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International Journal of Molecular... May 2023Curcumin is the principal curcuminoid found in the rhizomes of turmeric. Due to its therapeutic action against cancer, depression, diabetes, some bacteria, and oxidative... (Review)
Review
Curcumin is the principal curcuminoid found in the rhizomes of turmeric. Due to its therapeutic action against cancer, depression, diabetes, some bacteria, and oxidative stress, it has been used widely in medicine since ancient times. Due to its low solubility, the human organism cannot completely absorb it. Advanced extraction technologies, followed by encapsulation in microemulsion and nanoemulsion systems, are currently being used to improve bioavailability. This review discusses the different methods available for curcumin extraction from plant material, methods for the identification of curcumin in the resulting extracts, its beneficial effects on human health, and the encapsulation techniques into small colloidal systems that have been used over the past decade to deliver this compound.
Topics: Humans; Curcumin; Emulsions; Solubility; Neoplasms
PubMed: 37240220
DOI: 10.3390/ijms24108874 -
European Journal of Pharmaceutics and... Jan 2022Core-shell microspheres hold great promise as a drug delivery system because they offer several benefits over monolithic microspheres in terms of release kinetics, for... (Review)
Review
Core-shell microspheres hold great promise as a drug delivery system because they offer several benefits over monolithic microspheres in terms of release kinetics, for instance a reduced initial burst release, the possibility of delayed (pulsatile) release, and the possibility of dual-drug release. Also, the encapsulation efficiency can significantly be improved. Various methods have proven to be successful in producing these core-shell microspheres, both the conventional bulk emulsion solvent evaporation method and methods in which the microspheres are produced drop by drop. The latter have become increasingly popular because they provide improved control over the particle characteristics. This review assesses various production methods for core-shell microspheres and summarizes the characteristics of formulations prepared by the different methods, with a focus on their release kinetics.
Topics: Delayed-Action Preparations; Drug Compounding; Drug Delivery Systems; Drug Liberation; Emulsions; Kinetics; Microspheres; Particle Size; Polymers
PubMed: 34861359
DOI: 10.1016/j.ejpb.2021.11.007 -
Ultrasonics Sonochemistry Mar 2023A lysozyme-oregano essential oil (Lys-OEO) antibacterial emulsion was developed via ultrasonic treatment. Based on the general emulsion materials of ovalbumin (OVA) and...
A lysozyme-oregano essential oil (Lys-OEO) antibacterial emulsion was developed via ultrasonic treatment. Based on the general emulsion materials of ovalbumin (OVA) and inulin (IN), the addition of Lys and OEO successfully inhibited the growth of E. coli and S. aureus, two representatives of which were Gram-negative and Gram-positive bacteria respectively. The emulsion system in this study was designed to compensate for the limitation that Lys could only act on Gram-positive bacteria, and the stability of the emulsion was improved using ultrasonic treatment. The optimal amounts among OVA, Lys and OEO were found to be the mass ratio of 1:1 (Lys to OVA) and 20% (w/w) OEO. The ultrasonic treatment at the power of 200, 400, 600, and 800 W and time length of 10 min improved the stability of emulsion, in which the surface tension was below 6.04 mN/m and the Turbiscan stability index (TSI) did not exceed 10. The multiple light scattering showed that sonicated emulsions were less prone to delamination; salt stability and pH stability of emulsions were improved, CLSM image showed emulsion as oil-in-water type. In the meantime, the particles of the emulsions were found to become smaller and more uniform with ultrasonic treatment. The best dispersion and stability of the emulsion were both achieved at 600 W with a zeta potential of 7.7 mV, the smallest particle size and the most uniform particle distribution.
Topics: Oils, Volatile; Emulsions; Origanum; Muramidase; Escherichia coli; Staphylococcus aureus; Particle Size; Anti-Bacterial Agents; Water
PubMed: 36871524
DOI: 10.1016/j.ultsonch.2023.106348 -
International Journal of Pharmaceutics Jun 2023The objective of the current study is the formulation development and manufacturing of solid self-emulsifying drug delivery systems (HME S-SEDDS) via a single-step...
