{"title":"Protein-liposome interactions: the impact of surface charge and fluidisation effect on protein binding.","authors":"Efstathia Triantafyllopoulou, Natassa Pippa, Costas Demetzos","doi":"10.1080/08982104.2022.2071296","DOIUrl":"https://doi.org/10.1080/08982104.2022.2071296","url":null,"abstract":"<p><p>At the dawn of a new nanotechnological era in the pharmaceutical field, it is very important to examine and understand all the aspects that influence in vivo behaviour of nanoparticles. In this point of view, the interactions between serum proteins and liposomes with incorporated anionic, cationic, and/or PEGylated lipids were investigated to elucidate the role of surface charge and bilayer fluidity in protein corona's formation. 1,2-dipalmitoyl-sn-glycero-3- phosphocholine (DPPC), hydrogenated soybean phosphatidylcholine (HSPC), and 1,2-dioctadecanoyl-sn-glycero-3-phosphocholine (DSPC) liposomes with the presence or absence of 1,2-dipalmitoyl-sn-glycero-3-phospho-(1'-rac-glycerol) (sodium salt) (DPPG), 1,2-di-(9Z-octadecenoyl)-3-trimethylammonium-propane (chloride salt) (DOTAP), and/or 1,2-dipalmitoylsn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-5000] (DPPE-PEG 5000) lipids were prepared by the thin-film hydration method. The evaluation of their biophysical characteristics was enabled by differential scanning calorimetry and dynamic and electrophoretic light scattering. The physicochemical characteristics of mixed liposomes were compared before and after exposure to foetal bovine serum (FBS) and were correlated to calorimetric data. Our results indicate protein binding to all liposomal formulations. However, it is highlighted the importance of surface charge and fluidisation effect to the extent of protein adsorption. Additionally, considering the extensive use of cationic lipids for innovative delivery platforms, we deem PEGylation a key parameter, because even in a small proportion can reduce protein binding, and thus fast clearance and extreme toxicity without affecting positive charge. This study is a continuation of our previous work about protein-liposome interactions and fraction of stealthiness (Fs) parameter, and hopefully a design road map for drug and gene delivery.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 1","pages":"77-88"},"PeriodicalIF":4.4,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9213963","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}
Elsaied H Elsaied, Hamdy M Dawaba, El Sherbini A Ibrahim, Mohsen I Afouna
{"title":"Spanlastics gel-A novel drug carrier for transdermal delivery of glimepiride.","authors":"Elsaied H Elsaied, Hamdy M Dawaba, El Sherbini A Ibrahim, Mohsen I Afouna","doi":"10.1080/08982104.2022.2100902","DOIUrl":"https://doi.org/10.1080/08982104.2022.2100902","url":null,"abstract":"<p><p>Glimepiride (3rd-generation sulfonylurea) is used for treatment of type 2 diabetes, but its oral administration has been associated with severe gastric disturbances such as nausea, vomiting, heartburn, anorexia, haemolytic anaemia. Accordingly, the transdermal route may represent a potentially suitable alternative. This work investigates the usefulness of a novel drug carrier system for transdermal application. The system investigated were called spanlastics gels and constituted span 60 with edge activator (tween 60 or tween 80). Spanlastics gel has been introduced as a stable form alternative to the liquid formulations of spanlastics. Spanlastics gels were prepared by coacervation phase separation method. Entrapment efficiency and size of spanlastics vesicles produced from the hydration of spanlastics gels were characterised. In vitro release and skin permeation of glimepiride from various spanlastics gel formulations were investigated across mixed cellulose membrane and excised rabbit skin. The obtained results indicated that the maximum entrapment efficiency was 65.36% when the tween 60 content was 30%. The drug release and permeation were increase as the concentration of edge activator increased. Spanlastics gel prepared with Tween 80 at concentration 50% showed higher permeability and flux value (248.69 µg/cm<sup>2</sup>and 8.31 µg/cm<sup>2</sup>.h, respectively) through rabbit skin.