Chemistry and Physics of Lipids最新文献_第8页

EGFR-targeted hybrid lipid nanoparticles for chemo-photothermal therapy against colorectal cancer cells 靶向egfr的杂化脂质纳米颗粒用于化疗-光热治疗结直肠癌细胞

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2023-03-01 DOI: 10.1016/j.chemphyslip.2023.105280

Fang Fang , Xinming Zhang , Jin Tang , Yu Wang , Jinchen Xu , Yu Sun

{"title":"EGFR-targeted hybrid lipid nanoparticles for chemo-photothermal therapy against colorectal cancer cells","authors":"Fang Fang , Xinming Zhang , Jin Tang , Yu Wang , Jinchen Xu , Yu Sun","doi":"10.1016/j.chemphyslip.2023.105280","DOIUrl":"10.1016/j.chemphyslip.2023.105280","url":null,"abstract":"<div>Antibody-functionalized targeted nanocarriers have shown great–potential for minimizing the chemoresistance and systemic toxicity of cancer chemotherapies. The combination of chemotherapy and photothermal therapy has great potential in improving therapeutic effect. However, cetuximab-modified nanoparticles based lipids for chemo-phototherapy of EGFR overexpressing colorectal carcinoma (CRC) have seldom been investigated. Hence, this study aimed to fabricate cetuximab-conjugated and near infrared (NIR) light-responsive hybrid lipid-polymer nanoparticles (abbreviated as Cet-CINPs) for targeted delivery of irinotecan. Cet-CINPs were prepared with copolymer PLGA and various lipids DSPE-PEG, DSPE-PEG-Mal, lecithin as carriers. Cetuximab was conjugated on the surface of nanoparticles to achieve targeting anti-tumor efficacy. Cet-CINPs were characterized in terms of morphology (spherical), size (119 nm), charge (−27.2 mV), drug entrapment efficiency (43.27 %), and antibody conjugation efficiency (70.87 %). Cet-CINPs showed preferable photothermal response, pH/NIR-triggered drug release behavior, enhanced cellular uptake and ROS level compared with free ICG and CINPs. Meanwhile, in vitro cytotoxicity assay showed that Cet-CINPs with NIR irradiation had a higher cytotoxicity against Lovo cells than non-targeted or non-NIR activated nanoparticles. The IC50 values of Cet-CINPs with NIR irradiation was 22.84 ± 1.11 μM for 24 h and 5.01 ± 1.06 μM for 48 h, respectively. These investigations demonstrate that Cet-CINPs with good tumor-targeting ability and enhanced antitumor activity, are a promising multifunctional nanoplatform for CRC therapy.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"251 ","pages":"Article 105280"},"PeriodicalIF":3.4,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9485263","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}

引用次数: 2

Development of skin-permeable flexible liposome using ergosterol esters containing unsaturated fatty acids 利用含不饱和脂肪酸的麦角甾醇酯制备皮肤渗透性柔性脂质体

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2023-01-01 DOI: 10.1016/j.chemphyslip.2022.105270

