Medium Chain Triglyceride Oil Research Articles

Improving stability and bioavailability of curcumin by quaternized chitosan coated nanoemulsion

This study aims to enhance the stability and bioavailability of curcumin (Cur) using nanoemulsion coating technology. The nanoemulsion system was developed by encapsulating Cur with quaternized chitosan (QMNE), and the nanoemulsion containing Cur and medium-chain triglyceride (MCT) oil (MNE) was used as control sample. The microstructure of the nanoemulsion was examined using Dynamic light scattering (DLS), Transmission electron microscopy (TEM) and Fourier transform infrared spectroscopy (FT-IR). The storage, thermal, ionic strength, and pH stability of QMNE were also evaluated, respectively. The results indicate that QMNE demonstrates superior stability, in vitro gastric fluid stability, bioavailability compared to MNE. QMNE exhibits excellent emulsification activity and stability. In addition, QMNE shows significant protection against oxidation in both emulsion systems after different heat treatments. The antimicrobial activity results reveal that QMNE exhibits greater efficacy than that of MNE. Consequently, this study provides valuable insights into the formulation of a system to encapsulate Cur and the improvement of its stability and bioavailability.

Stability of Hydroxy-α-Sanshool in Medium-Chain Triglyceride Oil and Corresponding Oil/Water Emulsions.

The pungent component of sansho (Japanese pepper, Zanthoxylum pipritum) is sanshool, which is easily oxidized and decomposed. We have previously reported several sanshool stabilizers, such as α-tocopherol (α-Toc). Sansho pericarp powder treated with middle-chain triglycerides (MCTs) can be used to obtain extracts containing hydroxy-α-sanshool (HαS). Although HαS is stabilized when α-Toc is added to the MCT extracts, the loss of HαS is accelerated when it is mixed with a powder such as lactose. The separation of α-Toc from sanshools was thought to inevitably lead to their oxidation. Therefore, using sansho pericarp MCT extracts with or without α-Toc, oil/water (o/w) emulsions were prepared by adding a surfactant, glycerin, and water to these extracts. In both emulsions, HαS was stable in accelerated tests at 50 °C. However, when lactose powder was added to the emulsions and an accelerated test was performed, HαS in the emulsion containing α-Toc was stable, but HαS in the emulsion without α-Toc was unstable. These results highlight the importance of maintaining the close proximity of HαS and α-Toc in the emulsion. The stabilization of sanshools using emulsion technology can facilitate the production of various processed beverages, foods, cosmetics, and pharmaceuticals containing Japanese pepper.

Synthesis of Deuterated and Protiated Triacylglycerides by Using 1,1’‐Carbonyldiimidazole Activated Fatty Acids

AbstractSynthetic model triacylglyceride oils are important compounds for applications in pharmaceutical and food chemistry. Herein, a practical and highly efficient methodology for the synthesis of saturated and unsaturated triacylglycerides utilizing saturated and unsaturated fatty acids activated by 1,1’‐carbonyldiimidazole (CDI) has been developed and applied in the synthesis of deuterated medium chain triglyceride (MCT) oil for studies of plant‐based and diary food emulsions. The deuterium labelled compounds were used to gain new insight into the mechanism of the reaction, which was confirmed by density‐functional theory (DFT) calculations.

Impact of the lipid phase composition and state on the in vitro digestibility and chlorophyllin bioaccessibility of W1/O/W2 emulsions into whole milk

