Globule Size Research Articles

Fabrication of basil oil Nanoemulsion loaded gellan gum hydrogel—evaluation of its antibacterial and anti-biofilm potential

The pathogenic suppression of infectious agents is an ongoing strategy to tackle threats from microbial infections. In this regard, we developed and characterized a stable basil oil nanoemulsion-filled hydrogel that combats microbial pathogenicity and enhances the antimicrobial potential. Basil oil was extracted from Ocimum basilicum using the hydrodistillation extraction method. Furthermore, bioactive compounds of extracted basil oil were identified using GC-MS. Basil oil nanoemulsion (BNE) was developed using the ultrasonic emulsification method by incorporating basil oil, span 60, and water. Later, the formulated nanoemulsions were grafted with the gellan gum-based hydrogel matrix. The BNE was evaluated for globule size, zeta potential, FTIR analysis, and surface texture by SEM. A study was conducted to analyze antimicrobial sensitivity, the minimum inhibitory concentration, anti-biofilm potential, and membrane integrity for gram-positive, gram-negative bacterial and fungal strains. The BNE formed with minimum droplet dimensions of 49.2 nm with a zeta-potential of −33 mV showed much more kinetic stability. The developed basil oil nanoemulsion hydrogels (BNEHs) showed enhanced antibacterial activity against Bacillus subtilis and staphylococcus aureus with their ability to impair the consistency of the cell membrane. In addition, the BNEH reported a 20% increase in antibiofilm activity than BNE. The findings demonstrate the possibility of using BNE and BNEH against different microbial pathogens such as potential anti microbial and anti biofilm agents. Further it could be tested for its topical delivery efficacy.

Formulation Development, Optimization, and Characterization of Cilnidipine-Loaded Self-microemulsifying Drug Delivery System

Cilnidipine, a 2, 4-dihydropyridine antihypertensive, is poorly bioavailable and belongs to Biopharmaceutical Classification System Class II. The present study was carried out to develop and evaluate a cilnidipine-loaded self-microemulsifying drug delivery system (SMEDDS) using food grade oil for enhanced pharmacokinetic parameters. The SMEDDS was prepared by low-energy method. A pseudo-ternary phase diagram was developed using triacetin, Tween 20, and Transcutol HP as oil, surfactants, and cosurfactants, respectively. The statistically optimized formulation was obtained and was evaluated for relevant in vitro characterizations. Globule size, zeta potential, and polydispersity index (PDI) of the optimized formulation were found to be 9.045 nm, −2.32 mv and 0.203, respectively, indicating stable and uniformly distributed microemulsion nature of the formulation. Developed SMEDDS of viscosity 31 cps was found to be clear in 500 times dilution in water and phosphate buffer pH 1.2. Selection of the optimized SMEDDS was followed by various formulation characteristics, including goat intestinal membrane permeability. The in vitro dissolution study of optimized SMEDDS exhibited much better result as compared to the marketed tablet of cilnidipine.

THE USE OF CARROT SEED OIL (DAUCUS CAROTA L.) TO FORMULATE NANOEMULGELS AS AN EFFECTIVE NATURAL SUNSCREEN AND SKIN ANTI-AGING

Objective: The purpose of this study was to develop a nanoemulgel containing vegetable oil of carrot seed oil as an effective natural sunscreen and skin anti-aging. Methods: Nanoemulgels containing 4% carrot seed oil were formulated in three formulas with different ratios of Tween 80 and Sorbitol and prepared by using the high-energy emulsification method. The nanoemulgels were determined for the organoleptic characteristic, globule size, pH, physical stability during storage for 12 w at three different temperatures (room, high and low temperature), centrifugation, and cycling test. The Sun Protection Factor (SPF) value was determined by UV spectrophotometric method and the effectiveness of anti-aging was evaluated by using a skin analyzer and the results were compared with sunscreen emulgel. Results: Nanoemulgel containing 4% carrot seed oil with a ratio of Tween 80 as surfactant and Sorbitol as co-surfactant 40 and 20 resulted in the smallest mean droplet size of 338.34 nm and the sizes were increased during 12 w of storage at room temperature but still in the nano size and this nanoemulgel did not show phase separation or still stable. These nanoemulgels were also stable after the centrifugation and cycling test. The emulgel preparation was not stable or showed phase separation after the centrifugation test. The SPF value obtained from the nanoemulgel was 20.28±0.22 and these values were higher than the sunscreen emulgel (13.94±0.27). The pore size, spot, and wrinkles of the volunteer skin were reduced after using the nanoemulgel containing 4% carrot seed. Conclusion: The sunscreen and skin anti-aging activity of nanoemulgel preparation containing 4% carrot seed oil with a ratio of surfactant Tween 80 and co-surfactant Sorbitol 40 and 20 were more effective compare with emulgel preparation.