Sehyeon Park, Hyung Kwoun Kim

{"title":"Development of skin-permeable flexible liposome using ergosterol esters containing unsaturated fatty acids","authors":"Sehyeon Park, Hyung Kwoun Kim","doi":"10.1016/j.chemphyslip.2022.105270","DOIUrl":"10.1016/j.chemphyslip.2022.105270","url":null,"abstract":"<div>Ergosterol (Ergo) and cholesterol contribute to performances of liposomes by increasing membrane packing density and physical stability. However, as these sterols can reduce membrane flexibility, they can lower skin permeability of liposomes. We synthesized ergosterol ester (Ergo-Est) containing unsaturated fatty acid different from Ergo in size and physical properties. In this work, we investigated effects of Ergo-Est and Ergo on physical properties of liposomes. We incorporated Ergo, Ergo-oleate (EO18:1), Ergo-linoleate (EL18:2), and Ergo-linolenate (ELn18:3) into the liposomal membrane of egg phosphatidylcholine and soybean lecithin. Ergo-Est did not reduce membrane fluidity as much as Ergo. Nevertheless, Ergo-Est increased membrane packing density and physical stability of liposomes. EL18:2 and ELn18:3 almost maintained membrane flexibility and skin permeability of liposomes, while Ergo significantly reduced them. Skin permeation test demonstrated that EL18:2 and ELn18:3 liposomes permeated to the dermis, whereas Ergo liposome mostly remained in the stratum corneum. This is the first report to show that EL18:2 and ELn18:3 can be efficient sterol compounds for flexible liposome formulation.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"250 ","pages":"Article 105270"},"PeriodicalIF":3.4,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0009308422000986/pdfft?md5=c029d1e5a8339320c30578c2e837da0f&pid=1-s2.0-S0009308422000986-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10768952","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Synthetic star shaped tetra-tailed biocompatible supramolecular amphiphile as an efficient nanocarrier for Amphotericin B 合成星形四尾生物相容性超分子两亲体作为两性霉素B的高效纳米载体

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2023-01-01 DOI: 10.1016/j.chemphyslip.2022.105257

Imdad Ali , Samiullah Burki , Jawad ur Rehman , Shafi Ullah , Ibrahim Javid , Magda H. Abdellattif , Muhammad Raza Shah

{"title":"Synthetic star shaped tetra-tailed biocompatible supramolecular amphiphile as an efficient nanocarrier for Amphotericin B","authors":"Imdad Ali , Samiullah Burki , Jawad ur Rehman , Shafi Ullah , Ibrahim Javid , Magda H. Abdellattif , Muhammad Raza Shah","doi":"10.1016/j.chemphyslip.2022.105257","DOIUrl":"10.1016/j.chemphyslip.2022.105257","url":null,"abstract":"<div>Macrocycle-based amphiphiles are capable of self-assembling into multidimensional nano-architecture with defined dimensions for various applications. Herein we report the synthesis, physio-chemical characterizations and oral drug delivery profiling of resorcinarene-based amphiphilic supramolecular macrocycle. The macrocycle was synthesized in two-step reaction and characterized using 1H NMR, Mass spectrometry and IR spectroscopic techniques. The synthesized macrocycle was assessed for vesicles formation, checked for biocompatibility and then Amphotericin B (Amp-B) was entrapped in macrocycle-based vesicles. The drug loaded vesicles were characterized for shape, size, homogeneity, drug entrapment, surface charge, in-vitro release profile and stability. Amp-B loaded macrocycle based vesicles were examined in rabbits for in-vivo bioavailability and compared with plan drug suspension. The synthesized macrocycle was non-toxic in normal mouse fibroblast cells, compatible with blood and safe in mice. The drug loaded macrocycle based vesicles appeared spherical with 279.4 nm size and − 12.2 mV zeta potential loading 85.45 % drug. The drug loaded vesicles storage stability for 30 days and gastric fluid stability for 1 h were it retained nearly 90 % drug at 30th day and 83.79 % drug at 1 h in gastric fluid. Oral bioavailability of Amp-B in rabbits was markedly enhanced when delivered in synthesized macrocycle based vesicles in comparison with plan drug suspension. Results of this study indicate that the synthesized star shaped tetra-tailed supramolecular amphiphile could be used as an efficient nanocarrier for enhancing oral bioavailability of drugs with solubility and bioavailability issues like Amp-B.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"250 ","pages":"Article 105257"},"PeriodicalIF":3.4,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0009308422000858/pdfft?md5=5e400f18fe1b58c5009955bc928b8bed&pid=1-s2.0-S0009308422000858-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9320559","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Effect of the CER[NP]:CER[AP] a ratio on the structure of a stratum corneum model lipid matrix - a molecular dynamics study CER[NP]:CER[AP] a比值对角质层模型脂质基质结构的影响——分子动力学研究

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2023-01-01 DOI: 10.1016/j.chemphyslip.2022.105259

