Liposomal Encapsulation Research Articles

Encapsulation of Lidocaine nanoparticles in Gadus morhua derived lipoic acid

Local Anesthetics are used clinically for anesthesia and analgesia either following surgery or for management of acute and chronic pain conditions. Liposomal Encapsulation aids in improved delivery at the tissue level. This paper deals with formulation and characterization of Gadus morhua derived liposome encapsulated Lidocaine nanoparticles. Materials and methodsWater Soluble liposomes were synthesized and encapsulated to lidocaine. The prepared liposomes were assessed using field emission scanning electron microscope, TEM, FTIR, Zetapotential, Anti-inflammatory property and Drug release kinetics. ResultsThe structural and morphological characters of the conjugated liposomes were studied using SEM & TEM, surface charge Zetapotential. The cumulative drug release was studied for up to 72 h in which more than 70 % of the drug was released from the Liposomal nanoparticles. FTIR revealed similar functional groups like the control. Stability of the drug was superior than the control. ConclusionLiposomal conjugation delays the drug release which can be used in slow release applications. Improving the drug release kinetics can be advantageous in many chronic pain conditions. Additionally, the changes in the functional groups can also aid in reduction or masking of bitterness.

In vivo confocal Raman spectroscopy investigation of glabridin liposomes dermal penetration process in human skin

Encapsulating glabridin with liposome technology can contribute to the bioavailability and application in cosmetic formulations. At the same time, the small particle size of liposomes makes it feasible to penetrate the stratum corneum and enhance the dermal delivery of glabridin. Confocal Raman spectroscopy (CRS) can be employed to monitor the dermal penetration of cosmetic actives for topical applications. The method of CRS allows qualitatively and semi-quantitatively in vivo analysis of cosmetic actives based on the position and intensity of peaks in the Raman spectrum. In this work, CRS was used to evaluate epidermal penetration of glabridin and glabridin-containing liposome components. First, glabridin liposomes (GL), glabridin liposome essence (GLE), and glabridin essence (GE) were evenly applied on the forearms of six randomly-selected volunteers. Then, in vivo dermal penetration and of delivery mechanism of glabridin was clinically assessed at 0.5 h and 2 h with the non-invasive devices, confocal Raman spectrometer. The findings indicated that the glabridin transported by liposomes could penetrate the stratum corneum and reach deep layers of human skin, while the content of penetrated glabridin increased with time. Compared to the penetration of GLE and GE through the skin, it was found that the dermal penetration of liposome-encapsulated glabridin in the essence dosage form was 3.8 times higher than that of unencapsulated glabridin. From qualitative and semi-quantitative perspectives, it was demonstrated that glabridin liposomes have good skin permeability and a gradual release effect and the liposome encapsulation can efficiently enhance the poor dermal absorption and bioavailability of glabridin. We believe this in vivo confocal Raman spectroscopy research is benefit for revealing the permeability of glabridin and liposome formulations in cosmetics.

Impact of different chemotherapy regimens on intestinal mucosal injury assessed with bedside ultrasound: a study in 213 AML patients.

Neutropenic enterocolitis (NEC) is a life-threatening complication reported in patients with acute myeloid leukemia (AML) following chemotherapy (CHT). Intensive induction and consolidation CHT may damage intestinal mucosa leading to a NEC episode (NECe). NEC reported mortality may be up to 30-60%. Early US-guided bed-side diagnosis and prompt treatment may substantially improve the survival. An emerging worldwide concern is the intestinal colonization by multi-drug-resistant bacteria especially when patients are exposed to chemotherapy regimens potentially correlated to mucosal damage. In our study we prospectively enrolled all AML patients admitted in our leukemia unit to receive intensive induction and consolidation chemotherapy and experiencing chemotherapy-induced-neutropenia (CHTN). Overall, we enrolled N=213 patients from 2007 to March 2023. We recorded N=465 CHTN, and N=42 NECe (9.0% incidence). The aim of our study was to assess which chemotherapy regimens are more associated with NEC. We found that ALM1310, followed by 7 + 3 (daunorubicin), 7 + 3 (idarubicin), 5 + 3 + 3 (cytarabine, etoposide, idarubicin), and AML1310 (consolidation) were associated with a statistically higher incidence of NEC. We did not detect NEC episodes in patients treated with CPX-351, 5 + 2 (cytarabine, idarubicine), and high-dose cytarabine. Thus, we found that cytarabine could determine mucosal damage when associated with an anthracycline but not if delivered either alone or as dual-drug liposomal encapsulation of daunorubicin/cytarabine. We also describe NEC mortality, symptoms at diagnosis, intestinal sites involvement, and prognostic significance of bowel wall thickening.