Water-in-oil-in-water (W1/O/W2) emulsions offer the potential to deliver hydrophilic bioactive compounds into foods, yet their application remains limited due to their instability. Thus, the impact of lipid phase composition and state on the colloidal stability, in vitro lipid digestibility and chlorophyllin (CHL) bioaccessibility of W1/O/W2 emulsions before and after incorporation into whole milk was studied. Medium-chain triglyceride oil (MCT) was used as a liquid lipid phase and MCT with glyceryl stearate (GS) or pure hydrogenated palm oil (HPO) as gelled lipid phases. The lipid phase composition was crucial to forming W1/O/W2 emulsions. MCT or MCT+GS allowed the successful formation of W1/O/W2 emulsions, being more stable upon gastric conditions those formulated with MCT+GS than pure MCT. In contrast, the use of HPO led to phase separation, which was maintained after the gastric conditions. Regarding their lipid digestibility, W1/O/W2 emulsions formulated with MCT or MCT+GS were fully digested, whereas only 40% of the lipid was digested using HPO. In accordance, the CHL bioaccessibility was higher using MCT or MCT+GS than HPO. When co-digested with whole milk, the colloidal stability and lipid digestibility of the W1/O/W2 emulsions with MCT or MCT+GS were not altered, whereas the W1/O/W2 emulsion-HPO showed enhanced colloidal stability and lipid digestibility (57.71 ± 3.06%), due to the surface-active properties of milk protein. The present study provides useful information to develop stable functional foods enriched with hydrophilic bioactive compounds by using W1/O/W2 emulsions.

Pharmacokinetics of Oral Minor Cannabinoids in Blood and Brain.

Introduction: Minor cannabinoids are increasingly being consumed in oral formulations (i.e., edibles, tinctures) for medical and nonmedical purposes. This study examined the pharmacokinetics (PKs) of cannabinoids tetrahydrocannabivarin (THCV), cannabichromene (CBC), cannabinol (CBN), and delta-8-tetrahydrocannabinol (D8-THC) after the first and last oral dose during a 14-day administration period. Materials and Methods: Sprague-Dawley rats (N=6 animals/dose, 50% female) were given an assigned dose of one of four cannabinoids (THCV=3.2-100 mg/kg, CBC=3.2-100 mg/kg, CBN=1-100 mg/kg, or D8-THC=0.32-10 mg/kg) or vehicle (medium-chain triglyceride oil) through oral gavage once daily for 14 days. Blood was collected 45 min and 1.5, 3, and 24 h following the first dose (day 1) and the last dose (day 14) of repeated oral cannabinoid treatment for PK analysis. Outcomes of interest included time to maximum concentration (Tmax), maximum concentration (Cmax), and area under the concentration versus time curve (AUClast). Dose-normalized (DN) Cmax and DN AUClast were also calculated. Brain tissue was collected 24 h post-administration of the first (day 1) and the last (day 14) dose of each cannabinoid to determine concentrations in brain. Results: All cannabinoids tested were detectable in plasma after single and 14-day repeated dosing. DN Cmax and DN AUClast were highest for D8-THC, followed by CBC, CBN, and THCV. There was no sex difference observed in cannabinoid kinetics. Accumulation of D8-THC in plasma was observed after 14 days of administration. THCV levels in plasma were lower on day 14 compared to day 1, indicating potential adaptation of metabolic pathways and increased drug elimination. Cannabinoids were detected in brain tissue 24 h post-administration of the first and the last dose of 17-100 mg/kg THCV, 3.2-100 mg/kg CBC, 10-100 mg/kg CBN, and 10 mg/kg D8-THC. Conclusions: THCV, CBC, CBN, and D8-THC produced detectable levels in plasma and translocated to brain tissue after the first dose (day 1) and the last dose (day 14) of repeated oral dosing. Examination of PKs of these minor cannabinoids in blood and brain provides a critical step for informing target dose ranges and dosing schedules in future studies that evaluate the potential effects of these compounds.

Toxicological Evaluation and Pain Assessment of Four Minor Cannabinoids Following 14-Day Oral Administration in Rats.

