Emulsification Time Research Articles

Removal of furosemide from water by emulsion liquid membrane: Influence of experimental conditions and real water matrices

This work investigates the removal of furosemide (FSM) from low pH aqueous phase by emulsion liquid membrane (ELM). The influence of various experimental conditions on FSM permeation rate and subsequent emulsion stability, such as surfactant concentration, diluent type, stripping solution concentration, feed solution pH, stripping solution/membrane solution volume ratio, emulsification time and speed, stirring rate, initial FSM concentration, and emulsion/feed solution volume ratio, was evaluated. The ability to extract FSM in different natural complex matrices was examined. The ELM system is formed by Span 80 (5% w/w) as surfactant, hexane as diluent, NaOH (0.01 N) as stripping agent, stripping solution/membrane solution volume ratio of 1/1, treatment volume ratio of 20/200, and mixing rate of 200 rpm. The treatment process demonstrates complete removal of FSM within a remarkably short time span of 20 min. In seawater and natural mineral water, the extraction efficiency is 94.3% and 96.8%, respectively, after 20 min. Additionally, the stripping efficiency of FSM is reported to be excellent (100%), demonstrating the remarkable ability of ELM to remove and recover FSM from water. For these reasons, the ELM technique is a particularly interesting process for treating FSM-contaminated water.

Formulation Development of Solid Self-Nanoemulsifying Drug Delivery Systems of Quetiapine Fumarate via Hot-Melt Extrusion Technology: Optimization Using Central Composite Design.

Quetiapine fumarate (QTF) was approved for the treatment of schizophrenia and acute manic episodes. QTF can also be used as an adjunctive treatment for major depressive disorders. QTF oral bioavailability is limited due to its poor aqueous solubility and pre-systemic metabolism. The objective of the current investigation was the formulation development and manufacturing of solid self-nanoemulsifying drug delivery system (S-SNEDDS) formulation through a single-step continuous hot-melt extrusion (HME) process to address these drawbacks. In this study, Capmul® MCM, Gelucire® 48/16, and propylene glycol were selected as oil, surfactant, and co-surfactant, respectively, for the preparation of S-SNEDDS. Soluplus® and Klucel™ EF (1:1) were selected as the solid carrier. Response surface methodology in the form of central composite design (CCD) was utilized in the current experimental design to develop the S-SNEDDS formulations via a continuous HME technology. The developed formulations were evaluated for self-emulsifying properties, particle size distribution, thermal behavior, crystallinity, morphology, physicochemical incompatibility, accelerated stability, and in vitro drug release studies. The globule size and emulsification time of the optimized SNEDDS formulation was 92.27 ± 3.4 nm and 3.4 ± 3.38 min. The differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies revealed the amorphous nature of the drug within the formulation. There were no drug-excipient incompatibilities observed following the Fourier transform infrared (FTIR) spectroscopy. The optimized formulation showed an extended-release profile for 24 h. The optimized formulation was stable for three months (last time-point tested) at 40 °C/75% RH. Therefore, the developed S-SNEDDS formulation could be an effective oral delivery platform for QTF and could lead to better therapeutic outcomes.

Exploring the Effects of Process Parameters during W/O/W Emulsion Preparation and Supercritical Fluid Extraction on the Protein Encapsulation and Release Properties of PLGA Microspheres.

