Liposomal Bilayer Research Articles

Cholesterol Conjugated Elastin-like Recombinamers: Molecular Dynamics Simulations, Conformational Changes, and Bioactivity.

Current models for elastin-like recombinamer (ELR) design struggle to predict the effects of nonprotein fused materials on polypeptide conformation and temperature-responsive properties. To address this shortage, we investigated the novel functionalization of ELRs with cholesterol (CTA). We employed GROMACS computational molecular dynamic simulations complemented with experimental evidence to validate the in silico predictions. The ELRCTA was biosynthesized and characterized by using fluorescence assays, circular dichroism, dynamic light scattering, and differential scanning calorimetry. The in silico and in vitro data showed that CTA promotes the formation of intramolecular hydrogen bonds that favor β-sheet secondary structures. Compared with an unmodified ELRVKV, CTA enhanced the hydrophobicity and stability of the system, allowing the formation of monodisperse nanoaggregates at physiologically relevant temperatures. Importantly, calorimetry assays revealed that ELRCTA interacted and intercalated with the lipid bilayers of the DPPC liposomes. To demonstrate the implications of these changes for biomedical applications, ELRCTA and DPPC-ELRCTA hybrid nanoparticles were tested with cancer and immune cell lines. Interactions with the cell membranes demonstrated a synergistic effect of the composition and size of the modified recombinamer aggregates on the internalization. The results indicated the potential use of ELR-based nanoparticles for localized and systemic drug delivery. This work sets a new precedent to design elastin-inspired biomaterials with predictable self-assembly properties and develop novel drug delivery strategies.

Evaluating the potential of soy protein isolate /alginate hydrogel as polyphenolic liposome carrier during gastrointestinal tract: A case study on sumac extract

Sumac seed is one of the best sources of polyphenolic compounds and natural antioxidants. This study was conducted to protect the polyphenolic compounds of sumac extract. For this purpose, the chemical composition of sumac extract (SE) was identified using LC-MS technique. Then sumac extract was trapped in liposomal structures and physicochemical properties were evaluated. The results showed that the size and specific surface areas of the liposomes influenced the entrapment efficiency of SE. The zeta potential of liposomes containing SE indicated stability between bioactive substances and liposome bilayers. In the next step, three ratios of soy protein isolate-alginate hydrogel (P1A3, P1A1, and P3A1) were applied to cover the liposome-SE. Furthermore, the flow behavior, surface morphological analysis, texture, and release of phenolic compounds from soy protein isolate-alginate hydrogels containing SE were investigated. Quantitative data showed variations in particle size, sphericity, and loading efficiency according to the SPI to ALG ratio. Fourier-transform infrared spectroscopy confirmed the interactions between the components at a molecular level. This study provided valuable insights into the design and optimization of drug delivery systems and functional food ingredients, highlighting the complexities involved in the controlled release of bioactive substances.

Effect of Cyclodextrins Formulated in Liposomes and Gold and Selenium Nanoparticles on siRNA Stability in Cell Culture Medium

Background: Encapsulation of siRNA fragments inside liposome vesicles has emerged as an effective method for delivering siRNAs in vitro and in vivo. However, the liposome’s fluid-phospholipid bilayer of liposomes allows siRNA fragments to diffuse out of the liposome, decreasing the dose concentration and therefore the effectiveness of the carrier. We have previously reported that β-cyclodextrins formulated in liposomes help increase the stability of siRNAs in cell culture medium. Here, we continued that study to include α, γ, methyl-β-cyclodextrins and β-cyclodextrin-modified gold and selenium nanoparticles. Methods: We used Isothermal Titration Calorimetry to study the binding thermodynamics of siRNAs to the cyclodextrin-modified nanoparticles and to screen for the best adamantane derivative to modify the siRNA fragments, and we used gel electrophoresis to study the stabilization effect of siRNA by cyclodextrins and the nanoparticles. Results: We found that only β- and methyl-β-cyclodextrins increased siRNA serum stability. Cyclodextrin-modified selenium nanoparticles also stabilize siRNA fragments in serum, and siRNAs chemically modified with an adamantane moiety (which forms inclusion complexes with the cyclodextrin-modified-nanoparticles) show a strong stabilization effect. Conclusions: β-cyclodextrins are good additives to stabilize siRNA in cell culture medium, and the thermodynamic data we generated of the interaction between cyclodextrins and adamantane analogs (widely used in drug delivery studies), should serve as a guide for future studies where cyclodextrins are sought for the delivery and solvation of small organic molecules.

