Journal of Liposome Research最新文献

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Synthesis of liposomal nanoparticles to load 4-farnesyloxycoumarin and investigating its anti-cancer and anti-metastatic effects. 合成脂质体纳米颗粒以载入 4-法尼酰氧基香豆素,并研究其抗癌和抗转移作用。
IF 3.6 4区 医学
Journal of Liposome Research Pub Date : 2024-11-17 DOI: 10.1080/08982104.2024.2428168
Shima Abbas Salman Al-Baidhani, Vahid Pouresmaeil, Masoud Homayouni Tabrizi
{"title":"Synthesis of liposomal nanoparticles to load 4-farnesyloxycoumarin and investigating its anti-cancer and anti-metastatic effects.","authors":"Shima Abbas Salman Al-Baidhani, Vahid Pouresmaeil, Masoud Homayouni Tabrizi","doi":"10.1080/08982104.2024.2428168","DOIUrl":"10.1080/08982104.2024.2428168","url":null,"abstract":"<p><p>The aim of this study was to load 4-farnesyloxycoumarin (4-FLC) in nanoliposomes (4-FLC-LNPs) and evaluate its anti-cancer and anti-metastatic effects. 4-FLC-LNPs were synthesized using a combination of lecithin-cholesterol-polyethylene glycol. The physicochemical properties were evaluated using DLS, FTIR, and microscopy methods. The toxicity against breast cancer (MCF-7), prostate cancer (PS3), pancreatic cancer (PANC), gastric cancer (AGS), and normal cell lines (HUVEC) was evaluated using the MTT assay. Fluorescent staining and flow cytometry were used to assess the occurrence of apoptosis. Molecular analysis methods were used to study the apoptosis and metastasis effects of these nanoliposomes. The antioxidant power of 4-FLC-LNPs was measured using the ABTS and DPPH free radicals methods. 4-FLC-LNPs exhibit a spherical morphology, with an average size of 57.43 nm, a polydispersity index of 0.29, and a zeta potential of -31.4 mV. They demonstrate an encapsulation efficiency of 82.4% for 4-FLC. The IC50 value of 4-FLC-LNPs against the breast cancer cell line was reported as the most sensitive, at approximately 60 μg/mL. ABTS and DPPH results were reported at approximately 30 µg/mL. The inductive effects of nanoliposomes on the apoptosis process were confirmed by an increase in the number of apoptotic cells, as well as the arrest of cells in various phases of cell growth. The increased expression of BAX and decreased expression of Bcl-2, MMP-2, and MMP-9 confirmed the pro-apoptotic and anti-metastatic effects of 4-FLC-LNPs. These finding validate the therapeutic potential of 4-FLC-LNPs, which may be utilized in preclinical studies.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-10"},"PeriodicalIF":3.6,"publicationDate":"2024-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142644356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Microfluidics-based stable production of monodisperse giant unilamellar vesicles by oil-phase removal from double emulsion. 基于微流控技术,通过从双乳液中去除油相,稳定生产单分散巨型单酰胺囊泡。
IF 3.6 4区 医学
Journal of Liposome Research Pub Date : 2024-10-29 DOI: 10.1080/08982104.2024.2420337
Tomoki Yamada, Hiroaki Suzuki
{"title":"Microfluidics-based stable production of monodisperse giant unilamellar vesicles by oil-phase removal from double emulsion.","authors":"Tomoki Yamada, Hiroaki Suzuki","doi":"10.1080/08982104.2024.2420337","DOIUrl":"10.1080/08982104.2024.2420337","url":null,"abstract":"<p><p>Giant liposomes, or giant unilamellar vesicles (GUVs), have been utilized as cell-size bioreactors to replicate the physical and chemical properties of biological cells. However, conventional methods for preparing GUVs typically lack precise control over their size. Several research groups have recently developed microfluidic techniques to create monodisperse GUVs by generating water-in-oil-in-water (W/O/W) droplets with a thin oil layer that subsequently transform into GUVs. However, the formation of a thin oil shell requires the intricate control of the flow rate, which can be both challenging and unstable. In this study, we investigated the design of a two-step flow-focusing microfluidic channel to produce stable W/O/W droplets. These droplets underwent substantial oil layer reduction through spontaneous removal by fluidic shear forces. Consequently, the majority of the oil layer in the W/O/W droplets was reduced, improving uniformity of GUVs.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-7"},"PeriodicalIF":3.6,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142522125","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development and in vitro characterization of new carnosine-loaded liposomal formulations. 新型肉碱脂质体制剂的开发和体外表征。