Effect of liposomal encapsulation of curcumin and α-tocopherol on sensory and physicochemical properties, and retention of antioxidant capacity of fortified cookies during baking

Curcumin and α-tocopherol, which are potent antioxidants usable for food fortification, are sensitive to heat and air, thus showing the need for protection. The aim of this study was to increase the antioxidant capacity retention of curcumin and α-tocopherol in fortified cookies via liposomal encapsulation. Liposomes were prepared using the homogenization method and the liposomes were multilamellar according to light microscopic images. Liposomal encapsulation exhibited encapsulation efficiencies greater than 90 %. The sensory tests, conducted using a 5-point hedonic scale for nine attributes, revealed that the incorporation of liposomal antioxidants did not compromise the sensory attributes of the cookies. The color of liposomal-curcumin incorporated cookie deviated greater than that of free-curcumin incorporated cookie from the regular cookie. Nevertheless, the color of the α-tocopherol incorporated cookies improved on using the liposomal compound as opposed to the free compound. The antioxidant capacity of the cookies, along with the controls, was measured using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) assays. As expected, liposomal encapsulation of curcumin or α-tocopherol mitigated the reduction of antioxidant capacity of fortified cookies during baking. Briefly, liposomal encapsulation proves to be a potent method for retaining the antioxidant capacity of curcumin or α-tocopherol in cookies during baking.

Liposome-Mediated Delivery Improves the Efficacy of Lisosan G against Retinopathy in Diabetic Mice.

Nutraceuticals are natural substances whose anti-oxidant and anti-inflammatory properties may be used to treat retinal pathologies. Their efficacy is limited by poor bioavailability, which could be improved using nanocarriers. Lisosan G (LG), a fermented powder from whole grains, protects the retina from diabetic retinopathy (DR)-induced damage. For this study, we tested whether the encapsulation of LG in liposomes (LipoLG) may increase its protective effects. Diabetes was induced in mice via streptozotocin administration, and the mice were allowed to freely drink water or a water dispersion of two different doses of LG or of LipoLG. Electroretinographic recordings after 6 weeks showed that only the highest dose of LG could partially protect the retina from diabetes-induced functional deficits, while both doses of LipoLG were effective. An evaluation of molecular markers of oxidative stress, inflammation, apoptosis, vascular endothelial growth factor, and the blood-retinal barrier confirmed that the highest dose of LG only partially protected the retina from DR-induced changes, while virtually complete prevention was obtained with either dose of LipoLG. These data indicate that the efficacy of LG in contrasting DR is greatly enhanced by its encapsulation in liposomes and may lay the ground for new dietary supplements with improved therapeutic effects against DR.

Surface-Modified Silver Nanoparticles and Their Encapsulation in Liposomes Can Treat MCF-7 Breast Cancer Cells.

Silver nanoparticles (AgNPs) have emerged as a promising tool for cancer treatment due to their unique physicochemical and biological properties. However, their clinical applications are limited by their potential cytotoxicity caused due to oxidation stress and non-specific cellular uptake pathways. To overcome these barriers, surface modifications of AgNPs have been proposed as an effective strategy to enhance their biocompatibility and specificity toward cancer cells. In this study, AgNPs were synthesised using the chemical reduction method and subsequently conjugated with various capping agents such as Polyvinylpyrrolidone (PVP) and Bovine Serum Albumin (BSA). Further, this study involves the synthesis of liposomes by using dipalmitoyl phosphatidylcholine lipid (DPPC) and cholesterol to increase the biocompatibility and bioavailability of AgNPs to MCF-7 breast cancer cells. In vitro, cytotoxicity studies were performed to determine which surface modification method exhibited the highest cytotoxic effect on the MCF-7 breast cancer cells, which was determined through the MTT assay. The AgNPs conjugated with BSA exhibited the highest cytotoxicity at the lowest dosage, with an IC50 of 2.5 μL/mL. The BSA-AgNPs induced a dose-dependent rise in cytotoxicity through the enhancement of nucleophilic dissolution of the AgNPs in cancer cells. In comparison, the unmodified AgNPs had an IC50 value of 3.0 μL/mL, while the PVP-modified AgNPs had an IC50 of 4.24 μL/mL. AgNPs encapsulated in liposomes had an IC50 value of 5.08 μL/mL, which shows that the encapsulation of AgNPs in liposomes controls their entry into cancer cells. The findings of this research have provided insights into the potential use of surface-modified AgNPs and liposomal encapsulated AgNPs as novel therapeutic tools to overcome the conventional treatment limitations of breast cancer cells.