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 1","pages":"102-114"},"PeriodicalIF":4.4,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9201866","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":"Ethosomes as dermal/transdermal drug delivery systems: applications, preparation and characterization.","authors":"Atoosa Jafari, Saeid Daneshamouz, Parisa Ghasemiyeh, Soliman Mohammadi-Samani","doi":"10.1080/08982104.2022.2085742","DOIUrl":"https://doi.org/10.1080/08982104.2022.2085742","url":null,"abstract":"<p><p>Transdermal drug delivery systems (TDDSs) have gained substantial attention during the last decade. TDDS are versatile delivery systems in which active components are delivered to skin for local effects or systemic delivery of active pharmaceutical through the skin. Overcoming stratum corneum is the most challenging step of delivering drugs through the skin. Lipid-based vesicular delivery systems due to the capability of the delivery of both hydrophilic and hydrophobic drugs are becoming more popular during the recent years. Ethosomes are innovative, biocompatible, biodegradable and non-toxic form of lipid-based vesicles that efficiently enable to entrap drugs of various physicochemical properties. These are other forms of liposome which contain high amounts of ethanol in their structure that enabling ethosomes to efficiently penetrate through deeper layers of skin. Ethosomes have various compositions based on their type but are mainly composed of phospholipids, ethanol, water and the active components. Ethosomes are easily manufactured and they are superior compared to liposomes in terms of different aspects due to the presence of ethanol. The purpose of this review is to thoroughly focus on various aspects of ethosomes, including mechanism of penetration, advantages and disadvantages, characterisation and applications.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 1","pages":"34-52"},"PeriodicalIF":4.4,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9201371","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":"Recent updates in curcumin delivery.","authors":"Mohammad A Obeid, Manal Alsaadi, Alaa A Aljabali","doi":"10.1080/08982104.2022.2086567","DOIUrl":"https://doi.org/10.1080/08982104.2022.2086567","url":null,"abstract":"<p><p>Curcumin is a natural component extracted from the rhizomes of turmeric (<i>Curcuma longa</i>), a natural plat with known medicinal uses for more than 4000 years. Most turmeric therapeutic effects are attributed to curcumin, a yellow-coloured extract. Curcumin has received considerable attention due to its biological activities, such as its use in arthritis, liver and neurodegenerative diseases, obesity, and several types of cancers. Most of these curcumin therapeutic activities are related to its antioxidant and anti-inflammatory effects. However, the clinical application of curcumin is hampered by some limitations that prevent its extensive clinical application. Curcumin high hydrophobicity of curcumin and limited water solubility are among the most important limitations. This poor solubility will result in low bioavailability due to its poor absorption into plasma and the target tissues. Curcumin also has rapid metabolism, which will significantly lower its bioavailability and shorten its half-life. Moreover, curcumin is photosensitive with limited chemical stability during manufacturing and storage. These limitations have been overcome by applying nanotechnology using several types of nanoparticles (NPs). This includes using NPs such as liposomes, niosomes, gold nanoparticles, and many others to improve the curcumin solubility and bioavailability. This review focuses on the different types of NPs investigated and the outcomes generated by their use in the most recent studies in this field. To follow the latest advances in the field of site-specific drug delivery using nanomaterials, an electronic databases search was conducted using PubMed, Google scholar and Scopus using the following keywords: lipid-based nanoparticles, curcumin delivery, niosomes, and liposomes.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 1","pages":"53-64"},"PeriodicalIF":4.4,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9208021","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":"Rationale utilization of phospholipid excipients: a distinctive tool for progressing state of the art in research of emerging drug carriers.","authors":"Koilpillai Jebastin, Damodharan Narayanasamy","doi":"10.1080/08982104.2022.2069809","DOIUrl":"https://doi.org/10.1080/08982104.2022.2069809","url":null,"abstract":"<p><p>Phospholipids have a high degree of biocompatibility and are deemed ideal pharmaceutical excipients in the development of lipid-based drug delivery systems, because of their unique features (permeation, solubility enhancer, emulsion stabilizer, micelle forming agent, and the key excipients in solid dispersions) they can be used in a variety of pharmaceutical drug delivery systems, such as liposomes, phytosomes, solid lipid nanoparticles, etc. The primary usage of phospholipids in a colloidal pharmaceutical formulation is to enhance the drug's bioavailability with low aqueous solubility [i.e. Biopharmaceutical Classification System (BCS) Class II drugs], Membrane penetration (i.e. BCS Class III drugs), drug uptake and release enhancement or modification, protection of sensitive active pharmaceutical ingredients (APIs) from gastrointestinal degradation, a decrease of gastrointestinal adverse