Karolina Olechowska, Nikola Mielniczek, Katarzyna Hąc-Wydro
{"title":"The effect of selected bisphenols on model erythrocyte membranes of different cholesterol content","authors":"Karolina Olechowska, Nikola Mielniczek, Katarzyna Hąc-Wydro","doi":"10.1016/j.chemphyslip.2022.105224","DOIUrl":"https://doi.org/10.1016/j.chemphyslip.2022.105224","url":null,"abstract":"<div><p>Bisphenols belong to the group of environmental pollutants with proven harmful impact on human red blood cells. However, the exact effect of these substances may vary depending on the lipid composition of the cell membrane, since this structure is the first barrier between the cell interior and the external environment. The aim of this work was to analyze the influence of bisphenol A (BPA), bisphenol S (BPS) and their 1:1 mixture on model human erythrocyte membranes, composed of sphingomyelin (SM), phospatidylcholine (PC) and cholesterol (Chol). Due to the postulated correlation between the content of cholesterol in biomembranes and the toxic effect of bisphenols the model systems of different sterol concentrations (10, 20 and 40 mol% of Chol) were used in the studies. In the experiments, Langmuir monolayer technique accompanied with Brewster Angle Microscopy were applied and liposome properties were investigated. The obtained findings reveal that, in the investigated range of the sterol content, the effect of BPA, namely the changes of the organization and stability of model membranes and weakening of the attractive lipid-lipid interactions, is strongly dependent on the concentration of Chol in the system. The higher the sterol content, the stronger the BPA-induced alterations in membrane properties. However taking into account the results reported previously for the system containing 33.3% of cholesterol, it seems that the relationship between the effect of BPA and the amount of Chol is not linear for higher sterol concentrations. In contrast, BPS shows a much weaker influence on model erythrocyte membranes and does not act selectively on the systems studied. The effect of a mixture of BPA and BPS is intermediate between that of BPA and BPS used separately, however, the observed effects appear to be determined only by the presence of BPA in the system. Thus, the concentration of cholesterol in human erythrocyte membranes, which depends on factors such as age or health status, may play a key role in the toxic effects of BPA but not BPS.</p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"247 ","pages":"Article 105224"},"PeriodicalIF":3.4,"publicationDate":"2022-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"3337043","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Experimental and theoretical investigations into the mechanism of interactions between membrane-bound fatty acids and their binding protein: A model system to investigate the behavior of lipid acyl chains in contact with proteins","authors":"Shigeru Sugiyama , Daisuke Matsuoka , Toshiaki Hara , Masashi Sonoyama , Shigeru Matsuoka , Michio Murata","doi":"10.1016/j.chemphyslip.2022.105227","DOIUrl":"10.1016/j.chemphyslip.2022.105227","url":null,"abstract":"<div><p><span><span>The interaction of proteins with hydrophobic ligands in biological membranes<span> is an important research topic in the life sciences. The hydrophobic nature of ligands, especially their lack of water solubility, often makes it difficult to experimentally investigate their interactions with proteins, thus hampering quantitative evaluation based on thermodynamic parameters. The fatty acid-binding proteins, particularly FABP3, discussed in this review can recognize fatty acids, a primary component of </span></span>membrane lipids<span><span><span>, with high affinity. The precise three-dimensional structure of fatty acids and related ligands bound in FABP3 and their interaction with the binding pocket will contribute to the understanding of accurately determining physicochemical factors that cause the expression of affinity between protein surfaces and </span>lipids in biological membranes. During the research of FABP3, we encountered many of the problems that were widely implicated in experiments dealing with hydrophobic ligands. To address these issues, we developed experimental methodologies using X-ray crystallography, </span>calorimetry, and </span></span>surface plasmon resonance<span>. Using these methods and computational approaches, we have obtained several insights into the interaction of hydrophobic ligands with protein binding sites. Structural and functional studies of FABP potentially lead to a better understanding of the interaction between lipids and proteins, and thus, this protein may provide one of the model systems for investigating substance transport across cell membranes and inner membrane systems.