Journal of Liposome Research最新文献

{"title":"Prognosticating the effect of temperature and pH parameters on size and stability of the nanoliposome system based on thermodynamic modeling.","authors":"Fardin Rahimi, Pari Hajizadeh, Ghassem Amoabediny, Bahman Ebrahimi, Mansoor Khaledi, Fatemeh Sameni, Hamed Afkhami, Shahriar Bakhti, Elham Rafiee Taqanaki, Mahdi Zafari","doi":"10.1080/08982104.2023.2203250","DOIUrl":"10.1080/08982104.2023.2203250","url":null,"abstract":"<p><p>The main challenge of using nanoliposome systems is controlling their size and stability. In order to overcome this challenge, according to the research conducted at the Research Centre for New Technologies of Biological Engineering, University of Tehran, a model for predicting the size and stability of nanoliposome systems based on thermodynamic relations has been presented. In this model, by using the presented equations and without performing many experiments in the laboratory environment, the effect of temperature, ionic power and different pH can be considered simultaneously whereas examining the components of size, stability and any feature were considered before. Synthesis and application of liposomal nanocarriers in different operating conditions can be investigated and predicted, and due to the change in temperature and pH, the smallest size of th system can be obtained. In this study, we were able to model the synthesis and storage conditions of liposomal nanocarriers at different temperatures and acidic, neutral and alkaline pHs, based on the calculation of mathematical equations. This model also indicates that with increasing temperature, the radius increases but with increasing pH, the radius first increases and then decreases. Therefore, this model can be used to predict size and stability in different operating conditions. In fact, with this modelling method, there is no need to study through laboratory methods and analysis to determine the size, stability and surface loads, and in terms of Accuracy, time and cost savings are affordable.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"392-409"},"PeriodicalIF":4.4,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9452464","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}

{"title":"MC3/SAINT-O-Somes, a novel liposomal delivery system for efficient and safe delivery of siRNA into endothelial cells.","authors":"Yutong He, Mees Barlag, Josée A Plantinga, Grietje Molema, Jan A A M Kamps","doi":"10.1080/08982104.2023.2187821","DOIUrl":"10.1080/08982104.2023.2187821","url":null,"abstract":"<p><p>Increased understanding of chronic inflammatory diseases and the role of endothelial cell (EC) activation herein, have urged interest in sophisticated strategies to therapeutically intervene in activated EC to treat these diseases. Liposome-mediated delivery of therapeutic siRNA in inflammation-activated EC is such a strategy. In this study, we describe the design and characterisation of two liposomal siRNA delivery systems formulated with the cationic MC3 lipid or MC3/SAINT mixed lipids, referred to as MC3-O-Somes (MOS) and MC3/SAINT-O-Somes (MSS). The two formulations showed comparable physicochemical properties, except for better siRNA encapsulation efficiency in the MSS formulation. Antibody-mediated VCAM-1 targeting (Ab_VCAM-1) increased the association of the targeted MOS and MSS with activated EC, although the targeted MOS showed a significantly higher VCAM-1 specific association than the targeted MSS. Ab_VCAM-1 MSS containing RelA siRNA achieved significant downregulation of RelA expression, while Ab_VCAM-1 MOS containing RelA siRNA did not downregulate RelA expression in activated EC. Additionally, Ab_VCAM-1 MSS containing RelA siRNA showed low cytotoxicity in EC and at the same time prohibited endothelial inflammatory activation by reducing expression of cell adhesion molecules. The Ab_VCAM-1 MSS formulation is a novel siRNA delivery system based on a combination of the cationic lipids MC3 and SAINT, that shows good physicochemical characteristics, enhanced endothelial cell association, improved transfection activity, low toxicity and significant anti-inflammatory effect, thereby complying with the requirements for future in vivo investigations.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"328-337"},"PeriodicalIF":4.4,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9114679","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}