Glycerin diet affects the size of the fat globule and the fatty acid profile of goat's milk

The objective of this study was to evaluate the production, fat and fatty acids of milk as well as the diameter, classification and quantity of the milk fat globules (MFG) of goats consuming a diet with 15% of crude glycerin. Twelve multiparous Saanen goats weighing 40 ± 6 kg and 90 ± 5 days of lactation were used. The experimental design was completely randomized with two treatments (0 and 15% inclusion of glycerin). In this way, each milk sample is classified according to the percentage of milk fat globules that were included in these three size categories. For the variables milk production, fat, diameter, medium and large fat globules and amount of globules showed a significant effect of the inclusion of glycerin in the diet (p < 0.05). Fifteen fatty acids were found, mostly saturated. For caprylic, palmitic, and linoleic fatty acids, there was no significant influence of the inclusion of glycerin (p > 0.05). Can recommend the use of 15% double-distilled glycerin in the feeding of lactating goats increased milk production, the amount of fat, increased the size of the milk fat globule. Regarding the saturated and polyunsaturated fatty acids, they kept the level of 15% of glycerin.

Investigation of the process of structure formation during ultrasonic homogenization of milk

The article studies the processes of structure formation of milk during homogenization carried out on various equipment. A comparative analysis of the distribution of the sizes of fat globules before and after homogenization is given. The formulation of the probability mathematical model of milk and milk mixture homogenization give the opportunity to identify the real variabilities of the textural composition of milk and milk mixture in optimum performance with the use of statistics facts about dynamics of the fat globules size. The foundation for developing such model was used for experimental results of fat globules within the ultrasound process. The dependences of the density distribution of the sizes of fat globules after ultrasonic treatment are given. Obtained dependences allow conducting statistics analysis of the homogenization of food mass for the evaluation of its total effectiveness and determination of defects.

The gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulations

The objective of the study was to evaluate the gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulation. Mucilage was extracted from the fruits of Dillenia indica using established methods and characterized by rheology and swelling. Emulsion (F1) was prepared using the continental emulsification method. Gelling agents (2 %w /v) were prepared by dispersing in distilled water with constant stirring at a moderate speed using a magnetic stirrer. F1 was added to the gel (0-75 %w /w) to obtain emulgel formulations and evaluated using viscosity, globule size, pH, release profiles and kinetic modeling. Data were expressed as mean ± SD, and similarity factor (f2) was used to compare all formulations. Formulation viscosity was significantly higher with carbopol than with Dillenia; globule sizes increased with concentration of gelling agents, and pH reduced as the concentration of Dillenia increased. All formulations showed controlled release properties with t80 ranging between 114 and 660 min. The release was governed by Korsmeyer-Peppas model. Formulation F5 prepared with 50 % Dillenia showed highest similarity to F4 prepared with 75 %w /w carbopol. Dillenia indica demonstrated acceptable gelling properties comparable with that of carbopol and could be improved for use in emulgel formulations.

Formulation and Evaluation of Self Micro-Emulsifying drug delivery System of Carvedilol

The current work involves preparation and evaluation of self-micro emulsifying drug delivery system of carvedilol, an nonselective betablocker and alpha-1 blocker. Oral self micro-emulsifying drug delivery system of Carvedilol were prepared by studying the solubility in different oils, surfactants and co-surfactants and formulations were prepared using mixtures of oils, surfactants, and cosurfactants in various proportions. Based on the solubility study, the optimised self micro-emulsifying drug delivery system of carvedilol was prepared using Capryol 90 as oil phase and tween 20 and transcutol P as surfactant and co-surfactant, respectively. The formulations were evaluated for stability, globule size and in vitro performance. To estimate the drug content from various excipients, final microemulsion formulations and in vitro performance study, a stability-indicating validated high-performance liquid chromatography method was developed using Inertsil ODS-3V (150 mm×4.6 mm, 5 μm) high-performance liquid chromatography column. The method was validated for various parametes like accuracy, linearity, precision (intraday and interday) and robustness. All the validation parameters were in acceptable range. The developed method was found to be specific accurate and robust for estimation of carvedilol from its microemulsion formulations.

