Nanoliposomes a future based delivery vehicle of cyanidin-3-O-glucoside against major chronic disease.

BACKGROUND: Cyanidin-3-O-glucoside (C3G), is an anthocyanin mainly found in berries, and can also be produced by microorganisms. It has been traditionally used as a natural coloring agent for decades. Recently, it has been investigated for its high antioxidant activity and anti-cancer attributes. C3G has low bioavailability and is sensitive to oxidation and gastric pH; therefore, it is encapsulated in nanoliposomes to enhance its bio-availability, targeted delivery- and efficacy against chronic disease. SCOPE AND APPROACH: In this review, the role of C3G nanoliposomes against major chronic diseases has been discussed. The focus was on research findings and the mechanism of action to affect the proliferation of cancer, neuro disease and cardiovascular problems. It also discussed the formulation of nanoliposomes, their role in nutraceutical delivery and enhancement in C3G bioavailability. KEY FINDINGS AND CONCLUSIONS: Data suggested that nanoliposomes safeguard C3G, enhance bioavailability, and ensure safe, adequate and targeted delivery. It can reduce the impact of cancer and inflammation by inhibiting the ß-catenin/O6-methylguanine-DNA methyltransferase (MGMT) pathway and upregulating miR-214-5p. Formation of C3G nanoliposomes significantly enhances the nutraceutical efficacy of C3G against major chronic disease therefore, C3G nanoliposomes might be a future-based nutraceutical to treat major chronic diseases, including cancer, neuro problems and CVD, but challenges remain in finding correct dose and techniques to maximize its efficacy.

Encapsulation of gingerol into nanoliposomes: Evaluation of in vitro anti-inflammatory and anti-cancer activity.

Nanoliposomes (NLs) are ideal carriers for delivering complex molecules and phytochemical products, but ginger by-products, despite their therapeutic benefits, have poor bioavailability due to their low water solubility and stability. Crude ginger extracts (CGEs) and 6-gingerol were individually encapsulated within NLs for in vitro activity assessment. In vitro evaluation of anti-proliferative and anti-inflammatory properties of encapsulated 6-gingerol and CGE was performed on healthy human periodontal ligament (PDL) fibroblasts and MDA-MB-231 breast cancer cells. Encapsulation efficiency and loading capacity of 6-gingerol reached 25.23% and 2.5%, respectively. NLs were found stable for up to 30 days at 4°C with a gradual load loss of up to 20%. In vitro cytotoxic effect of encapsulated 6-gingerol exceeded 70% in the MDA-MB-231 cell line, in a comparable manner with non-encapsulated 6-gingerol and CGE. The effect of CGE with an IC50 of 3.11 ± 0.39, 7.14 ± 0.80, and 0.82 ± 0.55 µM and encapsulated 6-gingerol on inhibiting IL-8 was evident, indicating its potential anti-inflammatory activity. Encapsulating 6-gingerol within NLs enhanced its stability and facilitated its biological activity. All compounds, including vitamin C, were equivalent at concentrations below 2 mg/mL, with a slight difference in antioxidant activity. The concentrations capable of inhibiting 50% of 2,2-diphenyl-1-picrylhydrazyl (DPPH) substrate were comparable.

Targeted Delivery of Arctigenin Using Sialic Acid Conjugate-Modified Liposomes for the Treatment of Breast Cancer.

Arctigenin (ATG) is a broad-spectrum antitumor drug with an excellent inhibitory effect on malignant tumors such as breast cancer, glioblastoma, liver cancer, and colon cancer. However, the clinical application of ATG is limited by its poor water solubility and quick hydrolysis in the liver, intestine, and plasma, which might hinder its application. Sialic acid (SA) recognizes selectin receptors overexpressed on the surface of tumor-associated macrophages. In this study, SA was conjugated with octadecylamine (ODA) to prepare SA-ODA, which was employed to prepare SA functionalized nanoliposomes (SA-Lip) to achieve breast cancer targeting. The formulations were finely optimized using the Box-Behnken design to achieve higher ATG loading. The size, ζ potential, entrapment efficiency, drug loading, and release behavior of ATG@SA-Lip were fully investigated in comparison with conventional ATG@Lip. The ATG@SA-Lip displayed more potent cytotoxicity and higher cellular internalization compared to ATG@Sol and ATG@Lip in both MCF7 and 4T1 cells. Notably, ATG@SA-Lip showed the lowest impact on the immune system. Our study demonstrates that SA-Lip has strong potential as a delivery system for the targeted delivery of ATG.