Formulation and processing of solid self-emulsifying drug delivery systems (HME S-SEDDS): A single-step manufacturing process via hot-melt extrusion technology through response surface methodology.
The objective of the current study is the formulation development and manufacturing of solid self-emulsifying drug delivery systems (HME S-SEDDS) via a single-step continuous hot-melt extrusion (HME) process. For this study, poorly soluble fenofibrate was selected as a model drug. From the results of pre-formulation studies, Compritol® HD5 ATO, Gelucire® 48/16, and Capmul® GMO-50 were selected as oil, surfactant and co-surfactant respectively for manufacturing of HME S-SEDDS. Neusilin® US2 was selected as a solid carrier. The design of experiments (response surface methodology) was employed to prepare formulations via a continuous HME process. The formulations were evaluated for emulsifying properties, crystallinity, stability, flow properties and drug release characteristics. The prepared HME S-SEDDS showed excellent flow properties, and the resultant emulsions were stable. The globule size of the optimized formulation was 269.6 nm. The DSC and XRD studies revealed the amorphous nature of the formulation and FTIR studies showed no significant interaction between fenofibrate and excipients. The drug release studies showed significant (p < 0.05) improvement in solubility compared to the pure drug (DE = 45.04 for the optimized formulation), as >90% of drug release was observed within 15 min. The stability studies for the optimized formulation were conducted for 3 months at 40 °C/75% RH.
Topics: Fenofibrate; Drug Delivery Systems; Solubility; Drug Liberation; Hot Melt Extrusion Technology; Surface-Active Agents; Excipients; Emulsions; Drug Compounding
PubMed: 37207857
DOI: 10.1016/j.ijpharm.2023.123055 -
AAPS PharmSciTech Sep 2021Primaquine (PQ), an 8-aminoquinoline antimalarial drug, has been widely used for the eradication of hypnozoites from the liver and, therefore, recognized as the radical...
Primaquine Loaded Solid Lipid Nanoparticles (SLN), Nanostructured Lipid Carriers (NLC), and Nanoemulsion (NE): Effect of Lipid Matrix and Surfactant on Drug Entrapment, in vitro Release, and ex vivo Hemolysis.
Primaquine (PQ), an 8-aminoquinoline antimalarial drug, has been widely used for the eradication of hypnozoites from the liver and, therefore, recognized as the radical cure of malaria. However, the clinical applications of PQ are restricted to patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency due to severe dose-related hemolytic side effects. Nanoparticle carriers have shown great potential in achieving higher PQ concentrations in the target site, thereby reducing dose-related systemic toxicity caused by non-specific exposure. This work aims to develop, compare, and evaluate three PQ-loaded lipid-based drug carriers including solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and nano-emulsions (NE). The optimized PQ-SLN, PQ-NLC, and PQ-NE had a particle size of 250 nm, a PDI range of 0.1 to 0.3, a zeta potential of - 30 mV, and entrapment efficiency of ~ 90%. All lipid formulations showed sustained release in both simulated gastric and intestinal fluids over 6 h. Four empirical models - including zero-order, Higuchi, Korsmeyer-Peppas, and Hixson-Crowell models - were tested to understand the drug release mechanisms of PQ-SLN, PQ-NLC, and PQ-NE. The model fitness was found to be the highest in the Korsmeyer-Peppas model for all the PQ-loaded lipid formulations (R: 0.88-0.94). No significant changes were observed in the entrapment efficiency, particle size, and PDI of lipid formulations throughout 1 month of storage at 4 °C and 25 °C. PQ-SLN and PQ-NLC can be further lyophilized with cryoprotectants to improve long-term stability. Finally, the treatment of erythrocytes with PQ-SLN, PQ-NLC, and PQ-NE reduced erythrocyte hemolysis by approximately 4.5-fold compared to the free drug solution.
