Lipid Preparations Research Articles

Alleviation of Tumor Invasion by the Development of Natural Polymerbased Low-risk Chemotherapeutic Systems - review on the Malignant Carcinoma Treatments.

The spread of tumors (48% in men and 51% in women), as well as the protection of malignant tumors by stromal cells and complex blood vessels, pose significant challenges to drug delivery to tumors. Modern chemotherapy, on the other hand, addresses tumor growth suppression by at least 60% through versatile formulation systems and numerous modifications to drug delivery systems. The renewable and naturally occurring polymers present invariably in all living cells form the fundamental foundation for most anticancer drug development. The review aims to discuss in detail the preparations of polysaccharide, lipid, and protein-based drug-loading vehicles for the targeted delivery of prominent anticancer drugs. It also provides an explanation of drug distribution in blood (cumulative releases of nearly 80% drug) and drug accumulation at tumor sites (1-5 mg/kg) due to enhanced permeability and retention (EPR). Specific delivery examples for treating colorectal and breast carcinomas have been presented to distinguish the varied drug administration, bioavailability, and tumor internalization mechanisms between sugar, fatty acid, and amino acid polymers. Current therapy possibilities based on cutting-edge literature are provided, along with drug delivery systems tailored to tumor location and invasive properties. The unique combinations of the three natural polymers provide unparalleled solutions to minimize the toxicity (<20% drug release) of the chemotherapeutic drugs on normal tissues. Moreover, the development of a consolidated drug delivery system has contributed to a substantial reduction (dose reduction from 10.43 μM to 1.9 μM) in the undesirable consequences of higher dosages of chemotherapeutic drugs. The review extensively covers safe chemotherapeutic systems with significant advantages (tumor volume shrinkage of 4T1 cells from 1000 mm3 to 200 mm3) in clinical applications of carcinoma treatments using natural polymers.

A review on preparation and application of low-calorie structured lipids in food system

A review on preparation and application of low-calorie structured lipids in food system

Automated preparation of plasma lipids, metabolites, and proteins for LC/MS-based analysis of a high-fat diet in mice

Blood plasma is one of the most commonly analyzed and easily accessible biological samples. Here, we describe an automated liquid-liquid extraction platform that generates accurate, precise, and reproducible samples for metabolomic, lipidomic, and proteomic analyses from a single aliquot of plasma while minimizing hands-on time and avoiding contamination from plasticware. We applied mass spectrometry to examine the metabolome, lipidome, and proteome of 90 plasma samples to determine the effects of age, time of day, and a high-fat diet in mice. From 25 μl of mouse plasma, we identified 907 lipid species from 16 different lipid classes and subclasses, 233 polar metabolites, and 344 proteins. We found that the high-fat diet induced only mild changes in the polar metabolome, upregulated apolipoproteins, and induced substantial shifts in the lipidome, including a significant increase in arachidonic acid and a decrease in eicosapentaenoic acid content across all lipid classes.

Bioactive lipid‐enriched concentrates from squid discards by one‐step and two‐step extractions with non‐halogenated solvents

SummaryThis study focused on the preparation of lipid concentrates with high contents of bioactive molecules. Different one‐step and two‐step extractions with non‐halogenated solvents (hexane, HX; isopropanol, IP) were carried out on Patagonian squid (Doryteuthis gahi) discards. As a first step, HX extractions (one, two or three times) were carried out. The resulting substrates were extracted with IP (two, three or four times). Analysis of lipid extracts included total lipid, phospholipid (PL) and tocopherol values, and fatty acid (FA) profile. HX extractions led to remarkable α‐ and γ‐tocopherol values (ca. 1400 and 23 mg kg−1 lipids, respectively); no effect (P &gt; 0.05) of the number of HX extractions was observed. IP extracts provided high PL values (383–501 mg kg−1 lipids); the highest average values were detected with four IP extractions after three HX extractions. Values obtained for tocopherols and PLs were higher (P &lt; 0.05) than those obtained by employing the conventional (chloroform/methanol, 1:1) lipid extraction (ca. 496 and 11 mg kg−1 lipids and 400 g kg−1 lipids, respectively). Range values detected for eicosapentaenoic and docosahexaenoic acid values and the ω3/ω6 FA ratio were similar to those obtained by the conventional procedure. A valuable procedure is proposed for obtaining PL‐ and tocopherol‐enriched concentrates from marine waste with non‐halogenated solvents.