Nanoliposomal delivery systems of natural antibacterial compounds; properties, applications, and recent advances.

Todays, nanoliposomes (NLPs) are considered as one of the most efficient nanocarriers to deal with bacteria, practically in food products. These nanodelivery systems are able to be loaded with different bioactive compounds. The main aim of this review is investigating recent approaches (mostly from the years of 2018 to 2022) regarding development of nanoliposomal natural antibacterial compounds. In this regard, NLPs alone, combined with films, coatings, or fibers, and in coated forms are reviewed as advanced delivery systems of antibacterial substances. Moreover, a robust and comprehensive coverage of the morphological and physical properties of formulated NLPs as well as their interactions with antibacterial substances are discussed. The importance of NLPs to encapsulate antibacterial ingredients, advantages and drawbacks, antibacterial pathways of formulated NLPs, and comparison of them with pure antibacterial bioactive compounds are also explained.

The anti-spermatogenic activity of nanoliposomes loaded with Heracleum persicum phenolic compounds in Balb/C mice.

There are various types of bioactivities that have been reported for Heracleum persicum species, such as antioxidant, anti-inflammatory, and cytotoxicity properties. In the current study, the bio-accessibility of H. persicum bioactive compounds was improved by purifying its phenolic-enriched fractions (PEF) and encapsulating them into nanoliposomes to analyze its cytotoxic impacts on mice testicular tissue and their fertility status. Nano liposomal H. persicum PEF (NL-HPEF) was prepared by ultrasound-based encapsulation of HPEF and L-agranular lecithin mixture. The size, morphology, and stability of NL-HPEF were characterized by dynamic light scattering, field emission scanning electron microscopy, and zeta potential analysis. The 18 white male Balb/c mice (20-25 g) at 3 treatment groups were provided to study the NL-HPPF cytotoxicity by measuring the mice liver enzyme including aspartate aminotransferase (AST), ALP and alanine aminotransferase (ALT), testis lipid peroxidation, and testicular tissue destruction levels. Moreover, the mice's fertility was evaluated by studying the Adam3, Prm1, Spata19, and Tnp2 gene expression in the testicular tissues. The obtained results manifested that the synthesized NL-HPEF was stable (193.7 nm) and exhibited a notable cytotoxic impact on the mice's liver (ALT and AST enhancement levels) and testicular tissues. Moreover, their increasing treatment doses impaired the male mice's fertility by decreasing the sperm count, viability, and motility. In addition, fertility suppression was verified by decreasing serum testosterone and downregulating the Adam3, Prm1, Spata19, and Tnp2 gene expression in their testicular tissues. The male mice's fertility was significantly (p < 0.05) suppressed by increasing treatment doses of NL-HPEF. Hence, the NL-HPEF could be considered a promising alternative to replace the male chemical contraceptives drugs.

Synthesized nanoliposome-encapsulated kaempferol attenuates liver health parameters and gene expression in mice challenged by cadmium-induced toxicity.

In the present research, we encapsulated a flavonoid called kaempferol into nanoliposomal structures and the health-promoting effects of synthesized nanoliposome-loaded kaempferol (NLK) were evaluated in mice challenged by cadmium-induced . The NLK characteristics, such as size, zeta potential, and polydispersity index, were 218.4 nm, -28.55 mV, and 0.29, respectively. The in vivo experiment revealed that the mice receiving water containing cadmium (2 mg/kg body weight/day) showed significant (p < 0.05) weight loss, an increase in liver enzyme activities, and hepatic oxidative stress. Dietary supplementation with NLK at concentrations of 2.5 and 5 mg/kg mice body weight notably (p < 0.05) improved the body weight, liver enzyme activities, hepatic oxidative stress, and antioxidant potential of the liver. Our findings elucidated that NLK could alleviate the toxicity of cadmium in mice challenged by cadmium-induced toxicity.

