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The incorporation of hydrophobic drugs into liposomes improve their bioavailability and leads to increased stability and anticancer activity, along with decreased drug toxicity. Curcumin (Cur) is a natural polyphenol compound with a potent anticancer activity in pancreatic adenocarcinoma (PA). In the present study, different types of Cur-loaded liposomal formulations were prepared and characterized in terms of size, shape, zeta potential, optimal drug-to-lipid ratio and stability at 4°C, 37°C; and in human plasma in vitro. The best formulation in terms of these parameters was PEGylated, cholesterol-free formulation based upon hydrogenated soya PC (HSPC:DSPE-PEG2000:Cur, termed H5), which had a 0.05/10 molar ratio of drug-to-lipid, was found to be stable and had a 96% Cur incorporation efficiency. All Cur-loaded liposomal formulations had potent anticancer activity on the PA cancer cell lines AsPC-1 and BxPC-3, and were less toxic to a normal cell line (NHDF). Furthermore, apoptosis-induction induced by Cur in PA cells was associated with morphological changes including cell shrinkage, cytoplasmic blebbing, irregularity in shape and the externalization of cell membrane phosphatidylserine, which was preceded by an increase in intracellular reactive oxygen species (ROS) generation and caspase 3/7 activation. Because the liposomal formulations tested here, especially the H5 variant which exhibited slow release of the Cur in the human plasma test, the formulation may be stable enough to facilitate the accumulation of pharmacologically active amounts of Cur in target cancer tissue by EPR. Therefore, our formulations could serve as a promising therapeutic approach for pancreatic cancer and other cancers.

Quercetin is a chemical compound present in many fruits and vegetables, known for its antioxidant and anti-inflammatory effects. Additionally, this bioactive flavonoid can induce apoptosis in abnormally developing cells. The aim of the study was to develop an effective method for encapsulating quercetin in liposomes and to evaluate the drug encapsulation efficiency, stability of the formulation and anticancer effects on melanoma cells. The results showed that quercetin can be successfully encapsulated in the aqueous phase of liposomes by complexing it with copper ions. To assess the cytotoxicity of the liposomal quercetin, SRB assays were performed on two melanoma cell lines, A-375 and C32, as well as on normal human keratinocytes, HaCaT. This formulation exhibited a cytotoxic effect on melanotic melanoma cells but not on normal cells, indicating the possible use of liposomal quercetin in anticancer treatment.

The aim of the study was to achieve effective colon anticancer immunotherapy using the alkaloid berberine. In the presented paper we attempt to develop a formulation of berberine loaded into liposomal carriers using the vitamin C gradient method, characterized by efficient drug encapsulation, high stability during long-term storage, low drug release in human plasma with specific cytotoxicity towards colon cancer cells. Liposomal berberine was responsible for the induction of oxidative stress, the presence of Ca2+ ions in the cytosol, the reduction of Δψm, and ATP depletion with a simultaneous lack of caspase activity. Moreover, treatment with liposomal berberine led to CRT exposure on the surface of cancer cells, extracellular ATP, and HMGB1 release. The above-described mechanism of action was most likely associated with ICD induction, contributing to the increased number of phagocytic cancer cells. We have shown that cancer cells treated with liposomal berberine were phagocytosed more frequently by macrophages compared to the untreated cancer cells. What is more, we have shown that macrophage pre-treatment with liposomal berberine led to a 3-fold change in the number of phagocytosed SW620 cancer cells. The obtained results provide new insights into the role of berberine in maintaining the immune response against colorectal cancer.