Natalia Rivero, Martha C. Daza, Markus Doerr

{"title":"Effect of the CER[NP]:CER[AP] a ratio on the structure of a stratum corneum model lipid matrix - a molecular dynamics study","authors":"Natalia Rivero, Martha C. Daza, Markus Doerr","doi":"10.1016/j.chemphyslip.2022.105259","DOIUrl":"10.1016/j.chemphyslip.2022.105259","url":null,"abstract":"<div>In some dermal diseases with evident skin dehydration and desquamation, the natural ratio of CER[NP]:CER[AP] is altered in the extracellular matrix of the stratum corneum by increasing the concentration of CER[AP]. The extracellular matrix of the stratum corneum is composed of several stacked lipid bilayers. Molecular dynamics simulations were used to investigate the molecular nanostructure of CER[NP], CER[AP], cholesterol and lignoceric acid models of the extracellular matrix of the stratum corneum with a nativelike CER[NP]:CER[AP] 2:1 ratio and a CER[NP]:CER[AP] ratio of 1:2. Despite the very minor chemical difference between CER[NP] and CER[AP], which is only a single OH group, it was possible to observe differences between the structural influence of the two ceramides. In the models with 1:2 ratio, the higher CER[AP] content leads to a larger inclination of the acyl chains and a smaller overlap in the lamellar midplane, with a small increase of the repeat distance compared to the model with higher CER[NP] concentration. Because CER[AP] forms more H-bonds than CER[NP], the total number of hydrogen bonds in the headgroup region is larger in the models with higher CER[AP] concentration, reducing the mobility of the lipids towards the centre of the bilayer and resulting in less overlap and increased tilt angles.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"250 ","pages":"Article 105259"},"PeriodicalIF":3.4,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0009308422000871/pdfft?md5=b55a70e80128db04c5e7c63bb1cdb2b1&pid=1-s2.0-S0009308422000871-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10830364","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Nanostructured lipid carrier-loaded metformin hydrochloride: Design, optimization, characterization, assessment of cytotoxicity and ROS evaluation 纳米结构脂质载体负载盐酸二甲双胍:设计、优化、表征、细胞毒性评估和ROS评估

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2023-01-01 DOI: 10.1016/j.chemphyslip.2022.105256

Meghanath B. Shete , Ashwini S. Deshpande , Pravin K. Shende

{"title":"Nanostructured lipid carrier-loaded metformin hydrochloride: Design, optimization, characterization, assessment of cytotoxicity and ROS evaluation","authors":"Meghanath B. Shete , Ashwini S. Deshpande , Pravin K. Shende","doi":"10.1016/j.chemphyslip.2022.105256","DOIUrl":"10.1016/j.chemphyslip.2022.105256","url":null,"abstract":"<div>Metformin hydrochloride (MET) is commonly used in diabetes treatment. Recently, it has gained interest for its anticancer potential against a wide range of cancers. Owing to its hydrophilic nature, the delivery and clinical actions of MET are limited. Therefore, the present work aims to develop MET-encapsulated NLCs using the hot-melt emulsification and probe-sonication method. The optimization was accomplished by 33 BB design wherein lipid ratio, surfactant concentration, and sonication time were independent variables while the PS (nm), PDI, and EE (%) were dependent variables. The PS, PDI, % EE and ZP of optimized GMSMET-NLCs were found to be 114.9 ± 1.32 nm, 0.268 ± 0.04 %, 60.10 ± 2.23 %, and ZP − 15.76 mV, respectively. The morphological features, DSC and PXRD, and FTIR analyses suggested the confirmation of formation of the NLCs. Besides, optimized GMSMET-NLCs showed up to 88 % MET release in 24 h. Moreover, GMSMET-NLCs showed significant cell cytotoxicity against KB oral cancer cells compared with MET solution as shown by the reduction of IC50 values. Additionally, GMSMET-NLCs displayed significantly increased intracellular ROS levels suggesting the GMSMET-NLCs induced cell death in KB cells. GMSMET-NLCs can therefore be explored to deliver MET through different routes of administration for the effective treatment of oral cancer.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"250 ","pages":"Article 105256"},"PeriodicalIF":3.4,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0009308422000846/pdfft?md5=6a09818f299d76af879b2464e4bd3b8c&pid=1-s2.0-S0009308422000846-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9320968","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Fatty acid transport proteins (FATPs) in cancer 脂肪酸转运蛋白(FATPs)在癌症中的作用