Encapsulation of lemongrass essential oil by bilayer liposomes based on pectin, gum Arabic, and carrageenan: Characterization and application in chicken meat preservation

The volatile characteristics of lemongrass essential oil (LO) have seriously hindered its further application, and encapsulation it with multilayer modified liposomes may be an effective strategy to improve this dilemma. This study selected chitosan (CH) and three anionic polymers, pectin (P) / gum arabic (GA) / carrageenan (C), as the first and second coating polymers to modify nano liposomes (NL) by layer-by-layer electrostatic deposition, obtaining three bilayer liposomes, P-CH-NL, GA-CH-NL, and C-CH-NL as high-quality stabilized carriers of LO. The bilayer liposomes showed a dense membrane structure ranging from 110 to 150 nm uniformly, with good antioxidant properties. All bilayer liposomes had good stability during 28-day storage at 4 °C, while C-CH-NL performed relatively better inferred by smaller changes of size, PDI and Zeta potential. The total volatile base nitrogen (TVB-N) values of fresh chicken meat and a total number of bacterial colonies (TBC) experiments showed that GA-CH-NL and C-CH-NL could better retard the increase of volatile salt base nitrogen. All bilayer liposomes could delay the time for the total bacterial count to exceed 6 log CFU/g (from 7 days to 10 / 12 days). Therefore, the bilayer liposomes P-CH-NL, GA-CH-NL, and C-CH-NL may be promising natural preservatives for food products.

Moment analysis method for the determination of permeation kinetics of coumarin at lipid bilayers of liposomes by using capillary electrophoresis.

A method was developed for studying mass transfer kinetics at lipid bilayers of liposomes. Elution peaks of coumarin were measured by liposome electrokinetic chromatography (LEKC). Four types of phospholipids having different alkyl chains were used for preparing liposomes, which were used as pseudo-stationary phases in LEKC systems. Rate constants of permeation across lipid bilayers of liposomes or of adsorption at lipid membranes were determined by analyzing the first absolute and second central moments of the elution peaks measured by LEKC. The rate constants of permeation or adsorption tend to decrease with an increase in the carbon number of the alkyl chains of phospholipids. It was demonstrated that the moment analysis of elution peak profiles measured by LEKC is effective for determining lipid membrane permeability or adsorption kinetics. Compared with other conventional techniques, the method has some advantages for studying mass transfer kinetics at lipid bilayers. Solute permeation across or solute adsorption at real lipid bilayers of liposomes is analyzed. The principle of the method is the analysis of separation behavior in LEKC, which is different from that of the other ones. It is expected that the method contributes to the kinetic study of mass transfer at lipid bilayers from various perspectives.

HI-6-Loaded Vehicle of Liposomes Mediated by an Amphiphilic Pillar[5]arene against Paraoxon Poisoning.

Organophosphate (OP) intoxication has become a severe common health matter all over the world. For the treatment of acute OP poisoning, the effective intracerebral delivery of acetylcholinesterase reactivators is crucial. Here, an amphiphilic hydrazide-pillar[5]arene (HP5A-6C), which could be readily integrated into liposomal bilayers' zwitterionic disaturated phosphatidylcholine (DSPC), was synthesized. A T7 peptide-containing guest (G) was attached on the surface via a noncovalent interaction to make mixed liposomes a particularly appealing candidate for brain-targeting delivery. Such coassembly could remain stable at room temperature for up to 6 weeks, and safety evaluations initially verified its fine biological compatibility. The hydrophilic interiors of T7/HP5A-6C@DSPC could further load HI-6 with 89.70% encapsulation efficiency. Support for brain-targeting potency came from imaging results. Notably, intravenous injection of HI-6-loaded vesicles exhibited a remarkable therapeutic effect on paraoxon (POX)-poisoned mice, effectively alleviating seizures and brain damage and significantly increasing the improving survival rate to 60% over the course of 7 days.

Surfactant-Mediated Assembly of Precision-Size Liposomes.

