scholarly journals Liposomes Loaded with Unsaponifiable Matter from Amaranthus hypochondriacus as a Source of Squalene and Carrying Soybean Lunasin Inhibited Melanoma Cells

Nanomaterials ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 1960
Author(s):  
Erick Damian Castañeda-Reyes ◽  
Elvira Gonzalez de Mejia ◽  
Fred Joseph Eller ◽  
Mark A. Berhow ◽  
María de Jesús Perea-Flores ◽  
...  
Keyword(s):  
Particle Size ◽  
Unsaponifiable Matter ◽  
Encapsulation Efficiency ◽  
Inhibitory Concentration ◽  
Melanoma Cells ◽  
Amaranthus Hypochondriacus ◽  
Liposome Formulation ◽  
Reported Health ◽  
Amaranth Oil ◽  
Melanoma Cell Lines

Amaranthus hypochondriacus is a source of molecules with reported health benefits such as antioxidant activity and cancer prevention. The objective of this research was to optimize the conditions for preparing a liposome formulation using amaranth unsaponifiable matter as a source of squalene in order to minimize the particle size and to maximize the encapsulation efficiency of liposomes for carrying and delivering soybean lunasin into melanoma cell lines. Amaranth oil was extracted using supercritical dioxide carbon extraction (55.2 MPa pressure, 80 °C temperature, solvent (CO2)-to-feed (oil) ratio of 20). The extracted oil from amaranth was used to obtain the unsaponifiable enriched content of squalene, which was incorporated into liposomes. A Box–Behnken response surface methodology design was used to optimize the liposome formulation containing the unsaponifiable matter, once liposomes were optimized. Soybean lunasin was loaded into the liposomes and tested on A-375 and B16-F10 melanoma cells. The squalene concentration in the extracted oil was 36.64 ± 0.64 g/ 100 g of oil. The particle size in liposomes was between 115.8 and 163.1 nm; the squalene encapsulation efficiency ranged from 33.14% to 76.08%. The optimized liposome formulation contained 15.27 mg of phospholipids and 1.1 mg of unsaponifiable matter. Cell viability was affected by the liposome formulation with a half-maximum inhibitory concentration (IC50) equivalent to 225 μM in B16-F10 and 215 μM in A-375. The liposomes formulated with lunasin achieved 82.14 ± 3.34% lunasin encapsulation efficiency and improved efficacy by decreasing lunasin IC50 by 31.81% in B16-F10 and by 41.89% in A-375 compared with unencapsulated lunasin.

scholarly journals FORMULATION AND EVALUATION OF CURCUMIN LOADED LIPOSOME AND ITS BIO-ENHANCEMENT

2019 ◽  
Vol 9 (4-A) ◽  
pp. 425-437
Author(s):  
Khushboo Verma ◽  
Jhakeshwar Prasad ◽  
Suman Saha ◽  
Surabhi Sahu
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
High Performance ◽  
Encapsulation Efficiency ◽  
Mean Particle Size ◽  
Liposome Formulation

The aim of this work was to develop and evaluate curcumin loaded liposome and its bio- enhancement. Curcumin was selected as a natural drug for liposome formulation. Curcumin show variety of biological activity but it also shows poor bioavailability due to low aqueous solubility (1 µg/ml), poor absorption and rapid metabolism so that piperine was selected as bio enhancer to improve curcumin bioavailability. Soy lecithin and cholesterol were used to prepared curcumin and curcumin-piperine loaded liposome at different ratio by thin film hydration method because of easy to perform, and high encapsulation rates of lipid. The all liposome formulations (F1-F5) were evaluated by mean particle size, polydispersity index, zeta potential, encapsulation efficiency and drug release. Bioavailability was also determined on rat. Blood samples were collected at specific intervals, and plasma was separated by ultracentrifugation. Plasma was analyzed by high-performance liquid chromatography at 425 nm taking acetonitrile: water (75:25 v/v) acidified with 2% acetic acid as a mobile phase at a flow rate of 0.5 ml/min using C18 column. The mean particle size was found in the range between 800-1100 that indicate liposome are large unilamellar vesical types. By zeta potential study its conform that the all formulation was stable. The encapsulation efficiency of all liposome formulation are varied between 59-67%. In vitro drug release was analyse in 7.4 pH phosphate buffer, the maximum %CDR observed at the 12 hrs., and formulation are follow sustained release thus they reduce metabolism, good absorption rate which improve bioavailability of drug. From in-vivo study, it is clear that curcumin-piperine liposomal formulation, increases Cmax, area under the curve, and mean residence time significantly as compared to pure curcumin and pure curcumin liposome. Keywords: liposome; Curcumin; Piperine, Thin film hydration method; Bioavailability

scholarly journals Microencapsulation of Cannabidiol in Liposomes as Coating for Cellulose for Potential Advanced Sanitary Material

