerides to critically ill patients. Formulation components and process parameters play critical role in the success of lipid injectable emulsions as drug delivery vehicles and hence need to be well integrated in the formulation development strategies. Physico-chemical properties of active therapeutic agents significantly impact pharmacokinetics and tissue disposition following intravenous administration of drug-containing lipid emulsion and hence need special attention while selecting such delivery vehicles. In summary, this review provides a broad overview of recent advancements in the field of novel lipids, opportunities for intravenous drug delivery, and challenges associated with injectable lipid emulsions.
Topics: Critical Illness; Drug Compounding; Drug Delivery Systems; Fat Emulsions, Intravenous; Fatty Acids, Essential; Humans; Infusions, Intravenous; Parenteral Nutrition; Pharmaceutical Vehicles; Solubility; Triglycerides
PubMed: 20976577
DOI: 10.1208/s12249-010-9526-5 -
Acta Poloniae Pharmaceutica 2012In the recent years, there is a growing interest in the lipid-based formulations for delivery of lipophilic drugs. Due to their potential as therapeutic agents,... (Review)
Review
In the recent years, there is a growing interest in the lipid-based formulations for delivery of lipophilic drugs. Due to their potential as therapeutic agents, preferably these lipid soluble drugs are incorporated into inert lipid carriers such as oils, surfactant dispersions, emulsions, liposomes etc. Among them, emulsion forming drug delivery systems appear to be a unique and industrially feasible approach to overcome the problem of low oral bioavailability associated with the BCS class II drugs. Self-emulsifying formulations are ideally isotropic mixtures of oils, surfactants and co-solvents that emulsify to form fine oil in water emulsions when introduced in aqueous media. Fine oil droplets would pass rapidly from stomach and promote wide distribution of drug throughout the GI tract, thereby overcome the slow dissolution step typically observed with solid dosage forms. Recent advances in drug carrier technologies have promulgated the development of novel drug carriers such as control release self-emulsifying pellets, microspheres, tablets, capsules etc. that have boosted the use of "self-emulsification" in drug delivery. This article reviews the different types of formulations and excipients used in emulsion forming drug delivery system to enhance the bioavailability of lipophilic drugs.
Topics: Chemistry, Pharmaceutical; Drug Delivery Systems; Emulsions; Excipients; Solubility
PubMed: 22568032
DOI: No ID Found -
Molecules (Basel, Switzerland) Jun 2023Salidroside has been widely used in anti-tumor, cardiovascular, and cerebrovascular protection. However, there are few reports of its use for wound repair. Herein,...
Salidroside has been widely used in anti-tumor, cardiovascular, and cerebrovascular protection. However, there are few reports of its use for wound repair. Herein, salidroside inflammation-targeted emulsion gel and non-targeted emulsion gel were developed for wound repair. The inflammation-targeted emulsion gels showed an overall trend of better transdermal penetration and lower potential than non-targeted emulsion gels (-58.7 mV and -1.6 mV, respectively). The apparent improvement of the trauma surface was significant in each administration group. There was a significant difference in the rate of wound healing of the rats between each administration group and the model group at days 7 and 14. Pathological tissue sections showed that inflammatory cells in the epidermis, dermis, and basal layer were significantly reduced, and the granulation tissue was proliferated in the inflammation-targeted emulsion gel group and the non-targeted emulsion gel group. Regarding the expressions of EGF and bFGF, the expressions of bFGF and EGF in the tissues of the inflammation-targeted group at days 7, 14, or 21 were significantly higher than that of the non-targeted emulsion gel group and the model group, both of which were statistically significant compared with the model group ( < 0.05). These results demonstrated that salidroside has the potential as an alternative drug for wound repair.
Topics: Rats; Animals; Epidermal Growth Factor; Emulsions; Wound Healing; Inflammation; Gels
PubMed: 37446812
DOI: 10.3390/molecules28135151 -
International Journal of Nanomedicine 2020Nanoparticle solutions have been studied to improve antimicrobial effect. The aim of this study was to develop, characterize, and evaluate the in vitro and in vivo...
INTRODUCTION
Nanoparticle solutions have been studied to improve antimicrobial effect. The aim of this study was to develop, characterize, and evaluate the in vitro and in vivo antiseptic efficacy of 0.25% aqueous-based chlorhexidine nanoemulsion (NM-Cl 0.25% w/v).
METHODS
The NM-Cl 0.25% w/v (2.5mg/mL) and free chlorhexidine nanoemulsion (FCN; same composition of NM-Cl without the molecule of chlorhexidine) were synthetized by the spontaneous emulsification method. Characterization analyses of physical and chemical properties were performed. The NM-Cl 0.25% w/v was compared with chlorhexidine 0.5% alcohol base (CS-Cl 0.5%) in vitro studies (microdilution study and kill curve study), and in vivo study (antisepsis of rats dorsum). Kruskal-Wallis test was used between groups and inside the same group, at different sample times and the Mann-Whitney test was performed when difference was detected.