Liposomes can greatly improve the pharmacokinetics of therapeutic agents due to their ability to encapsulate drugs and accumulate in target tissues. Considerable effort has been focused on methods to synthesize these nanocarriers in the past decades. However, most methods fail to controllably generate lipid vesicles at specific sizes and with low polydispersity, especially via scalable approaches suitable for clinical product manufacturing. Here, we report a surfactant-assisted liposome assembly method enabling the precise production of monodisperse liposomes with diameters ranging from 50 nm to 1 μm. To overcome scalability limitations, we used tangential flow filtration, a scalable size-based separation technique, to readily concentrate and purify the liposomal samples from more than 99.9% of detergent. Further, we propose two modes of liposome self-assembly following detergent dilution to explain the wide range of liposome size control, one in which phase separation into lipid-rich and detergent-rich phases drives the formation of large bilayer liposomes and a second where the rate of detergent monomer partitioning into solution controls bilayer leaflet imbalances that promote fusion into larger vesicles. We demonstrate the utility of controlled size assembly of liposomes by evaluating nanoparticle uptake in macrophages, where we observe a clear linear relationship between vesicle size and total nanoparticle uptake.

Beyond Skin Deep: Phospholipid-Based Nanovesicles as Game-Changers in Transdermal Drug Delivery.

Transdermal administration techniques have gained popularity due to their advantages over oral and parenteral methods. Noninvasive, self-administered delivery devices improve patient compliance and control drug release. Transdermal delivery devices struggle with the skin's barrier function. Molecules over 500 Dalton (Da) and ionized compounds don't permeate through the skin. Drug encapsulation in phospholipid-based vesicular systems is the most effective skin delivery technique. Vesicular carriers include bi-layered liposomes, ultra-deformable liposomes, ethanolic liposomes, transethosomes, and invasomes. These technologies enhance skin drug permeation by increasing formula solubilization, partitioning into the skin, and fluidizing the lipid barrier. Phospholipid-based delivery systems are safe and efficient, making them a promising pharmaceutical and cosmeceutical drug delivery technique. Still, making delivery systems requires knowledge about the physicochemical properties of the drug and carrier, manufacturing and process variables, skin delivery mechanisms, technological advances, constraints, and regulatory requirements. Consequently, this review covers recent research achievements addressing the mentioned concerns.

In Vitro Photoselective Gene Transfection of Hepatocellular Carcinoma Cells with Hypericin Lipopolyplexes.

The lipopolyplex, a multicomponent nonviral gene carrier, generally demonstrates superior colloidal stability, reduced cytotoxicity, and high transfection efficiency. In this study, a new concept, photochemical reaction-induced transfection, using photosensitizer (PS)-loaded lipopolyplexes was applied, which led to enhanced transfection and cytotoxic effects by photoexcitation of the photosensitizer. Hypericin, a hydrophobic photosensitizer, was encapsulated in the lipid bilayer of liposomes. The preformed nanosized hypericin liposomes enclosed the linear polyethylenimine (lPEI)/pDNA polyplexes, resulting in the formation of hypericin lipopolyplexes (Hy-LPP). The diameters of Hy-LPP containing 50 nM hypericin and 0.25 μg of pDNA were 185.6 ± 7.74 nm and 230.2 ± 4.60 nm, respectively, measured by dynamic light scattering (DLS) and atomic force microscopy (AFM). Gel electrophoresis confirmed the encapsulation of hypericin and pDNA in lipopolyplexes. Furthermore, in vitro irradiation of intracellular Hy-LPP at radiant exposures of 200, 600, and 1000 mJ/cm2 was evaluated. It demonstrated 60- to 75-fold higher in vitro luciferase expression than that in nonirradiated cells. The lactate dehydrogenase (LDH) assay supported that reduced transfection was a consequence of photocytotoxicity. The developed photosensitizer-loaded lipopolyplexes improved the transfection efficiency of an exogenous gene or induced photocytotoxicity; however, the frontier lies in the applied photochemical dose. The light-triggered photoexcitation of intracellular hypericin resulted in the generation of reactive oxygen species (ROS), leading to photoselective transfection in HepG2 cells. It was concluded that the two codelivered therapeutics resulted in enhanced transfection and a photodynamic effect by tuning the applied photochemical dose.