Formulation and Evaluation of Dolutegravir Sodium Nanoemulsion for the Treatment of HIV

The purpose of this research was to develop and evaluate the Nanoemulsion of Dolutegravir sodium. Nanoemulsion was made by the high-shear homogenization method. Materials and method: Oleic acid was used as the oil phase, Tween 80, and Acconon&nbsp;MC8-2&nbsp;EP/NF (Smix; 1:1) were utilized as surfactant and co-surfactant respectively while distilled water was employed as an aqueous phase. The formulations were evaluated based on globule size, zeta potential, pH, viscosity, percentage transmittan

Microstructure and biomolecules mobility of human milk fat globules by fluorescence recovery after photobleaching with confocal scanning laser microscope

This work demonstrates the use of fluorescence recovery after photobleaching (FRAP) for direct measurement of the microstructure and biomolecules mobility of human milk fat globules (HMFGs). In particular, five fluorescent probes (three types), Nile Red, Rh-DOPE, NBD-PC, NBD-SM, and Nile Blue, were evaluated in a Confocal scanning laser microscope combined with FRAP for the detection of the molecular diffusion of neutral lipids, polar lipids and membrane proteins in HMFGs. Mobile fraction (Mf), half-life recovery time (t1/2) and diffusion coefficient (K) were calculated from the FRAP recovery curve of five fluorescent molecules. The Mf of fluorescent probes labeled neutral lipids, polar lipids, membrane proteins, phosphatidylcholine, sphingomyelin, and on HMFGs were 63%, 18%, 45%, 28% and 5%, respectively. The recovery times of fluorescent molecules labeled with membrane biomolecules were longer as the size of the milk fat globules decreased and the photobleaching area increased. This method was applied to the HMFG membrane cytoplasmic remnants (CR) region showing a similar trend and much higher fluorescence intensity to the membrane region, which suggests that CR might contain multiple layers of membrane lipids.

Effects of Using Soybean Protein Emulsion as a Meat Substitute for Chicken Breast on Physicochemical Properties of Vienna Sausage.

The aim of this study is to determine the effects of using emulsion manufactured with soybeans (ES) to substitute chicken breast in Vienna sausages. Four types of Vienna sausages (S1: 10% ES and 50% chicken, S2: 20% ES and 40% chicken, S3: 30% ES and 30% chicken, and S4: 40% ES and 20% chicken) for this study were made. The pH, color, proximate composition, sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), microphotographs, cooking yields, and texture profile analysis of sausages were examined. The pH value of uncooked and cooked sausages increased significantly with increasing ES content (p<0.05). The crude protein contents of S2, S3, and S4 were significantly higher than that of the control (p<0.05). Furthermore, the SDS-PAGE results showed that α-conglycinin, β-conglycinin, and the acidic subunit of glycinin all increased with increasing ES content. Microphotographs revealed that increasing the ES content decreased the size of fat globules. The cooking yields of samples increased significantly with increasing ES content (p<0.05). The hardness values of ES treated samples were significantly lower than that of the control (p<0.05). Therefore, 30% substitute of chicken breast with ES can improve the quality and structure of Vienna sausage, without inducing critical defects.