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2023-01-01 DOI: 10.1016/j.chemphyslip.2022.105269

Ranjitha Acharya , Shilpa S. Shetty , Suchetha Kumari N

{"title":"Fatty acid transport proteins (FATPs) in cancer","authors":"Ranjitha Acharya , Shilpa S. Shetty , Suchetha Kumari N","doi":"10.1016/j.chemphyslip.2022.105269","DOIUrl":"10.1016/j.chemphyslip.2022.105269","url":null,"abstract":"<div>Lipids play pivotal roles in cancer biology. Lipids have a wide range of biological roles, especially in cell membrane synthesis, serve as energetic molecules in regulating energy-demanding processes; and they play a significant role as signalling molecules and modulators of numerous cellular functions. Lipids may participate in the development of cancer through the fatty acid signalling pathway. Lipids consumed in the diet act as a key source of extracellular pools of fatty acids transported into the cellular system. Increased availability of lipids to cancer cells is due to increased uptake of fatty acids from adipose tissues. Lipids serve as a source of energy for rapidly dividing cancerous cells. Surviving requires the swift synthesis of biomass and membrane matrix to perform exclusive functions such as cell proliferation, growth, invasion, and angiogenesis. FATPs (fatty acid transport proteins) are a group of proteins involved in fatty acid uptake, mainly localized within cells and the cellular membrane, and have a key role in long-chain fatty acid transport. FATPs are composed of six isoforms that are tissue-specific and encoded by a specific gene. Previous studies have reported that FATPs can alter fatty acid metabolism, cell growth, and cell proliferation and are involved in the development of various cancers. They have shown increased expression in most cancers, such as melanoma, breast cancer, prostate cancer, renal cell carcinoma, hepatocellular carcinoma, bladder cancer, and lung cancer. This review introduces a variety of FATP isoforms and summarises their functions and their possible roles in the development of cancer.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"250 ","pages":"Article 105269"},"PeriodicalIF":3.4,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0009308422000974/pdfft?md5=de68eb83150446740aae95a58c16d224&pid=1-s2.0-S0009308422000974-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10830366","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Towards understanding the binding affinity of lipid drug carriers to serum albumin 探讨脂质药物载体与血清白蛋白的结合亲和力

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2023-01-01 DOI: 10.1016/j.chemphyslip.2022.105271

Katarzyna Dopierała , Marek Weiss , Martyna Krajewska , Justyna Błońska

{"title":"Towards understanding the binding affinity of lipid drug carriers to serum albumin","authors":"Katarzyna Dopierała , Marek Weiss , Martyna Krajewska , Justyna Błońska","doi":"10.1016/j.chemphyslip.2022.105271","DOIUrl":"10.1016/j.chemphyslip.2022.105271","url":null,"abstract":"<div>In the past several years there has been a rapid rise in the use of lipid-based drug formulations. In the case of intravenous drug administration the interaction of lipid carrier with serum albumin is crucial for the distribution of the bioactive molecules in the bloodstream and reaching the target tissue. In this work, we have explored the interaction of serum albumin with three-component lipid monolayer build of palmitoyloleoylphosphatidylcholine (POPC), sphingomyelin (SM), and cholesterol (Chol). Using wide range of lipid compositions and various concentrations of serum albumin we identified the factors governing the lipid-protein binding. Our study revealed that albumin can penetrate selectively the monolayers of POPC/SM/Chol depending on the lipid composition in the mixture. Moreover, the interaction of albumin with monolayer can be controlled by the molecular density of the film and the concentration of protein. The adsorbed albumin exists in the film on the top of lipid monolayer. This behavior may lead to the increase of the size and charge of the lipid carrier and affect the drug transport throughout the bloodstream. The results of this work provide essential physicochemical data that can be used for predicting the pharmacokinetic profile of lipid-based formulations.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"250 ","pages":"Article 105271"},"PeriodicalIF":3.4,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0009308422000998/pdfft?md5=73cb2869cfea3e1c8608521368fa2dc7&pid=1-s2.0-S0009308422000998-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10761361","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