Co(II) Macrocyclic Complexes with Amide-Glycinate Pendants as ParaCEST and Liposomal CEST Agents.

Macrocyclic Co(II) complexes with appended amide-glycinate groups were prepared to develop paramagnetic Co(II) chemical exchange saturation transfer (CEST) agents of reduced overall charge. Complexes with reduced charge and lowered osmolarity are important for their loading into liposomes and to provide complexes that are highly water soluble and well tolerated in animals. Co(L1) has two non-coordinating benzyl groups and two amide-glycinate pendants, whereas Co(L2) has two unsubstituted amide pendants and two amide-glycinate pendants on cyclam (1,4,8,11-tetraazacyclododecane). The 1H NMR spectrum of Co(L1) is consistent with a single cis-pendant isomer with both amide protons in the trans-configuration, as supported by an X-ray crystal structure. Co(L2) has a mixture of different isomers in solution, including the trans-1,4 and 1,8 pendant isomers. The Z-spectrum of Co(L1) shows one highly-shifted CEST peak, whereas Co(L2) exhibits six CEST peaks. Encapsulation of 40 mM Co(L1) in a liposome with osmotically-induced shrinking at 300 mOsm/L produces a liposomal CEST agent with saturation frequency offset of 3 ppm. Addition of the amphiphilic 1,4,7-triazacyclononane-based complex Co(L5) to the liposomal bilayer at 18 mM with Co(L1) encapsulated in the liposome at 50 mM changes the sign and increases the magnitude of the saturation frequency offset to -7.5 ppm at 300 mOsm/L.

Molecular Dynamics Simulations Reveal Octanoylated Hyaluronic Acid Enhances Liposome Stability, Stealth and Targeting.

Liposome-based drug delivery systems have been widely used in drug and gene delivery. However, issues such as instability, immune clearance, and poor targeting have significantly limited their clinical utility. Consequently, there is an urgent need for innovative strategies to improve liposome performance. In this study, we explore the interaction mechanisms of hyaluronic acid (HA), a linear anionic polysaccharide composed of repeating disaccharide units of d-glucuronic acid and N-acetyl-d-glucosamine connected by alternating β-1,3 and β-1,4 glycosidic linkages, and its octanoylated derivates (OHA) with liposomes using extensive coarse-grained molecular dynamics simulations. The octyl moieties of OHA spontaneously inserted into the phospholipid bilayer of liposomes, leading to their effective coating onto the surface of liposome and enhancing their structural stability. Furthermore, encapsulating liposome with OHA neutralized their surface potential, interfering with the formation of a protein corona known to contribute to liposomal immune clearance. Importantly, the encapsulated OHA maintained its selectivity and therefore targeting ability for CD44, which is often overexpressed in tumor cells. These molecular-scale findings shed light on the interaction mechanisms between HA and liposomes and will be useful for the development of next-generation liposome-based drug delivery systems.

Liposome-embedded PtCu nanozymes for improved immunoassay of accurate myocardial infarction

Herein, we developed a platinum-copper nano-enzyme-linked immunosorbent assay (NLISA) based split diagnostic platform for the ultrasensitive detection of cardiac troponin I (cTnI). The PtCu nanozyme synthesized by one-pot synthesis exhibited ultra-high peroxidase-like activity (35.17 U mg−1), which was about 4.5 times higher than that of the unmodified Pt nanozyme (8.83 U mg−1). Due to the efficient peroxidase-like activity of the copper-platinum complexed nanozyme, transduction and sequential amplification of cTnI biological signals were achieved in combination with a liposome-embedded amplification strategy. The encapsulation efficiency was calculated by introducing a liposomal bilayer model, which showed that the introduction of a single liposomal molecule could amplify the signal up to 870-fold, thus promising a high sensitivity test. Notably, the dynamic response of cTnI was in the range of 0.1–5000 pg mL−1 with an ultra-low detection limit (0.048 pg mL−1). The developed NLISA analysis system provides a new way to discover efficient and sensitive alternatives to ELISA kits, which can meet the practical needs of community healthcare testing conditions and rapid testing in hospitals.