IF 3.6 4区 医学
Journal of Liposome Research Pub Date : 2024-10-15 DOI: 10.1080/08982104.2024.2415664
Stefano Russo, Anna Privitera, Giuliana Greco, Lucia Di Pietro, Vincenzo Cardaci, Giuseppe Carota, Maria Grazia Sarpietro, Giuseppe Caruso
{"title":"Development and <i>in vitro</i> characterization of new carnosine-loaded liposomal formulations.","authors":"Stefano Russo, Anna Privitera, Giuliana Greco, Lucia Di Pietro, Vincenzo Cardaci, Giuseppe Carota, Maria Grazia Sarpietro, Giuseppe Caruso","doi":"10.1080/08982104.2024.2415664","DOIUrl":"https://doi.org/10.1080/08982104.2024.2415664","url":null,"abstract":"<p><p>Carnosine is an endogenous dipeptide characterized by a multimodal mechanism of action. However, its clinical potential is limited by serum and cytosolic carnosinases, which significantly reduce its bioavailability. Based on that, different research groups have worked on the development of new strategies able not only to prevent its rapid metabolization but also to improve its distribution and specific targeting. In the present study, the development and <i>in vitro</i> characterization of new liposomal formulations loaded with carnosine are described. Nanoliposomes, produced through Thin-Layer Hydration followed by Extrusion method, were first investigated for their physicochemical stability. Photon correlation spectroscopy and electrophoretic light scattering, assessing the stability of the formulations, showed a strong homogeneity-oriented tendency for up to two months. Particle size, polydispersity index, and zeta potential were determined through dynamic light scattering and electrophoretic light scattering, demonstrating an almost neutral charge of the formulation and an effective encapsulation of carnosine. The morphology assessment performed via scanning electron microscopy showed good conformity and polydispersity. Differential scanning calorimetry measurements suggest the ability of carnosine to stabilize the large unilamellar vesicles. Lastly, the newly developed carnosine-loaded liposomal formulations also showed a good safety profile in human microglia.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-8"},"PeriodicalIF":3.6,"publicationDate":"2024-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142467665","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preparation and characterization of niosomes for the delivery of a lipophilic model drug: comparative stability study with liposomes against phospholipase-A2. 用于递送亲脂模型药物的niosomes的制备和表征:与针对磷脂酶-A2的脂质体的稳定性比较研究。
IF 3.6 4区 医学
Journal of Liposome Research Pub Date : 2024-10-03 DOI: 10.1080/08982104.2024.2410748
Nazanin Kianinejad, Reza Razeghifard, Hossein H Omidian, Yadollah Omidi, Young M Kwon
{"title":"Preparation and characterization of niosomes for the delivery of a lipophilic model drug: comparative stability study with liposomes against phospholipase-A<sub>2</sub>.","authors":"Nazanin Kianinejad, Reza Razeghifard, Hossein H Omidian, Yadollah Omidi, Young M Kwon","doi":"10.1080/08982104.2024.2410748","DOIUrl":"https://doi.org/10.1080/08982104.2024.2410748","url":null,"abstract":"<p><p>Vesicular nanocarriers like niosomes and liposomes are widely researched for controlled drug delivery systems, with niosomes emerging as promising alternatives due to their higher stability and ease of manufacturing. This study aimed to develop and characterize a niosomal formulation for the encapsulation and sustained release of temozolomide (TMZ), a model lipophilic drug, and to compare the stability of niosomes and liposomes, with a particular focus on the behavior of their lipid bilayers. Niosomes were prepared using the thin-film hydration method, composed of Span 60 (Sorbitan monostearate), cholesterol, and soy lecithin in varying molar ratios. The study investigated critical properties such as drug loading capacity, release kinetics, and resistance to enzymatic degradation. The optimized formulation was analyzed for drug entrapment efficiency and stability against phospholipase A<sub>2</sub> (PLA<sub>2</sub>) degradation. The optimized niosomal formulation, with a 4:2:1 molar ratio of Span 60: cholesterol, achieved a high TMZ entrapment efficiency of 73.23 ± 1.02% and demonstrated sustained drug release over 24 hours. In comparison, liposomes released their TMZ payload within 4 hours upon exposure to PLA<sub>2</sub>, while the niosomes maintained their release profile, indicating superior stability. Spectroscopic and thermal analysis confirmed successful drug encapsulation with no component incompatibilities.