Introduction: Despite growing consumer interest and market availability, the safety of minor cannabinoids, generally present in low concentrations in Cannabis sativa L., is not well understood. Materials and Methods: Cannabichromene (CBC; 3.2, 10, 17, 22, 32, or 100 mg/kg-bw/day), cannabinol (CBN; 1, 3.2, 10, 17, 32, or 100 mg/kg-bw/day), delta-8-tetrahydrocannabinol (D8-THC; 0.32, 1, 3.2, or 10 mg/kg-bw/day), tetrahydrocannabivarin (THCV; 3.2, 10, 17, 22, 32, or 100 mg/kg-bw/day), and vehicle (medium-chain triglyceride oil) preparations were administered via oral gavage once daily for 14 days to Sprague Dawley rats. Changes in behavior, body weight, food consumption, clinical pathology, organ weights, body temperature, and thermal pain sensitivity (tail flick assay) were assessed. Select organ tissues were collected at terminal necropsy and fixed for histopathological examination. Results: No treatment-related deaths were observed throughout the study, and cannabinoids were generally well tolerated. While some significant trends in body weight differences from controls (increases and decreases) were observed, these occurred independently of food consumption. Overall, differences in serum chemistry and hematology parameters between cannabinoid groups and their respective control groups were considered to occur due to biological variation among rats. No treatment-related gross abnormalities were observed in examined organs. Significant changes in absolute and relative organ weights occurred primarily in males and were generally of negligible magnitude. There were no biologically significant histopathological observations. While pain tolerance was significantly improved in animals treated with D8-THC (3.2 and 10 mg/kg-bw/day, day 14), results across minor cannabinoids were inconsistent and warrant further study. Conclusion: Minor cannabinoids were well tolerated across 14 days of daily oral administration at the doses assessed. Modest, dose-dependent trends in relative organ weights and serum chemistry parameters warrant exploration at higher oral doses. These data will assist in dose selection for future studies investigating the long-term safety and effects of CBC, CBN, D8-THC, and THCV.

Physicochemical and sensory properties of plant-based meat patties using oil-in-water emulsion

This study investigated the effects of an oil-in-water (O/W) emulsion as an animal fat substitute on the physicochemical and sensory properties of plant-based meat patties. Vegetable oils (peanut, coconut, and medium-chain triglyceride (MCT) oils) and liquid additives (water, oil, water, oil, and surfactant; emulsion) were used to prepare the patties. Tween® 80 and soy protein isolate (SPI) were used to prepare the emulsion. The emulsion droplet size and ζ-potential were analyzed before mixing with the textured vegetable protein batter. The physicochemical, rheological, and sensory properties of the resulting plant-based meat patties were analyzed. The emulsions droplet sizes were approximately 5–10 μm, with a surface charge of >40 or 18 mV upon Tween® 80 or SPI addition, respectively. For patties containing MCT oil, cooking loss and hardness were reduced when using water, oil, Tween® 80, and emulsion samples. Additionally, these samples exhibited high liquid holding capacity, which affected tenderness. The creep recovery and viscoelasticity of the batters were unaffected by the oil type but generally higher in surfactant-containing batters. The L* value decreased irrespective of the type of oil or treatment, and the color difference was low in the sample containing Tween® 80. Moreover, based on the sensory test, MCT oil mixed with Tween® 80 resulted in patties with the highest levels of tenderness, juiciness, and overall acceptance. In conclusion, incorporating MCT oil and pre-manufactured emulsion as an animal fat substitute can improve the juiciness, liquid-holding capacity, and overall palatability of plant-based meat products.

Impact of fatty acid composition on markers of exocrine pancreatic stimulation in dogs.

Chronic pancreatitis in dogs is typically managed with a low-fat diet. Human research suggests that consumption of medium-chain triglycerides (MCT) may lessen pancreatic enzyme release compared to consumption of long-chain fatty acids (LCFA). Twelve healthy adult colony dogs were fed a meal of cod and rice with either 3% metabolizable energy (ME) fat (control), high MCT (25% ME MCT oil, 25% ME butter), high saturated LCFA (50% ME butter), or high unsaturated LCFA (50% ME canola oil) in a 4-period by 4-treatment crossover design. Serum concentrations of canine pancreatic lipase immunoreactivity, gastrin, cholesterol, triglycerides, and serum activities of amylase and DGGR lipase (1,2-o-dilauryl-rac-glycero-3-glutaric acid-(69-methylresorufin) ester lipase) were measured at times 0 (fasted), 30, 120 and 180 minutes post-prandially. Following a 3-or 4-day wash-out period, each dog was assigned a new diet and the process was repeated for all treatments. Data were analyzed as a repeated-measures mixed model ANOVA. Post-hoc pairwise comparisons were run using Tukey-Kramer adjusted p-values. Shapiro-Wilk tests were used to evaluate residual normality. All statistical assumptions were sufficiently met. Statistical significance was defined as P<0.05. Of the markers tested, only serum triglyceride concentrations were affected by treatment, with consumption of high MCT resulting in lower triglycerides than both LCFA groups at times 120 and 180 minutes (P<0.0001). As expected, the high MCT group had higher triglycerides compared to the control group (P<0.0001). The type of dietary fat consumed had little acute impact on most markers of exocrine pancreatic stimulation in healthy dogs.