</span></p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"247 ","pages":"Article 105227"},"PeriodicalIF":3.4,"publicationDate":"2022-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40588209","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Evaluation of liver specific ionizable lipid nanocarrier in the delivery of siRNA","authors":"Shilpa Rana , Archana Bhatnagar , Suman Singh , Nirmal Prabhakar","doi":"10.1016/j.chemphyslip.2022.105207","DOIUrl":"https://doi.org/10.1016/j.chemphyslip.2022.105207","url":null,"abstract":"<div><p><span><span>Hepcidin, a key regulator of </span>iron homeostasis, has been implicated in the pathogenesis of various iron-related diseases. Although </span>small interfering RNA<span><span><span> (siRNA) are potent to modulate the expression of hepcidin, their bioavailability remains a major issue. The β-galactopyranoside-conjugated liposomes (GAL-liposome) targeting liver synthesized hepcidin were prepared by thin lipid film<span><span> hydration method to encapsulate siRNA and the conjugation of β-galactopyranoside to the lipid </span>nanocarrier was achieved by covalent </span></span>chemistry<span>. The prepared siRNA loaded GAL-lip were spherical with around 50 nm radius in size as observed by HR-TEM. The zeta potential<span> and polydispersity index<span> of the prepared liposomes were − 19.9 ± 0.96 mV and 0.44 ± 0.05, respectively. The encapsulation efficiency as determined by dialysis bag method was around 91.76 ± 1.74%. The cell viability<span> and cellular uptake analysis was examined in HepG2 cells by MTT assay and flow </span></span></span></span></span>cytometry<span><span>, respectively. The stability and cumulative release of siRNA was also assessed. The hepcidin mRNA expression on administration of siRNA loaded GAL-lip was determined in HepG2 cells and in lipopolysaccharide-induced mice model followed by examining itsin vivo biodistribution by </span>fluorescence microscopy<span>. The results suggested thatsiRNA loaded GAL-lip reduced the hepcidin levels, thus, highlighting a novel ligand conjugated ionizable lipid-based nanocarrier for inducing RNA interference.</span></span></span></p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"246 ","pages":"Article 105207"},"PeriodicalIF":3.4,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"1856247","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Electrostatic interactions between cationic dendrimers and anionic model biomembrane","authors":"Khawla Qamhieh , Tommy Nylander","doi":"10.1016/j.chemphyslip.2022.105214","DOIUrl":"https://doi.org/10.1016/j.chemphyslip.2022.105214","url":null,"abstract":"<div><p>The electrostatic interactions<span><span><span> between cationic poly(amidoamine) (PAMAM) dendrimers of different generations, G3, G4, and G6, with net anionic model </span>biomembranes<span> have been predicted by adopting an analytical model based on two dissimilar soft spheres. The influence of bilayer surface charge density, </span></span>ionic strength, pH, temperature, membrane softness (modeled as changes in bilayer thickness), and dendrimer generation on the attractive interaction was investigated. The attraction was found to decrease with increasing salt concentration, dendrimer charge, and thickness (or softness) of the membrane. On the other hand, the attraction increased with the surface charge density of the membrane, and the size of dendrimer generation. In fact, the attraction was found to be much larger for large generations, like G6 dendrimer that have a higher charge, than it is with small ones like G3 and G4 dendrimers. These results have implications for the use of PAMAM dendrimers as potential gene transfection vectors.</span></p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"246 ","pages":"Article 105214"},"PeriodicalIF":3.4,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"3337044","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Mitchell DiPasquale , Tye G. Deering , Dhimant Desai , Arun K. Sharma , Shantu Amin , Todd E. Fox , Mark Kester , John Katsaras , Drew Marquardt , Frederick A. Heberle
