Ostrich oil has been used extensively in the cosmetic and pharmaceutical industries. However, rancidity causes undesirable chemical changes in flavour, colour, odour and nutritional value. Bleaching is an important process in refining ostrich oil. Bleaching refers to the removal of certain minor constituents (colour pigments, free fatty acid, peroxides, odour and non-fatty materials) from crude fats and oils to yield purified glycerides. There is a need to optimize the bleaching process of crude ostrich oil prior to its use for therapeutic purposes. The objective of our study was to establish an effective method to bleach ostrich oil using peroxide value as an indicator of refinement. In our study, we showed that natural earth clay was better than bentonite and acid-activated clay to bleach ostrich oil. It was also found that 1 hour incubation at a 150 °C was suitable to lower peroxide value by 90%. In addition, the nitrogen trap technique in the bleaching process was as effective as the continuous nitrogen flow technique and as such would be the recommended technique due to its cost effectiveness.
Palm oil is natural oil packed with important compounds and fatty acids ready to be exploited in lipid-based formulations and drug delivery. Palm oil and palm kernel oil contain long-chain and medium-chain triglycerides, respectively, including phytonutrients such as tocotrienol, tocopherol and carotenes. The exploitation of these compounds in a lipid-based formulation would be able to address hydrophobicity, lipophilicity, poor bioavailability and low water-solubility of many current drugs. The utilisation of palm oil as part of the drug delivery system seemed to improve the bioavailability and solubility of the drug, stabilising emulsification of formulation between emulsifier and surfactant, promoting enhanced drug permeability and performance, as well as extending the shelf-life of the drug. Despite the complexity in designing lipid-based formulations, palm oil has proven to offer dynamic behaviour in providing versatility in drug design, form and delivery. However, the knowledge and application of palm oil and its fractions in lipid-based formulation are scarce and interspersed. Therefore, this study aims to focus on the research and outcomes of using palm oil in lipid-based formulations and drug delivery systems, due to the importance of establishing its capabilities and benefits.
Surgical operations are impossible without administering proper analgesia. Advancement in the field of anesthesia has invariably resulted in the accomplishment of all surgical processes without any inconvenience. Admittedly, the use of noble gas is on the decline. The noble gases may not interact chemically with any other substance under normal temperature and pressure but they may interact with proteins and lipids. Different anesthetic molecules may stimulate either proteins or lipids in membrane. There is a connection between the anesthetic molecules and the hydrophobic region of the membrane. In the present review, we attempt to highlight the interaction between the anesthetic molecule with proteins and lipids and their effects. We sketched few noble gases and some other existing molecules such as halothane and alcohol which interacted with proteins and lipids.
Natural products contain bioactive compounds that are produced naturally via synthetic or semisynthetic processes. These bioactive compounds play significant biological roles, especially for growth as well as in defense mechanisms against pathogens. Bioactive compounds in natural products have been extensively studied in recent decades for their pharmacological activities, such as anticancer, wound healing, anti-microbial, anti-inflammatory, and anti-oxidative properties. However, their pharmaceutical significance has always been hindered by their low bioavailability and instability with variations in pH, temperature, and exposure to light. Nanotechnology paves the way for the development of drug delivery systems by enhancing therapeutic efficacy. Nanostructured lipid carriers, a lipidbased drug delivery system, are recently being studied to improve the biocompatibility, biodegradability, bioavailability, solubility, permeability, and shelf life of bioactive compounds in the pharmaceutical industry. The ideal component and preparation method for bioactive compounds in nanostructured lipid carrier development is necessary for their physicochemical properties and therapeutic efficiency. Therefore, this review seeks to highlight recent developments, preparation, and application of nanostructured lipid carriers as carriers for natural bioactive compounds in improving their therapeutic potential in drug delivery systems.
Local heterogeneity in lipid self-assembly is important for executing the cellular membrane functions. In this work, we chemically modified 2-(2'-hydroxyphenyl)benzoxazole (HBO) and attached a C8 alkyl chain in two different locations to probe the microscopic environment of four lipidic phases of dodecyl β-maltoside. The fluorescence change in HBO and the new probes (HBO-1 and HBO-2) shows that in all phases (micellar, hexagonal, cubic and lamellar) three HBO tautomeric species (solvated syn-enol, anionic, and closed syn-keto) are stable. The formation of multi tautomers reflects the heterogeneity of the lipidic phases. The results indicate that HBO and HBO-1 reside in a similar location within the head group region, whereas HBO-2 is slightly pushed away from the sugar-dominated area. The stability of the solvated syn-enol tautomer is due to the formation of a hydrogen bond between the OH group of the HBO moiety and an adjacent oxygen atom of a sugar unit. The detected HBO anions was proposed to be a consequence of this solvation effect where a hydrogen ion abstraction by the sugar units is enhanced. Our results point to a degree of local heterogeneity and ionization ability in the head group region as a consequence of the sugar amphoterism.