Preparation and isolation of hydrophilic mannosylerythritol lipids via chemical modification and stepwise extraction

AbstractMannosylerythritol lipids (MELs), a glycolipid biosurfactant, possess great potential in many high‐value‐added fields. However, its water‐insolubility is an important obstacle to its wide application, especially in home and personal care fields. In this study, a new strategy “killing two birds with one stone” based on the chemical modification of natural MELs was developed for the preparation of hydrophilic MELs. These newly prepared MELs can be efficiently isolated from the reacted solution via stepwise extraction with a methanol/n‐hexane system. 88% of hydrophilic MELs were recovered from natural MELs, with a corresponding yield of 50%. This is mainly attributed to the esterification of fatty acids, representing the main and relatively‐difficult‐to‐remove impurities in fermentative‐produced MELs, facilitating separation from the MEL product via extraction. Moreover, these new MELs presented comparable surface activities to natural MELs while exhibiting enhanced water solubility and biocompatibility. This originates from the generation of MEL‐D, resulting from the deacetylation of natural MELs and the formation of new hydrophilic MELs containing just one hydrophobic chain (named “MEL‐G”). Hence, the present strategy is not only beneficial for the removal of impurities (fatty acids) but also for the preparation of MELs with improved hydrophilicity.

Synthesis and biological evaluation of lipid A derived from commensal Bacteroides.

The inflammation-inducing properties of lipopolysaccharides (LPS) of Gram-negative bacteria reside in their lipid A moiety. Bacillus fragilis, which is a commensal Gram-negative bacterium, biosynthesises lipid A that is structurally distinct from that of E. coli and other enteric bacteria. It is composed of a β1,6-linked glucosamine (GlcN) disaccharide that is only phosphorylated at the anomeric center. The major species of B. fragilis has five fatty acids and the amine of the distal GlcN moiety carries the unusual (R)-3-(13-methyltetradecanoyloxy)-1.5-methylhexadecanoic acid. A recent study indicates that the LPS of B. fragilis has anti-viral activity by selective induction of interferon (IFN)-β and is protective in mouse models of vesicular stomatitis virus (VSV) and influenza A. Heterogeneity in the structures of LPS and lipid A and possible contamination with other inflammatory components make it difficult to unambiguously define the immune-modulatory properties of LPS or lipid A. Therefore, we developed a synthetic approach for the preparation of the unusual major lipid A species derived from B. fragilis, which includes a synthetic approach for (R)-3-(13-methyltetradecanoyloxy)-1.5-methylhexadecanoic acid by the Wittig olefination to install the terminal isopropyl moiety. The proinflammatory and antiviral responses of synthetic B. fragilis lipid A were investigated in several cell lines and primary human monocytes by examining the production of interleukin (IL)-6 and IFN-β. It was found that B. fragilis does not induce the production of IL-6 and IFN-β but can partially antagonize the production of pro-inflammatory cytokines induced by E. coli LPS and lipid A.

Comparison of metabolic parameters between oral and total parenteral nutrition in children with severe eating disorders.