effects, and even masking of the bitter taste of orally delivered drugs are other uses. Phospholipid-based colloidal drug products can be tailored to address a wide variety of product requirements, including administration methods, cost, product stability, toxicity, and efficacy. Such formulations that are also a cost-effective method for developing medications for topical, oral, pulmonary, or parenteral administration. The originality of this review work is that we comprehensively evaluated the unique properties and special aspects of phospholipids and summarized how the individual phospholipids can be utilized in various types of lipid-based drug delivery systems, as well as listing newly marketed lipid-based products, patents, and continuing clinical trials of phospholipid-based therapeutic products. This review would be helpful for researchers responsible for formulation development and research into novel colloidal phospholipid-based drug delivery systems.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"33 1","pages":"1-33"},"PeriodicalIF":4.4,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9561577","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}
Snehal Pardeshi, Amrendra Tiwari, Uday Titame, Pankaj K Singh, Pavan Kumar Yadav, Manish K Chourasia
{"title":"Development of asolectin-based liposomal formulation for controlled and targeted delivery of erlotinib as a model drug for EGFR monotherapy.","authors":"Snehal Pardeshi, Amrendra Tiwari, Uday Titame, Pankaj K Singh, Pavan Kumar Yadav, Manish K Chourasia","doi":"10.1080/08982104.2022.2040532","DOIUrl":"10.1080/08982104.2022.2040532","url":null,"abstract":"<p><p>The present investigation was envisaged to develop liposomal formulation for efficacious and targeted delivery of epidermal growth factor receptor (EGFR) inhibitor (erlotinib) against pancreatic cancer. The marketed formulations bearing current EGFR inhibitors exhibit serious adverse effects including severe skin, hemolytic and gastrointestinal toxicity. To address the obstacles, we have developed the liposomal formulation, by ether injection method, comprising erlotinib, a tyrosine kinase EGFR inhibitor, proposed to be targeted through enhanced permeability and retention effect (EPR) effect against pancreatic cancer. On succeeding, the liposomes were characterized for various pharmaceutical attributes. The developed liposomes found to sustain a particle size of 121 ± 10.7 nm, whereas PDI of 0.22 ± 0.01 with the surface charge value of -33.7 ± 2.30 mV. The entrapment efficiency and drug loading were found to be 82.60 and 15.89 (%w/w), respectively. The hemolysis study suggested that the developed formulation was safer compared with native drug solution. The proof of concept for enhanced efficacy and decreased toxicity has been established through <i>in vitro</i> assays. The IC50 for free erlotinib and formulation was found to be 2.0 ± 0.3 µg/ml and 1.1 ± 0.1 µg/ml, respectively. The effectivity was evident by cellular uptake study and apoptosis, whereas cell cycle arrest study indicated that erlotinib arrests the G0/G1 phase of cell cycle. Further the erlotinib-asolectin liposomal formulation enhanced cytotoxicity in PANC-1 cells at relatively low dose, proving to be an alternative for current chemotherapeutics against pancreatic cancer.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"32 1","pages":"386-395"},"PeriodicalIF":4.4,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"60049493","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":"Systematic review on activity of liposomal encapsulated antioxidant, antibiotics, and antiviral agents.","authors":"Reshna K R, Preetha Balakrishnan, Sreerag Gopi","doi":"10.1080/08982104.2021.2024568","DOIUrl":"https://doi.org/10.1080/08982104.2021.2024568","url":null,"abstract":"<p><p>Reactive oxygen species (ROS) like superoxide anion, hydrogen peroxide, and hydroxyl radical, can be formed as normal products of aerobic metabolism. Overproduction or insufficient removal of ROS results in significant damage to cell structure and functions. Antioxidants applied directly and at relatively high concentrations to cellular systems are effective in protection against the damaging actions of ROS. Microorganisms including Gram-positive and negative bacteria, fungi, protozoa, algae, etc., can be disease causing microorganism. Antimicrobial agents have the capability to inhibitor destroy the microorganisms. The problems arising from the use of antioxidant and antimicrobial agents include poor solubility, instability during storage, low bioavailability, and difficulty to reach target organs with sufficient doses. Liposomal antimicrobial agent and liposomal antioxidants enhance the solubility, bioavailability, and stability of antimicrobial agent and antioxidants.