P-Coumaric acid-loaded nanoliposomes: Optimization, characterization, antimicrobial properties and preservation effects on fresh pod pepper fruit

Novel p-coumaric acid (pCA)-loaded nanoliposomes were prepared by the thin-film hydration method, assisted with ultrasonic treatment, and optimized by the response surface methodology. The characterization showed that the fabricated pCA-loaded liposomes were nanosized spherical vesicles (83.55 ± 0.34 nm), exhibiting favorable dispersibility and encapsulation efficiency (55.70 ± 0.10 %). Fourier transform infrared spectroscopy analysis indicated that pCA was encapsulated into phospholipid bilayer through hydrophobic interaction and hydrogen bonding. Tests of temperature stability and centrifugal stability suggested that pCA-loaded nanoliposomes were less sensitive to aggregation and fusion during storage. Incubation experiments revealed that pCA-loaded nanoliposomes had a good inhibitory effect on the expansion of disease area on fresh pod pepper fruit caused by Botrytis cinerea. Additionally, pCA-loaded nanoliposomes effectively extended shelf life of fresh pod peppers by reducing weight loss and naturally-infected decays. The findings presented a viable strategy for designing liposomal encapsulation technology to efficiently enhance antimicrobial activity of pCA in food preservation.

Increased antibiofilm and growth inhibitory effect of Imipenem/Cilastatin nanoliposomes against clinical Pseudomonas aeruginosa isolates

Numerous infections are linked to Pseudomonas aeruginosa. It is one of the major medical concerns because of virulence and antibiotic resistance. Antibiotic encapsulation in liposomes is a good strategy for controlling infections caused by this microorganism. Evaluation of anti-Pseudomonas aeruginosa effect of liposomal form of Imipenem/Cilastatin in vitro condition. By using the disk agar diffusion technique, the isolates’ pattern of antibiotic resistance was identified. The antibiotic was placed into the nanoliposome after it had been made using the thin layer and ethanol injection techniques. SEM and DLS were used to determine the size, shape, and zeta potential of the encapsulated drug form and the empty nanoliposome. Additionally, Imipenem/Cilastatin encapsulation in nanoliposomes was studied using FT-IR spectroscopy. In the microbial assay experiments the MIC, MBC and MBEC of liposomal and free drug forms were determined. The nanoparticles were spherical, with a diameter ranging from 30 to 39 nm, and the EE% in the thin layer and ethanol injection procedures were 97 and 98, respectively. Imipenem/Cilastatin nanoliposomes showed peaks at 3009 cm−1 and 1650 cm−1, demonstrating the thermodynamic stability for the chemical structure of the drug enclosed and validating the encapsulation of antibiotic in the nanoliposomes. When compared to free drug forms, nanoliposomes had lower MIC and MBC values in the majority of the isolates and had a greater ability to eradicate the biofilm formation. It was shown that the two nanoliposome preparation techniques were more efficient in 80% of the isolates, which had outcomes that were consistent with those of numerous other investigations. Overall, we demonstrated that the antibacterial activity of nanoliposomes was higher than that of the free drug form based on the evaluation of their MIC and MBC. Pharmaceutical nanoliposome techniques provide an excellent future perspective on how to manage microbial infections that are resistant to antibiotics.Graphical