This study investigated changes of lipid parameters in children with severe eating disorders during refeeding in order to explore the optimal timing for lipid preparation administration. We prospectively assessed the physical conditions of patients with eating disorders after the start of nutrition therapy. The assessments were performed at admission and at 2 and 4 weeks. Lipid metabolism was assessed based on triglyceride (TG), total cholesterol (TC), and free carnitine (FC) levels, as well as acylcarnitine/free carnitine (AC/FC) ratio. A total of 18 patients were included. Of these, 12 and 6 received an oral diet (OD group) and total parenteral nutrition (TPN group), respectively. The mean body mass indexes at hospital admission were 12.8 kg/m2 in the OD group and 12.7 kg/m2 in the TPN group. At 2 weeks after the start of refeeding, TC, TG, and AC/FC levels were significantly lower in the TPN group than in the OD group. Other blood test results did not show any significant differences between the two groups. Fat-free glucose-based nutrition promoted lipid metabolism over a 2-week period after the start of refeeding, suggesting that balanced energy and lipid intake are essential, even in TPN.

Comparison of metabolic parameters between oral and total parenteral nutrition in children with severe eating disorders.

This study investigated changes of lipid parameters in children with severe eating disorders during refeeding in order to explore the optimal timing for lipid preparation administration. We prospectively assessed the physical conditions of patients with eating disorders after the start of nutrition therapy. The assessments were performed at admission and at 2 and 4 weeks. Lipid metabolism was assessed based on triglyceride (TG), total cholesterol (TC), and free carnitine (FC) levels, as well as acylcarnitine/free carnitine (AC/FC) ratio. A total of 18 patients were included. Of these, 12 and 6 received an oral diet (OD group) and total parenteral nutrition (TPN group), respectively. The mean body mass indexes at hospital admission were 12.8 kg/m2 in the OD group and 12.7 kg/m2 in the TPN group. At 2 weeks after the start of refeeding, TC, TG, and AC/FC levels were significantly lower in the TPN group than in the OD group. Other blood test results did not show any significant differences between the two groups. Fat-free glucose-based nutrition promoted lipid metabolism over a 2-week period after the start of refeeding, suggesting that balanced energy and lipid intake are essential, even in TPN.

Development of standard operating procedures and pharmaceutical study of herbal lipid preparation

Development of standard operating procedures and pharmaceutical study of herbal lipid preparation

Computational Amendment of Parenteral In Situ Forming Particulates' Characteristics: Design of Experiment and PBPK Physiological Modeling.

Lipid and/or polymer-based drug conjugates can potentially minimize side effects by increasing drug accumulation at target sites and thus augment patient compliance. Formulation factors can present a potent influence on the characteristics of the obtained systems. The selection of an appropriate solvent with satisfactory rheological properties, miscibility, and biocompatibility is essential to optimize drug release. This work presents a computational study of the effect of the basic formulation factors on the characteristics of the obtained in situ-forming particulates (IFPs) encapsulating a model drug using a 21.31 full factorial experimental design. The emulsion method was employed for the preparation of lipid and/or polymer-based IFPs. The IFP release profiles and parameters were computed. Additionally, a desirability study was carried out to choose the optimum formulation for further morphological examination, rheological study, and PBPK physiological modeling. Results revealed that the type of particulate forming agent (lipid/polymer) and the incorporation of structure additives like Brij 52 and Eudragit RL can effectively augment the release profile as well as the burst of the drug. The optimized formulation exhibited a pseudoplastic rheological behavior and yielded uniformly spherical-shaped dense particulates with a PS of 573.92 ± 23.5 nm upon injection. Physiological modeling simulation revealed the pioneer pharmacokinetic properties of the optimized formulation compared to the observed data. These results assure the importance of controlling the formulation factors during drug development, the potentiality of the optimized IFPs for the intramuscular delivery of piroxicam, and the reliability of PBPK physiological modeling in predicting the biological performance of new formulations with effective cost management.

Metabolism of serine/glycine lipids by human gingival cells in culture.