Arsenic trioxide and Erlotinib loaded in RGD-modified nanoliposomes for targeted combination delivery to PC3 and PANC-1 cell lines.

During the past few years, advances in drag delivery have provided many opportunities in the treatment of various diseases and cancer. Arsenic trioxide (ATO) and Erlotinib (Erlo) are two drugs, approved by the United States Food and Drug Administration to treat cancer, but their use is limited in terms of the toxicity of ATO and the low solubility of Erlo. This study aimed to prepare arginine-glycine-aspartic acid (RGD)-decorated nanoliposomes (NLPs) containing Erlo and ATO (NLPs-ATO-Erlo-RGD) to increase the solubility and reduce the toxicity of Erlo and ATO for cancer treatment. The results of transmission electron microscopy and dynamic light scattering showed that NLPs were synthesized uniformly, with spherical shape morphology and particle sizes between 140 and 160 nm. High-performance liquid chromatography and ICP-MS results showed that about 90% of the drug was loaded in the NLPs. In comparison with NLPs-ATO-Erlo, NLPs-ATO-Erlo-RGD demonstrated considerable toxicity against the αvß3 overexpressing PC3 cell line in the MTT experiment. It had no effect on the PANC-1 cell line. In addition, apoptosis assays using Annexin V/PI demonstrated that NLPs-ATO-Erlo-RGD generated the highest apoptotic rates in PC3 cells when compared with NLPs-ATO-Erlo and the combination of free ATO and Erlo. Furthermore, treatment with NLPs-ATO-Erlo-RGD in (p < 0.05) PC3 cell line significantly reduced EGFR level. It is concluded NLPs-ATO-Erlo-RGD as a novel drug delivery system may be a promising platform for the treatment of cancer.

Phosphorothioated amino-AS1411 aptamer functionalized stealth nanoliposome accelerates bio-therapeutic threshold of apigenin in neoplastic rat liver: a mechanistic approach.

Hepatocellular carcinoma (HCC) is a leading cause of death globally. Even though the progressive invention of some very potent therapeutics has been seen, the success is limited due to the chemotherapeutic resistance and recurrence in HCC. Advanced targeted treatment options like immunotherapy, molecular therapy or surface-engineered nanotherapeutics could offer the benefits here owing to drug resistance over tumor heterogenicity. We have developed tumor-sensing phosphorothioate and amino-modified aptamer (AS1411)-conjugated stealth nanoliposomes, encapsulating with apigenin for precise and significant biodistribution of apigenin into the target tumor to exploit maximum bio-therapeutic assistances. The stable aptamer functionalized PEGylated nanoliposomes (Apt-NLCs) had an average vesicle size of 100-150 nm, a smooth surface, and an intact lamellarity, as ensured by DLS, FESEM, AFM, and Cryo-TEM. This study has specified in vitro process of optimum drug (apigenin) extrusion into the cancer cells by nucleolin receptor-mediated cellular internalization when delivered through modified AS1411 functionalized PEGylated nanoliposomes and ensured irreversible DNA damage in HCC. Significant improvement in cancer cell apoptosis in animal models, due to reduced clearance and higher intratumor drug accumulation along with almost nominal toxic effect in liver, strongly supports the therapeutic potential of aptamer-conjugated PEGylated nanoliposomes compared to the nonconjugated formulations in HCC. The study has established a robust superiority of modified AS1411 functionalized PEGylated nanoliposomes as an alternative drug delivery approach with momentous reduction of HCC tumor incidences.

Preparation, characterization and wound-healing effect of PEGylated nanoliposomes loaded with oleuropein.