In this study, protein-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres were prepared via supercritical fluid extraction of emulsion (SFEE) technology. To understand the correlation between process parameters and the main quality characteristics of PLGA microspheres, a comprehensive prior study on the influence of process variables on encapsulation efficiency (EE), initial drug burst release (IBR), morphology, surface property, and particle size distribution (PSD) was conducted within a wide process condition range of each unit process step, from the double-emulsion preparation step to the extraction step. Bovine serum albumin (BSA), a high-molecular weight-protein that is difficult to control the IBR and EE of PLGA microspheres with, was used as a model material. As double-emulsion manufacturing process parameters, the primary (W/O) and secondary emulsion (W/O/W) homogenization speed and secondary emulsification time were evaluated. In addition, the effect of the SFEE process parameters, including the pressure (70-160 bar), temperature (35-65 °C), stirring rate (50-1000 rpm), and flow rate of supercritical carbon dioxide, SC-CO2 (1-40 mL/min), on PLGA microsphere quality properties were also evaluated. An increase in the homogenization speed of the primary emulsion resulted in an increase in EE and a decrease in IBR. In contrast, increasing the secondary emulsification speed resulted in a decrease in EE and an increase in IBR along with a decrease in microsphere size. The insufficient secondary emulsification time resulted in excessive increases in particle size, and excessive durations resulted in decreased EE and increased IBR. Increasing the temperature and pressure of SFEE resulted in an overall increase in particle size, a decrease in EE, and an increase in IBR. It was observed that, at low stirring rates or SC-CO2 flow rates, there was an increase in particle size and SPAN value, while the EE decreased. Overall, when the EE of the prepared microspheres is low, a higher proportion of drugs is distributed on the external surface of the microspheres, resulting in a larger IBR. In conclusion, this study contributes to the scientific understanding of the influence of SFEE process variables on PLGA microspheres.

Formulation and Characterization of Mefenamic Acid Self Nanoemulsifying Drug Delivery System (SNEDDS) Preparations

Mefenamic acid is included in BCS (biopharmaceutical classification system) class II, namely high permeability and low solubility. This research aims to obtain a good formula for oleic acid oil, tween 80, and PEG 400 according to the characterization test of emulsification time, % transmittance, drug loading, globule size, and zeta potential. This research was an experimental study by formulating mefenamic acid in the form of SNEDDS which was made 1 formula was made in the form of SNEDDS with the composition of oleic acid, tween 80, and PEG 400 and characterization tests were carried out for emulsification time, % transmittance, drug loading, globule size, zeta potential. The yield of the oleic acid formula is 1%, tween 80 is 8%, and PEG 400 is 1%. The emulsification time characterization test resulted in 17 seconds, % transmittance of 97%, drug loading of 179.81 mg, globular size of 85.8 nm and zeta potential of -1.6 mV.

Solubility enhancing lipid-based vehicles for artemether and lumefantrine destined for the possible treatment of induced malaria and inflammation: in vitro and in vivo evaluations

BackgroundThe lipid self-emulsifying system has been advanced as a promising delivery vehicle for improving the solubility and bioavailability of artemether and lumefantrine. However, the observed kinetic instability (propensity of lumefantrine to rapid crystallisation from nano-scale droplets) in aqueous acid has impelled some researchers to incorporate surfactants/solubilizers in the dissolution medium prior to dissolution studies. Thus, in our present work, we sought to prepare micro/large nano-scale (> 100 nm) and yet kinetically stable lumefantrine lipid self-emulsifying system (that would not require an external drug dissolution enhancing agent in the dissolution medium) and palm kernel oil-based 100 nm kinetically stable artemether lipid self-emulsifying system with rapid emulsification time. COVID-19 and Plasmodium falciparum-infected Africans with previous long exposure to malaria have manifested attenuated inflammatory cytokines more than malaria-naive patients. Therefore, the ingestion of artemether-lumefantrine with enhanced solubility may further promote blunting of cytokines. Therefore, this work was aimed at preparing (< 100 nm) stable artemether and aqueous acid-stable micro/large nano-scale (> 100 nm) lumefantrine lipid self-emulsifying system destined for improved antimalarial and anti-inflammatory activities.ResultsThe droplet sizes of all the liquid artemether and lumefantrine formulations were between 8.95–39.88 and 1018–4195 nm, respectively. The loading efficiency for all the formulations was, between 72.91 ± 2.89 and 100.00 ± 0.29%. All the artemether and lumefantrine batches emulsified within the range of 3.90 ± 0.69 to 12.26 ± 0.69 s. Stable and transparent emulsions were formed on aqueous dilution to 1000 ml. The percentage drug released for artemether and lumefantrine ranged from 76.25 ± 2.98 to 99.22 ± 1.61%. The solid lipid self-emulsifying systems produced, had fair and passable flow properties. Differential scanning calorimetry revealed that the solid artemether and lumefantrine lipid self-emulsifying system were amorphous. Solidification with Neusilin FH2 or surfactant replacement with Kolliphor EL and Kollidon VA 64 fine prevented micro-or large nano-scale lumefantrine lipid self-emulsifying system from crystallisation in aqueous acid (pH 1.2). Higher antimalarial activity and remarkable anti-inflammatory effects (P < 0.05) favoured the lipid self-emulsifying formulations.ConclusionOptimal in vitro and in vivo results (enhanced antimalarial and anti-inflammatory activities) were obtained with kinetically stable lumefantrine micro/large nano-scale droplets and kinetically stable palm kernel oil-based (< 50 nm) artemether lipid self-emulsifying system droplets.

