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Application Progress of Liposomes in Drug Development 2.0
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Application Progress of Liposomes in Drug Development 2.0

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (14 July 2023) | Viewed by 9219

Special Issue Editor

Dr. Carla Matos

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Guest Editor
FP-I3ID (Instituto de Investigação, Inovação e Desenvolvimento Fernando Pessoa), FP-BHS (Biomedical and Health Sciences), Universidade Fernando Pessoa, Praça 9 de Abril, 349, 4249-004 Porto, Portugal
Interests: liposomes; membrane interactions; topical vehicles
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Liposomes represent an intense field of research, with new developments in the field emerging each year. In recent years, significant attention has been focused on this subject and noteworthy progress has been made, especially regarding the application of liposomes as site-specific drug-delivery systems. These lipid-based nanocarriers have the capacity to improve the retention and release of pharmacologically active compounds at the sites of action, minimizing the associated systemic side effects; they can also be used for the topical administration of drugs, improving penetration through the skin. Their characteristics of biocompatibility and physicochemical stability promote their potential for use as drug delivery systems, increasing drug stability and bioavailability. Liposomes can also be used as cell models in drug development for the study of the interaction and partition of drugs with biomembranes.

Authors are warmly invited to submit original papers, communications, and reviews regarding the potential applications of different types of liposomes in drug development and drug delivery systems to be published in this Special Issue of the International Journal of Molecular Sciences.

Dr. Carla Matos
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • liposomes
  • drug-delivery systems
  • membrane interactions
  • drug development
  • biocompatible

Published Papers (6 papers)

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Editorial

Jump to: Research

3 pages, 169 KiB  
Editorial
Special Issue “Application Progress of Liposomes in Drug Development”
by Carla M. Matos
Int. J. Mol. Sci. 2024, 25(6), 3454; https://doi.org/10.3390/ijms25063454 - 19 Mar 2024
Viewed by 411
Abstract
The second edition of the Special Issue entitled the “Application Progress of Liposomes in Drug Development” featured contributions predominantly focused on leveraging liposomes as enhancers and carriers in drug delivery in the context of cancer treatment, although this was not the initial intent [...] Read more.
The second edition of the Special Issue entitled the “Application Progress of Liposomes in Drug Development” featured contributions predominantly focused on leveraging liposomes as enhancers and carriers in drug delivery in the context of cancer treatment, although this was not the initial intent of this Special Issue [...] Full article
(This article belongs to the Special Issue Application Progress of Liposomes in Drug Development 2.0)