Coatings ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 3
Author(s):  
Julija Volmajer Valh ◽  
Zdenka Peršin ◽  
Bojana Vončina ◽  
Kaja Vrezner ◽  
Lidija Tušek ◽  
...  
Keyword(s):  
Particle Size ◽  
Composite Material ◽  
Encapsulation Efficiency ◽  
Fibrous Composite ◽  
Antimicrobial Properties ◽  
Desorption Kinetics ◽  
Liquid Formulation ◽  
Fibrous Composite Material ◽  
Antioxidant Efficiency ◽  
Liposome Formulation

The microencapsulation of the cannabidiol and its integration into the tampon can eliminate vaginal inflammation, which at the same time lead to relaxation of the abdominal muscles. The tampon, which contains the active substance cannabidiol (CBD), was developed as an advanced fibrous composite for sanitary application. The active substances were microencapsulated, and, as a carrier, liposomes micro/nano capsules were used. The CBD liposome formulation was analyzed by particle size, polydispersity index, zeta potential, and encapsulation efficiency. Particle size of the CBD liposome liquid formulation was increased by 19%, compared to the liposome liquid formulation and the encapsulation efficiency of CBD in liposome particles, which was 90%. The CBD liposome formulation was applied to cellulose material. The composition of the fibrous composite material was evaluated by Fourier transform infrared spectroscopy, the fiber morphology was analyzed by scanning electron spectroscopy, while the bioactive properties were assessed by antioxidant efficiency, antimicrobial properties, and desorption kinetics. CBD liposome functionalized tampons have both antioxidant and antimicrobial properties. Antimicrobial properties were more pronounced against Gram-positive bacteria. The desorption kinetics of the CBD liposome immobilized on the surface of the composite material was studied using antioxidant activity in the desorption bath. The prepared CBD liposome functionalized tampon additionally shows higher biodegradability compared to references. This high-quality, biodegradable sanitary material based on microencapsulated CBD components as a functional coating provides a platform for many different applications besides medical textiles, also for packaging, pharmaceuticals, paper and wood-based materials, etc.

Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Size Distribution ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Glycol Succinate ◽  
Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

scholarly journals Synergy, Additivity, and Antagonism between Cisplatin and Selected Coumarins in Human Melanoma Cells

2021 ◽  
Vol 22 (2) ◽  
pp. 537
Author(s):  
Paula Wróblewska-Łuczka ◽  
Aneta Grabarska ◽  
Magdalena Florek-Łuszczki ◽  
Zbigniew Plewa ◽  
Jarogniew J. Łuszczki
Keyword(s):  
Cell Lines ◽  
Melanoma Cell ◽  
Melanoma Cells ◽  
Human Melanoma ◽  
Type I ◽  
Antiproliferative Effects ◽  
Isobolographic Analysis ◽  
Natural Substances ◽  
Additive Interactions ◽  
Melanoma Cell Lines

(1) Cisplatin (CDDP) is used in melanoma chemotherapy, but it has many side effects. Hence, the search for natural substances that can reduce the dose of CDDP, and CDDP-related toxicity, is highly desired. Coumarins have many biological properties, including anticancer and antiproliferative effects. (2) An in vitro 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay on two human melanoma cell lines (FM55P and FM55M2) examined the antitumor properties of CDDP and five naturally occurring coumarins (osthole, xanthotoxin, xanthotoxol, isopimpinellin, and imperatorin). The antiproliferative effects produced by combinations of CDDP with the coumarins were assessed using type I isobolographic analysis. (3) The most potent anticancer properties of coumarins were presented by osthole and xanthotoxol. These compounds were characterized by the lowest median inhibitory concentration (IC50) values relative to the FM55P and FM55M2 melanoma cells. Isobolographic analysis showed that for both melanoma cell lines, the combination of CDDP and osthole exerted synergistic and additive interactions, while the combination of CDDP and xanthotoxol exerted additive interactions. Combinations of CDDP with xanthotoxin, isopimpinellin, and imperatorin showed antagonistic and additive interactions in two melanoma cell lines. (4) The combination of CDDP and osthole was characterized by the most desirable synergistic interaction. Isobolographic analysis allows the selection of potential candidates for cancer drugs among natural substances.