{"title":"Influence of ceramide on lipid domain stability studied with small-angle neutron scattering: The role of acyl chain length and unsaturation","authors":"Mitchell DiPasquale , Tye G. Deering , Dhimant Desai , Arun K. Sharma , Shantu Amin , Todd E. Fox , Mark Kester , John Katsaras , Drew Marquardt , Frederick A. Heberle","doi":"10.1016/j.chemphyslip.2022.105205","DOIUrl":"10.1016/j.chemphyslip.2022.105205","url":null,"abstract":"<div><p><span>Ceramides<span><span> and diacylglycerols are groups of </span>lipids<span> capable of nucleating and stabilizing ordered lipid domains, structures that have been implicated in a range of biological processes. Previous studies have used fluorescence reporter molecules to explore the influence of ceramide acyl chain structure on sphingolipid-rich ordered phases. Here, we use small-angle neutron scattering (SANS) to examine the ability of ceramides and diacylglycerols to promote lipid domain formation in the well-characterized domain-forming mixture DPPC/DOPC/cholesterol. SANS is a powerful, probe-free technique for interrogating membrane heterogeneity, as it is differentially sensitive to hydrogen’s stable isotopes </span></span></span>protium<span><span> and deuterium. Specifically, neutron contrast is generated through selective deuteration of lipid species, thus enabling the detection of nanoscopic domains enriched in deuterated saturated lipids dispersed in a matrix of protiated unsaturated lipids. Using large </span>unilamellar vesicles<span>, we found that upon replacing 10 mol% DPPC with either C16:0 or C18:0 ceramide, or 16:0 diacylglycerol (dag), lipid domains persisted to higher temperatures. However, when DPPC was replaced with short chain (C6:0 or C12:0) or very long chain (C24:0) ceramides, or ceramides with unsaturated acyl chains of any length (C6:1(3), C6:1(5), C18:1, and C24:1), as well as C18:1-dag, lipid domains were destabilized, melting at lower temperatures than those in the DPPC/DOPC/cholesterol system. These results show how ceramide acyl chain length and unsaturation influence lipid domains and have implications for how cell membranes might modify their function through the generation of different ceramide species.</span></span></p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"245 ","pages":"Article 105205"},"PeriodicalIF":3.4,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9728142","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Paweł Misiak , Katarzyna Niemirowicz-Laskowska , Iwona Misztalewska-Turkowicz , Karolina H. Markiewicz , Przemysław Wielgat , Halina Car , Agnieszka Z. Wilczewska
{"title":"Doxorubicin delivery systems with an acetylacetone-based block in cholesterol-terminated copolymers: Diverse activity against estrogen-dependent and estrogen-independent breast cancer cells","authors":"Paweł Misiak , Katarzyna Niemirowicz-Laskowska , Iwona Misztalewska-Turkowicz , Karolina H. Markiewicz , Przemysław Wielgat , Halina Car , Agnieszka Z. Wilczewska","doi":"10.1016/j.chemphyslip.2022.105194","DOIUrl":"https://doi.org/10.1016/j.chemphyslip.2022.105194","url":null,"abstract":"<div><p>The study presents the synthesis of original cholesterol-terminated copolymers comprising acetylacetone-based (AcacI) and <em>N</em>-isopropylacrylamide (NIPAAm) units with a varied arrangement (block and random copolymers). The nanoprecipitation method was used to form empty and doxorubicin-loaded polymeric nanoparticles (PNPs) from these copolymers, which were further studied in terms of their physicochemical and biological properties. Unexpectedly, it was revealed that even empty PNPs are effective against breast cancer cells, specifically towards estrogen-dependent MCF-7 cell line. The anti-cancer efficacy was further improved when a low dose of doxorubicin was introduced to the tested systems. It was shown that the proposed carriers modulate doxorubicin (DOX) compatibility with representatives of normal cells, including immune cells, cardiomyocyte cells, and fibroblasts, and reduce side effects associated with standard chemotherapy. The use of these carriers might be a strategy leading to enhancement of DOX activity in cancer cells which develop resistance through decreased drug penetration or drug efflux.</p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"245 ","pages":"Article 105194"},"PeriodicalIF":3.4,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"2363500","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
José Geraldo de Alencar Santos Júnior , Henrique Douglas Melo Coutinho , João Pedro Viana Rodrigues , Vanessa Pinheiro Gonçalves Ferreira , José Bezerra de Araújo Neto , Maria Milene Costa da Silva , Ana Carolina Justino de Araújo , Raimundo Luiz Silva Pereira , Pedro Everson Alexandre de Aquino , Cícera Datiane de Morais Oliveira–Tintino , Roberto Nicolete