Research

Jump to: Editorial

23 pages, 6867 KiB  
Article
Chitosomes Loaded with Docetaxel as a Promising Drug Delivery System to Laryngeal Cancer Cells: An In Vitro Cytotoxic Study
by Christian R. Moya-Garcia, Nicole Y. K. Li-Jessen and Maryam Tabrizian
Int. J. Mol. Sci. 2023, 24(12), 9902; https://doi.org/10.3390/ijms24129902 - 08 Jun 2023
Cited by 4 | Viewed by 1733
Abstract
Current delivery of chemotherapy, either intra-venous or intra-arterial, remains suboptimal for patients with head and neck tumors. The free form of chemotherapy drugs, such as docetaxel, has non-specific tissue targeting and poor solubility in blood that deters treatment efficacy. Upon reaching the tumors, [...] Read more.
Current delivery of chemotherapy, either intra-venous or intra-arterial, remains suboptimal for patients with head and neck tumors. The free form of chemotherapy drugs, such as docetaxel, has non-specific tissue targeting and poor solubility in blood that deters treatment efficacy. Upon reaching the tumors, these drugs can also be easily washed away by the interstitial fluids. Liposomes have been used as nanocarriers to enhance docetaxel bioavailability. However, they are affected by potential interstitial dislodging due to insufficient intratumoral permeability and retention capabilities. Here, we developed and characterized docetaxel-loaded anionic nanoliposomes coated with a layer of mucoadhesive chitosan (chitosomes) for the application of chemotherapy drug delivery. The anionic liposomes were 99.4 ± 1.5 nm in diameter with a zeta potential of −26 ± 2.0 mV. The chitosan coating increased the liposome size to 120 ± 2.2 nm and the surface charge to 24.8 ± 2.6 mV. Chitosome formation was confirmed via FTIR spectroscopy and mucoadhesive analysis with anionic mucin dispersions. Blank liposomes and chitosomes showed no cytotoxic effect on human laryngeal stromal and cancer cells. Chitosomes were also internalized into the cytoplasm of human laryngeal cancer cells, indicating effective nanocarrier delivery. A higher cytotoxicity (p < 0.05) of docetaxel-loaded chitosomes towards human laryngeal cancer cells was observed compared to human stromal cells and control treatments. No hemolytic effect was observed on human red blood cells after a 3 h exposure, proving the proposed intra-arterial administration. Our in vitro results supported the potential of docetaxel-loaded chitosomes for locoregional chemotherapy delivery to laryngeal cancer cells. Full article
(This article belongs to the Special Issue Application Progress of Liposomes in Drug Development 2.0)
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23 pages, 3682 KiB  
Article
Hispolon Cyclodextrin Complexes and Their Inclusion in Liposomes for Enhanced Delivery in Melanoma Cell Lines
by Ishwor Poudel, Manjusha Annaji, Fajar Setyo Wibowo, Robert D. Arnold, Oladiran Fasina, Brian Via, Vijaya Rangari, Maria Soledad Peresin, Forrest Smith, Muralikrishnan Dhanasekaran, Amit K. Tiwari and R. Jayachandra Babu
Int. J. Mol. Sci. 2022, 23(22), 14487; https://doi.org/10.3390/ijms232214487 - 21 Nov 2022
Cited by 4 | Viewed by 1779
Abstract
Hispolon, a phenolic pigment isolated from the mushroom species Phellinus linteus, has been investigated for anti-inflammatory, antioxidant, and anticancer properties; however, low solubility and poor bioavailability have limited its potential clinical translation. In this study, the inclusion complex of hispolon with Sulfobutylether-β-cyclodextrin [...] Read more.
Hispolon, a phenolic pigment isolated from the mushroom species Phellinus linteus, has been investigated for anti-inflammatory, antioxidant, and anticancer properties; however, low solubility and poor bioavailability have limited its potential clinical translation. In this study, the inclusion complex of hispolon with Sulfobutylether-β-cyclodextrin (SBEβCD) was characterized, and the Hispolon-SBEβCD Complex (HSC) was included within the sterically stabilized liposomes (SL) to further investigate its anticancer activity against melanoma cell lines. The HSC-trapped-Liposome (HSC-SL) formulation was investigated for its sustained drug delivery and enhanced cytotoxicity. The inclusion complex in the solid=state was confirmed by a Job’s plot analysis, molecular modeling, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), Proton nuclear magnetic resonance (NMR) spectroscopy, and scanning electron microscopy (SEM). The HSC-SL showed no appreciable deviation in size (<150 nm) and polydispersity index (<0.2) and improved drug encapsulation efficiency (>90%) as compared to control hispolon liposomes. Individually incorporated hispolon and SBEβCD in the liposomes (H-CD-SL) was not significant in loading the drug in the liposomes, compared to HSC-SL, as a substantial amount of free drug was separated during dialysis. The HSC-SL formulation showed a sustained release compared to hispolon liposomes (H-SLs) and Hispolon-SBEβCD liposomes (H-CD-SLs). The anticancer activity on melanoma cell lines (B16BL6) of HSC and HSC-SL was higher than in H-CD-SL and hispolon solution. These findings suggest that HSC inclusion in the HSC-SL liposomes stands out as a potential formulation approach for enhancing drug loading, encapsulation, and chemotherapeutic efficiency of hispolon and similar water insoluble drug molecules. Full article
(This article belongs to the Special Issue Application Progress of Liposomes in Drug Development 2.0)
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19 pages, 17222 KiB  
Article
Dual-Functionalized Nanoliposomes Achieve a Synergistic Chemo-Phototherapeutic Effect
by Ana Lazaro-Carrillo, Beatriz Rodríguez-Amigo, Margarita Mora, Maria Lluïsa Sagristá, Magdalena Cañete, Santi Nonell and Angeles Villanueva
Int. J. Mol. Sci. 2022, 23(21), 12817; https://doi.org/10.3390/ijms232112817 - 24 Oct 2022
Cited by 1 | Viewed by 1442
Abstract
The enhancement of photodynamic therapy (PDT) effectiveness by combining it with other treatment modalities and improved drug delivery has become an interesting field in cancer research. We have prepared and characterized nanoliposomes containing the chemotherapeutic drug irinotecan (CPT11lip), the photodynamic agent [...] Read more.