In parenteral nutrition-fed piglets, fatty acids vary by lipid emulsion and tissue sampled.

Children with intestinal failure without liver disease may be given soy-based lipid emulsion (SLE) or mixed lipid emulsion (MLE; containing soy, medium-chain triglyceride, olive, and/or fish oils). Both differ in essential fatty acid content: MLE has added arachidonic acid (AA) and docosahexaenoic acid (DHA). The aim of this study, in neonatal piglets, was to compare serum and tissue fatty acid composition when the emulsions were given at unrestricted doses. We compared SLE (n = 15) and MLE (n = 15) at doses of 10-15 g/kg/day in parenteral nutrition (PN). On day 14 we collected serum and tissues. Using gas-liquid chromatography, percentage fatty acids were measured in serum, brain, and liver phospholipid. Comparisons were made to reference values from litter-matched controls (n = 8). Comparing median values, linoleic acid (LA) was lower for MLE vs SLE in serum (-27%), liver (-45%), and brain (-33%) (P < 0.001). AA was lower for MLE in serum (-25%), liver (-40%), and brain (-10%). DHA was higher for MLE in serum (+50%), liver (+200%), and brain (+10%). AA levels were lower for MLE vs control piglets in serum (-81%), liver (-63%), and brain (-9%). DHA levels were higher in serum (+41%), liver (+38%), and brain (+19%). This study in piglets has shown that, at unrestricted doses, MLE treatment is associated with low serum and tissue AA compared with SLE and healthy litter-matched controls. Although not yet proven, low tissue AA levels may have functional consequences, and these data support current practice avoiding MLE dose restriction.

Safety of an ethanolic extract of the dried biomass of the microalga Phaeodactylum tricornutum as a novel food pursuant to Regulation (EU) 2015/2283.

Following a request from the European Commission, the EFSA Panel on Nutrition, Novel Foods and Food Allergens (NDA) was asked to deliver an opinion on an ethanolic extract of the dried biomass of the microalga Phaeodactylum tricornutum as a novel food (NF) pursuant to Regulation (EU) 2015/2283. The NF is an ethanolic extract of the dried biomass of the microalga P. tricornutum diluted in a medium-chain triglyceride oil carrier, with standardised fucoxanthin and tocopherol content. The main component of the NF is fat (78% on average), followed by crude protein (10% on average). The Panel is of the view that a consistent and safe production process has not been demonstrated. Additionally, the Panel considers that the information provided on the composition of the NF is not complete and may raise safety concerns. The applicant proposed to use the NF as a food supplement at the use level of 437 mg/day, with the target population being adults, excluding pregnant and breastfeeding women. There is no history of use of the NF or of its source, i.e. P. tricornutum. The Panel notes that the source of the NF, P. tricornutum, was not granted the qualified presumption of safety (QPS) status by the EFSA Panel on Biological Hazards (BIOHAZ), due to the lack of a safe history of use in the food chain and on its potential for production of bioactive compounds with toxic effects. There were no concerns regarding genotoxicity of the NF. In the 90-day study provided, a number of adverse effects were observed, some of them seen already at the lowest dose tested (750 mg/kg body weight (bw) day), which was identified by the Panel as the lowest-observed-adverse-effect-level (LOAEL). The potential phototoxicity of pheophorbide A and pyropheophorbide A in the NF was not addressed in this study. Although noting the uncertainties identified by the Panel regarding the analytical determination of these substances in the NF and the limitations in the publicly available toxicity data, a low margin of exposure (MoE) was calculated for these substances at the proposed use levels. The Panel concludes that the safety of the NF under the proposed uses and use levels has not been established.

Citrin Deficiency: Clinical and Nutritional Features.