The study explores on upstream and downstream process in Microcystis aeruginosa for biodiesel production. The alga was isolated from temple tank, acclimatized and successfully mass cultivated in open raceway pond at semi-continuous mode. A two step combined process was designed and harvested 99.3% of biomass, the daily dry biomass productivity was recorded up to 28gm(-2)day(-1). The lipid extraction was optimized and achieved 21.3%; physicochemical properties were characterized and found 11.7% of FFA, iodine value 72% and 99.2% of ester content. The lipid was transesterified by a two step simultaneous process and produced 90.1% of biodiesel; the calorific value of the biodiesel was 38.8MJ/kg. Further, the physicochemical properties of biodiesel was characterized and found to be within the limits of American ASTM D6751. Based on the areal and volumetric biomass productivity estimation, M. aeruginosa can yield 84.1 tons of dry biomass ha(-1)year(-1).
Two different procedures for the methylation of fatty acids (FAs) and trans fatty acids (TFAs) in food fats were compared using gas chromatography (GC-FID). The base-catalyzed followed by an acid-catalyzed method (KOCH3/HCl) and the base-catalyzed followed by (trimethylsilyl)diazomethane (TMS-DM) method were used to prepare FA methyl esters (FAMEs) from lipids extracted from food products. In general, both methods were suitable for the determination of cis/trans FAs. The correlation coefficients (r) between the methods were relatively small (ranging from 0.86 to 0.99) and had a high level of agreement for the most abundant FAs. The significant differences (P = 0.05) can be observed for unsaturated FAs (UFAs), specifically for TFAs. The results from the KOCH3/HCl method showed the lowest recovery values (%R) and higher variation (from 84% to 112%), especially for UFAs. The TMS-DM method had higher R values, less variation (from 90% to 106%), and more balance between variation and %RSD values in intraday and interday measurements (less than 4% and 6%, resp.) than the KOCH3/HCl method, except for C12:0, C14:0, and C18:0. Nevertheless, the KOCH3/HCl method required shorter time and was less expensive than the TMS-DM method which is more convenient for an accurate and thorough analysis of rich cis/trans UFA samples.
The adulteration of edible fats is a kind of fraud that impairs the physical and chemical features of the original lipid materials. It has been detected in various food, pharmaceutical and cosmeceutical products. Differential scanning calorimetry (DSC) is the robust thermo-analytical machine that permits to fingerprint the primary crystallisation of triacylglycerols (TAGs) molecules and their transition behaviours. The aims of this study was to assess the cross-contamination caused by lard concentration of 0.5-5% in the mixture systems containing beef tallow (BT) and chicken fat (CF) separately. TAGs species of pure and adulterated lipids in relation to their crystallisation and melting parameters were studied using principal components analysis (PCA). The results showed that by using the heating profiles the discrimination of LD from BT and CF was very clear even at low dose of less than 1%. Same observation was depicted from the crystallisation profiles of BT adulterated by LD doses ranging from 0.1% to 1% and from 2% to 5%, respectively. Furthermore, CF adulterated with LD did not exhibit clear changes on its crystallisation profiles. Consequently, DSC coupled with PCA is one of the techniques that might use to monitor and differentiate the minimum adulteration levels caused by LD in different animal fats.
Today, virgin coconut oil (VCO) is becoming valuable oil and is receiving an attractive topic for researchers because of its several biological activities. In cosmetics industry, VCO is excellent material which functions as a skin moisturizer and softener. Therefore, it is important to develop a quantitative analytical method offering a fast and reliable technique. Fourier transform infrared (FTIR) spectroscopy with sample handling technique of attenuated total reflectance (ATR) can be successfully used to analyze VCO quantitatively in cream cosmetic preparations. A multivariate analysis using calibration of partial least square (PLS) model revealed the good relationship between actual value and FTIR-predicted value of VCO with coefficient of determination (R2) of 0.998.