There is a growing interest in the role of sphingolipids in the background of multiple sclerosis (MS). The goal of this study was to evaluate the serum levels of antibodies against ceramide-1-phosphate (C1P) subclasses and their relationships with clinical status in MS. The study groups comprised 39 patients with relapsing-remitting MS (RRMS), 26 patients with other neurological diseases (OND) and 12 healthy subjects (HS). Anti-C1P IgG levels in serum were determined using ELISA test. Levels of anti-C18:0-C1P and anti-C24:1-C1P IgG were significantly increased ( p  = 0.003; p  < 0.0001, respectively) in RRMS compared to HS, while anti-C16:0-C1P and anti-C24:0-C1P IgG – significantly lower p  < 0.0001 in RRMS compared to OND, with large effect size ( r  ≥ 0.5) in all above cases. In both settings the acceptable discriminatory performance for RRMS subtype from HS (AUC = 78.1%, 95% CI 66.1–90.4 and AUC = 76.9%, 95% CI 60.3–93.6, respectively) as well as from OND (AUC = 79.8%, 95% CI 68.2–91.4 and AUC = 94.2%, 95% CI 88.6–99.8, accordingly) by receiver operating curve (ROC) was shown. Validation of ROC by cluster analysis confirmed the ability of these anti-C1P IgG panels to discriminate between the study groups. No relationships were found between levels of antibodies in the anti-C1P IgG panel in RRMS group and disease duration, degree of disability or Link index. These findings highlight the relevant role of C1P as a target and/or mediator of autoimmune response in MS and potential value of anti-C1P antibodies as biomarkers in differential diagnosis of this disease.

This study focused on investigating the enhanced photoactive properties of liposomal aloe-emodin for photodynamic treatment (PDT). Aloe-emodin (A-E) was encapsulated in liposomes by using the copper ion gradient method. This study aimed to highlight the function of naturally occurring photoactive plant-based derivatives in liposomal formulations as simple alternative photosensitizers (PS) for melanoma photodynamic therapy (PDT). Furthermore, we aimed to show that phototoxic chemicals loaded into liposomes are less cytotoxic than non-encapsulated molecules, which we used in our previous study. To assess the effectiveness of liposome aloe-emodin as a photosensitizer in PDT on melanoma cell lines, we performed cellular uptake by flow cytometry, MTT assay to measure the cytotoxicity of a natural compound, wound healing assay, ROS analysis by confocal microscopy, ROS analysis by flow cytometry, immunocytochemistry staining to measure the level of apoptotic proteins, and Real-Time PCR gene expression analysis. The melanoma cells showed increased phototoxicity after therapy compared to the normal cells in the MTT assay. Moreover, liposome aloe-emodin-based photodynamic therapy resulted in an increased ratio of apoptotic cells, increased ROS levels, and increased or decreased gene expression. This study also demonstrated that aloe-emodin encapsulated in liposomes significantly decreased melanoma cell motility following PDT treatment. In conclusion, our study provides evidence that aloe-emodin-mediated PDT exhibits potential for clinical development as a novel, safe, and effective photosensitizer for melanoma treatment.

The needles of conifer trees are one of the richest sources of natural polyprenols. Polyprenol homologs from Abies sibirica L. lipophilic 80% purified extract were analyzed and quantified. In total, 10 peaks (Prenol-11 to Prenol-20) were observed in the ultra-high-performance liquid chromatography–diode array detector (UHPLC-DAD) chromatogram of Siberian fir with the most abundant compound being Prenol-15 (relative amount 37.23 + 0.56% of the total polyprenol yield). Abies sibirica L. polyprenol solubility and incorporation efficiency into liposomes were studied in various commercially available lecithin mixtures (Phosal IP40, Phosal 75SA, and Lipoid P45). The resulting multilamellar polyprenol liposomes were morphologically characterized by Light and Transmission Electron Microscopy, and the liposome size was discovered to be polymodal with the main peak at 1360 nm (90% of the volume). As polyprenols are fully soluble only in lipids, a liposomal formulation based upon co-solubilization and a modified ethanol injection method of polyprenols into the ethanol-phospholipid system was developed for the entrapment and delivery of polyprenols for potential commercial applications in food supplement and cosmetic industries.