RESULTS
The NM-Cl 0.25% w/v presented adequate physicochemical characteristics for a nanoemulsion, revealing a more basic pH than FCN and difference between zeta potential of NM-Cl 0.25% w/v and FCN. The NM-Cl 0.25% w/v and CS-Cl 0.5% solutions were more effective on Gram-positive than on Gram-negative bacteria (≤0.05). NM-Cl 0.25% w/v presented upper antiseptic effect in the microdilution study and residual antiseptic effect was maintained for a longer time when compared to CS-Cl 0.5% (kill curve study). The four-fold (minimal inhibitory concentration) of NM-Cl 0.25% were the formulations with most durable effect within those tested, presenting residual effect until T6 for both bacteria. In the in vivo study, both formulations (NM-Cl 0.25% w/v and CS-Cl 0.5%) had a reduction of the microorganisms in the skin of the rats (<0.0001) not revealing any difference between the formulations at different times, showing the antiseptic effect of NM-Cl (≤0.05).
CONCLUSION
Both in vitro and in vivo experiments demonstrated that NM-Cl showed promising future as an antiseptic for cutaneous microbiota.
Topics: Animals; Anti-Infective Agents, Local; Chlorhexidine; Emulsions; Ethanol; Gram-Negative Bacteria; Gram-Positive Bacteria; Male; Microbial Sensitivity Tests; Nanostructures; Rats, Wistar; Skin
PubMed: 33061360
DOI: 10.2147/IJN.S228280 -
Molecules (Basel, Switzerland) Sep 2009Squalene is a linear triterpene that is extensively utilized as a principal component of parenteral emulsions for drug and vaccine delivery. In this review, the chemical... (Review)
Review
Squalene is a linear triterpene that is extensively utilized as a principal component of parenteral emulsions for drug and vaccine delivery. In this review, the chemical structure and sources of squalene are presented. Moreover, the physicochemical and biological properties of squalene-containing emulsions are evaluated in the context of parenteral formulations. Historical and current parenteral emulsion products containing squalene or squalane are discussed. The safety of squalene-based products is also addressed. Finally, analytical techniques for characterization of squalene emulsions are examined.
Topics: Animals; Drug Delivery Systems; Emulsions; Humans; Infusions, Parenteral; Squalene; Vaccines
PubMed: 19783926
DOI: 10.3390/molecules14093286 -
Scandinavian Journal of Trauma,... Oct 2010Intravenous lipid emulsion is an established, effective treatment for local anesthetic-induced cardiovascular collapse. The predominant theory for its mechanism of... (Review)
Review
Intravenous lipid emulsion is an established, effective treatment for local anesthetic-induced cardiovascular collapse. The predominant theory for its mechanism of action is that by creating an expanded, intravascular lipid phase, equilibria are established that drive the offending drug from target tissues into the newly formed 'lipid sink'. Based on this hypothesis, lipid emulsion has been considered a candidate for generic reversal of toxicity caused by overdose of any lipophilic drug. Recent case reports of successful resuscitation suggest the efficacy of lipid emulsion infusion for treating non-local anesthetic overdoses across a wide spectrum of drugs: beta blockers, calcium channel blockers, parasiticides, herbicides and several varieties of psychotropic agents. Lipid emulsion therapy is gaining acceptance in emergency rooms and other critical care settings as a possible treatment for lipophilic drug toxicity. While protocols exist for administration of lipid emulsion in the setting of local anesthetic toxicity, no optimal regimen has been established for treatment of acute non-local anesthetic poisonings. Future studies will shape the evolving recommendations for lipid emulsion in the setting of non-local anesthetic drug overdose.
Topics: Anesthesia; Cardiotoxins; Fat Emulsions, Intravenous; Humans
PubMed: 20923546
DOI: 10.1186/1757-7241-18-51 -
European Journal of Pharmaceutical... May 2022Critically ill and anesthetized patients commonly receive life-sustaining medications by pump-driven continuous intravenous infusion. Microinfusion refers to delivering...
Critically ill and anesthetized patients commonly receive life-sustaining medications by pump-driven continuous intravenous infusion. Microinfusion refers to delivering concentrated drugs with low flow carriers to conserve fluid administration. Most infused medications are water-soluble. Delivery onset lag times have been identified for microinfusions of water-soluble drugs or experimental surrogates. Drugs may be formulated as emulsions. Initiation of emulsion microinfusions has not been described. We tested in vitro the hypothesis that an emulsion's physical characteristics would influence its microinfusion delivery onset. We adapted an established in vitro model of pump-driven continuous intravenous microinfusion to compare the delivery of methylene blue as a surrogate for water-soluble drugs and a 10% lipid emulsion as a surrogate for a drug formulated as an emulsion. The drug surrogates joined the carrier with carrier flow vertically upwards, vertically downwards or horizontally. We measured the times to 5%, 50% and 95% of plateau delivery. Emulsion entry into a vertical (upwards) carrier flow resulted in a rapid initial emulsion delivery exceeding predictions of delivery models. Emulsion entry into both horizontal and vertical (downwards) carrier flows resulted in long lag times to steady state. Methylene blue delivery was unaffected by carrier flow orientation. Initiating microinfusion emulsion delivery with upward flow can result in a relative bolus, whereas long delivery lags would be expected with horizontal or downwards flow. An emulsion might carry a high potency drug having significant physiologic effects, e. g. clevidipine. Unrecognized, differences in initial emulsion delivery kinetics depending on carrier flow orientation may have clinical implications for both efficacy and safety.
Topics: Administration, Intravenous; Drug Delivery Systems; Emulsions; Equipment Design; Humans; Infusions, Intravenous
PubMed: 35227840
DOI: 10.1016/j.ejps.2022.106154