Challenges and emerging strategies for next generation liposomal based drug delivery: An account of the breast cancer conundrum 新一代基于脂质体的药物递送的挑战和新兴策略:对乳腺癌难题的解释

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2023-01-01 DOI: 10.1016/j.chemphyslip.2022.105258

Aliesha Moudgil , Rajesh Salve , Virendra Gajbhiye , Bhushan P. Chaudhari

{"title":"Challenges and emerging strategies for next generation liposomal based drug delivery: An account of the breast cancer conundrum","authors":"Aliesha Moudgil , Rajesh Salve , Virendra Gajbhiye , Bhushan P. Chaudhari","doi":"10.1016/j.chemphyslip.2022.105258","DOIUrl":"10.1016/j.chemphyslip.2022.105258","url":null,"abstract":"<div>The global cancer burden is witnessing an upsurge with breast cancer surpassing other cancers worldwide. Furthermore, an escalation in the breast cancer caseload is also expected in the coming years. The conventional therapeutic regimens practiced routinely are associated with many drawbacks to which nanotechnological interventions offer a great advantage. But how eminent could liposomes and their advantages be in superseding these existing therapeutic modalities? A solution is reflected in this review that draws attention to a decade-long journey embarked upon by researchers in this wake. This text is a comprehensive discussion of liposomes, the front runners of the drug delivery systems, and their active and passive targeting approaches for breast cancer management. Active targeting has been studied over the decade by many receptors overexpressed on the breast cancer cells and passive targeting with many drug combinations. The results converge on the fact that the actively targeted formulations exhibit a superior efficacy over their non-targeted counterparts and the all liposomal formulations are efficacious over the free drugs. This undoubtedly underlines the dominion of liposomal formulations over conventional chemotherapy. These investigations have led to the development of different liposomal formulations with active and passive targeting capacities that could be explored in depth. Acknowledging and getting a deeper insight into the liposomal evolution through time also unveiled many imperfections and unchartered territories that can be explored to deliver dexterous liposomal formulations against breast cancer and more in the clinical trial pipeline.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"250 ","pages":"Article 105258"},"PeriodicalIF":3.4,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S000930842200086X/pdfft?md5=0af4570b2051f2c1366c023f08b0c6e2&pid=1-s2.0-S000930842200086X-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9320970","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Modulation of function and structure of stratum corneum in sphingomyelin synthase 2-deficient mice 鞘磷脂合酶2缺陷小鼠角质层功能和结构的调控

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2022-11-01 DOI: 10.1016/j.chemphyslip.2022.105255