Porphyromonas gingivalis produces five classes of serine/glycine lipids that are recovered in lipid extracts from periodontitis-afflicted teeth and diseased gingival tissues, particularly at sites of periodontitis. Because these lipids are recovered in diseased gingival tissues, the purpose of the present study was to evaluate the capacity of cultured human gingival fibroblasts (HGF), keratinocytes, and macrophages to hydrolyze these lipids. We hypothesize that one or more of these cell types will hydrolyze the serine/glycine lipids. The primary aim was to treat these cell types for increasing time in culture with individual highly enriched serine/glycine lipid preparations. At specified times, cells and culture media samples were harvested and extracted for hydrolysis products. The serine/glycine lipids and hydrolysis products were quantified using liquid chromatography-mass spectrometry (LC-MS) and free fatty acids were quantified using gas chromatograph-mass spectrometer. LC-MS analysis used two different mass spectrometric methods. This study revealed that treatment of HGF or macrophage (THP1) cells with lipid (L) 654 resulted in breakdown to L342 and subsequent release into culture medium. However, L654 was converted only to L567 in gingival keratinocytes. By contrast, L1256 was converted to L654 by fibroblasts and macrophages but no further hydrolysis or release into medium was observed. Gingival keratinocytes showed no hydrolysis of L1256 to smaller lipid products but because L1256 was not recovered in these cells, it is not clear what hydrolysis products are produced from L1256. Although primary cultures of gingival fibroblasts and macrophages are capable of hydrolyzing specific serine/glycine lipids, prior analysis of lipid extracts from diseased gingival tissues revealed significantly elevated levels of L1256 in diseased tissues. These results suggest that the hydrolysis of bacterial lipids in gingival tissues may reduce the levels of specific lipids, but the hydrolysis of L1256 is not sufficiently rapid to prevent significant accumulation at periodontal disease sites.

Valorisation of prawn/shrimp shell waste through the production of biologically active components for functional food purposes.

The aim of the work was to develop a technology for using waste from prawn and shrimp processing as a source of active ingredients that could be used in the promotion of healthy foods. From fresh and freeze-dried prawn and shrimp shells, protein hydrolysates (carotenoproteins) were obtained using two different enzymes, Flavourzyme and Protamex. The obtained hydrolysates were characterised in terms of protein content, degree of hydrolysis, and antioxidant and antimicrobial activity. The hydrolysate with the best antioxidant properties (FRAP value of 2933.33 μmol L-1 TE; ORAC value of 115.58 μmol L-1 TE) was selected and tested for its possible use as a component of functional foods. Molecular weight distribution, amino acid profile and free amino acids, the solubility of the hydrolysate in different pH ranges as well as foaming ability were determined. It was found that this hydrolysate was characterised by an amino acid profile with high nutritional value, flavour enhancement properties and excellent solubility in a wide pH range (from 97.06% to 100%). Afterward, the possibility of using carotenoproteins from prawn waste as a component of an emulsion with furcellaran and a lipid preparation of astaxanthin, taken from post-hydrolysate production waste, was investigated. The obtained complexes were stable as proved by the measurement of zeta potential (ζ = -23.87 and -22.32 to -27.79 mV). It is possible to produce stable complexes of the hydrolysate with furcellaran and to emulsify a lipid preparation of astaxanthin, obtained from waste following production of the hydrolysate, in them. © 2023 Society of Chemical Industry.

Synthesis of ether lipids: natural compounds and analogues.

Ether lipids are compounds present in many living organisms including humans that feature an ether bond linkage at the sn-1 position of the glycerol. This class of lipids features singular structural roles and biological functions. Alkyl ether lipids and alkenyl ether lipids (also identified as plasmalogens) correspond to the two sub-classes of naturally occurring ether lipids. In 1979 the discovery of the structure of the platelet-activating factor (PAF) that belongs to the alkyl ether class of lipids increased the interest in these bioactive lipids and further promoted the synthesis of non-natural ether lipids that was initiated in the late 60's with the development of edelfosine (an anticancer drug). More recently, ohmline, a glyco glycero ether lipid that modulates selectively SK3 ion channels and reduces in vivo the occurrence of bone metastases, and other glyco glycero ether also identified as GAEL (glycosylated antitumor ether lipids) that exhibit promising anticancer properties renew the interest in this class of compounds. Indeed, ether lipid represent a new and promising class of compounds featuring the capacity to modulate selectively the activity of some membrane proteins or, for other compounds, feature antiproliferative properties via an original mechanism of action. The increasing interest in studying ether lipids for fundamental and applied researches invited to review the methodologies developed to prepare ether lipids. In this review we focus on the synthetic method used for the preparation of alkyl ether lipids either naturally occurring ether lipids (e.g., PAF) or synthetic derivatives that were developed to study their biological properties. The synthesis of neutral or charged ether lipids are reported with the aim to assemble in this review the most frequently used methodologies to prepare this specific class of compounds.