{"title":"Liposome evaluation in inhibiting pump efflux of NorA of Staphylococcus aureus","authors":"José Geraldo de Alencar Santos Júnior , Henrique Douglas Melo Coutinho , João Pedro Viana Rodrigues , Vanessa Pinheiro Gonçalves Ferreira , José Bezerra de Araújo Neto , Maria Milene Costa da Silva , Ana Carolina Justino de Araújo , Raimundo Luiz Silva Pereira , Pedro Everson Alexandre de Aquino , Cícera Datiane de Morais Oliveira–Tintino , Roberto Nicolete","doi":"10.1016/j.chemphyslip.2022.105204","DOIUrl":"10.1016/j.chemphyslip.2022.105204","url":null,"abstract":"<div><p><span><span>Liposomes, in addition to providing greater efficacy to antibiotics, decrease toxicity and increase selectivity. This work has as main objectives the sensitization of the need to solve bacterial resistance to antibiotics, addressing the potential of antibiotics carried by liposome. In the preparation of the liposomes, the </span>lipids dipalmitoyl </span>phosphatidylcholine<span><span><span><span> (DPPC), dipalmitoyl phosphatidylserine (DPPS), and cholesterol (COL) with > 99% purity were used. The </span>Staphylococcus aureus strains used were SA-1199B, which expresses the NorA gene encoding the NorA efflux protein, which expels hydrophilic fluoroquinolones and other drugs intercalating </span>DNA dyes, and the wild strain SA-1199. The liposomes associated with antibiotics in the wild type of strain SA-1199 and the carrier strain of pump 1199B, had a better representation </span>of growth inhibition than the wild type strain SA-1199. Given the potential for inhibition of efflux pump seen in the results, we highlight the creation of new drugs or alteration of existing drugs. They are not recognized by the efflux pumps and removed from the target cell.</span></p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"245 ","pages":"Article 105204"},"PeriodicalIF":3.4,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44276443","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Development of optimized novel liposome loaded with 6-gingerol and assessment of its therapeutic activity against NSCLC In vitro and In vivo experimental models","authors":"Priyadharshini Thangavelu , Viswanathan Sundaram , Kaavya Gunasekaran , Bonaventure Mujyambere , Sowndarya Raju , Arya Kannan , Ashok Arasu , Kadirvelu Krishna , Jayaraj Ramamoorthi , Sivasamy Ramasamy , Thirunavukkarasu Velusamy , Suja Samiappan","doi":"10.1016/j.chemphyslip.2022.105206","DOIUrl":"10.1016/j.chemphyslip.2022.105206","url":null,"abstract":"<div><p><span><span><span>6-Gingerol (Gn) is an active compound derived from ginger which possesses various biological activities. The therapeutic applications of Gn are limited due to its hydrophobic nature. To ease its administration, one of the nano-emulsion methods, liposome was selected to encapsulate Gn. Response Surface Methodology<span> (RSM) was used to optimize liposome ratio. 97.2% entrapment efficiency was achieved at the ratio of 1:20:2 (Drug: Lipid: Cholesterol). The optimized liposome attained size below 200 d nm, spherical shape, negative surface charge and showed sustain release upon physical characterization methods such as FESEM, DLS, </span></span>Zeta potential, Drug release. The signature </span>FTIR peaks of both free Gn and free liposome (FL) were also observed in Lipo-Gn peak. Lipo-Gn showed significant cytotoxic effect on A549 cells (IC50 160.5 ± 0.74 µM/ml) as well as inhibits the cell migration. </span>DAPI<span> staining showed higher apoptotic nuclear morphological change in the cells treated with Lipo-Gn, and also Lipo-Gn increased the apoptotic percentage in A549 as 39.89 and 70.32 for 12 and 24 h respectively which were significantly more than free Gn. Moreover, the formulation of Lipo-Gn showed significant cell cycle arrest<span> at the G2/M phase compared with free Gn (28.9% and 34.9% in Free Gn vs. 42.7% and 50.1% in Lipo -Gn for 12 and 24 h respectively). Lipo-Gn have been assessed in NSCLC induced BALB/c mice and showed significantly improved pharmacological properties compared to those of free Gn. Thus, Lipo-Gn may be considered for its widening applications against lung cancer.</span></span></p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"245 ","pages":"Article 105206"},"PeriodicalIF":3.4,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49377899","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Yuta Murai , Kohei Yuyama , Daisuke Mikami , Yasuyuki Igarashi , Kenji Monde