Chronic wounds have become a major concern for healthcare systems, as they have been related to diabetic foot ulcers, venous leg ulcers and pressure ulcers. Oleuropein is an active compound that is extracted from olive leaves and it has the ability to reduce injury to tissues owing to its antioxidant effect, hence improving wound healing. The poor pharmacokinetics of oleuropein have limited its use clinically. This work is aimed toward studying the impact of PEGylated and non-PEGylated nanoliposomes loaded with oleuropein, as a carrier model, on wound-healing activity. The thin film hydration method was used to compose PEGylated and non-PEGylated liposomes, both loaded with oleuropein. The results indicated that each free, PEGylated and non-PEGylated composition was within the limit of optimum nanoliposome characterization. The results showed that non-PEGylated compositions produced higher efficiency in encapsulation (47.09 ± 10.06%) than the PEGylated ones (20.97 ± 10.52%). The PEG-nanoliposomes loaded with oleuropein (PEG-oleu) had mean size, charge and polydispersity index of 129.35 nm, -9.55 mV and 0.1010, respectively. The scratch assay results proved that PEGylated liposomal compositions have a more rapid wound-healing activity than non-PEGylated ones at different time intervals at 0, 2, 24 and 28 h.

Preparation, Characterization, and Anticancer Activity of PEGylated Nano Liposomal Loaded with Rutin against Human Carcinoma Cells (HT-29).

The abstract discusses the development of rutin-loaded nanoliposomes and their anti-colorectal cancer activity against human carcinoma cells (HT-29). The study characterizes the nanoliposomes using the thin-film hydration method and analyzes their size, charge, and polydispersity index. The encapsulation efficiency and drug loading ability of rutin at different concentrations were investigated. The nanoliposomes were found to be stable for up to one month at 4 °C and showed sustained drug release for up to 24 h. The anti-cancer activity of the rutin-loaded nanoliposomes was found to be concentration-dependent and significantly improved compared to free rutin. PEGylated nanoliposomes with rutin (1.8 mg/ml) showed the highest encapsulation efficiency and drug loading ability, along with improved selectivity against cancer cells. Overall, the study provides important insights into the potential use of rutin-loaded nanoliposomes for the treatment of colorectal cancer.

Evaluation of suitability and detection range of fluorescent dye-loaded nanoliposomes for sensitive and rapid sensing of wide ranging osmolarities.

Measurement of osmolarity is critical for optimizing bioprocesses including antibody production and detecting pathologies. Thus, rapid, sensitive, and in situ sensing of osmolarity is desirable. This study aims to develop and assess the suitability of calcein- and sulforhodamine-loaded nanoliposomes for ratiometric sensing of osmolarity by fluorescence spectroscopy and evaluate the range of detection. The detection is based on concentration-dependent self-quenching of calcein fluorescence (sensor dye at 6-15 mM) and concentration-independent fluorescence of sulforhodamine (reference dye) due to osmotic shrinkage of the nanoliposomes when exposed to hyperosmotic solutions. Using mathematical modeling, 6 mM calcein loading was found to be optimal to sense osmolarity between 300 and 3000 mOsM. Calcein (6 mM)- and sulforhodamine (2 mM)-loaded nanoliposomes were produced by thin-film hydration and serial extrusion. The nanoliposomes were unilamellar, spherical (108 ± 9 nm), and uniform in size (polydispersity index [PDI] 0.12 ± 0.04). Their shrinkage induced by exposure to hyperosmotic solutions led to rapid self-quenching of calcein fluorescence (FGreen), but no effect on sulforhodamine fluorescence (FRed) was observed. FGreen/FRed decreased linearly with increasing osmolarity, obeying Boyle van't Hoff's relationship, thus proving that the nanoliposomes are osmosensitive. A calibration curve was generated to compute osmolarity based on FGreen/FRed measurements. As a proof-of-concept, dynamic changes in osmolarity in a yeast-based fermentation process was demonstrated. Thus, the nanoliposomes have great potential as sensors to rapidly and sensitively measure wide-ranging osmolarities.

A novel nano material for anti-cerebral ischaemia: preparation and application of borneol angelica polysaccharide liposomes.