Fabrication and characterization of hydroquinone in liposomal gel for transdermal drug delivery

This study aimed to formulate a gel for hydroquinone dermal therapy using liposomes to maintain the active agents' concentration in the skin's deepest layers. Cholesterol was incorporated to enhance the liposome's bilayer characteristics, increasing microviscosity, membrane stability, and blister rigidity. Various methods for liposome preparation exist, but the film hydration method, being the most common, was utilized here. Results for formulation HL6, which had lower levels of Lecithin Cholesterol and rotation speed, revealed a vesicle size of 180.4 nm, a Zeta potential of -37.5 mV, and an entrapment efficiency of 69.10±1.52%. In-vitro drug release data for formulations F1, F2, and F3 within 30 minutes showed hydroquinone release rates of 97.75±0.28%, 98.92±0.56%, and 94.45±0.36%, respectively. The order of drug release was F2 > F1 > F3, with F2 demonstrating the maximum release rate. The study concludes that liposomal gel is an effective transdermal drug delivery system for therapeutic molecules. Lipid vesicles, such as liposomes, are among the best mechanisms for delivering medications to their intended locations while minimizing their dissemination to non-target tissues. This liposomal gel-based formulation shows significant potential for effectively treating acne by maintaining high concentrations of active agents in the skin's deepest layers and ensuring a controlled and sustained drug release.

Unravelling the interactions between small molecules and liposomal bilayers via molecular dynamics and thermodynamic modelling

Lipid-based drug delivery systems hold immense promise in addressing critical medical needs, from cancer and neurodegenerative diseases to infectious diseases. By encapsulating active pharmaceutical ingredients – ranging from small molecule drugs to proteins and nucleic acids – these nanocarriers enhance treatment efficacy and safety. However, their commercial success faces hurdles, such as the lack of a systematic design approach and the issues related to scalability and reproducibility.This work aims to provide insights into the drug-phospholipid interaction by combining molecular dynamic simulations and thermodynamic modelling techniques. In particular, we have made a connection between the structural properties of the drug-phospholipid system and the physicochemical performance of the drug-loaded liposomal nanoformulations. We have considered two prototypical drugs, felodipine (FEL) and naproxen (NPX), and one model hydrogenated soy phosphatidylcholine (HSPC) bilayer membrane. Molecular dynamic simulations revealed which regions within the phospholipid bilayers are most and least favoured by the drug molecules. NPX tends to reside at the water-phospholipid interface and is characterized by a lower free energy barrier for bilayer membrane permeation. Meanwhile, FEL prefers to sit within the hydrophobic tails of the phospholipids and is characterized by a higher free energy barrier for membrane permeation. Flory-Huggins thermodynamic modelling, small angle X-ray scattering, dynamic light scattering, TEM, and drug release studies of these liposomal nanoformulations confirmed this drug-phospholipid structural difference. The naproxen-phospholipid system has a lower free energy barrier for permeation, higher drug miscibility with the bilayer, larger liposomal nanoparticle size, and faster drug release in the aqueous medium than felodipine. We suggest that this combination of molecular dynamics and thermodynamics approach may offer a new tool for designing and developing lipid-based nanocarriers for unmet medical applications.

Fine-tuning of membrane permeability by reversible photoisomerization of aryl-azo derivatives of thymol embedded in lipid nanoparticles

Responsiveness of liposomes to external stimuli, such as light, should allow a precise spatial and temporal control of release of therapeutic agents or ion transmembrane transport. Here, some aryl-azo derivatives of thymol are synthesized and embedded into liposomes from 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine to obtain light-sensitive membranes whose photo-responsiveness, release behaviour, and permeability towards Cl- ions are investigated. The hybrid systems are in-depth characterized by dynamic light scattering, atomic force microscopy and Raman spectroscopy. In liposomal bilayer the selected guests undergo reversible photoinduced isomerization upon irradiation with UV and visible light, alternately. Non-irradiated hybrid liposomes retain entrapped 5(6)-carboxyfluorescein (CF), slowing its spontaneous leakage, whereas UV-irradiation promotes CF release, due to guest trans-to-cis isomerization. Photoisomerization also influences membrane permeability towards Cl- ions. Data processing, according to first-order kinetics, demonstrates that Cl- transmembrane transport is enhanced by switching the guest from trans to cis but restored by back-switching the guest from cis to trans upon illumination with blue light. Finally, the passage of Cl- ions across the bilayer can be fine-tuned by irradiation with light of longer λ and different light-exposure times. Fine-tuning the photo-induced structural response of the liposomal membrane upon isomerization is a promising step towards effective photo-dynamic therapy.