Gelucire 50/13 alone and solid dispersions in this material containing two model drugs (10% w/w caffeine and paracetamol) have been studied with a view to establishing the mechanism underpinning changes in drug-release characteristics as a function of storage time and temperature. The lipid systems were fabricated into tablets and stored for up to 180 days at temperatures of 20 and 37 degrees C. The dispersions were studied using differential scanning calorimetry (DSC), scanning electron microscopy, and dissolution testing. DSC studies indicated that the Gelucire 50/13 exists in two principal melting forms (melting points 38 and 43 degrees C) that undergo transformation to the higher melting form on storage at 37 degrees C. Scanning electron microscopy studies indicated that the systems exhibit "blooming," with crystal formation on the surface being apparent on storage at both temperatures. The dissolution rate increased on storage, with the effect being particularly marked at higher storage temperatures and for the paracetamol systems. However, whereas these changes corresponded well to those seen for the morphology, the correlation between the changes in dissolution and those of the DSC profiles was poor. The study has suggested a novel explanation for the storage instability of Gelucire 50/13 whereby the change in dissolution is associated not with molecular rearrangement as such but with the gross distribution of the constituent components, this in turn altering the physical integrity of the lipid bases.
Different fractions of fully hydrogenated soybean oil (FHSBO) in soybean oil (10-30% w/w) and the addition of 1% salt (sodium chloride) were used to investigate the effect of high-pressure treatments (HP) on the crystallization behaviors and physical properties of the binary mixtures. Sample microstructure, solid fat content (SFC), thermal and rheological properties were analyzed and compared against a control sample (crystallized under atmospheric condition). The crystallization temperature (Ts) of all model fats under isobaric conditions increased quadratically with pressure until reaching a pressure threshold. As a result of this change, the sample induction time of crystallization (tc) shifted from a range of 2.74-0.82 min to 0.72-0.43 min when sample crystallized above the pressure threshold under adiabatic conditions. At the high solid mass fraction, the addition of salt reduced the pressure threshold to induce crystallization during adiabatic compression. An increase in pressure significantly reduced mean cluster diameter in relation to the reduction of tc regardless of the solid mass fraction. In contrast, the sample macrostructural properties (SFC, storage modulus) were influenced more significantly by solid mass fractions rather than pressure levels. The creation of lipid gel was observed in the HP samples at 10% FHSBO. The changes in crystallization behaviors indicated that high-pressure treatments were more likely to influence crystallization mechanisms at low solid mass fraction.
Cell-penetrating peptides are used in the delivery of peptides and biologics, with some cell-penetrating peptides found to be more efficient than others. The exact mechanism of how they interact with the cell membrane and penetrate it, however, remains unclear. This study attempts to investigate the difference in free energy profiles of three cell-penetrating peptides (TAT, CPP1 and CPP9) with a model lipid bilayer (DOPC) using molecular dynamics pulling simulations with umbrella sampling. Potential mean force (PMF) and free energy barrier between the peptides and DOPC are determined using WHAM analysis and MM-PBSA analysis, respectively. CPP9 is found to have the smallest PMF value, followed by CPP1 and TAT, consistent with the experimental data. YDEGE peptide, however, does not give the highest PMF value, although it is a non-cell-permeable peptide. YDEGE is also found to form water pores, alongside with TAT and CPP9, suggesting that it is difficult to distinguish true water pore formation from artefacts arising from pulling simulations. On the contrary, free energy analysis of the peptide-DOPC complex at the lipid-water interface with MM-PBSA provides results consistent with experimental data with CPP9 having the least interaction with DOPC and lowest free energy barrier, followed by CPP1, TAT and YDEGE. These findings suggest that peptide-lipid interaction at the lipid-water interface has a direct correlation with the penetration efficiency of peptides across the lipid bilayer.