Disulfide bridge-targeted metabolome mining unravels an antiparkinsonian peptide

Peptides are a particular molecule class with inherent attributes of some small-molecule drugs and macromolecular biologics, thereby inspiring continuous searches for peptides with therapeutic and/or agrochemical potentials. However, the success rate is decreasing, presumably because many interesting but less-abundant peptides are so scarce or labile that they are likely ‘overlooked’ during the characterization effort. Here, we present the biochemical characterization and druggability improvement of an unprecedented minor fungal RiPP (ribosomally synthesized and post-translationally modified peptide), named acalitide, by taking the relevant advantages of metabolomics approach and disulfide-bridged substructure which is more frequently imprinted in the marketed peptide drug molecules. Acalitide is biosynthetically unique in the macrotricyclization via two disulfide bridges and a protease (AcaB)-catalyzed lactamization of AcaA, an unprecedented precursor peptide. Such a biosynthetic logic was successfully re-edited for its sample supply renewal to facilitate the identification of the in vitro and in vivo antiparkinsonian efficacy of acalitide which was further confirmed safe and rendered brain-targetable by the liposome encapsulation strategy. Taken together, the work updates the mining strategy and biosynthetic complexity of RiPPs to unravel an antiparkinsonian drug candidate valuable for combating Parkinson's disease that is globally prevailing in an alarming manner.

Encapsulation Of β-Carotene And Curcumin In Liposome From Soybean Lecithin And L-α-Phosphatidylcholine Using SC-CO2 With The Assistance Of Ultrasonication

The newest method to maintain better bioavailability of antioxidant compounds in the human digestive process is encapsulation using liposomes. The liposomes used were lecithin from soybean seeds and L-α-Phosphatidylcholine. Furthermore, curcumin and β-carotene were encapsulated in soy lecithin liposomes using SC-CO2 with 100% ethanol, aquadest 50% v/v ethanol and 100% aquadest at 50°C, 60°C, and 70°C and pressure 15 MPa, 20 MPa and 25 MPa by ultrasonication for 60 minutes. This research was conducted to obtain liposomes from curcumin and β-carotene encapsulation, analyse the effect of lecithin from soybean seeds on the formation of encapsulation in liposomes, analyse the effect of operating conditions on the encapsulation process on the size of curcumin and β-carotene in liposomes and determine the size characteristics of liposomes. This was analysed using a UV-Vis Spectrophotometer and Particle Size Analyzer (PSA) with the Dynamic Light Scattering method and also using the Scanning Electron Microscope (SEM) method. The results of the PSA test showed that the increase in operating temperature and pressure resulted in an increase in liposome particle size. UV-Vis analysis proved that the content of curcumin and β-carotene in liposomes from L-α-Phosphatidylcholine had better results. It was found that using SC-CO2+Sonicator had higher concentrations of curcumin and β-carotene with the condition that the higher the temperature, the higher the curcumin content. The use of liposomes has increased the stability of encapsulated suspensions and prevented flocculation. SEM analysis proved that the encapsulation of curcumin with L-α-Phosphatidylcholine has the smallest particle size distribution of 2 micro meters so that it can be categorized as multilamellar vesicles (MLV).

Modified Curcuminoid-Rich Extract Liposomal CRE-SDInhibits Osteoclastogenesis via the Canonical NF-κB Signaling Pathway.

Curcuminoids, namely curcumin, demethoxycurcumin, and bisdemethoxycurcumin, are the major active compounds found in Curcuma longa L. (turmeric). Although their suppressive effects on bone resorption have been demonstrated, their pharmacokinetic disadvantages remain a concern. Herein, we utilized solid dispersion of a curcuminoid-rich extract (CRE), comprising such curcuminoids, to prepare CRE-SD; subsequently, we performed liposome encapsulation of the CRE-SD to yield liposomal CRE-SD. In vitro release assessment revealed that a lower cumulative mass percentage of CRE-SD was released from liposomal CRE-SD than from CRE-SD samples. After culture of murine RANKL-stimulated RAW 264.7 macrophages, our in vitro examinations confirmed that liposomal CRE-SD may impede osteoclastogenesis by suppressing p65 and IκBα phosphorylation, together with nuclear translocation and transcriptional activity of phosphorylated p65. Blind docking simulations showed the high binding affinity between curcuminoids and the IκBα/p50/p65 protein complex, along with many intermolecular interactions, which corroborated our in vitro findings. Therefore, liposomal CRE-SD can inhibit osteoclastogenesis via the canonical NF-κB signaling pathway, suggesting its pharmacological potential for treating bone diseases with excessive osteoclastogenesis.

Pegylated Liposomal Alendronate Biodistribution, Immune Modulation, and Tumor Growth Inhibition in a Murine Melanoma Model.