{"title":"Liposomal drug delivery to the lungs: a post covid-19 scenario.","authors":"S Swathi Krishna, M S Sudheesh, Vidya Viswanad","doi":"10.1080/08982104.2023.2199068","DOIUrl":"10.1080/08982104.2023.2199068","url":null,"abstract":"<p><p>High local delivery of anti-infectives to the lungs is required for activity against infections of the lungs. The present pandemic has highlighted the potential of pulmonary delivery of anti-infective agents as a viable option for infections like Covid-19, which specifically causes lung infections and mortality. To prevent infections of such type and scale in the future, target-specific delivery of drugs to the pulmonary region is a high-priority area in the field of drug delivery. The suboptimal effect of oral delivery of anti-infective drugs to the lungs due to the poor biopharmaceutical property of the drugs makes this delivery route very promising for respiratory infections. Liposomes have been used as an effective delivery system for drugs due to their biocompatible and biodegradable nature, which can be used effectively for target-specific drug delivery to the lungs. In the present review, we focus on the use of liposomal drug delivery of anti-infectives for the acute management of respiratory infections in the wake of Covid-19 infection.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"410-424"},"PeriodicalIF":4.4,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9420297","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}

{"title":"Enhanced protection against hypoxia/reoxygenation-induced apoptosis in H9c2 cells by puerarin-loaded liposomes modified with matrix metalloproteinases-targeting peptide and triphenylphosphonium.","authors":"Fengmei Li, Yan Wang, Wenqun Li, Junyong Wu, Shengnan Li, Xiongbin Hu, Tiantian Tang, Xinyi Liu","doi":"10.1080/08982104.2023.2193845","DOIUrl":"10.1080/08982104.2023.2193845","url":null,"abstract":"<p><p>Based on the inhibition of mitochondrial permeability transition pore (mPTP) opening, puerarin (PUE) has a good potential to reduce myocardial ischemia/reperfusion injury (MI/RI). However, the lack of targeting of free PUE makes it difficult to reach the mitochondria. In this paper, we constructed matrix metalloproteinase-targeting peptide (MMP-TP) and triphenylphosphonium (TPP) cation co-modified liposomes loaded with PUE (PUE@T/M-L) for mitochondria-targeted drug delivery. PUE@T/M-L had a favorable particle size of 144.9 ± 0.8 nm, an encapsulation efficiency of 78.9 ± 0.6%, and a sustained-release behavior. The results of cytofluorimetric experiments showed that MMP-TP and TPP double-modified liposomes (T/M-L) enhanced intracellular uptake, escaped lysosomal capture, and promoted drug targeting into mitochondria. In addition, PUE@T/M-L enhanced the viability of hypoxia-reoxygenation (H/R) injured H9c2 cells by inhibiting mPTP opening and reactive oxygen species (ROS) production, reducing Bax expression and increasing Bcl-2 expression. It was inferred that PUE@T/M-L delivered PUE into the mitochondria of H/R injured H9c2 cells, resulting in a significant increase in cellular potency. Based on the ability of MMP-TP to bind the elevated expression of matrix metalloproteinases (MMPs), T/M-L had excellent tropism for Lipopolysaccharide (LPS) -stimulated macrophages and can significantly reduce TNF-α and ROS levels, thus allowing both drug accumulation in ischemic cardiomyocytes and reducing inflammatory stimulation during MI/RI. Fluorescence imaging results of the targeting effect using a DiR probe also indicated that DiR@T/M-L could accumulate and retain in the ischemic myocardium. Taken together, these results demonstrated the promising application of PUE@T/M-L for mitochondria-targeted drug delivery to achieve maximum therapeutic efficacy of PUE.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"378-391"},"PeriodicalIF":4.4,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9241762","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}