The Nanoemulgel drug delivery system is a formulation related intervention to improve the systemic delivery and therapeutic profile of lipophilic drugs. Nanoemulgel is an amalgamated formulation of two different systems in which nanoemulsion containing drug is incorporated into a gel base. The fusion of the two systems makes this formulation advantageous in several ways. Lipophilic drugs can be easily incorporated and the skin permeability of the incorporated drugs can be enhanced in several folds due to the finely distributed droplets of nanoemulsion phase. As a result, the pharmacokinetic and pharmacodynamic profiles of the lipophilic drugs are improved significantly. An increasing trend in topical nanoemulgel use in recent years has been noticed because of the better acceptability of the preparation to the patients due to their noninvasive delivery, avoidance of gastrointestinal side effects, easier applicability and good therapeutic and safety profile. Despite of having few limitations, nanoemulgel formulation can be considered as a potential and promising candidates for topical delivery of lipophilic drugs in the future. The aim of this review is to evaluate and report the current potential and future scope of nanoemulgel formulation for becoming an effective delivery system for poorly water soluble drugs. In this review, we have summarized and discussed the outcome of different studies on permeability, pharmacokinetic, pharmacodynamic and safety profile of the drugs delivered topically through nanoemulgel. Rationality of use along with the major challenges to overcome for nanoemulgel formulation has been discussed.
The physico-chemical properties of lipids influencing the solubilisation of imatinib mesylate (IM) in lipid matrix were evaluated and a statistical model to predict the same has been derived in the present study. After experimental quantification of IM solubility in various lipids, Hansen Hildebrand's total solubility parameters were calculated in order to study the role of various forces connected to lipid-drug interaction. To develop a relationship between the various descriptors of the lipids and experimental solubility of IM in lipids (% w/w), quantitative structure-solubility relationship (QSSR) was used. To generate equations that can predict the solubility of IM in lipids (%w/w), multiple linear regression was used. Amongst the various lipids tested, glyceryl monostearate and behenic acid solubilised the highest (6.19 ± 0.22%) and lowest (0.01 ± 0.01%) amounts of IM respectively. Our results suggested that alkyl chain length, polarity of the lipids, index of cohesive interaction in solids, estimated number of hydrogen bonds that would be accepted by the solute from water molecules in an aqueous solution, estimated number of hydrogen bonds that would be donated by the solute to water molecules in an aqueous solution and solvent accessible surface area collectively play a significant role in solubilising IM in the lipids. The equation developed could predict the solubility of IM in lipids with good accuracy (R2pred = 0.912).
LML-type structured lipids are one type of medium- and long-chain triacylglycerols. LML was synthesized using immobilized Talaromyces thermophilus lipase (TTL)-catalyzed interesterification of tricaprylin and ethyl linoleate. The resin AB-8 was chosen, and the lipase/support ratio was determined to be 60 mg/g. Subsequently, the immobilized TTL with strict sn-1,3 regiospecificity was applied to synthesize LML. Under the optimized conditions (60 °C, reaction time 6 h, enzyme loading of 6% of the total weight of substrates, substrate of molar ratio of ethyl linoleate to tricaprylin of 6:1), Triacylglycerols with two long- and one medium-chain FAs (DL-TAG) content as high as 52.86 mol% was obtained. Scale-up reaction further verified the industrial potential of the established process. The final product contained 85.24 mol% DL-TAG of which 97 mol% was LML after purification. The final product obtained with the high LML content would have substantial potential to be used as functional oils.
The kinetics of lipid extraction utilizing microwave-assisted extraction (MAE) from Nannochloropsis sp. microalgae were studied using a low cost and green solvent, namely brine (NaCl) solution. The kinetic modelling of the lipid extraction was performed to evaluate the mechanism of the lipid mass transfer using different extraction models, including Fick's Law, First and Second-order Rate Law and the Patricelli mathematical model. The Patricelli mathematical model described the kinetics of lipid extraction well, with the highest average values of determination coefficient (R2 ≥ 0.952) and the lowest average values of mean relative percentage deviation (MRPD ≤ 8.666%). The lipid analysis indicated a positive influence of the microwave temperature and time on the quantity and quality of extracted lipids. SEM analysis of spent microalgae clearly shows an increase in the distorted cell with increase microwave temperature and time, which could be directly correlated to the mechanism of the MAE-brine technique.
