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BioMed Research International 2022Hypertension is one of the most important causes of mortality, affecting the health status of the patient. At the same time, hypertension causes a huge health and... (Review)
Review
Hypertension is one of the most important causes of mortality, affecting the health status of the patient. At the same time, hypertension causes a huge health and economic burden on the whole world. The incidence and prevalence of hypertension are rising even among young people in both urban as well as rural communities. Although various conventional therapeutic moieties are available for the management of hypertension, they have serious flaws such as hepatic metabolism, reduced dose frequency, poor aqueous solubility, reduced bioavailability, and increased adverse effects, making the drug therapy ineffective. Therefore, it is required to design a novel drug delivery system having the capability to solve the constraints associated with conventional treatment of hypertension. Nanotechnology is a new way of using and manipulating the matter at the molecular level, whose functional organization is measured in nanometers. The applications of nanotechnology in the field of medicine provide an alternative and novel direction for the treatment of cardiovascular diseases and show excellent performance in the field of targeted drug therapy. Various nanotechnologies based drug delivery systems, such as solid lipid nanoparticles, nanosuspension, nanoemulsion, liposome, self-emulsifying systems, and polymeric nanoparticles, are available. Among them, nanoemulsion has provided a niche to supplement currently available therapeutic choices due to numerous benefits like stability, ease of preparation, enhanced drug absorption, reduced hepatic metabolism, increased dose frequency, enhanced bioavailability, and encapsulation of hydrophilic as well as hydrophobic drugs. This present review provides an in-depth idea about progression in treatment of hypertension, constraints for antihypertensive drug therapy, need of nanoemulsions to overcome these constraints, comparative analysis of nanoemulsions over other nanostructure drug delivery systems, pharmacodynamics studies of nanoemulsions for treatment of hypertension, recent patents for drug-loaded nanoemulsions meant for hypertension, and marketed formulations of nanoemulsions for hypertension.
Topics: Adolescent; Antihypertensive Agents; Drug Delivery Systems; Emulsions; Humans; Hypertension; Liposomes; Nanoparticles
PubMed: 35463984
DOI: 10.1155/2022/4109874 -
Journal of Infusion Nursing : the... 2016Intravenous fat emulsion (IVFE) is an important source of calories and essential fatty acids for patients receiving parenteral nutrition (PN). Administered as an... (Review)
Review
Intravenous fat emulsion (IVFE) is an important source of calories and essential fatty acids for patients receiving parenteral nutrition (PN). Administered as an individual infusion or combined with PN, the fats provided by IVFE are vital for cellular structural function and metabolism. The affinity of some medications to lipids has led to the use of IVFE as a treatment for any lipophilic drug overdose. This article will explain the available formulations of IVFE, administration, and maintenance issues, as well as the risks and benefits for various applications.
Topics: Antidotes; Fat Emulsions, Intravenous; Humans; Lipids; Nutrition Policy; Parenteral Nutrition
PubMed: 27828934
DOI: 10.1097/NAN.0000000000000194 -
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 -
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 -
Brain and Behavior Jun 2023To determine whether the blood-brain barrier (BBB) opens to enhance drug delivery during the acute stage of unsaturated fat embolism.
AIMS
To determine whether the blood-brain barrier (BBB) opens to enhance drug delivery during the acute stage of unsaturated fat embolism.
METHODS
We infused oleic, linoleic, and linolenic acid emulsions through the right common carotid artery of rats, followed by trypan blue for gross and lanthanum for electron microscopic (EM) examination. Doxorubicin and temozolomide were also administered, and then the rats were euthanized at 30 min, 1 h, and 2 h. Trypan blue hue was analyzed to semiquantitatively measure BBB opening. Desorption electrospray ionization-mass spectrometry (DESI-MS) imaging was used to evaluate drug delivery.
RESULTS
Trypan blue staining observed in each group 30 min after emulsion infusion increased at 1 h and decreased after 2 h in the oleic acid group. The linoleic and linolenic acid groups showed weak staining over time. The hue and trypan blue analysis results were corroborative. EM showed tight junction opening, whereas DESI-MS imaging showed increased doxorubicin and temozolomide signal intensities in ipsilateral hemispheres of all three groups.
CONCLUSION
We demonstrated that oleic, linoleic, and linolenic acid emulsions opened the BBB, promoting drug delivery to the brain. Hue analysis and DESI-MS imaging are appropriate for analysis of doxorubicin and temozolomide concentrations in brain tissue.
Topics: Rats; Animals; Fatty Acids, Nonesterified; Emulsions; Temozolomide; alpha-Linolenic Acid; Trypan Blue; Brain; Carotid Arteries; Carotid Artery, Common; Doxorubicin
PubMed: 37218399
DOI: 10.1002/brb3.2994 -
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 -
Annals of Palliative Medicine Dec 2021The purpose of this study was to evaluate the effects of monovalent and divalent cations on the stability of a fat emulsion (Lipovenoes MCT) in total nutrient admixtures...
BACKGROUND
The purpose of this study was to evaluate the effects of monovalent and divalent cations on the stability of a fat emulsion (Lipovenoes MCT) in total nutrient admixtures (TNAs) by testing the percentage of fat residing in globules >5 µm (PFAT5) values.
METHODS
TNAs with different combinations of glucose (5% and 10%), amino acids (3.35 and 4.5 g/100 mL), Na+/K+ (100/39 mmol/L), Mg2+ (3.4 and 2.7 mmol/L), and fat emulsion (2.4%) were tested in triplicate at room temperature. The pH, mean droplet size (MDS), and PFAT5 were assessed at 0, 6, 12, 24, 36, and 48 h.