OBJECTIVE: To investigate the preparation of novel nanoliposomes (Borneol Angelica Polysaccharide Liposomes, BAPL) for anti-cerebral ischaemia and verify its curative effects and mechanism. METHODS: By applying a uniform experiment design to investigate the fitting combination of BAPL. Encapsulation Efficiency Evaluation of BAPL Preparation; Particle Size and Surface Potential Evaluation of BAPL Biological activity; Cerebral ischaemia models of rats Evaluation of BAPL curative effects and mechanism. RESULTS: (1) The fitting combination of lecithin, Cholesterol, AP mass and the borneol mass was 60 mg, 60 mg, 45 mg and 5 mg. the highest encapsulation efficiency was 80.4%, the particle size was 179.1 nm, and the surface zeta potential was -17.2 mV. It conforms to the nano-material standards. (2) The results of animal experiments show that: In the BAPL group, the infarct volume of TTC staining was significantly decreased, and the expression levels of NF-κBp65, TLR-4, IL-8, IL-6, IL-1ß in brain tissue were significantly decreased, while the expression levels of ZO-1, ZO-2, IL-10 were significantly increased after cerebral ischaemia-reperfusion. CONCLUSION: BAPL is a novel nano and effective material for anti-cerebral ischaemia.

Systematic Study of Resveratrol Nanoliposomes Transdermal Delivery System for Enhancing Anti-Aging and Skin-Brightening Efficacy.

Due to the stratum corneum barrier, resveratrol is difficult to be absorbed transdermally, limiting its anti-aging and skin-brightening effects. Furthermore, there is a lack of systematic studies on the efficacy of resveratrol in human skin, especially in three-dimensional skin models and clinical trials. To overcome the low transdermal delivery issue, we encapsulated resveratrol into nanoliposomes using the high-pressure homogenization method to develop an efficient transdermal drug delivery system, and systematically evaluated its anti-aging and skin-brightening efficacy via cell line models, a three-dimensional skin model and human skin. The resveratrol nanoliposomes effectively improved the transdermal penetration and retention of resveratrol and enhanced cellular uptake. In addition, compared to free resveratrol, resveratrol nanoliposomes remarkably enhanced the skin-care effects by promoting the antioxidant capacity and collagen synthesis, inhibiting the secretion of matrix metalloproteinases, tyrosine activity and melanin synthesis. Notably, human clinical trials proved the anti-wrinkle and skin-brightening effectiveness of resveratrol nanoliposomes. Three levels of systematic studies indicated that resveratrol nanoliposomes could be a promising transdermal drug delivery system to enhance the anti-aging and skin-brightening effects of resveratrol.

Interaction of Doxorubicin Embedded into Phospholipid Nanoparticles and Targeted Peptide-Modified Phospholipid Nanoparticles with DNA.

The interactions of dsDNA with new targeted drug delivery derivatives of doxorubicin (DOX), such as DOX embedded into phospholipid nanoparticles (NPhs) and DOX with the NGR targeted peptide-modified NPhs were studied electrochemically by differential pulse voltammetry technique. Screen-printed electrodes (SPEs), modified with stable fine dispersions of carbon nanotubes (CNTs), were used for quantitative electrochemical investigations of direct electrochemical oxidation of guanine, adenine, and thymine heterocyclic bases of dsDNA, and their changes in the presence of DOX nanoderivatives. Analysing the shifts of peak potentials of nucleobases in the presence of drug, we have shown that the doxorubicin with NGR targeted peptide changed the mode of interaction in DNA-drug complexes from intercalative to electrostatic. Binding constants (Kb) of DNA-drug complexes were calculated in accordance with adenine, guanine, and thymine oxidation signals. Based on our experiments, we have proven that the surface modification of a drug delivery system with NGR targeted peptide dramatically changed the mechanism of interaction of drug with genetic material. DNA-mediated drug toxicity was calculated based on the concentration-dependent "response" of heterocyclic nucleobases on drug influence. DOX, DOX-loaded phospholipid nanoparticles (NPhs), and DOX with NGR addressed peptide-modified NPhs were moderately toxic in the concentration range of 0.5-290 µM.

Comparative study of the properties of lutein nanoliposomes coated with chitosan/(-)-epigallocatechin- 3-gallate (EGCG) complexes.