FORMULATION AND DEVELOPMENT OF LIPID BASED NON-AQUEOUS NANO EMULSION FOR SELECTED NSAID

Oral administration of non-steroidal anti-inflammatory drugs is avoided in patients with disease like peptic ulcer, gastro esophageal reflux (GERD), irritable bowel syndrome. Administration of drug through topical route through the skin could reduce the above side effects associated with oral administered drug formulation. Hence, the aim of present study was to develop Nonaqueous Nanoemulsion (NANEs) of Naproxen for topical administration. NANEs is a multiphase colloidal dispersion heterogeneous system consist of fine nonaqueous polar solvent in oil dispersion with surfactant. NANEs of naproxen were prepared using high energy emulsification method, which break large micro droplets into nano size droplets. Drug-excipients Compatibility was studied by FT-IR. Rheology, Flow behavior, Viscosity, pH, Globule size, Drug content, in-vitro drug release of NANE were performed. For optimization of nonaqueous nanoemulsion Box- Behnken experimental design was implemented. The variables selected are phase volume ratio, surfactant concentration and stirring time. Data analysis showed that surfactant concentration and phase volume ratio significantly affect the viscosity of the formulation. From the present study, it can be concluded that a stable non-aqueous nanoemulsion can be obtained by using glycerin as dispersed phase, mineral oil as continuous phase and glycerol monostearate as surfactant, which can be used as vehicle for the water sensitive materials. This nonaqueous nanoemulsion has improved the stability of Naproxen and overcome the oral drawback associated with it.

FORMULATION AND CHARACTERIZATION OF Γ-ORYZANOL LOADED SOLID SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEMS (S-SNEDDS)

In recent years, much attention has been paid to solid self-nanoemulsifying drug delivery systems (S-SNEDDS), which have shown reasonable successes in improving oral bioavailability of poorly soluble drugs. This drug delivery system combines the advantages of liquid SNEDDS with those of a solid dosage form and overcomes the limitations associated with liquid formulations. One optimized SNEDDS formulae F-5 were selected to be solidified by spray drying technique using Aerosil 200 as solid carrier. Characterization of GOZ Loaded S-SNEDDS by angle of repose of the one S-SNEDDS formulae F-5 were 24.12°± 1.10°, these values indicate that all formulae have good flow ability. The bulk density of the two formulae F-5 was found to be 0.47 ± 0.03 g/mL. However, tapped density was 0.57±0.02 g/mL for formula F-5. Carr’s index of formulae F-5 was found to be 13.57±1.09 which give an indication about the good flowability of the one S-SNEDDS formulae. The efficiency of self-emulsification can also be estimated by measuring the emulsification time. The emulsification time was 41.57±1.12 s. for formula F-5. The small values of PDI shown by S-SNEDDS formulae F-5 (0.403±1.12) indicate homogenous droplet population and narrow globule size distribution. The thermo gram of pure GOZ exhibited a sharp endothermic peak at about 137.25°C, corresponding to its melting point. The drug loading efficiency was found to be 96.23±0.65 for formula F-5. Within the initial one hour of the in vitro release study, only 41.02%±1.23% of GOZ was dissolved from pure drug and marketed tablets, whereas the S-SNEDDS formulae showed improved release within the same time period. GOZ dissolved and released from S-SNEDDS reached 90.02%±1.02% for formula F-5, within one hour.

Fluconazole and Curcumin Loaded Nanoemulsion Against Multiple Drug Resistance Dermatophytes

Purpose: Topical nanoemulsion comprising of fluconazole and curcumin was developed to target multiple drug resistance dermatophytes infection and to facilitate cutaneous delivery of these poorly water soluble drugs. Methods: Almond oil, sesame oil and paraffin light were used to formulate nanoemulsions and screened for the stability. The solubility of fluconazole and curcumin in surfactants, co-surfactants and oils was screened to decide the various components of the nanoemulsion. The oil phase was light paraffin whereas tween 80 and span 80 were the surfactants and ethanol was used as a co-surfactant. To identify the area of nanoemulsion existence, a pseudoternary diagram was drawn and optimum systems were developed. Drug-loading efficiency was assessed and the developed nanoemulsions were characterized for globule size, stability, robustness to dilution and pH. The optimized nanoemulsion was further evaluated for drug content, viscosity, skin permeation study (ex vivo) and assay of antifungal activity. Results: The globule size was below 200 nm and uniform for the optimized nanoemulsion formulation. It showed enhanced skin permeation (ex vivo) and better antifungal efficacy as compared to the native form of fluconazole and curcumin suspensions. Antimicrobial assay confirmed the synergistic effect of fluconazole and curcumin combination against multiple drug resistance Trychophytum rubrum and Trichophyton metagrophytes as compared to the fluconazole alone. Conclusion: The results clearly indicate an optimized delivery of fluconazole and curcumin in a synergistic way from the nanoemulsion formulation. This resulted in better penetration of these poorly soluble molecules and overall enhanced antifungal activity as compared to these drugs as such against multiple drug resistance dermatophytes.