Extraction of Alpha-cypermethrin Pesticides from Aqueous Solution by Emulsion Liquid Membrane

This research examines the emulsion liquid membrane (ELM) extraction efficiency and stability to abstraction of alpha-cypermethrin pesticides from aqueous solution when blended surfactants are used in the liquid membrane composition. The stability of the membrane was examined in the aspect of the emulsion breakdown time and distribution of droplet size. The ingredients employed in ELM were Span80 (sorbitan monooleate) and Tween80 (polyoxyethylene sorbitan monooleate) as surfactants and a mixture of kerosene, sunflower oil (3:7) as diluents and stripping agent was used sodium hydroxide (NaOH). Some parameters were assessed, including the value of Hydrophilic Lipophilic Balance (HLB), blended surfactant concentration, homogenizer speed, emulsification time, and NaOH concentration as a stripping agent. According to the results, a stable emulsion was created at HLB (5.37), blended surfactant 3 % (w/v), 12,700 rpm of homogenizer speed, 9 min of emulsification time, and 0.05 N of NaOH. Under these circumstances, 89.2 % of the alpha-cypermethrin was extracted with 1.8 % emulsion breakage. As a result, the combinations of (Span80 with Tween80) have enormous potential as surfactants and they can improve the stability of the emulsion. Additionally, completed was mass transfer investigation and extraction kinetics

ADVANCEMENTS IN CIVIL EXPLOSIVES: NOVEL FORMULATIONS AND SUSTAINABLE FUEL SOLUTIONS

ABSTRACT. The article presents the development of a new explosive mixture based on agricultural ammonium nitrate, possessing high detonation capability, increased water resistance, and physical stability. The concept for its creation is based on obtaining an oil-in-water (O/W) type microemulsion, produced using vegetable oil. Calculations conducted showed that the use of 100 % rapeseed oil methyl esters compared to diesel fuel improves emulsification by 14 %, reducing emulsification time by 15 %. Due to the structure of the microemulsion, ordinary agricultural ammonium nitrate can successfully retain around 7.5 % of the microemulsion. This amount of fuel phase is sufficient for obtaining an explosive composition with an appropriate oxygen balance. Substituting the porous ammonium nitrate (PAN) with agricultural ammonium nitrate - the cheapest oxidizer for the production of the newly developed explosive mixture, reduces its production cost and significantly increases the competitiveness of the product.

Screening of Process Parameters for Aspirin Loaded PLGA Microsphere

Background amp Aim Aspirin a non-steroidal anti-inflammatory drug has the potential to stimulate various dental stem cells and promotes regeneration of dental tissues. Polylactic glycolic acid PLGA a biocompatible and biodegradable polymer has the potential to stimulate multiple processes such as proliferation osteogenic differentiation initiation of mechanical support and formation of three-dimensional niches for the growth of new tissue. Hence this study aimed to identify the most effective formulation and process variables for developing aspirin polylactic glycolic acid microspheres using the Placket-Burman method.Method In the screening study Placket-Burman screening was systematically employed to estimate all of the parameter effects and interactions. The microspheres were formulated using the double-emulsion solvent extraction method by varying various variables and performing statistical analysis. Eight independent variables were considered for screening with encapsulation efficiency as the dependent variable. These variables included the volume of the internal phase of primary emulsion solvent system ethyl acetate ethanol homogenization time stirring speed emulsification time flow rate poly vinyl alcohol concentration and PLGA concentration.Results Encapsulation efficiency varied between 50.11 and 88.98. The concentration of PLGA and Poly vinyl alcohol and the volume of the internal phase were found to have a significant influence on encapsulation efficiency in the synthesis of Aspirin PLGA microsphere.Conclusion Among the eight independent variables assessed for screening the concentrations of PLGA and polyvinyl alcohol and the volume of the internal phase were found to significantly impact the encapsulation efficiency in the formulation of aspirin PLGA microspheres.