The research focused on the investigation of curcumin encapsulated in hydrogenated soy phosphatidylcholine liposomes and its increased photoactive properties in photodynamic therapy (PDT). The goal of this study was two-fold: to emphasize the role of a natural photoactive plant-based derivative in the liposomal formulation as an easily bioavailable, alternative photosensitizer (PS) for the use in PDT of skin malignancies. Furthermore, the goal includes to prove the decreased cytotoxicity of phototoxic agents loaded in liposomes toward normal skin cells. Research was conducted on melanoma (MugMel2), squamous cell carcinoma (SCC-25), and normal human keratinocytes (HaCaT) cell lines. The assessment of viability with MTT (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide) evaluated cell death after exposure to blue light irradiation after 4 h of pre-incubation with free and encapsulated curcumin. Additionally, the wound healing assay, flow cytometry, and immunocytochemistry to detect apoptosis were performed. The malignant cells revealed increased phototoxicity after the therapy in comparison to normal cells. Moreover, liposome curcumin-based photodynamic therapy showed an increased ratio of apoptotic and necrotic cells. The study also demonstrated that nanocurcumin significantly decreased malignant cell motility following PDT treatment. Acquired results suggest that liposomal formulation of a poor soluble natural compound may improve photosensitizing properties of curcumin-mediated PDT treatment in skin cancers and reduce toxicity in normal keratinocytes.

Pancreatic cancer (PC) is one of the deadliest cancers so there is an urgent need to develop new drugs and therapies to treat it. Liposome-based formulations of naturally-derived bioactive compounds are promising anticancer candidates due to their potential for passive accumulation in tumor tissues, protection against payload degradation, and prevention of non-specific toxicity. We chose the naturally-derived flavonoid baicalein (BAI) due to its promising effect against pancreatic ductal adenocarcinoma (PDAC) and encapsulated it into a liposomal bilayer using the passive loading method, with an almost 90% efficiency. We performed a morphological and stability analysis of the obtained BAI liposomal formulation and evaluated its activity on two-dimensional and three-dimensional pancreatic cell models. As the result, we obtained a stable BAI-encapsulated liposomal suspension with a size of 100.9 nm ± 2.7 and homogeneity PDI = 0.124 ± 0.02, suitable for intravenous administration. Furthermore, this formulation showed high cytotoxic activity towards AsPC-1 and BxPC-3 PDAC cell lines (IC50 values ranging from 21 ± 3.6 µM to 27.6 ± 4.1 µM), with limited toxicity towards normal NHDF cells and a lack of hemolytic activity. Based on these results, this new BAI liposomal formulation is an excellent candidate for potential anti-PDAC therapy.

are the most common cause of food poisoning, which manifests itself in diarrhoea of varying severity. Additionally, because of the increasing number of people with immune deficiencies, more frequent serious complications of infections are being observed. The main source of infection is the consumption of contaminated poultry meat, which is a consequence of the insufficiency of current hygiene and biosecurity to control or eliminate it from the poultry food chain. Two hybrid proteins, presenting selected epitopes of the antigens CjaD and EF-Tu, were developed based on the highly immunogenic proteins CjaA and CjaC. Four groups of chickens were vaccinated with different preparations (a mixture of both hybrid proteins encapsulated in anionic or neutral liposomes) and different doses (a single dose given on the day of hatching or two doses given on days 1 and 14 of life). The number of was assessed in the intestinal contents of vaccinated birds. No statistically significant differences in colonisation levels were observed between chickens immunised with neutral liposomes containing hybrid proteins and their non-immunised counterparts, regardless of dosage regimen. Although immunisation of chickens did not produce the expected results, the approach used has great potential, which is worth further investigation and development.

The correct spelling is: Mahmud M, Piwoni A, Filipczak N, Janicka M, Gubernator J (2016) Long-Circulating Curcumin-Loaded Liposome Formulations with High Incorporation Efficiency, Stability and Anticancer Activity towards Pancreatic Adenocarcinoma Cell Lines In Vitro. Mahmud M, Piwoni A, Filiczak N, Janicka M, Gubernator J (2016) Long-Circulating Curcumin-Loaded Liposome Formulations with High Incorporation Efficiency, Stability and Anticancer Activity towards Pancreatic Adenocarcinoma Cell Lines In Vitro.