Liposome‐Based Delivery of a Bis‐benzimidazole Derivative to Duplex DNA: A Spectroscopic Study

AbstractDue to the immense pharmacological significance, the interaction of small molecules with liposome and the exact knowledge of their binding location and distribution within the lipid bilayer of liposome is an active field of biophysical research. Here, we have studied the binding interaction of H33258 with DPPC liposome, a model biological membrane. From the steady‐state fluorescence spectroscopy it was revealed that H33258 bounded to DPPC liposome and the estimated binding constant value was 2.5×102 M−1. It was also revealed that the H33258 essentially partitioned within the lipid bilayer of DPPC liposome. Moreover, from steady‐state fluorescence, time‐resolved lifetime, time‐resolved anisotropy and ITC studies it was established that the probe molecules were sequestrated from the lipid bilayer and bounded to a duplex DNA structure. Our results on the binding consequences of H33258 with liposome will aid development of a simple and safe strategy to deliver drugs to the target sites using liposome, endogenously.

Tracking Drugs and Lipids: Quantitative Mass Spectrometry Imaging of Liposomal Doxorubicin Delivery and Bilayer Fate in Three-Dimensional Tumor Models.

Targeted therapy to the tumor would greatly advance precision medicine. Many drug delivery vehicles have emerged, but liposomes are cited as the most successful to date. Recent efforts to develop liposomal drug delivery systems focus on drug distribution in tissues and ignore liposomal fate. In this study, we developed a novel method to elucidate both drug and liposomal bilayer distribution in a three-dimensional cell culture model using quantitative matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI qMSI) alongside fluorescence microscopy. Imaging liposomal distribution in a cell culture model is challenging, as lipids forming the bilayer are endogenous to the model system. To resolve this issue, we functionalized the bilayer by chemically cross-linking a fluorescent tag to the alkyne-containing lipid hexynoyl phosphoethanolamine (HPE). We synthesized liposomes incorporating the tagged HPE lipid and encapsulated within them doxorubicin, yielding a theranostic liposome capable of both drug delivery and monitoring liposomal uptake. We employed an "in-tissue" MALDI qMSI approach to generate a calibration curve with R2 = 0.9687, allowing for quantification of doxorubicin within spheroid sections at multiple time points. After 72 h of treatment with the theranostic liposomes, full doxorubicin penetration was observed. The metabolites doxorubicinone and 7-deoxydoxorubicinone were also detected after 48 h. Modification of the bilayer allowed for fluorescence microscopy tracking of liposomes, while MALDI MSI simultaneously permitted the imaging of drugs and metabolites. While we demonstrated the utility of our method with doxorubicin, this system could be applied to examine the uptake, release, and metabolism of many other liposome-encapsulated drugs.

Development of Liposomes Loaded with Chloroaluminum Phthalocyanine for Application of Photodynamic Therapy in Breast Cancer

Chloraluminium phthalocyanine (ClAlPc) has potential therapeutic effect for the treatment of cancer; however, the molecule is lipophilic and may present self-aggregation which limits its clinical success. Thus, nanocarriers like liposomes can improve ClAlPc solubility, reduce off-site toxicity and increase circulation time. For this purpose, developing suitable liposomes requires the evaluation of different lipid compositions. Herein, we aimed to develop liposomes containing soy phosphatidylcholine (SPC), 1,2-distearoyl-sn-glycero- 3-phosphoethanolamine-N-[amino(polyethylene glycol)-2000] (DSPEPEG2000), cholesterol and oleic acid loaded with ClAlPc using the surface response methodology and the Box-Behnken design. Liposomes with particle size from 110.93 to 374.97 nm and PdI from 0.265 to 0.468 were obtained. The optimized formulation resulted in 69.09 % of ClAlPc encapsulated, with particle size and polydispersity index, respectively, at 153.20 nm and 0.309, providing stability and aggregation control. Atomic force microscopy revealed vesicles in a spherical or almost spherical shape, while the analyzes by Differential Scanning Calorimetry (DSC), Powder X-ray Diffraction (PXRD), and Fourier transform infrared spectroscopy (FTIR) suggested that the drug was adequately incorporated into the lipid bilayer of liposomes, in its amorphous state or molecularly dispersed. In vitro studies conducted in breast cancer cells (4T1) showed that liposome improved phototoxicity compared to the ClAlPc solution. ClAlPc-loaded liposomes also enhanced the production of ROS 3-fold compared to the ClAlPc solution. Finally, confocal microscopy and flow cytometry demonstrated the ability of the liposomes to enter cells and deliver the fluorescent ClAlPc photosensitizer with dose and time-dependent effects. Thus, this work showed that Box-Behnken factorial design was an effective strategy for optimizing formulation development. The obtained ClAlPc liposomes can be applied for photodynamic therapy in breast cancer cells.