Nozomi Honma , Ichiro Hatta , Toshiro Okazaki , Yoshihiro Tokudome

{"title":"Modulation of function and structure of stratum corneum in sphingomyelin synthase 2-deficient mice","authors":"Nozomi Honma , Ichiro Hatta , Toshiro Okazaki , Yoshihiro Tokudome","doi":"10.1016/j.chemphyslip.2022.105255","DOIUrl":"10.1016/j.chemphyslip.2022.105255","url":null,"abstract":"<div>Sphingomyelin synthase (SMS) synthesizes sphingomyelin (SM) from ceramide (Cer), a precursor of Cer. The effects of SMS deficiency on stratum corneum (SC) barrier function and SC lamellar structure are unknown. In this report, permeation of hydrophilic and lipophilic compounds through full-thickness skin or stripped skin of SMS2-knockout (KO) and wild-type (WT) mice was examined. Furthermore, small-angle and wide-angle X-ray scattering (SAXS and WAXS) measurements of the SC were performed as a function of temperature to analyze the lamellar structure and hydrocarbon chain packing, where a SC sample was changed from 10 °C to 120 °C at 2 °C/min and the X-ray diffraction profile in the small-angle region and the wide-angle region was observed. Skin permeability of the hydrophilic compound increased significantly for SMS2-KO mice when compared with that of WT mice. In contrast, no difference was observed in the penetration of lipophilic compounds in the skin of both SMS2-KO and WT mice. In SC of SMS2-KO mice, two sharp SAXS peaks were observed due to the lamellar structure with a repetition period of 4.8 nm. The WAXS revealed that the intensity ratio R0.42/0.37 of the 0.42 nm peak at 2.4 nm–1 to the 0.37 nm peak at 2.7 nm–1 was smaller in the SMS2-KO mouse than in the WT mouse. Due to the temperature dependence of the WAXS, the peaks of 2.4 and 2.7 nm−1 remained until the higher temperatures in SMS2-KO mouse SC than those in WT mouse SC. The results of X-ray diffraction suggest that deficiency of SMS2 may cause the appearance of highly ordered structures of SC, which in turn may reduce the barrier function of SC.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"249 ","pages":"Article 105255"},"PeriodicalIF":3.4,"publicationDate":"2022-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10572299","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}

引用次数: 1

Synthesis of pH-responsive dimethylglycine surface-modified branched lipids for targeted delivery of antibiotics 用于抗生素靶向递送的ph响应二甲基甘氨酸表面修饰支链脂质的合成

IF 3.4 3区生物学

Chemistry and Physics of Lipids Pub Date : 2022-11-01 DOI: 10.1016/j.chemphyslip.2022.105241

Sifiso S. Makhathini , Calvin A. Omolo , Lucy W. Kiruri , Pavan Walvekar , Nikita Devnarain , Chunderika Mocktar , Thirumala Govender

{"title":"Synthesis of pH-responsive dimethylglycine surface-modified branched lipids for targeted delivery of antibiotics","authors":"Sifiso S. Makhathini , Calvin A. Omolo , Lucy W. Kiruri , Pavan Walvekar , Nikita Devnarain , Chunderika Mocktar , Thirumala Govender","doi":"10.1016/j.chemphyslip.2022.105241","DOIUrl":"10.1016/j.chemphyslip.2022.105241","url":null,"abstract":"<div>The rampant antimicrobial resistance crisis calls for efficient and targeted drug delivery of antibiotics at the infectious site. Hence, this study aimed to synthesize a pH-responsive dimethylglycine surface-modified branched lipid (DMGSAD-lipid). The structure of the synthesized lipid was fully confirmed. The lipid polymer hybrid nanoparticles (LPHNPs) were formulated using the solvent evaporation method and characterised. Two LPHNPs (VCM_HS15_LPHNPs and VCM_RH40_LPHNPs) were formulated and characterised for size, polydispersity index (PDI), and zeta potential (ZP). Atomistic molecular dynamics simulations revealed that both the systems self-assembled to form energetically stable aggregates. The ZP of RH40_VCM_LPHNPs changed from 0.55 ± 0.14–9.44 ± 0.33 Vm, whereas for SH15_VCM_LPHNPs, ZP changed from − 1.55 ± 0.184 Vm to 9.83 ± 0.52 Vm at pH 7.4 and 6.0, respectively. The encapsulation efficiencies of VCM were above 40% while the drug release was faster at acidic pH when compared to pH 7.4. The antibacterial activity of LPHNPs against MRSA was eight-fold better in MICs at pH 6.0, compared to 7.4, when compared to bare VCM-treated specimens. The study confirms that pH-responsive LPHNPs have the potential for enhancing the treatment of bacterial infections and other diseases characterised by acidic conditions at the target site.</div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"249 ","pages":"Article 105241"},"PeriodicalIF":3.4,"publicationDate":"2022-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10575444","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}

引用次数: 1