RESULTS
In all seven groups, the TNA globule distribution was uniform, the pH value fluctuated in the range of 5.93-6.06, and the MDS met the limit of the United States Pharmacopeia (USP) within 48 h. The PFAT5 value of the control group 0 without electrolytes was the lowest; group 1 added monovalent ions of 139 mmol/L was significantly higher (P<0.05) but without exceed the USP limit after 48 h. Groups 2 and 3 added Mg2+ 3.4 and 2.7 mmol/L respectively, based on group 1. Group 4 increased the amino acid concentration from 3.35% to 4.5% based on group 2, and group 5 reduced the glucose concentration from 10% to 5% based on group 4. Group 6 removed monovalent ions and retained only Mg2+ based on group 5. The PFAT5 values of group 2, 3, 4, and 5 exceeded the limit after 6 h and group 6 after 12 h. There was no statistical difference between group 2 and 4 (P>0.05) or between group 4 and 5 (P>0.05).
CONCLUSIONS
When the concentration of glucose is 10-25% and the amino acid is 2.5-4.5%, The addition of monovalent ions affects the stability of fat emulsion in TNAs, however when the concentrations of Na+ ≤100 mmol/L and K+ ≤39 mmol/L, the PFAT5 value will not exceed the USP limit within 24 h. Mg2+ has a significant effect, the PFAT5 value will exceed the USP limit after 6 h when the concentration ≥2.7 mmol/L, which may cause potential safety hazards.
Topics: Drug Stability; Fat Emulsions, Intravenous; Glucose; Humans; Nutrients; Particle Size
PubMed: 35016476
DOI: 10.21037/apm-21-3353 -
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 -
Drug Delivery Dec 2022Self-emulsifying drug delivery systems (SEDDS) are a proven method for poorly soluble substances works by increasing the solubility and bioavailability. SEDDS and... (Review)
Review
Self-emulsifying drug delivery systems (SEDDS) are a proven method for poorly soluble substances works by increasing the solubility and bioavailability. SEDDS and isotropic mixtures, are composed of oils, surfactants, and occasionally cosolvents. The ability of these formulations and methods to produce microemulsions or fine oil-in-water (o/w) emulsions after moderate stirring and dilution by water phase along the GI tract might be a promising technique for lipophilic agents with dissolution rate-limited absorption. This review provides an outline of SEDDS's numerous advances and biopharmaceutical elements, types, manufacturing, characterization, limitations, and future prospects. The evaluation of SEDDS and its applications are also discussed, focusing on the advances of SEDDS's solid self-emulsifying delivery mechanism and dosage form. By integrating suitable polymer into the formulation, SEDDS may be studied for the creation of a formulation with sustained drug release. This technology's improvement might lead to a new application in the field of medicine delivery. SEDDS has been demonstrated to be quite efficient in increasing oral bioavailability of lipophilic products. SEDDS is one of the promising methods for controlling the characteristics of medications that are not great choices for oral delivery. It is also worth mentioning that SEDDS may be made in variety of solid dosage forms that are acceptable for both oral and parenteral administration.
Topics: Administration, Oral; Biological Availability; Drug Delivery Systems; Emulsions; Solubility; Water
PubMed: 35666090
DOI: 10.1080/10717544.2022.2083724 -
Molecular Pharmaceutics Sep 2023Delamanid (DLM) is a hydrophobic small molecule therapeutic used to treat drug-resistant tuberculosis (DR-TB). Due to its hydrophobicity and resulting poor aqueous...
Delamanid (DLM) is a hydrophobic small molecule therapeutic used to treat drug-resistant tuberculosis (DR-TB). Due to its hydrophobicity and resulting poor aqueous solubility, formulation strategies such as amorphous solid dispersions (ASDs) have been investigated to enhance its aqueous dissolution kinetics and thereby improve oral bioavailability. However, ASD formulations are susceptible to temperature- and humidity-induced phase separation and recrystallization under harsh storage conditions typically encountered in areas with high tuberculosis incidence. Nanoencapsulation represents an alternative formulation strategy to increase aqueous dissolution kinetics while remaining stable at elevated temperature and humidity. The stabilizer layer coating the nanoparticle drug core limits the formation of large drug domains by diffusion during storage, representing an advantage over ASDs. Initial attempts to form DLM-loaded nanoparticles via precipitation-driven self-assembly were unsuccessful, as the trifluoromethyl and nitro functional groups present on DLM were thought to interfere with surface stabilizer attachment. Therefore, in this work, we investigated the nanoencapsulation of DLM via emulsification, avoiding the formation of a solid drug core and instead keeping DLM dissolved in a dichloromethane dispersed phase during nanoparticle formation. Initial emulsion formulation screening by probe-tip ultrasonication revealed that a 1:1 mass ratio of lecithin and HPMC stabilizers formed 250 nm size-stable emulsion droplets with 40% DLM loading. Scale-up studies were performed to produce nearly identical droplet size distribution at larger scale using high-pressure homogenization, a continuous and industrially scalable technique. The resulting emulsions were spray-dried to form a dried powder, and dissolution studies showed dramatically enhanced dissolution kinetics compared to both as-received crystalline DLM and micronized crystalline DLM, owing to the increased specific surface area and partially amorphous character of the DLM-loaded nanoparticles. Solid-state NMR and dissolution studies showed good physical stability of the emulsion powders during accelerated stability testing (50 °C/75% RH, open vial).
Topics: Humans; Tuberculosis, Oral; Emulsions; Nanoparticles; Solubility; Excipients; Water; Particle Size
PubMed: 37578286
DOI: 10.1021/acs.molpharmaceut.3c00240