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"1-12"},"PeriodicalIF":3.6,"publicationDate":"2024-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142372067","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Comparison of free vs. liposomal naringenin in white adipose tissue browning in C57BL/6j mice 游离与脂质体柚皮苷对 C57BL/6j 小鼠白色脂肪组织褐变的影响比较
IF 4.4 4区 医学
Journal of Liposome Research Pub Date : 2024-09-19 DOI: 10.1080/08982104.2024.2405131
Kübra Uçar Baş, Aslıhan Ağaçdiken, Elif Didem Örs Demet, Dilem Tuğal Aslan, Tuba Reçber, Süleyman Can Öztürk, Tugba Gulsun, Mustafa Çelebier, Zeynep Göktaş
{"title":"Comparison of free vs. liposomal naringenin in white adipose tissue browning in C57BL/6j mice","authors":"Kübra Uçar Baş, Aslıhan Ağaçdiken, Elif Didem Örs Demet, Dilem Tuğal Aslan, Tuba Reçber, Süleyman Can Öztürk, Tugba Gulsun, Mustafa Çelebier, Zeynep Göktaş","doi":"10.1080/08982104.2024.2405131","DOIUrl":"https://doi.org/10.1080/08982104.2024.2405131","url":null,"abstract":"Naringenin may play a role in browning by increasing thermogenic gene expression. In this study, we encapsulated naringenin using a liposomal formulation and examined the effects of both free and l...","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"5 1","pages":""},"PeriodicalIF":4.4,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258682","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A comparative study of sensitizers and liposome composition in radiation-induced controlled drug release for cancer therapy. 辐射诱导癌症治疗药物控释中敏化剂和脂质体成分的比较研究。
IF 4.4 4区 医学
Journal of Liposome Research Pub Date : 2024-09-11 DOI: 10.1080/08982104.2024.2401800
E Loscertales,J Mateo,S España
{"title":"A comparative study of sensitizers and liposome composition in radiation-induced controlled drug release for cancer therapy.","authors":"E Loscertales,J Mateo,S España","doi":"10.1080/08982104.2024.2401800","DOIUrl":"https://doi.org/10.1080/08982104.2024.2401800","url":null,"abstract":"This study investigates drug-loaded liposomes designed for controlled release under ionizing radiation to refine cancer treatment precision. Liposomes as carriers enable targeted chemotherapy delivery, reducing healthy tissue damage risk. Liposomes containing poly- or mono-unsaturated fatty acids and various sensitizing agents were assessed for responsiveness to UV light and γ photon irradiation including rose bengal (RB), protoporphyrin IX (PPIX), verteporfin (VP), cercosporin (CERC) and hypericin (HYP). Carboxyfluorescein (CF) was used as a surrogate for drug release measurements. VP and PPIX induced rapid drug release and lipid peroxidation under UV light, while RB prompted quick drug release under UV light and a modest immediate release under γ irradiation, eventually reaching full release a few hours after irradiation, demonstrating dose-dependent effects. Smaller liposomes displayed accelerated release, emphasizing size-dependent kinetics. In vitro analyses evaluated radiosensitizing effects of RB-loaded liposomes. Clonogenic assays indicated that RB-filled liposomes had minimal direct radiobiological effects but increased indirect radiation damage, as shown by the curvature of the cell survival curve. Our study sheds light on factors influencing liposomal drug release under ionizing radiation, spotlighting RB as a promising radiosensitizer requiring further investigation for cancer therapy potential.","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"29 1","pages":"1-12"},"PeriodicalIF":4.4,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142180938","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design and preparation of pH-sensitive cytotoxic liposomal formulations containing antitumor colchicine analogues for target release. 含有抗肿瘤秋水仙碱类似物的pH敏感细胞毒性脂质体制剂的设计和制备。
IF 4.4 4区 医学
Journal of Liposome Research Pub Date : 2024-09-01 Epub Date: 2023-11-01 DOI: 10.1080/08982104.2023.2274428