Optimization of Soursop (Annona muricata L.) Leaf Extract in Nanoemulgel and Antiacnes Activity Test Against Propionibacterium acnes, Staphylococcus aureus, Staphylococcus epidermidis Bacteria

Soursop leaf extract (Annona muricata L.) has antibacterial activity with active components of alkaloids, flavonoids, steroids, and saponins. This research aims to optimize the use of VCO, Tween 80, and PEG 400 in the nanoemulsion system, which will be added Carbopol 940 as a gelling agent to form a nanoemulgel and to determine antibacterial activity. By utilizing the simplex lattice design method in Design Expert 13.0, the nanoemulsion formula has been successfully optimized involving a mixture of VCO, Tween 80, and PEG 400. A total of 14 different nanoemulsion formulas were produced through this process. The process of making nanoemulsion is carried out by mixing extracts, oils, surfactants and cosurfactants, homogenized using a vortex, then sonicated. Evaluation of % transmittance, emulsification time, and pH were carried out to determine nanoemulsion physical properties. The nanoemulsion optimal formula was evaluated for particle size, polydispersity index, and zeta potential and made into nanoemulgel with the addition of Carbopol 940. The optimal formula has a composition of 10.86% VCO, 67.33% Tween 80, 21.81% PEG 400 form homogeneous and clear nanoemulsion with % transmittance of 91.97±1.11%, emulsification time of 56.42±0.72 seconds, and pH of 5.67±0.24. Particle size, polydispersity index, and zeta potential of the optimal formula were 229.47±38.79 nm, 0.41±0.10, and -39.13±0.19 mV, respectively. Evaluation of nanoemulgel physical properties showed homogeneous, pH value of 5.83±0.24, spreadability of 5.57±0.25 cm, adhesive force of 3.80±0.25 seconds, viscosity of 11479.33±167.49 cP, antibacterial activity against P. acnes, Staphylococcus aureus, and Staphylococcus epidermidis with inhibition zone diameters of 9.67±0.47 mm, 7.33±0.47 mm, and 5.67±0.47 mm. respectively. Nanoemulgel soursop leaf extract has suitable physical properties, and antibacterial activity is in the medium category.

Optimization and Characterization of Fenofibrate Self-Nanoemulsifying Drug Delivery System (SNEDDS) Preparations

Fenofibrate is a third-generation fibric acid derivative included in BCS (biopharmaceutical classification system) class II, namely high permeability, low solubility. This research aims to obtain the optimum formula for miglyol oil, cremophor RH 40 and PEG 400 according to characterization tests of emulsification time, % transmittance, drug loading, globule size, and zeta potential. This research is an experimental study by formulating fenofibrate in the form of SNEDDS, which was made in 16 formulas using the D-optimal method, which was formulated in the form of SNEDDS with the composition miglyol, cremophor RH 40 and PEG 400 and characterization tests were carried out for emulsification time, % transmittance, drug loading, size. globules, zeta potential to obtain the optimum formula, and then analyzed using the one sample T-Test. The optimization results obtained the optimum formula, namely miglyol at 4%; cremophor RH 40 is 5%, and PEG 400 at 1%. Characterization test: emulsification time was 24 seconds, Transmittance % was 98.7%, Drug loading was 181 mg, globule size was 126 nm, and zeta potential of 12.26 mV. The dissolution test of the fenofibrate capsule dissolved 57.05%, while the fenofibrate SNEDDS capsule was 64.86%. This means that the dissolution of the optimum formula for SNEDDS fenofibrate is better than pure fenofibrate.