BACKGROUND: Numerous positive effects have been attributed to lutein, a lipophilic nutrient, including resisting ultraviolet radiation and protecting retinal pigment epithelial (RPE) cells against blue light damage. It also has preventive effects against cardiovascular disease and cancer. However, its use could be limited by its poor stability and low bioaccessibility in the human digestive system. An encapsulation delivery system was therefore developed to resolve these limitations. In this study, chitosan-modified lutein nanoliposomes (CS-LNLs), chitosan-EGCG covalently modified lutein nanoliposomes (C-CS-EGCG-LNLs), and chitosan-EGCG noncovalently modified lutein nanoliposomes (non-C-CS-EGCG-LNLs) were designed. The average particle size, ζ-potential, and retention of lutein during storage were measured to indicate the physicochemical stability of the modified lutein nanoliposomes. The bioaccessibility of modified lutein nanoliposomes was also investigated to demonstrate the availability of lutein in the human digestive system. RESULTS: First, Fourier-transform infrared spectroscopy (FTIR) verified that covalent bonds between chitosan and EGCG were formed. Subsequently, ζ-potential results revealed that C-CS-EGCG-LNLs had a relatively stable structure in comparison with lutein nanoliposomes (LNLs). The retention rate of lutein in CS-LNLs, C-CS-EGCG-LNLs, and non-C-CS-EGCG-LNLs was improved, especially in C-CS-EGCG-LNLs (at around 70% of lutein in initial system). An in vitro digestion experiment illustrated that CS-LNLs, C-CS-EGCG-LNLs, and non-C-CS-EGCG-LNLs presented relatively higher bioaccessibility, especially in C-CS-EGCG-LNLs (at around 33% of luein in initial system), which increased 2.5 and 1.65 times in comparison with free lutein and LNLs, respectively. CONCLUSION: Overall, the results showed that C-CS-EGCG-LNLs presented greater physicochemical stability and bioaccessibility than LNLs, CS-LNLs, and non-C-CS-EGCG-LNLs. © 2023 Society of Chemical Industry.

Nano-vesicular carriers for bioactive compounds and their applications in food formulations.

The most commonly used vesicular systems in the food industry include liposomes, niosomes, phytosomes, or transfersomes. This review focuses on showing how nano-vesicular carriers (NVCs) amend the properties of bioactive compounds (bioactives), making them suitable for food applications, especially functional foods. In this research, we elaborate on the question of whether bioactive-loaded NVCs affect various food aspects such as their antioxidant capacity, or sensory properties. This review also shows how NVCs improve the long-term release profile of bioactives during storage and at different pH values. Besides, the refinement of digestibility and bioaccessibility of diverse bioactives through NVCs in the gastrointestinal tract is elucidated. NVCs allow for stable vesicle formation (e.g. from anthocyanins) which reduces their cytotoxicity and proliferation of cancer cells, prolongs the release bioactives (e.g. d-limonene) with no critical burst, reduces the biofilm formation capacity of both Gram-positive/negative strains and their biofilm gene expression is down-regulated (in the case of tannic acid), low oxidation (e.g. iron) is endured when exposed to simulated gastric fluid, and unpleasant smell and taste are masked (in case of omega-3 fatty acids). After the incorporation of bioactive-loaded NVCs into food products, their antioxidant capacity is enhanced, maintaining high encapsulation efficiency and enduring pasteurization conditions, and they are not distinguished from control samples in sensory evaluation despite the reverse situation about free bioactives.

Field application of nanoliposomes delivered quercetin by inhibiting specific hsp70 gene expression against plant virus disease.

BACKGROUND: The annual economic loss caused by plant viruses exceeds 10 billion dollars due to the lack of ideal control measures. Quercetin is a flavonol compound that exerts a control effect on plant virus diseases, but its poor solubility and stability limit the control efficiency. Fortunately, the development of nanopesticides has led to new ideas. RESULTS: In this study, 117 nm quercetin nanoliposomes with excellent stability were prepared from biomaterials, and few surfactants and stabilizers were added to optimize the formula. Nbhsp70er-1 and Nbhsp70c-A were found to be the target genes of quercetin, through abiotic and biotic stress, and the nanoliposomes improved the inhibitory effect at the gene and protein levels by 33.6 and 42%, respectively. Finally, the results of field experiment showed that the control efficiency was 38% higher than that of the conventional quercetin formulation and higher than those of other antiviral agents. CONCLUSION: This research innovatively reports the combination of biological antiviral agents and nanotechnology to control plant virus diseases, and it significantly improved the control efficiency and reduced the use of traditional chemical pesticides.