Ekaterina S Shchegravina, Daria S Tretiakova, Alsu R Sitdikova, Sofia D Usova, Ivan A Boldyrev, Anna S Alekseeva, Elena V Svirshchevskaya, Elena L Vodovozova, Alexey Yu Fedorov
{"title":"Design and preparation of pH-sensitive cytotoxic liposomal formulations containing antitumor colchicine analogues for target release.","authors":"Ekaterina S Shchegravina, Daria S Tretiakova, Alsu R Sitdikova, Sofia D Usova, Ivan A Boldyrev, Anna S Alekseeva, Elena V Svirshchevskaya, Elena L Vodovozova, Alexey Yu Fedorov","doi":"10.1080/08982104.2023.2274428","DOIUrl":"10.1080/08982104.2023.2274428","url":null,"abstract":"<p><p>Herein, we describe the synthesis of pH-sensitive lipophilic colchicine prodrugs for liposomal bilayer inclusion, as well as preparation and characterization of presumably stealth PEGylated liposomes with above-mentioned prodrugs. These formulations liberate strongly cytotoxic colchicinoid derivatives selectively under slightly acidic tumor-associated conditions, ensuring tumor-targeted delivery of the compounds. The design of the prodrugs is addressed to pH-triggered release of active compounds in the slight acidic media, that corresponds to tumor microenvironment, while keeping sufficient stability of the whole formulation at physiological pH. Correlations between the structure of the conjugates, their hydrolytic stability, colloidal stability, ability of the prodrug retention in the lipid bilayer are described. Several formulations were found promising for further development and in vivo investigations.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"399-410"},"PeriodicalIF":4.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49690922","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Antibacterial effect of protease-responsive cationic eugenol liposomes modified by gamma-polyglutamic acid against Staphylococcus aureus. γ -聚谷氨酸修饰蛋白酶反应性阳离子丁香酚脂质体对金黄色葡萄球菌的抑菌作用。
IF 3.6 4区 医学
Journal of Liposome Research Pub Date : 2024-09-01 Epub Date: 2023-11-15 DOI: 10.1080/08982104.2023.2280829
Xiaochen Chen, Yiwei Wang, Changzhu Li, Zichun Hua, Haiying Cui, Lin Lin
{"title":"Antibacterial effect of protease-responsive cationic eugenol liposomes modified by gamma-polyglutamic acid against <i>Staphylococcus aureus</i>.","authors":"Xiaochen Chen, Yiwei Wang, Changzhu Li, Zichun Hua, Haiying Cui, Lin Lin","doi":"10.1080/08982104.2023.2280829","DOIUrl":"10.1080/08982104.2023.2280829","url":null,"abstract":"<p><p>Eugenol, as a natural antibacterial agent, has been widely studied for its inhibitory effect on the common food-borne pathogen <i>Staphylococcus aureus</i> (<i>S. aureus</i>). However, the widespread application of eugenol is still limited by its instability and volatility. Herein, γ-polyglutamic acid coated eugenol cationic liposomes (pGA-ECLPs) were successfully constructed by self-assembly with an average particle size of 170.7 nm and an encapsulation efficiency of 36.2%. The formation of pGA shell significantly improved the stability of liposomes, and the encapsulation efficiency of eugenol only decreased by 20.7% after 30 days of storage at 4 °C. On the other hand, the pGA layer can be hydrolyzed by <i>S. aureus</i>, achieving effective control of release through response to bacterial stimuli. The application experiments further confirmed that pGA-ECLPs effectively prolonged the antibacterial effect of eugenol in fresh chicken without causing obvious sensory effects on the food. The above results of this study provide an important reference for extending the action time of natural antibacterial substances and developing new stimuli-responsive antibacterial systems.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"411-420"},"PeriodicalIF":3.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"107591491","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Calcium phosphates enhanced with liposomes - the future of bone regeneration and drug delivery. 脂质体增强磷酸钙-骨再生和药物输送的未来。
IF 4.4 4区 医学
Journal of Liposome Research Pub Date : 2024-09-01 Epub Date: 2023-12-07 DOI: 10.1080/08982104.2023.2285973
Marite Skrinda-Melne, Janis Locs, Andra Grava, Arita Dubnika