While tumor-associated macrophages (TAM) have pro-tumoral activity, the ablation of macrophages in cancer may be undesirable since they also have anti-tumoral functions, including T cell priming and activation against tumor antigens. Alendronate is a potent amino-bisphosphonate that modulates the function of macrophages in vitro, with potential as an immunotherapy if its low systemic bioavailability can be addressed. We repurposed alendronate in a non-leaky and long-circulating liposomal carrier similar to that of the clinically approved pegylated liposomal doxorubicin to facilitate rapid clinical translation. Here, we tested liposomal alendronate (PLA) as an immunotherapeutic agent for cancer in comparison with a standard of care immunotherapy, a PD-1 immune checkpoint inhibitor. We showed that the PLA induced bone marrow-derived murine non-activated macrophages and M2-macrophages to polarize towards an M1-functionality, as evidenced by gene expression, cytokine secretion, and lipidomic profiles. Free alendronate had negligible effects, indicating that liposome encapsulation is necessary for the modulation of macrophage activity. In vivo, the PLA showed significant accumulation in tumor and tumor-draining lymph nodes, sites of tumor immunosuppression that are targets of immunotherapy. The PLA remodeled the tumor microenvironment towards a less immunosuppressive milieu, as indicated by a decrease in TAM and helper T cells, and inhibited the growth of established tumors in the B16-OVA melanoma model. The improved bioavailability and the beneficial effects of PLA on macrophages suggest its potential application as immunotherapy that could synergize with T-cell-targeted therapies and chemotherapies to induce immunogenic cell death. PLA warrants further clinical development, and these clinical trials should incorporate tumor and blood biomarkers or immunophenotyping studies to verify the anti-immunosuppressive effect of PLA in humans.

A review of the role of liposome-encapsulated phytochemicals targeting PPAR Ɣ and associated pathways to combat obesity.

A limited number of studies have directly examined the effects of liposomal encapsulated phytochemicals and their anti-obesity effects in adults. This study aimed to summarize the evidence on the effect of liposomal encapsulated phytochemicals and their role in regulating major pathways involved in the anti-obesity mechanism. A systematic search was performed using several search engines like Science Direct, Google Scholar, and other online journals, focusing on laboratory research, systematic reviews, clinical trials, and meta-analysis that focused on liposomal encapsulated phytochemicals with anti-obesity properties, and followed the preferred reporting terms for this systematic review. An initial search provided a result of 1810 articles, and 93 papers were selected after the inclusion and exclusion criteria. Very few studies have been conducted on the liposomal encapsulation of phytochemicals or its synergistic study to combat obesity; hence this review paves the way for future obesity research and is mainly helpful for the pediatric obesity population. Liposomal encapsulation of phytochemicals has improved the efficiency of freely administered phytochemicals. Targeted delivery improved drug utilization and regulated the anti-obesity pathways. PPARƔ is a major therapeutic target for obesity as it inhibits adipocyte differentiation and maintains energy homeostasis.

Development and Characterization of Inula britannica Extract-Loaded Liposomes: Potential as Anti-Inflammatory Functional Food Ingredients.

We investigated the potential of Inula britannica extract encapsulated in liposomes as a functional food ingredient with enhanced bioavailability and stability. Inula britannica, known for its anti-inflammatory properties and various health benefits, was encapsulated using a liposome mass production manufacturing method, and the physical properties of liposomes were evaluated. The liposomes exhibited improved anti-inflammatory effects in lipopolysaccharide-activated RAW 264.7 macrophages, suppressing the production of pro-inflammatory mediators such as nitric oxide and prostaglandin E2 and downregulating the expression of iNOS and COX-2 transcription factors. Additionally, we observed reduced production of pro-inflammatory cytokines TNF-α, IL-6, and IL-1β, and modulation of the NF-κB and mitogen-activated protein kinase signaling pathways. These findings suggest that Inula britannica extract encapsulated in liposomes could serve as a valuable functional food ingredient for managing and preventing inflammation-related disorders, making it a promising candidate for incorporation into various functional food products. The enhanced absorption and stability provided by liposomal encapsulation can enable better utilization of the extract's beneficial properties, promoting overall health and well-being.