{"title":"N'-(3-Aminopropyl)-N-(3'-(carbamoyl cholesteryl) propyl)-glycine amide liposomes for delivery of pTRAIL-EGFP.","authors":"Wanlop Weecharangsan, Nuttapon Apiratikul, Jantana Yahuafai","doi":"10.1080/08982104.2023.2193638","DOIUrl":"10.1080/08982104.2023.2193638","url":null,"abstract":"<p><p>In this study, N'-(3-aminopropyl)-N-(3'-(carbamoyl cholesteryl) propyl)-glycine amide (A) and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE, D) (AD) liposomes were synthesised at molar ratios of 50:25 (AD5025), 50:50 (AD5050) and 50:75 (AD5075) and complexed with plasmid, pTRAIL-EGFP. AD liposome/pTRAIL-EGFP were evaluated for their complex ability, particle size, polydispersity index, zeta potential, expression of pTRAIL-EGFP, cytotoxicity, cell growth inhibition and apoptosis induction in KB cells. AD liposomes complexed completely with pTRAIL-EGFP at AD liposome/DNA ratios of above 4.5/1. The particle size of AD liposome/pTRAIL-EGFP ranged from 180 ± 8 to 1,072 ± 657 nm depending on the proportion of lipid composition and liposome/DNA ratio. The extent of gene expression of pTRAIL-EGFP via AD liposome/pTRAIL-EGFP was significantly higher than that of the cells treated with pTRAIL-EGFP and depended on the AD liposome/DNA ratio. Cytotoxicity of AD liposomes was dependent on A and D molar ratio. Cell growth inhibition of AD liposome/pTRAIL-EGFP was significantly higher than that of the cells treated with pTRAIL-EGFP. The amount of late apoptotic and dead cells of AD liposome/pTRAIL-EGFP was significantly higher than that of cells treated with pTRAIL-EGFP. From this study that one can conclude that AD liposomes can carry and deliver pTRAIL-EGFP into KB cells resulting in cell growth inhibition and cell death.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"368-377"},"PeriodicalIF":3.6,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9188610","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}

{"title":"Long-circulating doxorubicin and Schizandrin A liposome with drug-resistant liver cancer activity: <i>in vitro</i> and <i>in vivo</i> evaluation.","authors":"Shi-Yi Xu, Wei-Wei Wang, Zi-Hui Qu, Xiang-Ke Zhang, Ming Chen, Xin-Yu Zhang, Nan-Nan Xing, Hui Su, Xue-Ying Wang, Ming-Yu Cui, Xue-Ying Yan, Wei Ma","doi":"10.1080/08982104.2023.2190810","DOIUrl":"10.1080/08982104.2023.2190810","url":null,"abstract":"<p><p>Co-loading doxorubicin (DOX) and Schizandrin A (SchA) long-circulating liposome (SchA-DOX-Lip) have been confirmed to have good antitumor activity <i>in vitro</i>. However, <i>in vivo</i> pharmacodynamics, targeting, safety, and mechanism of action of SchA-DOX-Lip still need to be further verified. We investigated the tumor inhibition effect, targeting, safety evaluation, and regulation of tumor apoptosis-related proteins of the SchA-DOX-Lip. MTT assay was used to investigate the inhibitory effect of SchA-DOX-Lip on CBRH7919 cells. The drug uptake of CBRH7919 cells was observed by inverted fluorescence microscope. The tumor-bearing nude mice models of CBRH7919 were established, and the anti-tumor effect of SchA-DOX-Lip <i>in vivo</i> was evaluated by tumor biological observation, H&E staining, and TUNEL staining. The distribution and targeting of SchA-DOX-Lip in nude mice models were investigated by small animal imaging and tissue distribution experiment of CBRH7919. The biosafety of SchA-DOX-Lip was evaluated by blood routine parameters, biochemical indexes, and H&E staining. The expression of tumor-associated apoptotic proteins (Bcl-2, Bax, and Caspase-3) was detected by immunohistochemistry anvd western blotting. The results showed that SchA-DOX-Lip had cytotoxicity to CBRH7919 cells which effectively inhibited the proliferation of CBRH7919 cells, improved the uptake of drugs by CBRH7919 cells and the targeting effect of drugs on tumor site. H&E staining and biochemical detection results showed that SchA-DOX-Lip had high biosafety and did not cause serious damage to normal tissues. Western-blotting and TUNEL staining results showed that SchA-DOX-Lip could improve the regulatory effect of drugs on tumor apoptosis proteins. It was demonstrated that SchA-DOX-Lip had high safety and strong tumor inhibition effects, providing a new method for the clinical treatment of hepatocellular carcinoma (HCC).</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":" ","pages":"338-352"},"PeriodicalIF":4.4,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9971950","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}