Formulation and in vitro characterization of nanoemulsions containing remdesivir or licorice extract: A potential subcutaneous injection for coronavirus treatment

The management of coronavirus necessitates that medicines are available, reasonably priced, and easy to administer. The work aimed at formulating and characterizing remdesivir and licorice extract nanoemulsions and comparing their efficacy against coronavirus for further subcutaneous injection. First, the solubility of remdesivir was determined in different oils, surfactants, and co-surfactants to choose the optimal nanoemulsion components. Nanoemulsions were optimized concerning surfactant: co-surfactant ratio (5:1, 4:1, 3:1, 2:1, and 1:1) and oil to surfactant: co-surfactant ratio (1:9, 1:8, 1:7, 1:6, 1:5, 1:4, 1:3, 1:2, and 1:1). The formulations were evaluated concerning % transmittance, emulsification time, pH, viscosity, droplet size, polydispersity index, zeta potential, drug content, transmission electron microscopy, in-vitro drug release, stability (of the optimal formulas), and antiviral effect against coronavirus. The optimal nanoemulsion formula was F7, exhibiting an acceptable pH level, a rapid emulsification rate, a viscosity of 20 cP, and 100% drug content. The formulation droplet size was 16 and 17 nm, the polydispersity index was 0.18 and 0.26, and the zeta potential was − 6.29 and − 10.34 mV for licorice extract and remdesivir nanoemulsions, respectively. However, licorice extract nanoemulsion exhibited better release and physical stability. Licorice extract nanoemulsion may be a potential subcutaneous injection for combating mild to moderate coronavirus.

Highly effective emulsion liquid membrane based on Triethylamine for extraction of heavy metals: Investigation of extraction, de-extraction, swelling, and osmotic pressure gradient

The aim of this work is to produce a stable W/O primary emulsion which is able to extract a wide variety of heavy metals, namely Cu2+, Zn2+, Pb2+, Ni2+, Co2+ and Hg2+. The appropriate conditions through which a better extraction was obtained are: concentration of Span 80 (4 wt%); concentration of TEA (10 wt%); internal phase (HCl 0.5 M); emulsification time (4 min); Vmemb/Vint (2.08); Vemul/Vext (0.1); pH of the external solution (4.7) and stirring speed (150 rpm). A second recycling of the emulsion resulted in a drop in extraction about 40 %. The morphological study confirmed a good dispersion of internal globules and a good stability of emulsion for up to 60 days. The extraction of metal cations showed very high extraction (> 90 %) with very fast kinetics. However, it has been shown that the type of anion to which the metal cation is bound, only affects the extraction efficiency above 100 mg/L. Results extraction of heavy metals are in good analogy with evolution of the osmotic pressure difference between the internal and external phases, leading to a significant swelling of emulsion, while de-extraction also appears to be in accord with extraction with a slightly slower rate.

Formulation Of Self Micro-emulsifying Drug Delivery System For Ketoconazole

The present investigation was undertaken with an objective to prepare the SMEDDS of ketoconazole in order to improve the bioavailability of lipophilic drugs. A ternary phase diagram was constructed in the absence of ketoconazole. The results revealed that span 60 and PEG 600 used in ratios of 2:1 (F17-18) and 3:1 (F23-24) exhibited largest micro-emulsion area and shortest emulsification time (less than 1 min). It was observed that with increase in the ratio of the PEG 600, spontaneity of the self-emulsification process got increased. A fixed ketoconazole concentration of 5% w/w was selected to be loaded in all self-emulsifying formulations. The prepared formulations were kept in closed containers and tested for thermodynamic stability. All the formulations passed the thermodynamic stability studies without any signs of phase separation and precipitation during alternative temperature cycles (4°C and 40°C), freeze thaw cycles (-21°C and +25°C) and centrifugation at 10,000 g indicating good stability of formulations and their emulsions. The in vitro dissolution studies revealed the drug release profiles for the SMEDDS. All the formulations exhibited quick drug release characteristics and almost complete drug release in 15-20 minutes. In contrast, the pure drug exhibited only a maximum of 39.63% release in 60 min duration.