SLC25A13 gene mutations are responsible for diseases related to citrin deficiency (CD), such as neonatal intrahepatic cholestasis caused by citrin deficiency and adult-onset type II citrullinemia (CTLN2). From childhood to adulthood, CD patients are apparently healthy due to metabolic compensation with peculiar dietary habits-disliking high-carbohydrate foods and liking fat and protein-rich foods. Carbohydrate overload and alcohol consumption may trigger the sudden onset of CTLN2, inducing hyperammonemia and consciousness disturbance. Well-compensated asymptomatic CD patients are sometimes diagnosed as having non-obese (lean) non-alcoholic fatty liver disease and steatohepatitis, which have the risk of developing into liver cirrhosis and hepatocellular carcinoma. CD-induced fatty liver demonstrates significant suppression of peroxisome proliferator-activated receptor α and its downstream enzymes/proteins involved in fatty acid transport and oxidation and triglyceride secretion as a very low-density lipoprotein. Nutritional therapy is an essential and important treatment of CD, and medium-chain triglycerides oil and sodium pyruvate are useful for preventing hyperammonemia. We need to avoid the use of glycerol for treating brain edema by hyperammonemia. This review summarizes the clinical and nutritional features of CD-associated fatty liver disease and promising nutritional interventions.

Neuroprotective Effect of a Pharmaceutical Extract of Cannabis with High Content on CBD Against Rotenone in Primary Cerebellar Granule Cell Cultures and the Relevance of Formulations.

Introduction: Preclinical research supports the benefits of pharmaceutical cannabis-based extracts for treating different medical conditions (e.g., epilepsy); however, their neuroprotective potential has not been widely investigated. Materials and Methods: Using primary cultures of cerebellar granule cells, we evaluated the neuroprotective activity of Epifractan (EPI), a cannabis-based medicinal extract containing a high level of cannabidiol (CBD), components like terpenoids and flavonoids, trace levels of Δ9-tetrahydrocannabinol, and the acid form of CBD. We determined the ability of EPI to counteract the rotenone-induced neurotoxicity by analyzing cell viability and morphology of neurons and astrocytes by immunocytochemical assays. The effect of EPI was compared with XALEX, a plant-derived and highly purified CBD formulation (XAL), and pure CBD crystals (CBD). Results: The results revealed that EPI induced a significant reduction in the rotenone-induced neurotoxicity in a wide range of concentrations without causing neurotoxicity per se. EPI showed a similar effect to XAL suggesting that no additive or synergistic interactions between individual substances present in EPI occurred. In contrast, CBD did show a different profile to EPI and XAL because a neurotoxic effect per se was observed at higher concentrations assayed. Medium-chain triglyceride oil used in EPI formulation could explain this difference. Conclusion: Our data support a neuroprotective effect of EPI that may provide neuroprotection in different neurodegenerative processes. The results highlight the role of CBD as the active component of EPI but also support the need for an appropriate formulation to dilute pharmaceutical cannabis-based products that could be critical to avoid neurotoxicity at very high doses.

Fat Supplementation of Human Milk with MCT Oil for Promoting Weight Gain in Preterm Infants