Three short sediment cores from inner continental shelf of the southern South China Sea (5-50 km) off Terengganu were analyzed for lipid contents (i.e., homologous aliphatic compounds and sterols) using gas chromatography-mass spectrometry. The concentrations of the total aliphatic hydrocarbons (TAHs) ranged from 0.152 to 6.91 μg/g dry weight. The n-alkane distribution was from nC₁₃ to nC₃₆, with a carbon preference index (CPI₁₃₋₃₅) from 1.08 to 4.28 and a carbon number maximum (Cmax), depending on a sample, at 31 or 18. In addition, a strong odd-to-even carbon number predominance was observed in nC₂₅-nC₃₅ range. The distribution of the n-alkanoic acids and n-alkanols in all samples exhibited an even-to-odd carbon number predominance and ranged from C₁₀ to C₂₆ and from C₁₂ to C₃₄, respectively. The n-alkanols were dominated by the long-chain homologs with Cmax at 22; on the other hand, the n-alkanoic acid distributions showed a predominance of short-chain homologs with a Cmax at 16. The total sterol concentrations ranged from 0.41 to 3.57 μg/g dry weight. Cholesterol was most abundant at the offshore stations, whereas sitosterol was dominant at near-shore station. Pentacyclic triterpenoids such as friedelin and taraxerol α- and β-amyrins, which are known biomarkers for higher plants, were detected at all stations with a dilution trend offshore. In conclusion, the marine sediments off southern Terengganu can still be considered uncontaminated, where the compound sources are biogenic from terrestrial plants superimposed with a marine productivity input.
Biodiesel with improved yield was produced from microalgae biomass under simultaneous cooling and microwave heating (SCMH). Nannochloropsis sp. and Tetraselmis sp. which were known to contain higher lipid species were used. The yield obtained using this novel technique was compared with the conventional heating (CH) and microwave heating (MWH) as the control method. The results revealed that the yields obtained using the novel SCMH were higher; Nannochloropsis sp. (83.33%) and Tetraselmis sp. (77.14%) than the control methods. Maximum yields were obtained using SCMH when the microwave was set at 50°C, 800W, 16h of reaction with simultaneous cooling at 15°C; and water content and lipid to methanol ratio in reaction mixture was kept to 0 and 1:12 respectively. GC analysis depicted that the biodiesel produced from this technique has lower carbon components (<19 C) and has both reasonable CN and IV reflecting good ignition and lubricating properties.
The gastrointestinal (GI) transit behavior of and absorption from an amphotericin B (AmB) solid lipid nanoformulation (SLN) in rats was investigated. We aimed to estimate the gastric emptying time (GET) and cecal arrival time (CAT) of AmB SLN in rats as animal models. From these two parameters, an insight on the absorption window of AmB was ascertained. Three types of SLNs, AmB, paracetamol (PAR), and sulfasalazine (SSZ), were similarly formulated using beeswax/theobroma oil composite as the lipid matrix and characterized with regard to size, viscosity, density, migration propensity within agarose gel, in vitro drug release, morphology, gastrointestinal transit, and in vivo absorption. The GET and CAT were estimated indirectly using marker drugs: PAR and sulfapyridine (SP). All three types of SLNs exhibited identical properties with regard to z-average, viscosity, relative density, and propensity to migrate. PAR was absorbed rapidly from the small intestine following emptying of the SLNs giving the T50E (time for 50% absorption of PAR) to be 1.6 h. SP was absorbed after release and microbial degradation of SSZ from SLN in the colon with a lag time of 2 h post-administration, serving as the estimated cecal arrival time of the SLNs. AmB within SLN was favorably absorbed from the small intestine, albeit slowly.
Cancer nanotherapy is progressing rapidly with the introduction of many innovative drug delivery systems to replace conventional therapy. Although the antitumor activity of zerumbone (ZER) has been reported, there has been no information available on the effect of ZER-loaded nanostructured lipid carrier (NLC) (ZER-NLC) on murine leukemia cells. In this study, the in vitro and in vivo effects of ZER-NLC on murine leukemia induced with WEHI-3B cells were investigated. The results from 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide, Hoechst 33342, Annexin V, cell cycle, and caspase activity assays showed that the growth of leukemia cells in vitro was inhibited by ZER-NLC. In addition, outcomes of histopathology, transmission electron microscopy, and Tdt-mediated dUTP nick-end labeling analyses revealed that the number of leukemia cells in the spleen of BALB/c leukemia mice significantly decreased after 4 weeks of oral treatment with various doses of ZER-NLC. Western blotting and reverse-transcription quantitative polymerase chain reaction assays confirmed the antileukemia effects of ZER-NLC. In conclusion, ZER-NLC was shown to induce a mitochondrial-dependent apoptotic pathway in murine leukemia. Loading of ZER in NLC did not compromise the anticancer effect of the compound, suggesting ZER-NLC as a promising and effective delivery system for treatment of cancers.