Preparation of liposomes co-encapsulating doxorubicin and mifepristone for treating multidrug-resistant cancer

The emergence of multidrug resistance (MDR) is well-known to decrease the therapeutic effects of anticancer drugs. To increase anticancer drug efficacy and decrease adverse effects, we prepared liposomes co-encapsulating doxorubicin (DXR) and mifepristone (MIF) (DXR/MIF-LPs) for treating MDR cancer and evaluated the MDR reversal effect in DXR-resistant Colon-26 cancer cells (C26/DXR). Liposomal encapsulation was performed using remote loading methods: amphipathic DXR was encapsulated using the ammonium sulfate gradient method, whereas hydrophobic MIF was encapsulated in preformed liposomes by incubating with water-miscible dimethyl sulfoxide. Both drugs were successfully encapsulated in liposomes by simultaneously incubating with blank liposomes without remarkably altering the particle size. The release of each drug from DXR/MIF-LPs corresponded to that from liposomes encapsulating a single drug, indicating that drug encapsulation did not influence drug release. Treatment with MIF did not impact the overexpression of P-glycoprotein (P-gp) in C26/DXR cells. However, DXR/MIF-LPs increased the cellular association of DXR and enhanced cytotoxicity compared with liposomes encapsulating DXR against C26/DXR cells, indicating that MIF inhibits P-gp function and increases the cytotoxicity of DXR in MDR cells. Collectively, our findings suggest that the co-delivery of DXR and MIF using a liposomal formulation is a promising approach for reversing MDR.

Synthesis and characterization of liposomes encapsulating silver nanoprisms obtained by millifluidic-based production for drug delivery

Silver nanoprisms (SNPs) have attracted significant attention due to their surface plasmon resonance behaviour, which is strongly dependent on their size and shape. The enhanced light absorption and scattering capacity of SNPs, make them a promising candidate system for non-invasive imaging and drug delivery in nanoparticle-assisted diagnostics and therapy. However, systemic administration of silver nanoparticles (AgNPs) at high concentrations may result in toxic side-effects, arising from non-targeted bio-distribution. These drawbacks could be mitigated by employing liposomes as carriers for AgNPs. However, there is a lack of systematic studies on production and subsequent physico-chemical characterisation of liposomal systems encapsulating SNPs. The present study therefore investigated the synthesis of liposomes encapsulating SNPs (Lipo/SNPs) using a continuous-flow millimetre-scale reactor, whereby liposome formation was governed by a solvent exchange mechanism. An aqueous phase and an ethanolic lipid phase were conveyed through two separate inlet channels, and subsequently travelled through a serpentine-shaped channel where mixing between the two phases took place. The synthesis process was optimised by varying both liposome formulation and the operating fluidic parameters, including the ratio between inlet flow rates (or flow rate ratio) and the total flow rate. The obtained Lipo/SNPs were characterised for their size and electrostatic charge, using a dynamic light scattering apparatus. Liposome morphology and encapsulation efficiency of SNPs within liposomes were determined by transmission electron microscopy (TEM) imaging. The synthesised negatively charged Lipo/SNP samples were found to have an average size of ∼150 nm (size dispersity < 0.3). The AgNPs encapsulation efficiency was equal to 77.48%, with mostly single SNPs encapsulated in liposomes. By using a multiangle TEM imaging approach, quasi-3D images were obtained, further confirming the encapsulation of nanoparticles within liposomes. Overall, the formulation and production technique developed in the present study has potential to contribute towards mitigating challenges associated with AgNP-mediated drug delivery and diagnostics.

Proteinase K/Retinoic Acid-Loaded Cationic Liposomes as Multifunctional Anti-Acne Therapy to Disorganize Biofilm and Regulate Keratinocyte Proliferation.