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"32 4","pages":"340-353"},"PeriodicalIF":4.4,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10370724","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 drift on liposomes to proliposomes: recent advances and promising approaches.","authors":"Neha Dhiman, Jayrajsinh Sarvaiya, Poorti Mohindroo","doi":"10.1080/08982104.2021.2019762","DOIUrl":"https://doi.org/10.1080/08982104.2021.2019762","url":null,"abstract":"<p><p>Liposomes are nano-structured vesicles, made up of phospholipids that provide active ingredients at the site of action at a predetermined rate and add the advantage of the sustained-release formulation. Liposomes have stability issues that tend to agglomerate and fuse upon storage, which reflects their drawback. Hence to overcome the aggregation, fusion, hydrolysis, and/or oxidation problems associated with liposomes a new technology named Proliposomes has been introduced. Proliposomes are defined as carbohydrate carriers coated with phospholipids, which upon addition of water generate liposomes. The objective of the review is to cover the concept of proliposomes for pulmonary or alveolar delivery of drugs and compare it with that of liposomes; highlight the methods used for preparations along with the characterization parameters. This is the first systematic review that covers the categorization of liposomes, characteristic methods, and recent examples of drugs from 2015 to 2021, supplied in form of proliposomes to the macrophages as well as others and offers an advantage over the free drug by offering a prolonged drug release and sufficient bioavailability in addition to overcome the stability issues related to liposomes. Since this is a very new technology and many scientists are continuously working in this field to make the drug available for clinical trials and ultimately in the market for the targeted delivery of drugs with better storage life.HIGHLIGHTSProliposomes as an alternative to overwhelm the stability and storage-related issues of liposomes.Anhydrous carbohydrate carriers are utilized for proliposomal preparation.Inhaled delivery of drugs as solid lipid nanoparticles offers a significant impact on pulmonary tract infections, particularly in cystic fibrosis.Size of liposomes attained after proliposome hydrolysis is critical for drug delivery <i>via</i> respiration.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"32 4","pages":"317-331"},"PeriodicalIF":4.4,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10357132","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}
Gang Wang, Yu Yang, Du Yi, Lu Yuan, Pei-Hao Yin, Xu Ke, Wang Jun-Jie, Min-Fang Tao
{"title":"Eudragit S100 prepared pH-responsive liposomes-loaded betulinic acid against colorectal cancer <i>in vitro</i> and <i>in vivo</i>.","authors":"Gang Wang, Yu Yang, Du Yi, Lu Yuan, Pei-Hao Yin, Xu Ke, Wang Jun-Jie, Min-Fang Tao","doi":"10.1080/08982104.2021.1999974","DOIUrl":"https://doi.org/10.1080/08982104.2021.1999974","url":null,"abstract":"<p><p>This study aimed to develop polymer Eudragit S100 for preparing pH-responsive liposomes-loaded betulinic acid (pH-BA-LP) to improve the therapeutic index of chemotherapy for colorectal cancer. BA-loaded liposomes were coated with Eudragit S100 by a thin film dispersion and easily scalable pH-driven method. The prepared liposomes were evaluated for size, surface morphology, entrapment efficiency, stability, <i>in vitro</i> drug release, and antitumor activity. In particular, pH-BA-LP showed advantages such as lower size (<100 nm), encapsulation efficiency of 90%, high stability, and stably cumulative release. By detecting the antitumor effects of pH-BA-LP <i>in vivo</i>, it showed that the tumor proliferation and cell migration were significantly inhibited in colorectal cancer. The pH-BA-LP also inhibited tumor growth via the regulation of Akt/TLR-mediated signalling and significantly down-regulated the expression of NFAT1 and NFAT4 proteins. It was found that pH-BA-LP can increase NK cells and CD3<sup>+</sup> cells in tumor tissues, and the proportion of CD8<sup>+</sup> cells in CD3<sup>+</sup> cells was also increased, which proved that pH-BA-LP can play an antitumor effect by enhancing the autoimmunity level in tumor-bearing mice. The positive infiltration rates of CD8 and CD68 were increased and CD163 was relatively decreased by using pH-BA-LP, which proved that pH-BA-LP can regulate the immune infiltration levels in tumor-bearing mice. Therefore, the present work provides an effective method to prepare pH-responsive polymer-coated liposomes for colonic delivery with biologically active compounds.</p>","PeriodicalId":16286,"journal":{"name":"Journal of Liposome Research","volume":"32 3","pages":"250-264"},"PeriodicalIF":4.4,"publicationDate":"2022-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39592531","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}