{"title":"A transfersomes hydrogel patch for cutaneous delivery of propranolol hydrochloride: formulation, <i>in vitro</i>, <i>ex vivo</i> and <i>in vivo</i> studies.","authors":"Changzhao Jiang,&nbsp;Rui Ma,&nbsp;Xiumei Jiang,&nbsp;Renhua Fang,&nbsp;Jincui Ye","doi":"10.1080/08982104.2022.2162539","DOIUrl":"https://doi.org/10.1080/08982104.2022.2162539","url":null,"abstract":"<p><strong>Objective: </strong>In this work, a propranolol hydrochloride (PRH) transfersomes loaded cutaneous hydrogel patch was developed for topical drug delivery in the affected area of infantile haemangioma.</p><p><strong>Methods: </strong>Sodium cholate was used as the edge activator to prepare the transfersomes. Based on the central composite design, transfersomes hydrogel patch formulation was optimised with 48 h cumulative penetration and time lag as response values. Particle sizes and morphology of the prepared transfersomes were assessed. They were loaded in a cutaneous hydrogel patch, after which their skin permeation abilities were evaluated, and histopathological effects were investigated using guinea pigs. Moreover, in vivo pharmacokinetics studies were performed in rats.</p><p><strong>Results: </strong>The transfersomes system had a encapsulation efficiency of 81.84 ± 0.53%, particle size of 186.8 ± 3.38 nm, polydispersity index of 0.186 ± 0.002, and a zeta potential of -28.6 ± 2.39 mV. Transmission electron microscopy images revealed sphericity of the particles. The <i>ex vivo</i> drug's penetration of the optimised transfersomes hydrogel patch was 111.05 ± 11.97 μg/cm² through rat skin within 48 h. Assessment of skin tissue did not reveal any histopathological alterations in epidermal and dermal cells. Pharmacokinetic studies showed that skin <i>C</i>_max (68.22 μg/cm²) and AUC_0-24 (1007.33 μg/cm² × h) for PRH transfersomes hydrogel patch were significantly higher than those of commercially available oral dosage form and hydrogel patch without transfersomes. These findings imply that the transfersomes hydrogel patch can prolong drug accumulation in the affected skin area, and reduce systemic drug distribution via the blood stream.</p><p><strong>Conclusions: </strong>The hydrogel patch-loaded PRH transfersomes is a potentially useful drug formulation for infantile haemangioma.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 3","pages":"258-267"},"PeriodicalIF":4.4,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9870189","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}

{"title":"Development and validation of HPLC method for simultaneous estimation of erlotinib and niclosamide from liposomes optimized by screening design.","authors":"Amruta Prabhakar Padakanti,&nbsp;Sachin Dattaram Pawar,&nbsp;Pramod Kumar,&nbsp;Naveen Chella","doi":"10.1080/08982104.2022.2162540","DOIUrl":"https://doi.org/10.1080/08982104.2022.2162540","url":null,"abstract":"<p><p>The emerging drug resistance to the approved first-line drug therapy leads to clinical failure in cancer. Drug repurposing studies lead to the identification of many old drugs to be used for cancer treatment. Combining the repurposed drugs (niclosamide) with first-line therapy agents like erlotinib HCl showed improved efficacy by inhibiting erlotinib HCl acquired resistance. But there is a need to develop a sensitive, accurate, and excellent analytical method and drug delivery system for successfully delivering drug combinations. In the current study, an HPLC method was developed and validated for the simultaneous estimation of niclosamide and erlotinib HCl. The retention time of niclosamide and erlotinib hydrochloride was 6.48 and 7.65 min at 333 nm. The developed method was rapid and sensitive to separating the two drugs with reasonable accuracy, precision, robustness, and ruggedness. A Plackett-Burman (PBD) screening design was used to identify the critical parameters affecting liposomal formulation development using particle size, size distribution, zeta potential, and entrapment efficiency as the response. Lipid concentration, drug concentration, hydration temperature, and media volume were critical parameters affecting the particle size, polydispersity index (PDI), ZP, and %EE of the liposomes. The optimized NCM-ERL liposomes showed the particle size (126.05 ± 2.1), PDI (0.498 ± 0.1), ZP (-16.2 ± 0.3), and %EE of NCM and ERL (50.04 ± 2.8 and 05.42 ± 1.3). <i>In vitro</i> release studies indicated the controlled release of the drugs loaded liposomes (87.06 ± 9.93% and 42.33 ± 0.89% in 24 h).</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 3","pages":"268-282"},"PeriodicalIF":4.4,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9870191","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}