The enhancement of photodynamic therapy (PDT) effectiveness by combining it with other treatment modalities and improved drug delivery has become an interesting field in cancer research. We have prepared and characterized nanoliposomes containing the chemotherapeutic drug irinotecan (CPT11lip), the photodynamic agent protoporphyrin IX (PpIXlip), or their combination (CPT11-PpIXlip). The effects of individual and bimodal (chemo-phototherapeutic) treatments on HeLa cells have been studied by a combination of biological and photophysical studies. Bimodal treatments show synergistic cytotoxic effects on HeLa cells at relatively low doses of PpIX/PDT and CPT11. Mechanistic cell inactivation studies revealed mitotic catastrophe, apoptosis, and senescence contributions. The enhanced anticancer activity is due to a sustained generation of reactive oxygen species, which increases the number of double-strand DNA breaks. Bimodal chemo-phototherapeutic liposomes may have a very promising future in oncological therapy, potentially allowing a reduction in the CPT11 concentration required to achieve a therapeutic effect and overcoming resistance to individual cancer treatments. Full article
(This article belongs to the Special Issue Application Progress of Liposomes in Drug Development 2.0)
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17 pages, 3002 KiB  
Article
Cardiolipin for Enhanced Cellular Uptake and Cytotoxicity of Thermosensitive Liposome-Encapsulated Daunorubicin toward Breast Cancer Cell Lines
by Hamad Alrbyawi, Sai H. S. Boddu, Ishwor Poudel, Manjusha Annaji, Nur Mita, Robert D. Arnold, Amit K. Tiwari and R. Jayachandra Babu
Int. J. Mol. Sci. 2022, 23(19), 11763; https://doi.org/10.3390/ijms231911763 - 04 Oct 2022
Cited by 3 | Viewed by 1631
Abstract
Daunorubicin (DNR) and cardiolipin (CL) were co-delivered using thermosensitive liposomes (TSLs). 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), 1-myristoyl-2-stearoyl-sn-glycero-3-phosphocholine (MSPC), cholesterol, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] or DSPE-mPEG (2000) and CL were used in the formulation of liposomes at a molar ratio of 57:40:30:3:20, respectively. CL forms raft-like microdomains that may [...] Read more.
Daunorubicin (DNR) and cardiolipin (CL) were co-delivered using thermosensitive liposomes (TSLs). 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), 1-myristoyl-2-stearoyl-sn-glycero-3-phosphocholine (MSPC), cholesterol, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] or DSPE-mPEG (2000) and CL were used in the formulation of liposomes at a molar ratio of 57:40:30:3:20, respectively. CL forms raft-like microdomains that may relocate and change lipid organization of the outer and inner mitochondrial membranes. Such transbilayer lipid movement eventually leads to membrane permeabilization. TSLs were prepared by thin-film hydration (drug:lipid ratio 1:5) where DNR was encapsulated within the aqueous core of the liposomes and CL acted as a component of the lipid bilayer. The liposomes exhibited high drug encapsulation efficiency (>90%), small size (~115 nm), narrow size distribution (polydispersity index ~0.12), and a rapid release profile under the influence of mild hyperthermia. The liposomes also exhibited ~4-fold higher cytotoxicity against MDA-MB-231 cells compared to DNR or liposomes similar to DaunoXome® (p < 0.001). This study provides a basis for developing a co-delivery system of DNR and CL encapsulated in liposomes for treatment of breast cancer. Full article
(This article belongs to the Special Issue Application Progress of Liposomes in Drug Development 2.0)
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14 pages, 2417 KiB  
Article
Cysteine-Encapsulated Liposome for Investigating Biomolecular Interactions at Lipid Membranes
by Trang Thi Thuy Nguyen, Seungjoo Haam, Joon-Seo Park and Sang-Wha Lee
Int. J. Mol. Sci. 2022, 23(18), 10566; https://doi.org/10.3390/ijms231810566 - 12 Sep 2022
Cited by 2 | Viewed by 1711
Abstract
The development of a strategy to investigate interfacial phenomena at lipid membranes is practically useful because most essential biomolecular interactions occur at cell membranes. In this study, a colorimetric method based on cysteine-encapsulated liposomes was examined using gold nanoparticles as a probe to [...] Read more.
The development of a strategy to investigate interfacial phenomena at lipid membranes is practically useful because most essential biomolecular interactions occur at cell membranes. In this study, a colorimetric method based on cysteine-encapsulated liposomes was examined using gold nanoparticles as a probe to provide a platform to report an enzymatic activity at lipid membranes. The cysteine-encapsulated liposomes were prepared with varying ratios of 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) and cholesterol through the hydration of lipid films and extrusions in the presence of cysteine. The size, composition, and stability of resulting liposomes were analyzed by scanning electron microscopy (SEM), dynamic light scattering (DLS), nuclear magnetic resonance (NMR) spectroscopy, and UV-vis spectrophotometry. The results showed that the increased cholesterol content improved the stability of liposomes, and the liposomes were formulated with 60 mol % cholesterol for the subsequent experiments. Triton X-100 was tested to disrupt the lipid membranes to release the encapsulated cysteine from the liposomes. Cysteine can induce the aggregation of gold nanoparticles accompanying a color change, and the colorimetric response of gold nanoparticles to the released cysteine was investigated in various media. Except in buffer solutions at around pH 5, the cysteine-encapsulated liposomes showed the color change of gold nanoparticles only after being incubated with Triton X-100. Finally, the cysteine-encapsulated liposomal platform was tested to report the enzymatic activity of phospholipase A2 that hydrolyzes phospholipids in the membrane. The hydrolysis of phospholipids triggered the release of cysteine from the liposomes, and the released cysteine was successfully detected by monitoring the distinct red-to-blue color change of gold nanoparticles. The presence of phospholipase A2 was also confirmed by the appearance of a peak around 690 nm in the UV-vis spectra, which is caused by the cysteine-induced aggregation of gold nanoparticles. The results demonstrated that the cysteine-encapsulated liposome has the potential to be used to investigate biological interactions occurring at lipid membranes. Full article
(This article belongs to the Special Issue Application Progress of Liposomes in Drug Development 2.0)
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