Topics: Drug Carriers; Emulsions; Hemolysis; Humans; Lipids; Nanoparticles; Particle Size; Primaquine; Surface-Active Agents
PubMed: 34590195
DOI: 10.1208/s12249-021-02108-5 -
International Journal of Nanomedicine 2022This work was aimed to develop a Curcuma oil-based self-nanoemulsifying drug delivery system (SNEDDS) 3D-printed polypills containing glimepiride (GMD) and rosuvastatin...
INTRODUCTION
This work was aimed to develop a Curcuma oil-based self-nanoemulsifying drug delivery system (SNEDDS) 3D-printed polypills containing glimepiride (GMD) and rosuvastatin (RSV) for treatment of dyslipidemia in patients with diabetes as a model for metabolic syndrome (MS).
METHODS
Compartmentalized 3D printed polypills were prepared and studied in streptozotocin/poloxamer induced diabetic/dyslipidemic rats. The pharmacokinetic parameters of GMD and RSV in the prepared polypills were evaluated. Blood glucose level, lipid profile, antioxidant, and biochemical markers activities were investigated. Also, histopathological examination of the liver and pancreas was carried out. The atherosclerotic index, the area of islets of Langerhans, and liver steatosis lesion scores were calculated.
RESULTS
The developed SNEDDS-loaded GMD/RSV polypills showed acceptable quality control characteristics with a high relative bioavailability of 217.16% and 224.28% for GMD and RSV, respectively, when compared with the corresponding non-SNEDDS pills. The prepared polypills showed dramatic lowering in blood glucose levels and substantial improvement in lipid profile and hepatic serum biomarkers as well as remarkable decrease in serum antioxidants in response to Poloxamer 407 intoxication. The prepared polypills decreased the risk of atherosclerosis and coronary disease by boosting the level of high-density lipoprotein and lowering both triglyceride and low-density lipoprotein. Microscopic examination showed normal hepatic sinusoids and high protection level with less detectable steatosis in the examined hepatocytes. Normal size pancreatic islets with apparently normal exocrine acini and pancreatic duct were also noticed.
CONCLUSION
This formulation strategy clearly shows the potential of the developed polypills in personalized medicine for treatment of patients with MS.
Topics: Administration, Oral; Animals; Blood Glucose; Emulsions; Humans; Lipids; Metabolic Syndrome; Nanoparticles; Nanotechnology; Particle Size; Printing, Three-Dimensional; Rats; Rosuvastatin Calcium; Solubility
PubMed: 35479768
DOI: 10.2147/IJN.S357356 -
European Journal of Pharmaceutical... Aug 2022Intranasally administered non-steroidal anti-inflammatory drugs (NSAIDs) offer an innovative opportunity in the field of pain management. Combination of the nasal...
Intranasally administered non-steroidal anti-inflammatory drugs (NSAIDs) offer an innovative opportunity in the field of pain management. Combination of the nasal physiological advantages such as the rich vascularization and large absorption area along with novel nanomedical formulations can fulfill all the necessary criteria of an advanced drug delivery system. Nanoemulsions represent a versatile formulation approach suitable for nasal drug delivery by increasing the absorption and the bioavailability of many drugs for systemic and nose-to-brain delivery due to their stability, small droplet size and optimal solubilization properties. In this study we aimed to develop meloxicam (MX)-loaded mucoadhesive nanoemulsions and to investigate the nasal applicability of the optimized formulations. Our results indicated the optimized nanoemulsion formulation (MX-NE3) had a droplet size of 158.5 nm in monodisperse droplet size distribution (polydispersity index of 0.211). The surface charge was -11.2 mV, which helped with the colloidal stability upon dilution at simulated nasal conditions and storage. The high encapsulation efficiency (79.2%) mediated a 15-fold drug release and a 3-fold permeability increase at nasal conditions compared to the initial MX. Proper wetting properties associated with high mucoadhesion prosper the increased residence time on the surface of the nasal mucosa. No cytotoxic effect of the formulations was observed on NIH/3T3 mouse embryonic fibroblast cell lines, which supports the safe nasal applicability.