{"title":"Evaluation of suitability and detection range of fluorescent dye-loaded nanoliposomes for sensitive and rapid sensing of wide ranging osmolarities.","authors":"Debjyoti Roy,&nbsp;Gangaram H S Udugiri,&nbsp;Sudhir H Ranganath","doi":"10.1080/08982104.2023.2172582","DOIUrl":"https://doi.org/10.1080/08982104.2023.2172582","url":null,"abstract":"<p><p>Measurement of osmolarity is critical for optimizing bioprocesses including antibody production and detecting pathologies. Thus, rapid, sensitive, and <i>in situ</i> sensing of osmolarity is desirable. This study aims to develop and assess the suitability of calcein- and sulforhodamine-loaded nanoliposomes for ratiometric sensing of osmolarity by fluorescence spectroscopy and evaluate the range of detection. The detection is based on concentration-dependent self-quenching of calcein fluorescence (sensor dye at 6-15 mM) and concentration-independent fluorescence of sulforhodamine (reference dye) due to osmotic shrinkage of the nanoliposomes when exposed to hyperosmotic solutions. Using mathematical modeling, 6 mM calcein loading was found to be optimal to sense osmolarity between 300 and 3000 mOsM. Calcein (6 mM)- and sulforhodamine (2 mM)-loaded nanoliposomes were produced by thin-film hydration and serial extrusion. The nanoliposomes were unilamellar, spherical (108 ± 9 nm), and uniform in size (polydispersity index [PDI] 0.12 ± 0.04). Their shrinkage induced by exposure to hyperosmotic solutions led to rapid self-quenching of calcein fluorescence (F_Green), but no effect on sulforhodamine fluorescence (F_Red) was observed. F_Green/F_Red decreased linearly with increasing osmolarity, obeying Boyle van't Hoff's relationship, thus proving that the nanoliposomes are osmosensitive. A calibration curve was generated to compute osmolarity based on F_Green/F_Red measurements. As a proof-of-concept, dynamic changes in osmolarity in a yeast-based fermentation process was demonstrated. Thus, the nanoliposomes have great potential as sensors to rapidly and sensitively measure wide-ranging osmolarities.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 3","pages":"300-313"},"PeriodicalIF":4.4,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9882465","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}

{"title":"Co-delivery of gemcitabine and salinomycin in PEGylated liposomes for enhanced anticancer efficacy against colorectal cancer.","authors":"Lucia Ruxandra Tefas,&nbsp;Ioana Toma,&nbsp;Alina Sesarman,&nbsp;Manuela Banciu,&nbsp;Ancuta Jurj,&nbsp;Ioana Berindan-Neagoe,&nbsp;Lucia Rus,&nbsp;Rares Stiufiuc,&nbsp;Ioan Tomuta","doi":"10.1080/08982104.2022.2153139","DOIUrl":"https://doi.org/10.1080/08982104.2022.2153139","url":null,"abstract":"<p><p>Colorectal cancer remains one of the major causes of morbidity and mortality in both developed and emerging countries. Cancer stem cells (CSCs) are a subpopulation of cells within the tumor mass harboring stem cell characteristics, considered responsible for tumor initiation, growth, relapse, and treatment failure. Lately, it has become clear that both CSCs and non-CSCs have to be eliminated for the successful eradication of cancer. Drug delivery systems have been extensively employed to enhance drug efficacy. In this study, salinomycin (SAL), a selective anti-CSC drug, and gemcitabine (GEM), a conventional anticancer drug, were co-loaded in liposomes and tested for optimal therapeutic efficacy. We employed the Design of Experiments approach to develop and optimize a liposomal delivery system for GEM and SAL. The antiproliferative effect of the liposomes was evaluated in SW-620 human colorectal cancer cells. The GEM and SAL-loaded liposomes exhibited adequate size, polydispersity, zeta potential, and drug content. The <i>in vitro</i> release study showed a sustained release of GEM and SAL from the liposomes over 72 h. Moreover, no sign of liposome aggregation was seen over 1 month and in a biological medium (FBS). The <i>in vitro</i> cytotoxic effects of the co-loaded liposomes were superior to that of single GEM either in free or liposomal form. The combination therapy using GEM and SAL co-loaded in liposomes could be a promising strategy for tackling colorectal cancer.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 3","pages":"234-250"},"PeriodicalIF":4.4,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9876410","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}