Development of Linagliptin Ultra Fine Solid Supersaturated Bio-SNEDDS Using Triangular Mixture Design for Enhancement of Oral Bioavailability: Impact of P-gp Inhibition

Linagliptin (LIN) is a newly developed dipeptidyl peptidase 4 (DPP-4) inhibitor oral antidiabetic drug. LIN is considered a P-gp substrate, thus suffers from poor bioavailability (&lt; 30%). The aim of this study was to develop and characterize LIN bioactive self-nanoemulsifying drug delivery system to circumvent its poor bioavailability and enhance its therapeutic efficacy.&#x0D; Methodology: In this study, we developed solid supersaturated bioactive self-nanoemulsifying drug delivery system (Ss-bio-SNEDDS) of LIN, using clove oil as an oil phase, cremophor CO 40 as a surfactant, labrasol as a co-surfactant and Hydroxy-propyl-B-cyclodextrin (HPBCD) as a precipitation inhibitor (PI); all components are of established P-gp inhibition activity. Optimization was performed by means of triangular mixture design based on particle size, poly dispersity index (PDI) and percent transmittance. The two optimized formulations (F4 and F8) were designated and evaluated for stability and cloud point. Also, the effect of pH on particle size and PDI was assessed. Additionally, examination of particles’ surface morphology of the two optimized formulations was performed by transmission electron microscope (TEM). The prepared liquid supersaturated-SNEDDS (s-SNEDDS) were converted into solid supersaturated-SNEDDS (Ss-SNEDDS) via adsorption on microcrystalline cellulose (MCC). Further evaluations were carried out, including in vitro drug release, in vitro precipitation and in vivo studies.&#x0D; Results: The optimized formulations F4 and F8 manifested promising characteristics concerning particle size (&lt; 50 nm), PDI (&lt; 0.3) and percent transmittance (&gt; 99%). Stability study showed no phase separation or precipitation with rapid emulsification time. The two optimized formulations showed high cloud point temperature (above 70°C). TEM images of F4 and F8 showed spheroid like appearance with relatively smooth surface. Results of the in vivo study in rats revealed a significant increase in AUC of solid-F4, solid-F8 and solid supersaturated-F4 (S-F4, S-F8 and Ss-F4) by 2.32, 2.89 and 2.54 folds, respectively compared to LIN solution; with a noticeable reduction in blood glucose level at each point.&#x0D; Conclusion: In a nutshell, Ss-bio-SNEDDS are considered as auspicious nano-carriers for LIN with the virtue of augmented bioavailability and possible dose reduction.&#x0D;

Copper Extraction Using LIX 84 as a Mobile Carrier in the Emulsion Liquid Membrane Process

Extensive research has been conducted to address the growing global demand for copper by exploring effective methods of extraction and recovery across various industries. The emulsion liquid membrane (ELM) has emerged as a viable option for efficiently extracting and recovering metals from waste solutions. Due to its advantageous features, the extraction and recovery of copper from a simulated copper solution was investigated. In the ELM, various parameters can affect the stability and efficiency of copper extraction which include agitation speed, treat ratio (TR), stripping agent, and carrier concentration. However, certain parameters such as homogenizer speed, emulsification time, surfactant concentration, extraction time, and pH of the simulated feed solution were kept constant in this study. The most favourable parameters for achieving maximum copper extraction and recovery were determined such as TR of 1:3, agitation speed (250 rpm), LIX 84 (0.2 M) in kerosene as the carrier, and H2SO4 (0.5 M) as the stripping agent. Using these conditions, approximately 74% of the copper was extracted while 37% was recovered with an acceptable ELM stability indicated by a 20% membrane swelling. This research demonstrates the significant potential of the ELM process for extracting copper from wastewater generated by various industries.