Background: The addition of medium chain triglycerides is preferable as they are more easily digested and quickly absorb in bloodstream than long chain fat and provide ready supply of energy by increasing fatty acid bioavailability. Modular products like micro lipids and medium-chain triglyceride (MCT) oils are now focused as a fat supplementation. The rate of weight gain with MCT is not well known, and there is very less research done in Pakistan. Objective: To determine the effect of MCT oil supplemented human milk compared with un supplemented human milk fed to preterm infants on promoting weight gain. Study Design: Randomized controlled trial Study Setting: This study was conducted in Department of Neonatology, Children Hospital, PIMS, Islamabad, Pakistan from 20th August 2022 to 20th February 2023. Methodology: The study conducted after approval from institutional ethical committee. A total of 160 preterm infants fulfilling the inclusion criteria and enrolled in the study after informed consent from parents. The patients were receiving enteral feeding of human milk within neonatology department of hospital was included and they were randomly assigned to Group NF (receiving 20 ml of human milk without MCT oil), Group F (receiving 20ml of human milk with 1 ml of MCT oil fat). Primary outcomes were including growth in term of weight gain at measured at 1st ,5th and 10th day of MCT oil intake after hospital admission. Secondary outcome included feeding intolerance, diarrhoea, sepsis and necrotising enterocolitis. All the data was collected in the form of a questionnaire. The statistical analysis was done by using SPSS version 20. Results: One sixty very low birth weight infants were analyzed in this study. All infants were randomly divided into two groups: F and NF, the demographic details. The weight of infants was measured on first day, fifth day and tenth day and noted that the frequency of infants improved the weight gain after taking human milk without fat supplementation or human milk with fat supplementation. We found the gradually infants more increasing their weights in Group F as compared to Group NF. On tenth day 75% infants reaches between1400-1490 gm weight (p&lt;0.001). The average daily gain in weight of Group F infants (g/kg). 12.2 Group A, 13.6 in group B were calculated on day first. The average daily weight was shifted in Group B from 13.6 to 14.9 on day fifth then it was further increased as 15.6 in Group C, and 15.8 in Group D. Practical Implication: The fat in the milk of humans is a significant source of energy. In an underdeveloped State like Pakistan that is short on resources, (MCT) oil can be a useful substitute for MCT due to its high MCT content. Few research studies have been conducted into this area thus far. Previous studies have had a low number of participants and produced contradictory findings. Therefore, this study was carried out to compare the efficacy of feeding preterm infants human milk supplemented with MCT oil to that of feeding them human milk without the supplement. Conclusion: Our study shows the average weight gain in those infants fed fat supplementation of MCT oil added in breast milk. The study provides data regarding the selection and use of fat supplemented human milk over non-supplemented human milk and this reduces the morbidity and mortality rate due to insufficiency of nutrients. Keyword: Fat supplementation, MCT oil, breast milk, preterm infants, weight gain rate.

The Efficacy of Medium-Chain Triglyceride on the Prognosis and Outcome of Suspected COVID-19 Outpatients: A Randomized Controlled Trial

Background: The novel coronavirus disease (COVID-19), as a global concern, has affected different economic and social aspects, as well as health costs in various communities. Finding effective and available treatment is an urgent need. A recent study has demonstrated that the ketogenic diet (KD) activates innate immunity and has a protective property against virus infection. Accordingly, we conducted this study to find the effect of oral medium-chain triglyceride (MCT) on COVID-19 and its clinical manifestations. Methods: This was a randomized clinical trial on 195 patients clinically suspected of COVID-19 referred to infectious disease clinics of Kerman. Patients were randomly assigned into two groups. The Control group received standard supportive treatment, the recommendation for carbohydrate avoiding and diet modification. Patients in the intervention group received all mentioned recommendations beside MCT oil. Patients` clinical symptoms, including body temperature, respiratory rate, body pain, and dyspnea, were recorded in a checklist and analyzed. Results: The mean age of patients was 37.78±12.42 years in the intervention group and 40.81±13.23 years in controls (P=0.231). The patients in the intervention group had lower duration of weakness (P=0.004), body pain (P=0.004), dyspnea (P=0.004), gastrointestinal manifestations (P&lt;0.001), sore throat (P&lt;0.001), increased respiratory rate (P&lt;0.001), and high intensity of cough (P=0.002). Indeed, weakness, cough frequency, sore throat, and gastrointestinal complications were significantly lower in the females of the intervention group (P=0.006, P=0.030, P=0.005, and P=0.001, respectively). In contrast, in the males of the intervention group, manifestations such as respiratory rates, dyspnea, cough intensity, and sore throat were significantly lower than those in the control group. Conclusion: Administration of MCT in outpatients suspected of COVID-19 alleviated clinical symptoms such as increased respiratory rate, cough intensity, dyspnea, body pain, and gastrointestinal symptoms and helps them overcome the probable disease morbidity.