A Concise review on application of solid lipids and various techniques in the formulation development

Lipids have wide range of applications in food and pharmaceuticals. The pharmaceuticals application of lipid is to improve solubility of drug also helps to improve the bioavailability. The dissolution/dissolving phase, which is probably the rate-limiting component for oral absorption of poorly water-soluble drugs, is eliminated by pre-dissolving pharmaceuticals in lipids, surfactants, or combinations of lipid excipients and surfactants. The most widely used co-solvents, together with lipid excipients, are propylene glycol, glycerol, and polyethylene glycols-400, poloxamer etc. various technologies are used such as melt extrusion, melt granulation for preparation of lipid based oral modified released dosage forms. This review summaries the overview of the lipid excipients in terms of their classification, methods of absorption, and lipid-based product development. The manufacture of solid and semi-solid lipid formulations using various methodologies, applications, phase behaviour, and the regulatory outlook of lipid excipients are covered.&#x0D; Keywords: Solid lipids, lipid classification, solidification techniques, modified released.

First case of Rhinocladiella mackenziei brain abscess in Turkey: Case report and review of the literature.

Rhinocladiella mackenziei is a highly neurotropic fungus, mainly reported from the Middle East. However, in recent years, there have been some cases from outside this region. We described an additional fatal case of R. mackenziei cerebral infection for the first time from Turkey and made a literature review of all previously reported cases. During 34 years (1988-2022), there have been 42 R. mackenziei brain abscess cases. Most patients have been reported from Saudi Arabia (n = 14, 33.3%). It is noteworthy that 40.5% of patients, including our case, were immunocompetent at initial diagnosis and mostly presented with a single lesion (n = 10, 23.8%). The most frequent comorbidities were solid organ transplant (n = 9, 21.4%), diabetes mellitus (n = 6, 14.3%), malignancy (n = 6, 14.3%) and prior surgery (n = 3, 7.1%). The most commonly used initial antifungal regimen were amphotericin B together with itraconazole (n = 9, 21.4%), combinations of lipid preparations of amphotericin B, voriconazole and/or posaconazole (n = 9, 21.4%) and amphotericin B alone (n = 8, 19%). Although both surgical procedures and antifungal medication in the majority of patients were performed, mortality rates remained high (90.4%). The area at risk of R. mackenziei cerebral abscess cases extends to other countries. Clinicians should be aware of this emerging disease and take a detailed travel history in patients with atypical and undocumented brain abscesses. Our case confirms the hypothesis that this fungus might spread more widely than previously predicted regions.

Comparative Study of Physico-Chemical Analysis of Changeri Ghrita Prepared with Murchita and Amurchita Ghrita

Changeri ghrita is a medicated ghee formulation, mentioned in Grahani rog chikitsa. Sneha murchana is a procedure prior to Snehapaka. Snehapaka and Murchana bring changes in Sneha. Materials and Methods: Two batches of Changeri ghrita prepared using Murchita and Amurchit ghrita. Prepared Ghrita subjected to physico-chemical analysis. Result and Discussion: Specific gravity increased in Murchita ghrita. Refractive index, viscosity, saponification value, iodine values were increased. While acid value is decreased. Peroxide value is slightly increased. Unsaponifiable matter remains unchanged. There was change in organoleptic properties after Murchana. Physico-chemical changes have been occurring except in unsaponifiable matter and congealing point. Peroxide was present in both samples of Amurchit and Murchit Changeri ghrita. Saponification value was increased in Murchit Changeri Ghrita Conclusion: It can be concluded that antioxidants were added during Murchana. Murchana maintains stability of lipid preparation and offer good health impact, increases palatability.