Formulation and Evaluation of Microemulsion of Curcumin in Thymol-Menthol Carrier System

Aim: To formulate and evaluate the Micro emulsion of curcumin in thymol-menthol carrier system.&#x0D; Study Design: Curcumin dissolves in mixture of thymol &amp; menthol to reasonable extent.100 mg of curcumin in 1 g of thymol and 0.6 g of menthol mixture was finalized as product mixture. The solution of curcumin in eutectic mixture being oily liquid, it gave the idea for development for the micro emulsion&#x0D; Place and Duration of Study: Department of Pharmaceutics and Department of Pharmacognosy, STES’s Smt. Kashibai Navale College of Pharmacy, Kondhwa (BK), National Chemical Laboratory, Pune between June 2016 and May 2017.&#x0D; Methodology: Micro emulsion system with eutectic mixture of thymol and menthol was chosen as oil phase and carrier for curcumin, tween 80 as surfactant and ethanol as co-surfactant. Ternary phase diagrams were constructed to obtain the optimum concentration range of oil phase, surfactant and co-surfactant. The micro emulsion of 100 mg curcumin containing 4.95 % oil phase, 33.39 % surfactant, 11.13% co-surfactant, 50:50% of water was optimum. Micro emulsion of curcumin was prepared by water titration method and evaluated for globule size, drug content, pH, viscosity, conductivity and In vitro drug release study. The ex-vivo permeation study for micro emulsion of curcumin was carried out on excised mice skin using Franz Diffusion apparatus. The cytotoxicity study for thymol, menthol was performed on healthy L929 murine fibroblast cell line. Anticancer activity of thymol-menthol eutectic mixture alone and with curcumin was performed on HeLa cell lines.&#x0D; Results: The preformulation studies did clearly indicate good compatibility of drug with thymol menthol carrier system. The cytotoxicity study was done on thymol – menthol(TM) as a preformulation aspect to ascertain the toxicity of these two excipients to be tried. It was found that TM was not cytotoxic in 120ug/mL concentration and thus was safe to be used in concentration below 120ug/mL. Batch B1 was optimised. The average globule size of micro emulsion was found to be 131.54 nm, zeta potential was found to be -0.57 mV. The drug content in micro emulsion batch B1 was determined and found to be 74.6%.Permeability study across mice skin ex-vivo model showed 52.38% permeability compared with curcumin alone which was 22.41%. So permeability of curcumin is enhanced substantially with micro emulsion made in thymol and menthol, owing to fact that thymol and menthol act as good permeation enhancers. The In vitro drug release study of micro emulsion was compared with curcumin alone. About 48.75% of curcumin was released from micro emulsion showed increase in release rate.&#x0D; Conclusion: Eutectic mixture of thymol and menthol showed promising results as penetration and solubility enhancer for curcumin. Solubility of curcumin was improved so as its rate of permeation which was used to develop formulation of micro emulsion with proven anticancer activity. The solubility of curcumin formulated with combination of eutectic mixture was increased up to 50 %.

Optimization and Characterization of Self Nano Emulsifying Drug Delivery System loaded with 18- β Glycerrhetinic acid