Manufacturing process of liposomal Formation: A coarse-grained molecular dynamics simulation

A method of producing liposomes has been previously developed using a continuous manufacturing technology that involves a co-axial turbulent jet in co-flow. In this study, coarse-grained molecular dynamics (CG-MD) simulations were used to gain a deeper understanding of how the self-assembly process of liposomes is affected by the material attributes (such as the concentration of ethanol) and the process parameters (such as temperature), while also providing detailed information on a nano-scale molecular level. Specifically, the CG-MD simulations yield a comprehensive internal view of the structure and formation mechanisms of liposomes containing DPPC, DPPG, and cholesterol molecules. The importance of this work is that structural details on the molecular level are proposed, and such detail is not possible to obtain through experimental studies alone. The assessment of structural properties, including the area per lipid, diffusion coefficient, and order parameters, indicated that a thicker bilayer was observed at higher ethanol concentrations, while a thinner bilayer was present at higher temperatures. These conditions led to more water penetrating the interior of the bilayer and an unstable structure, as indicated by a larger contact area between lipids and water, and a higher coefficient of lipid lateral diffusion. However, stable liposomes were found through these evaluations at lower ethanol concentrations and/or lower process temperatures. Furthermore, the CG-MD model was further compared and validated with experimental and computational data including liposomal bilayer thickness and area per lipid measurements.

Liposomal drug delivery for glaucoma: Recent advancement in ocular therapy

Glaucoma affects millions worldwide. Untreated, it might cause lifelong blindness. Traditional treatments have been limited and intrusive. Liposomes are changing glaucoma treatment. Phospholipid bilayer liposomes can carry medications for targeted administration. This innovative glaucoma medication has huge potential to transform the way we treat it. This essay will explain liposomes, how they function, and why they are a glaucoma therapy game-changer. Eyes have several sensory compartments. Eyes send brain impulses. Eye-aqueous humour production causes glaucoma. It mostly affects the over-50s. Glaucoma destroys retinal ganglion cells and the optic nerve, causing blindness. CO2 inhibitors treat it. This inhibitor keeps aqueous humour from the ocular fluid. Normal eye medication dosage. This ocular drug administration approach relies on nasolacrimal drainage and tears turnover to provide the usual dose form. Low bioavailability. Novel pharmaceutical delivery dose formulations can fix this. Nano co-adhesive compositions prolong ocular drug delivery. Liposomes cure glaucoma uniquely. Bioavailability lowers toxicity and dosage. Novel Drug Delivery System helps glaucoma patients worldwide. Liposomes drop IOP slowly. Aqueous liposomes have natural and synthetic phospholipid bilayers. Liposomes contain hydrophilic medicines. Liposomes resemble cells. Their properties make them cling to cells. Biocompatible liposomes increase drug solubility, stability, absorption, and toxicity. Conjunctiva and cornea interactions with liposomes impact tear dynamics and medication duration and frequency. Novel eye medication delivery methods are being investigated. This medicine administration at the proper place challenges drug delivery systems. Here are innovative ocular drug-delivery methods. Biocompatible liposomes improve drug solubility, stability, absorption, and toxicity. Liposomes affect tear dynamics and medication duration and frequency via interacting with the conjunctiva and cornea. Novel ocular medicine delivery techniques for various eye ailments are being explored. This medication administration at the right place challenges drug delivery systems. Innovative ocular drug-delivery systems will be reviewed here.