Topics: Administration, Intranasal; Animals; Drug Delivery Systems; Emulsions; Fibroblasts; Meloxicam; Mice; Nasal Mucosa; Particle Size
PubMed: 35662634
DOI: 10.1016/j.ejps.2022.106229 -
Journal of Ocular Pharmacology and... May 2023Prostaglandin analogue topical medications are one of the most effective therapeutic approaches for the chronic management of glaucoma and ocular hypertension, through... (Review)
Review
Prostaglandin analogue topical medications are one of the most effective therapeutic approaches for the chronic management of glaucoma and ocular hypertension, through the reduction of elevated intra ocular pressure (IOP). While many of the first generations of anti-glaucoma eye drops were preserved with benzalkonium chloride, their repeated use may induce chronic ocular surface toxicity that leads to ocular surface disease (OSD) signs and symptoms. As a result, soft-preservatives and preservative-free formulations have been developed with the goal to avoid the long-term iatrogenic toxicity of the preservative agents. In addition, it has been suggested that OSD and its associated inflammation may negatively impact the efficacy of the IOP-lowering medications, including treatment adherence and compliance. Hence, it may be particularly interesting that glaucoma medications can concomitantly protect and "heal" the ocular surface and its environment while lowering elevated IOP, for the greater benefit of glaucoma patients. The objective of the present review is to briefly present the preclinical data of the cationic oil-in-water emulsion of latanoprost (latanoprost-CE) to shed some light on its mechanisms of action. It overall supports the following hypothesis: the restoration of a healthy ocular surface environment and treatment of the OSD signs and symptoms will allow for an improved elevated IOP reduction and glaucoma management. This would be achieved with a once daily dosing regimen to preserve glaucoma patients' vision, ocular surface, and quality-of-life and wellness.
Topics: Humans; Latanoprost; Glaucoma, Open-Angle; Emulsions; Intraocular Pressure; Prostaglandins F, Synthetic; Antihypertensive Agents; Glaucoma; Ocular Hypertension; Ophthalmic Solutions; Preservatives, Pharmaceutical
PubMed: 37015075
DOI: 10.1089/jop.2022.0155 -
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 -
World Journal of Gastroenterology Jan 2021The infusion of triolein emulsion (TE) induced increased vascular permeability and a negligible and temporary decrease in liver function without specific...
BACKGROUND
The infusion of triolein emulsion (TE) induced increased vascular permeability and a negligible and temporary decrease in liver function without specific histopathological damage.
AIM
To assess changes in doxorubicin concentration according to the percentage of TE infused a hepatic artery to study the vascular permeability in the rabbit liver.
METHODS
Thirty-nine healthy rabbits were divided into five groups according to the concentration of emulsified triolein infused into the hepatic arteries: Group 0, saline infusion (control group, = 5); group 1, 0.3% TE ( = 13); group 2, 0.6% TE ( = 6); group 3, 0.9% TE ( = 8); and group 4, 1.5% TE ( = 6). Doxorubicin (2.4 mg/kg) was infused immediately after TE injection the hepatic arteries. After 2 h, the livers were harvested, and doxorubicin concentrations were calculated fluorometrically. The doxorubicin concentrations were compared between TE groups and the control group, and the optimal concentrations within the TE groups were calculated. Statistical analysis was performed using the nonparametric Mann-Whitney test and Kruskal-Wallis test. < 0.05 were considered statistically significant.
RESULTS
In the liver, doxorubicin concentrations were 2.06, 2.07, 2.16 and 1.66 times higher in groups 1 through 4, respectively, and significantly higher in the TE groups than in the control group (all < 0.05). However, there were no significant differences in the mean doxorubicin concentrations between the four TE groups ( = 0.642). In the lungs, the mean doxorubicin concentrations were not significantly different between the control and TE groups ( > 0.05).
CONCLUSION
TE infusion into the hepatic arteries significantly increased the doxorubicin concentration approximately twofold but was not different between the TE groups. These findings suggest that TE infusion might be a useful adjuvant treatment of liver cancers.
Topics: Animals; Capillary Permeability; Doxorubicin; Emulsions; Hepatic Artery; Infusions, Intra-Arterial; Liver; Rabbits; Triolein
PubMed: 33510556
DOI: 10.3748/wjg.v27.i2.152