FORMULATION AND IN VIVO EVALUATION OF PEMIGATINIB SUPER SATURABLE SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM

Objective: Pemigatinib is an active component in treatment of cholangiocarcinoma, but the low solubility and bioavailability of Pemigatinib limit its wide application. The aim of the present study was to prepare and evaluate supersaturable self-nanoemulsifying drug delivery systems (sSNEDDS) followed by investigating and comparing the pharmacokinetic profiles of Pemigatinib and Pemigatinib sSNEDDS in rat plasma by HPLC. Methods: Pemigatinib loaded SNEDDS were obtained by dissolving drug in the isotropic mixture of oil, surfactant, and co-surfactant. The conventional SNEDDS were converted to sSNEDDS by precipitation method by using an experimented polymer. An appropriate high sensitivity and selectivity was applied to the comparison of plasma pharmacokinetics in Pemigatinib and Pemigatinib sSNEDDS using Entrectinib as an internal standard (IS). Results: The droplet of sSNEDDS ranges from 166.78±3.14 to 178.86±1.24 nm with PDI 0.212–0.256, transmission electron microscopy images revealed the spherical shape of the nanodroplets, emulsification time was 15 secs when added to physiological fluids, percent transmittance of the diluted formulation was 99.12±0.46, and viscosity was 574±26 centipoises indicating the good flow ability. FTIR and DSC studies indicated the amorphization of the drug. The dissolution profile of sSNEDDS indicated the faster release of drug compared to both pure drug suspension and SNEDDS formulation. Cmax of the sSNEDDS 3.52±0.13ng/ml was significant (P&lt;0.05) as compared to the pure drug suspension formulation 2.82±0.42 ng/ml. The AUC0-t, AUC0–∞ of sSNEDDS was increased, while the Tmax and t1/2 was decreased. Moreover, the AUC value in the sSNEDDS group was significantly increased and the relative bioavailability was calculated to be 69% when compared with that of the Pemigatinib group. Conclusion: These results concluded that Pemigatinib sSNEDDS when compared with pure drug after a single oral administration and the formulation modification of Pemigatinib into sSNEDDS can effectively enhance gastrointestinal absorption and relative bioavailability by improving solubility and dissolution rate.

Interactions Among Temperature, pH, and Agitation May Cause Instability in an Oil-in-water Emulsion

Introduction: Two key features of an emulsion, stability and viscosity, are not only considered dependent on ingredient quantities but also delicately affected by emulsification conditions, such as pH, temperature, and mixing conditions. Methods: In the laboratory, we formulated an O/W emulsion made up of 41% water, 9.8% silicon (polydimethylsiloxane), 22.1% liquid sucrose (700 mg/ml), 22.1% light liquid paraffin, and 1.5 to 5% paraffin emulsifier by volume % purposed for large-scale production as a rubber coating for decorative purposes. Results: This emulsion became faulty after large-scale production, while it was fine on the laboratory scale. This study investigated the probability of a complicated interaction among pH, temperature, solutes, and agitation intensity on the stability and viscosity of our emulsion by focusing on sugar degradation effects on these parameters. This emulsion was made in two different temperatures and agitation rates, and the emulsification time was 20 minutes for all samples. The critical roles of appropriate pH regulators or buffers in the stability were also investigated. Conclusion: It was found that applying intense agitations at 1500 rpm during emulsifications in high temperatures may lead to absurdly high emulsion viscosity, accompanied by a sharp pH fall.

Natural microbial surfactant containing self-nanoemulsifying formulation with improved performance of paclitaxel therapy: A newer avenue in breast cancer treatment