Biotechnology in Future Food Lipids: Opportunities and Challenges.

Lipids are a large group of essential nutrients in daily diets that provide energy and maintain various physiological functions. As the global population is rapidly expanding, there is an urgent need to enhance the production and quality of food lipids. The development of modern biotechnology allows the manipulation of oil production in plants and microorganisms and the improvement of the nutritional value of food lipids. Various metabolic engineering strategies have been exploited to increase oil production and produce value-added oils in traditional oil crops and other novel lipid sources (e.g., plant vegetative tissues, microalgae, and oleaginous microorganisms). Furthermore, natural lipid structures can be modified by lipases to prepare functional lipids, e.g., diacylglycerols, medium-long-medium-type structured triacylglycerols, human milk-fat substitutes, and structuralphospholipids, for specific nutritional demands. In this review, we focus on the recent advances in metabolic engineering of lipid production in plants and microorganisms, and the preparation of functional lipids via biocatalysis.

Impact of particle size of multivesicular liposomes on the embolic and therapeutic effects in rabbit VX2 liver tumor

Transcatheter arterial chemoembolization (TACE) is usually considered more efficacious in the local treatment of parenchyma-sparing hepatocellular carcinoma (HCC). At present, embolic agents commonly used in TACE, include DC pellets, Hepasphere, Lipiodol, etc. Except that iodine oil is a viscous fluid embolic agent, other solid microsphere particles used clinically range from 70 to 700 µm, among which 100 to 300 µm is the most commonly used. With the technology development of micro-invasive interventional therapy, the specific distal embolization through TACE to occlude tumor arterial blood supply in patients with HCC is also required more accurately. Effective terminal embolization is considered to be a preferred option for TACE therapy due to significantly improving the survival rate of patients and preserving liver function. In this article, we prepared the multifunctional multivesicular liposomes (IVO-DOX-MVLs) (<100 µm) that can simultaneously encapsulate ioversol and doxorubicin based on the high-phase transition temperature (T m) lipid ingredients, and evaluated its local artery embolization and therapeutic effect in rabbit VX-2 tumor model. The influence of particle size on occlusion and therapeutic effect of MVLs on rabbit VX-2 liver tumor models were well evaluated, including the tumor volume change, tumor growth rate, and necrosis rate, which were evaluated by magnetic resonance (MR). MVL samples with average particle size distribution of 50–60 µm exhibited fewer off-target embolization. Through TACE, IVO-DOX-MVLs were directly transported to the tumor tissues, playing roles of embolization performance, CT imaging effect, and local tumor killing effect. The feasibility of MVLs as a multifunctional embolic agent in its clinical application can be further improved by optimization of lipid composition and preparation process.

Phospholipid Preparations to Characterize Protein-Lipid Interactions In Vitro.

The lipid bilayers of the cell are composed of various lipid classes and species. These engage in cell signaling and regulation by recruiting cytosolic proteins to the membrane and interacting with membrane-embedded proteins to alternate their activity and stability. Like lipids, membrane proteins are amphipathic and are stabilized by the hydrophobic forces of the lipid bilayer. Membrane protein-lipid interactions are difficult to investigate since membrane proteins need to be reconstituted in a lipid-mimicking environment. A common and well-established approach is the detergent-based solubilization of the membrane proteins in detergent micelles. Nowadays, nanodiscs and liposomes are used to mimic the lipid bilayer and enable the work with membrane proteins in a more natural environment. However, these protocols need optimization and are labor intensive. The present protocol describes straightforward instructions on how the preparation of lipids is performed and how the lipid detergent mixture is integrated with the membrane protein MARCH5. The lipidation protocol was performed prior to an activity assay specific to membrane-bound E3 ubiquitin ligases and a stability assay that could be used for any membrane protein of choice.

Editorial introductions.

Editorial introductions.