{"title":"Penta-deuterium-labeled 4E, 8Z-sphingadienine for rapid analysis in sphingolipidomics study","authors":"Yuta Murai , Kohei Yuyama , Daisuke Mikami , Yasuyuki Igarashi , Kenji Monde","doi":"10.1016/j.chemphyslip.2022.105202","DOIUrl":"https://doi.org/10.1016/j.chemphyslip.2022.105202","url":null,"abstract":"<div><p><span><span><span>The use of deuterium-incorporated bioactive compounds<span> is an efficient method for tracing their metabolic fate and for quantitative analysis by </span></span>mass spectrometry<span> without complicated HPLC separation even if their amounts are extremely small. Plant sphingolipids and their metabolites, which have C4, 8-olefins on a common backbone as a </span></span>sphingoid<span> base, show unique and fascinating bioactivities compared to those of sphingolipids in mammals. However, the functional and metabolic mechanisms of exogenous plant sphingolipids have not been elucidated due to the difficulty in distinguishing exogenous sphingolipids from endogenous sphingolipids having the same polarity and same molecular weight by mass spectrometric analysis. Their roles might be elucidated by the use of deuterated probes with original biological and physicochemical properties. In this study, we designed (2</span></span><em>S</em>,3<em>R</em>,4<em>E</em>,8<em>Z</em>)-2-aminooctadeca-4,8-diene-17,17,18,18,18-<em>d</em><sub>5</sub>-1,3-diol (penta-deuterium-labeled 4<em>E</em>, 8<em>Z</em>-sphingadienine) as a tracer for exogenous metabolic studies. In addition, the sphingadienine was confirmed to be metabolized in HEK293 cells and showed distinct peaks in mass spectrometric analysis.</p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"245 ","pages":"Article 105202"},"PeriodicalIF":3.4,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"2363501","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"The in-vitro study of novel phospholipid micelles loaded with amphotericin B on plasmodium falciparum protozoan","authors":"Khadijeh Rajablou , Hossein Attar , Seyed Kazem Sadjady , Amir Heydarinasab","doi":"10.1016/j.chemphyslip.2022.105180","DOIUrl":"https://doi.org/10.1016/j.chemphyslip.2022.105180","url":null,"abstract":"<div><p><span>Malaria is one of the most challenging parasitic infectious diseases in tropical and subtropical regions all over the world. The increasing drug resistance of plasmodium falciparum<span><span> even makes the treatment procedure of malaria challenging and more problematic. Therefore, it is essential to develop new antimalarial drugs for effective treatments. In this study, the encapsulated </span>amphotericin B<span> (Constantinides et al.) in DSPC/DSPE-PEG2000 micelles was investigated as an antimalarial drug against </span></span></span><em>P. falciparum</em><span><span> 3D7 strain. The mean particle size, morphological and microstructural properties of drug-free and drug-loaded micelles prepared with amphotericin B were determined through DLS, </span>FESEM<span><span><span><span>, and TEM analysis. The synthesized </span>phospholipid micelles containing AmB drug with a mean diameter of 115 nm and a </span>polydispersity<span> index of 0.331. The TEM and SEM studies indicate the uniform and homogeneous morphology of the micelles. Drug encapsulation efficiency is 88.3%. The slow release of the micellar system shows the maximum drug release of 75.67% within 24 h. This </span></span>in vitro study was conducted on </span></span><em>P. falciparum</em> 3D7 to investigate the interactions between AmB micelles and <em>P. falciparum</em> parasites using different drug ratios. According to the findings, the IC<sub>50</sub> of free AmB is 4.834 µg/ml, while the nano-diameter AmB has a significantly lower IC<sub>50</sub> of 2.394 µg/ml. The results of this study suggest that the drug-loaded phospholipid micelles have significantly higher bioactivity and greater plasmodial properties compared to the direct application of AmB against <em>P. falciparum</em><span><span>. Moreover, according to the results of this study, the encapsulated AmB drugs are promising nanostructures for malaria treatment. Therefore the </span>nanoencapsulation AmB showed promising application for malaria treatment.</span></p></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"245 ","pages":"Article 105180"},"PeriodicalIF":3.4,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"1737310","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}