Due to the presence of a high concentration of surfactants (e.g., Cremophor EL, Tween 80), paclitaxel (PTX) drug delivery systems administered orally and intravenously demonstrate severe toxicity. In the current research work, a unique self-nanoemulsifying drug delivery system (SNEDDS) comprising surfactin, a microbial biosurfactant was used for reducing the formulation toxicity and improving the biopharmaceutical performance. The preformulation study including solubility analysis indicated suitability of corn oil as the natural lipophile. Nanoemulsion boundaries were delineated by aqueous titration of the lipid phase (ethyl oleate: plurol oleique), surfactants (Tween 80 and Surfactin) and cosolvent (Transcutol HP) to identify the optimum compositions on the basis of formulation quality attributes with globule size <250 nm, emulsification time <3 min and in vitro drug release >85% in 60 min. Biocompatibility evaluation of PTX-Surfactin SNEDDS on rat hepatocytes by H2DCF assay to determine the ROS level indicated an insignificant increase in fluorescence intensity, while PTX Tween 80-SNEDDS showed nearly 20% increase in ROS levels compared to the control cells. Furthermore, histopathology examination showed the absence of any signs of inflammation from intestinal segments treated with PTX Surfactin-SNEDDS, while PTX Tween 80-SNEDDS revealed infiltration of cells and the presence of inflammation on the intestinal villous microstructures. The anticancer activity evaluation by in vitro cytotoxicity on MCF-7 cells showed PTX Surfactin-SNEDDS and PTX Tween 80-SNEDDS with IC50 of 2.65 μM and 11.52 μM, respectively, while PTX suspension showed IC50 of 18.5 μM. Moreover, blank Surfactin-SNEDDS showed IC50 of 15.23 μM, while no cytotoxicity was observed for blank Tween 80-SNEDDS. Overall, the study interpreted high suitability of biosurfactant for developing the self-nanoemulsifying formulation of PTX with enhanced bioavailability, biocompatibility and synergistic improvement in the anticancer activity over the formulations containing synthetic surfactant.

Enhancement of Icariin Aphrodisiac Effect by Solid-SNEDDS Method Using Shark Liver Oil Phase

The Epimedium brevicornu Maxim plant contains icariin, a flavonoid compound known for its aphrodisiac effects. However, icariin has low solubility and bioavailability. This study aims to find the best formula for S-SNEDDS icariin, its physical properties, characteristics, and aphrodisiac activity. Using the S-SNEDDS (Solid-Self Nanoemulsifying Drug Delivery System) method with shark liver oil phase is expected to increase the solubility and bioavailability of icariin. The optimum formula used is tween 80 (72.5%): PEG 400 (13.75%) and shark liver oil (13.75%). The optimal formula of S-SNEDDS icariin with the adsorption method to solid carriers requires aerosol 200 as much as 783±28.86mg per 1mL. S-SNEDDS icariin has characteristics with an average emulsification time of 12.88±0.26 seconds, transmittance value of 98.08±0.94%, droplet size 171.8±8.9 nm, zeta potential -35.2±1.1 mV, flow speed less than 10 seconds, resting angle 35.159°. The dissolution test of S-SNEDDS icariin is better than icariin instead of S-SNEDDS. S-SNEDDS icariin dose 50 mg/KgBW has a better aphrodisiac effect than pure icariin 100 mg/kgBW.

Self-emulsifying drug delivery systems (SEDDS): How organic solvent release governs the fate of their cargo

Organic solvents are commonly used in self-emulsifying drug delivery systems (SEDDS) to increase payloads of orally administered poorly soluble drugs. Since such solvents are released to a varying extent after emulsification, depending on their hydrophilic nature, they have a substantial impact on the cargo.To investigate this impact in detail, quercetin and curcumin as model drugs were incorporated in SEDDS comprising organic solvents (SEDDS-solvent) of logP < 2 and > 2. SEDDS were characterized regarding size, payload, emulsification time and solvent release. The effect of solvent release on the solubility of these drugs was determined.Preconcentrates of SEDDS-solventlogP < 2 emulsified more rapidly (< 1.5 min) forming smaller droplets than SEDDS-solventlogP > 2. Although, SEDDS-solventlogP < 2 preconcentrates provided higher quercetin solubility than the latter, a more pronounced solvent release caused a more rapid quercetin precipitation after emulsification (1.5 versus 4 h). In contrast, the more lipophilic curcumin was not affected by solvent release at all. Particularly, SEDDS-solventlogP < 2 preconcentrates provided high drug payloads without showing precipitation after emulsification.According to these results, the fate of moderate lipophilic drugs such as quercetin is governed by the release of solvent, whereas more lipophilic drugs such as curcumin remain inside the oily phase of SEDDS even when the solvent is released.