The purpose of this study was to prepare, optimize and evaluate self nano emulsifying drug delivery system (SNEDDS) containing 18- β glycerrhetinic acid which enhances the dissolution profile or bioavailability of the drug in comparison to pure suspension of 18- β glycerrhetinic acid.18- β glycerrhetinic acid loaded SNEDDS having geranium oil as oil phase, tween 80 as a surfactant, and dimethyl sulfoxide (DMSO) as co-surfactant were prepared using pseudo ternary phase diagram and Box-Behnken experimental design was used to optimize the different formulations. Optimized formulations were characterized for self-emulsifying time, globule size, zeta potential, and drug release. The mean droplet size and PDI of the optimized formulation were found to be in a variation of 93.42 nm and 0.401 respectively. FTIR data showed no physicochemical interaction between excipients and drug. The encapsulation efficiency of optimised 18- β glycerrhetinic acid SNEDDS was found 80.12±1.52% , % transmittance was found 99.34±0.134% and the viscosity of all the formulations was found 0.8872 cp. Three-dimensional response surface plots and two-dimensional contour plots of the responses across the selected factors were constructed that explained the relationship between the independent and dependent variables. Release kinetics was calculated by using KinetDS3.0. It was concluded that prepared formulations were formulated with approximately desired mean droplet size confirmed by Box- Behnken experimental design as well as properly optimized and characterized.

Microemulsion for Simulataneous Intransal Delivery of Carbamazepine and Vitamin B6 for Treatment of Epilepsy

<p style="text-align: justify;"><strong>Background: </strong>Status epilepsy is a neurological emergency characterized by severe bouts of seizure. It has been reported that combination of antiepileptic drug with Vitamin supplements reduce the drug resistance and rapid improvement was also observed in epilepsy patients. In this study, we tried to develop novel intranasal microemulsion for simultaneous delivery of carbamazepine and Vitamin B₆ for treatment of epilepsy. <strong>Materials and Methods: </strong>For simultaneous estimation of Carbamazepine and Vitamin B₆, second derivative spectroscopy method was developed and validated. The ME containing CBZ, in lipophilic phase and Vitamin B₆ in aqueous phase was studied for physicochemical characters and ex vivo diffusion through sheep nasal mucosa. The maximal electroshock (MES)- induced seizure models was used to establish the pharmacodynamic credentials of the microemulsion. <strong>Results: </strong>The wavelength selected for Carbamazepine and Vitamin B₆ were 231 nm and 250 nm respectively. It was found that prepared microemulsion is stable with globule size of 395+12 nm. Diffusion across sheep nasal mucosa followed zero order kinetics for carbamazepine and Vitamin B₆ in the prepared microemulsion. It was found that the hind limb extension time and the recovery time were significantly different from control group (<em>p</em>&lt;0.05). The microemulsion remained stable after dilution, centrifugation and freeze thaw cycle as tested for particle size, zeta potential and percentage transmission. <strong>Conclusion:</strong> The proposed microemulsion should form the basis for treatment of epilepsy which warrants co-administration of micronutrients. <strong>Key words:</strong> Carbamazepine, Intranasal Microemulsion, Pharmacodynamic, Simultaneous Delivery, Vitamin B₆.

Human milk-based fortifier is associated with less alteration of milk fat globule size than cow milk-based fortifier.

We aimed to evaluate if human milk-based fortifier (HMBF) affects human milk fat globule (MFG) size less than cow milk-based fortifier (CMBF), which may impact overall infant feeding tolerance. Measurements of donated human milk were performed before fortification as well as at 1 hour, 24 hours, and 48 hours after fortification with CMBF or HMBF. MFG size in each sample of fortified milk was measured by laser light scattering. MFG size in the fortified milks increased gradually over time. At 24 and 48 hours after fortification, MFG size in the milk with CMBF was larger than that in the milk with HMBF (4.8 ± 0.5 vs 4.3 ± 0.3 μm, p<0.01, 5.1 ± 0.7 vs 4.5 ± 0.4 μm, p = 0.03, respectively). HMBF is associated with less alteration of MFG size than CMBF. This may have an impact on feeding tolerance of very preterm infants.

Exposure to per- and polyfluoroalkyl substances associates with an altered lipid composition of breast milk.