Fish oil fat emulsion alleviates traumatic brain injury in mice by regulation of microglia polarization

Microglia activation, a hallmark of brain neuroinflammation, contributes to the secondary damage following traumatic brain injury (TBI). To explore the potential roles of different fat emulsions-long chain triglyceride (LCT) / medium chain triglyceride (MCT) and fish oil (FO) fat emulsion in neuroprotection and neuroinflammation in TBI, in this study, we first generated the controlled cortical impact (CCI) model of TBI mice. Then either LCT/MCT or FO fat emulsion treated mice were studied by Nissl staining to assess the lesion volume. Sham and TBI mice treated with 0.9% saline were used as controls. The fatty acid composition in different TBI mouse brains was further evaluated by gas chromatography. Immunofluorescent staining and quantitative RT-PCR both demonstrated the suppression of pro-inflammatory microglia and upregulated anti-inflammatory microglia in FO fat emulsion treated TBI brain or primary microglia induced by lipopolysaccharide (LPS) in vitro. Furthermore, motor and cognitive behavioral tests showed FO fat emulsion could partially improve the motor function in TBI mice. Together, our results indicate that FO fat emulsion significantly alleviates the TBI injury and neuroinflammation probably by regulating microglia polarization.

Investigating Key Molecular Descriptors Affecting Particle Size: A Predictive Exemplary Approach for Self-Emulsifying System.

The self-nano/microemulsifying drug delivery system is one of the well-established techniques for enhancing the solubility of poorly water-soluble drug molecules. The ratio of oil:surfactant:cosolvent plays a key role in globule size on dispersion into water, but there is very limited information on how a drug molecule affects the size. The rationale of this project was to illustrate the correlation between the particle size of nanoemulsion droplets and molecular descriptors of a drug. In the study, a self-nanoemulsifying preconcentrate containing drug with medium chain triglycerides (oil), dimethylacetamide (DMA, cosolvent), and Kolliphor EL (surfactant) was prepared for 40 drug molecules with diverse physicochemical properties. The self-nanoemulsifying preconcentrate was dispersed in water, and dynamic light scattering particle size was analyzed. A majority of drugs showed a significant increase in globule size compared to blank formulation, while few drugs showed a stark reduction in globule size. It is interesting to understand the attributes of molecules driving the self-emulsification and the diameter of nanoglobules. A systematic correlation of resultant particle size with 1D, 2D, and 3D molecular descriptors (overall more than 700 descriptors) was carried out for the data set using the PaDEL tool kit. The data compilation, curation, and analysis were performed using the SIMCA14 software. In the process of molecular descriptors screening, thereafter curation, 50 descriptors were selected using the genetic algorithm screening. The PLS-DA statistical method was employed for conversion of data into binomial systems. Final group of 5 descriptors: SpMiSpMin2_Bhe, RNCS, TDB9i, JG17, and ETA_Shape showed the correlation with particle size and classifying the drug molecules facilitating increase or decrease in particle size.

Assessment of glyceride-structured oleogels as an injectable extended-release delivery system of bupivacaine

This manuscript systematically assesses three different glycerides (tripalmitin, glyceryl monostearate, and a blend of mono-, di- and triesters of palmitic and stearic acids (Geleol™)) as potential gelator structuring agents of medium-chain triglyceride oil to form an oleogel-based injectable long-acting local anesthetic formulation for postoperative pain management. Drug release testing, oil-binding capacity, injection forces, x-ray diffraction, differential scanning calorimetry, and rheological testing were serially performed to characterize the functional properties of each oleogel. After benchtop assessment, the superior bupivacaine-loaded oleogel formulation was compared to bupivacaine HCl, liposomal bupivacaine, and bupivacaine-loaded medium-chain triglyceride oil in a rat sciatic nerve block model to assess in vivo long-acting local anesthetic performance. In vitro drug release kinetics were similar for all formulations, indicating that drug release rate is primarily dependent on the drug’s affinity to the base oil. Glyceryl monostearate-based formulations had superior shelf-life and thermal stability. The glyceryl monostearate oleogel formulation was selected for in vivo evaluation. It was found to have a significantly longer duration of anesthetic effect than liposomal bupivacaine and was able to provide anesthesia twice as long as the equipotent bupivacaine-loaded medium-chain triglyceride oil, indicating that the increased viscosity of the oleogel provided enhanced controlled release over the drug-loaded oil alone.