{"title":"Calcium phosphates enhanced with liposomes - the future of bone regeneration and drug delivery.","authors":"Marite Skrinda-Melne, Janis Locs, Andra Grava, Arita Dubnika","doi":"10.1080/08982104.2023.2285973","DOIUrl":"10.1080/08982104.2023.2285973","url":null,"abstract":"<p><p>Effective healing and regeneration of various bone defects is still a major challenge and concern in modern medicine. Calcium phosphates have emerged as extensively studied bone substitute materials due to their structural and chemical resemblance to the mineral phase of bone, along with their versatile properties. Calcium phosphates present promising biological characteristics that make them suitable for bone substitution, but a critical limitation lies in their low osteoinductivity. To supplement these materials with properties that promote bone regeneration, prevent infections, and cure bone diseases locally, calcium phosphates can be biologically and therapeutically modified. A promising approach involves combining calcium phosphates with drug-containing liposomes, renowned for their high biocompatibility and ability to provide controlled and sustained drug delivery. Surprisingly, there is a lack of research focused on liposome-calcium phosphate composites, where liposomes are dispersed within a calcium phosphate matrix. This raises the question of why such studies are limited. In order to provide a comprehensive overview of existing liposome and calcium phosphate composites as bioactive substance delivery systems, the authors review the literature exploring the interactions between calcium phosphates and liposomes. Additionally, it seeks to identify potential interactions between calcium ions and liposomes, which may impact the feasibility of developing liposome-containing calcium phosphate composite materials. Liposome capacity to protect bioactive compounds and facilitate localized treatment can be particularly valuable in scenarios involving bone regeneration, infection prevention, and the management of bone diseases. This review explores the implications of liposomes and calcium phosphate material containing liposomes on drug delivery, bioavailability, and stability, offering insights into their advantages.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"507-522"},"PeriodicalIF":4.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138176386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Impact of micelle characteristics on cholesterol absorption and ezetimibe inhibition: Insights from Niemann-Pick C1-like 1 binding and molecular structure. 胶束特性对胆固醇吸收和依折麦布抑制的影响:来自Niemann-Pick C1样1结合和分子结构的见解。
IF 3.6 4区 医学
Journal of Liposome Research Pub Date : 2024-09-01 Epub Date: 2023-10-31 DOI: 10.1080/08982104.2023.2274424
Hideki Aizawa
{"title":"Impact of micelle characteristics on cholesterol absorption and ezetimibe inhibition: Insights from Niemann-Pick C1-like 1 binding and molecular structure.","authors":"Hideki Aizawa","doi":"10.1080/08982104.2023.2274424","DOIUrl":"10.1080/08982104.2023.2274424","url":null,"abstract":"<p><p>Yamanashi et al., conducted a study on the absorption of cholesterol and β-sitosterol, as well as the inhibitory effect of ezetimibe (EZE). They used CaCo-2 cells to simulate the intestines and investigated how different mixed micelles, acting as carriers, were absorbed into these cells through the Niemann-Pick C1-like 1 (NPC1L1) protein. The study focused on the impact of micelle shape, size, and zeta potential on absorption and the inhibitory effect of EZE. I utilized small-angle X-ray scattering and a zeta potential measuring device to measure these characteristics. The findings revealed a two-step mechanism: NPC1L1 selectively bound micelles based on their shape and size, and once bound, the absorption was regulated by the molecular structure of the micelle components. EZE's inhibitory effect changed with micelle composition, influencing micelle size and shape. EZE initially acted on the micelle's shape and size, and then NPC1L1 selectively bound micelles based on their shape and size, allowing EZE to directly inhibit absorption by interacting with NPC1L1. This groundbreaking discovery challenges existing concepts and holds significant implications for researchers in drug development, as well as physicians and pharmacists.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"386-398"},"PeriodicalIF":3.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71412572","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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