Investigation of dimyristoyl phosphatidyl glycerol and cholesterol based nanocochleates as a potential oral delivery carrier for methotrexate.

Methotrexate (MTX), a biopharmaceutical classification system-IV anticancer drug, exhibits low therapeutic efficacy. Moreover, its clinical applications were restricted due to its multidrug resistance (MDR) in cancer and its toxic effects. The present investigation was to fabricate 1, 2-dimyristoyl-sn-glycero-3-phospho-rac-(1-glycerol) sodium (DMPG-Na), (3ß)-cholest-5-en-3-ol (cholesterol) and calcium-based nanocochleates (NCs) as a potential oral delivery carrier for MTX to enhance its therapeutic efficacy with low toxicity. MTX-loaded NCs (MTX-NCs) was developed by the addition of calcium ion into preformed nanoliposomes (MTX-NLs) comprising MTX, DMPG-Na, with cholesterol and evaluated by in-vitro and in-vivo methods in comparison with MTX-NLs and pure MTX. Stable tubular rod structure of MTX-NCs possessing particle size, encapsulation efficiency and zeta potential of 374.1 ± 2.2 nm, 78.63 ± 2.12% and -71.2 mV, respectively were obtained from homogenous unilamellar, discrete and spherical structured MTX-NLs with a diameter and zeta potential of 363.3 ± 3.7 nm and -74.6 mV respectively. A thermal study revealed an amorphous state of MTX in MTX-NCs. Pharmacokinetics study in rats, MTX-NLs and MTX-NCs were showed controlled release with 5 and 6 fold improvements in oral bioavailability. Moreover, MTX-NCs showed low tissue distribution. These results collectively suggest that the developed system could be used to improve the therapeutic efficacy of MTX.

Investigations on the influence of the structural flexibility of nanoliposomes on their properties.

In the present study, nanoliposomes with tuneable structure elasticity were prepared by reverse-phase evaporation. Both Fluorescence Polarization and Fluorescence Resonance Energy Transfer was employed to characterize the structural elasticity of resultant nanoliposomes. Temozolomide, a kind of hydrophilic drug as the first-line treatment choice for glioblastoma, was encapsulated into nanoliposomes. The results showed that the flexibility of nanoliposomes gradually increased with sodium cholate, while decreasing with cholesterol, Labrafac CC and Labrafac PG adding. Furthermore, the structural flexibility of nanoliposomes was positively correlated with the encapsulation efficiency and release rate and cellular uptake. Our research reveals the structural flexibility of nanoliposomes could affect in vitro characteristics and thereafter in vivo behaviors of nanoliposomes.

Colorimetric detection of alkaline phosphatase activity based on pyridoxal phosphate-induced chromatic switch of polydiacetylene nano-liposomes.

A colorimetric assay based on polydiacetylenes (PDA) nano-liposomes is reported for facile and sensitive detection of alkaline phosphatase (ALP) activity. The critical basis of this method is that the interaction of pyridoxal phosphate (PLP) with nitrogenous group functionalized PDA nano-liposomes induces distinct blue-to-red color changes of PDA nano-liposomes. In the presence of ALP, as a nature substrate, PLP is enzymatically hydrolyzed to form pyridoxal, which cannot interact with PDA nano-liposomes. As a result, the concentration of PLP is reduced and the color change of PDA nano-liposomes is retarded, which is associated with ALP level. Under optimal conditions, the proposed method showed good linear relationship with ALP activity in the range 10-200 U/L with a limit of detection of 2.8 U/L. The detection process could be vividly observed with the naked eye. Additional attempts by using the method for the evaluation of inhibitor efficiency were also achieved with satisfying results. The method was further challenged with real human serum samples, showing consistent results when compared with a commercial standard assay kit. Such simple and easy-to-use approach may provide a new alternative for clinical and biological detection of ALP.