Synthesis of eicosapentaenoic acid-enriched medium- and long-chain triglyceride by lipase-catalyzed transesterification: a novel strategy for clinical nutrition intervention.

Eicosapentaenoic acid (EPA) has been recognized as a promising nutrient to improve therapeutic efficacy for cancer patients. Nevertheless, there are certain limitations to the application of EPA due to its structural characteristics. To maximize the nutritive value of EPA, a type of medium- and long-chain triacylglycerol (MLCT) enriched with EPA was designed and synthesized using the lipase-catalyzed transesterification of medium-chain triglyceride (MCT) and EPA-enriched fish oil (FO). The optimum synthesis conditions for EPA-enriched MLCT used Lipozyme RM as catalyst, and had a substrate mass ratio (MCT/EPA-enriched FO) of 3:1, lipase loading of 80 g kg-1 , a reaction temperature of 60 °C, and a reaction time of 6 h. The MLCT content was as high as 80.79% after the transesterification reaction and the purification, and the content of MLCT containing EPA accounted for 70.21%. The distribution of EPA at the sn-2 position showed a significant increase in MLCT compared with the original substrate, from 18.89% to 26.93%. The in vitro digestion results demonstrated that MLCT had a significantly higher EPA bioaccessibility than the original substrate. Eicosapentaenoic acid-enriched MLCT was developed. This may provide a novel strategy for clinical nutritional intervention. © 2023 Society of Chemical Industry.

Investigating the Effect of Medium Chain Triglycerides on the Elasticity of Pulmonary Surfactant

In recent years, vaping has increased in both popularity and ease of access. This has led to an outbreak of a relatively new condition known as e-cigarette/vaping-associated lung injury (EVALI). This injury can be caused by physical interactions between the pulmonary surfactant (PS) in the lungs and toxins typically found in vaping solutions, such as medium chain triglycerides (MCT). MCT has been largely used as a carrier agent within many cannabis products commercially available on the market. Pulmonary surfactant ensures proper respiration by maintaining low surface tensions and interface stability throughout each respiratory cycle. Therefore, any impediments to this system that negatively affect the efficacy of this function will have a strong hindrance on the individual's quality of life. Herein, neutron spin echo (NSE) and Langmuir trough rheology were used to probe the effects of MCT on the mechanical properties of pulmonary surfactant. Alongside a porcine surfactant extract, two lipid-only mimics of progressing complexity were used to study MCT effects in a range of systems that are representative of endogenous surfactant. MCT was shown to have a greater biophysical effect on bilayer systems compared to monolayers, which may align with biological data to propose a mechanism of surfactant inhibition by MCT oil.

Determination of penetration and protection of fatty acids in bleached hair according to the fatty acid chain length and the application to understanding the protective effects of MCT oil and coconut oil

Hair treatments containing vegetable oils protect the damaged hair by surface coating and by penetrating in hair thereby filling the gaps caused by oxidative damage. Vegetable oil is composed mostly of medium-chain or long-chain fatty acids which exist as triglycerides. Although there are literatures which deal with the penetration of specific natural oils into hair there is a lack of research which provide the empirical data that can be used to explain the penetration of larger population of vegetable oils. This research was aimed to examine whether the chain length of fatty acid affect the penetration of fatty acid and protection in hair and also to apply the results on explaining the protective effect of Medium-Chain Triglyceride oil (MCT oil) and Coconut oil. Nine different hair treatments were formulated with three medium-chain fatty acids (C8:0, C10:0, C12:0), three long-chain fatty acids (C14:0, C16:0, C18:0), MCT oil, Coconut oil, and a blank. Composition of fatty acids of hair was examined by the Gas chromatography mass spectrometry. Penetration of fatty acid in hair was examined by the UV–VIS spectrophotometry. Protection of damaged hair was examined by the differences in color, tensile strength, thickness, and the concentration of protein leak of 21-day vs. 0-day measurements. Results of t-test indicated that the penetration and the protection of the medium-chain fatty acid was significantly better than those of the long-chain fatty acid, and that MCT oil and coconut oil were not significantly different.