Simultaneous anti-Cutibacterium acnes and anti-inflammatory actions are highly beneficial in treating acne vulgaris. In this study, we present novel anti-acne nanovesicles based on liposomes loaded with proteinase K (PK), retinoic acid (RA), and soyaethyl morpholinium ethosulfate (SME) to achieve an effective and safe treatment. This study examined in vitro planktonic and biofilm C. acnes elimination, as well as the keratinocyte proliferation suppression by liposomes. The multifunctional liposomes for treating C. acnes in mice were also evaluated. We acquired multifunctional liposomes with a size of 71 nm and zeta potential of 31 mV. The antimicrobial activity of SME was enhanced after liposomal encapsulation according to the reduction of minimum bactericidal concentration (MBC) by 6-fold. The multifunctional liposomes exhibited a synergistically inhibitory effect on biofilm C. acnes colonization compared with the liposomes containing PK or those containing SME individually. The adhesive bacterial colony in the microplate was lessened by 62% after multifunctional liposome intervention. All liposomal formulations tested here demonstrated no cytotoxicity against the normal keratinocytes but inhibited C. acnes-stimulated cell hyperproliferation. The in vitro scratch assay indicated that the liposomal RA-but not free RA-restrained keratinocyte migration. The animal study showed that free RA combined with SME and multifunctional nanovesicles had a similar effect on diminishing C. acnes colonies in the skin. On the other hand, liposomes exhibited superior performance in recovering the impaired skin barrier function than the free control. We also found that RA-loaded nanovesicles had greater skin tolerability than free RA. The cationic liposomes containing dual PK and RA represented a potential treatment to arrest bacterial infection and associated inflammation in acne.

Liposomal Encapsulation of Chemotherapeutics Agents Combined with the Use of Ultrasound in Cancer Treatment

Ultrasound (US) has numerous uses in the medical field, including imaging, tumor ablation, and lithotripsy; another interesting application of US in cancer therapy is as an external trigger in targeted drug delivery. Cancer-targeted drug delivery involves delivering chemotherapeutic drugs to tumor sites with a high degree of precision, which would minimize the adverse side effects experienced by patients. Several nanocarriers have been studied as possible nanocarriers; however, liposomes stood out from the rest because of their non-immunogenicity, amphiphilic nature, ease of functionalization, and stimuli-responsiveness. This review addresses the role of US in the synthesis of liposomes, its ability to induce localized and controlled drug release from liposomes, as well as the integration of US-induced release and US-imaging using liposomes as contrast agents utilizing thermal and/or mechanical effects.

P-685 Extracellular vesicles of human follicular fluid as biomarkers of ovarian disease

Abstract Study question Our aim is to analyze the morphology of follicular fluid extracellular vesicles (EVs) according to ovarian pathology by labeling the vesicles with luminescent gold nanoclusters. Summary answer Cryo-TEM analysis reveals that EVs from the follicular fluid of patients presenting with polycystic ovary syndrome have a particularly complex morphology compared to normo-ovulatory women. What is known already EVs are particles enclosed by a lipid membrane and secreted by cells. Previously considered as cellular debris, they are in fact involved in a multitude of biological functions and are potential biomarkers. Development of an optical biosensor based on luminescent nanoparticles would make it possible to analyze them in biological fluids. Study design, size, duration Samples were provided by GERMETHEQUE, Biobank dedicated to human fertility. Samples from 32 patients presenting with ovarian pathology (ovarian failure, polycystic ovary syndrome) and 32 normo-ovulatory patients were analyzed. Participants/materials, setting, methods Luminescent gold nanoclusters (1 to 2 nm in diameter) have been synthesized and functionalized in order to interact with extracellular vesicles. Analysis of the morphology of EVs was carried out by cryoTEM. Qualitative results were analyzed by Chi2 or Fisher tests. The quantitative results were analyzed by the Kruskal Wallis test. Main results and the role of chance The interactions between luminescent gold nanoclusters and lipid membranes show that it is possible to induce electrostatically and in a controlled manner either significant structural changes in the membranes or membrane labeling. Patients presenting with ovarian pathology have more oval vesicles (p = 0.0014). Differences are especially significant in polycystic ovary syndrome showing that simple vesicles are less abundant than controls (p &amp;lt; 0.0001) and large tubules more frequent (p = 0.0023). Limitations, reasons for caution The first results concerning the interactions between luminescent nanoclusters and vesicles demonstrate their potential for labeling these membrane structures Wider implications of the findings The characterization of these anomalies could allow a better understanding of ovarian pathology and open up new therapeutic fields. An efficient method of encapsulation in liposomes of gold nanoclusters has been developed. Trial registration number GERM 20220705

Remotely Rutin-Loaded into Liposomes for Efficient Encapsulation and Enhancement of Bioavailability and Brain Targeting in vivo

Remotely Rutin-Loaded into Liposomes for Efficient Encapsulation and Enhancement of Bioavailability and Brain Targeting in vivo