The composition of human breast milk is highly variable inter- and intra-individually. Environmental factors are suspected to contribute to such compositional variation, however, their impact on breast milk composition is currently poorly understood. We sought to (1) define the impact of maternal exposure to per- and polyfluoroalkyl substances (PFAS) on lipid composition of human breast milk, and (2) to study the combined impact of maternal PFAS exposure and breast milk lipid composition on the growth of the infants.In a mother-infant study (n=44) we measured the levels of PFAS and lipids in maternal serum and conducted lipidomics analysis of breast milk collect 2-4days after the delivery and at 3months of infant age, by using ultra high performance liquid chromatography combined with quadrupole-time-of-flight mass spectrometry. Gastrointestinal biomarkers fecal calprotectin and human beta defensin 2 were measured in the stool samples at the age of 3, 6, 9, and 12months. Maternal diet was studied by a validated food frequency questionnaire. PFAS levels were inversely associated with total lipid levels in the breast milk collected after the delivery. In the high exposure group, the ratio of acylated saturated and polyunsaturated fatty acids in triacylglycerols was increased. Moreover, high exposure to PFAS associated with the altered phospholipid composition, which was indicative of unfavorable increase in the size of milk fat globules. These changes in the milk lipid composition were further associated with slower infant growth and with elevated intestinal inflammatory markers. Our data suggest that the maternal exposure to PFAS impacts the nutritional quality of the breast milk, which, in turn, may have detrimental impact on the health and growth of the children later in life.

Development of bioflavonoid containing chemotherapeutic delivery systems for UV-damaged skin and kangri cancer

Abstract Background The lower abdomen and inner thighs are most likely to become affected by kangri cancer because those areas are exposed to continuous exposure to kangri. Objective In this article, formulation and characterization of a water-in-oil microemulsion of 5-fluorouracil with rutin (R-5FU) for better skin penetration and inhibition of kangri cancer (skin cancer surfactant) is discussed. Method To produce R-5-FU microemulsions, surfactant-cosurfactant was mixed with oil. Distilled water was added dropwise with the help of a burette by gentle stirring at a constant temperature. The surfactant and co-surfactant were mixed into three particular ratios 1:1, 2:1, and 3:1. Further characterizations were performed, such as visual inspection and thermodynamic stability including a stress test and centrifugation. In visual inspection included assessment of the colour, homogeneity, and odour of the formulation of FU microemulsion. Result All three microemulsions, labeled RME1, RME2, and RME3, are highly stable. An oval shape of surface morphology of 5-FU was noticed by using a TEM image. The viscosity of RME3 was found to be 17.25±0.22 pa-s. The average globule size was 100–300 nm for all three RME. The results of human cadaver skin permeability are almost of the same pattern, butRME3 indicates the best skin permeability with negligible side effects on the skin. Conclusion The quantity of 5-FU released from all formulations at 3-hr ranged from 95.57% to 83.67%. None of the three formulations resulted in skin irritation, with irritancy score of zero (IS=0). Observation revealed no lysis, hemorrhage, or coagulation after application.

Novel Self-micro Emulsifying Drug Delivery System for Safe Intramuscular Delivery with Improved Pharmacodynamics and Pharmacokinetics.

Diclofenac Sodium (DS) injection is widely used in the management of acute or chronic pain and inflammatory diseases. It incorporates 20% w/v Transcutol-P as a solubilizer to make the stable injectable formulation. However, the use of Transcutol-P in high concentration leads to adverse effects such as severe nephrotoxicity, etc. Some advancements have resulted in the formulation of an aqueous-based injectable but that too used benzyl alcohol which is reported to be toxic for human use. This study aimed to develop an injectable Self-Micro Emulsifying Drug Delivery System (SMEDDS) as a novel carrier of DS for prompt release with better safety and efficacy. A solubility study was performed with different surfactants and co-surfactants. The conventional stirring method was employed for the formulation of SMEDDS. Detailed in vitro characterization was done for different quality control parameters. In vivo studies were performed using Wistar rats for pharmacokinetic evaluation, toxicological analysis, and analgesic activity. The optimized formulation exhibited good physical stability, ideal globule size (156±0.4 nm), quick release, better therapeutics, and safety, increase in LD50 (221.9 mg/kg) to that of the commercial counterpart (109.9 mg/kg). Furthermore, pre-treatment with optimized formulation reduced the carrageenan-induced rat paw oedema by 88±1.2% after 4 h, compared to 77±1.6% inhibition with commercial DS formulation. Moreover, optimized formulation significantly (p<0.05) inhibited the pain sensation in the acetic-acid induced writhing test in mice compared to its commercial equivalent with a better pharmacokinetic profile. The above findings confirmed that liquid SMEDDS can be a successful carrier for the safe and effective delivery of DS.