scholarly journals 708 Application of a novel mSENS drug delivery technology for mRNA therapeutics

2020 ◽  
Vol 8 (Suppl 3) ◽  
pp. A750-A750
Author(s):  
Sojin Lee ◽  
Joon Young Park ◽  
Goo-Young Kim ◽  
Sang Woo Jo ◽  
Minhyuk Yun ◽  
...  
Keyword(s):  
Particle Size ◽  
Protein Expression ◽  
Cancer Vaccine ◽  
Encapsulation Efficiency ◽  
Tumor Model ◽  
Cell Responses ◽  
Delivery Platform ◽  
Mrna Therapeutics

BackgroundSuccessful clinical translation of mRNA therapeutics requires an appropriate delivery strategy to overcome instability of mRNA and facilitate cellular uptake into the cells.1 Several lipid based nanoparticle approaches that encapsulate mRNA, notably lipid nanoparticle (LNP), have been developed, but their efficiency for delivery to certain target tissues and toxicity profiles still have room for improvement. The application of a novel polymer based nanoparticle technology platform, so called Stability Enhanced Nano Shells (SENS) for mRNA (mSENS) as a mRNA delivery platform for a cancer vaccine was demonstrated.MethodsThe physicochemical properties of mSENS formulation, particle size and encapsulation efficiency, were characterized using dynamic light scattering (DLS) and gel retardation assay. Using luciferase-encoding mRNA, the protein expression levels in vitro and in vivo were evaluated by luciferase assay or bioluminescence imaging (BLI), respectively. For cancer vaccine studies, antigen (tyrosinase-related protein 2 (Trp-2))-specific T cell responses were assessed by immunophenotyping mouse splenocytes using flow cytometry and by the enzyme-linked immunosorbent spot (ELISPOT) assay. The anti-tumor efficacy was studied in B16F10 lung tumor model in C57BL/6 mice. Liver and systemic toxicity of mSENS treated mice was evaluated through blood chemistry and complete blood count (CBC) tests.ResultsA library of mSENS formulations complexed with luciferase-encoding mRNA, were characterized for their particle size, surface charge, encapsulation efficiency, colloidal stability, and in vitro and in vivo luciferase protein expression level. Upon systemic administration in mice, varying biodistribution profiles were observed, implicating the potential for tailored delivery to target tissues. Particularly, cancer vaccine application was further developed leveraging the formulation with preferential spleen delivery. Following vaccination with Trp-2 mRNA encapsulated with mSENS (Trp-2 mRNA-mSENS) in B16F10 tumor bearing mice, strong Trp-2 antigen-specific IFN-γ T-cell responses were observed. Generated anti-tumor immunity also marked suppression of B16F10 lung tumors were observed in Trp-2-mSENS immunized mice compared to non-immunized controls, demonstrating the potential of mSENS as a mRNA delivery platform for the application for vaccine.ConclusionsProprietary biodegradable polymer based-mSENS platform offers an attractive delivery strategy for mRNA by tailoring to specific therapeutic applications. Depending on the application, whether it’s a vaccine or protein replacement, a rationally designed mSENS formulation can efficiently distribute mRNA to specific tissues. In particular, application of a splenic mSENS formulation for a cancer vaccine has been demonstrated in murine tumor model. In summary, mRNA delivery through mSENS platform is expected to provide significant opportunities in clinical development for mRNA therapeutics.Ethics ApprovalThe study was approved by Samyang Biopharmaceuticals’ IACUC (Institutional Animal Care and Use Committee), approval number SYAU-2027.ReferencePiotr S. Kowalski, Arnab Rudra, Lei Miao, and Daniel G. Anderson, delivering the messenger: advances in technologies for therapeutic mRNA delivery. Molecular Therapy Vol. 27 No 4 April 2019.

scholarly journals Development and Stability Studies of Novel Liposomal Vancomycin Formulations

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Krishna Muppidi ◽  
Andrew S. Pumerantz ◽  
Jeffrey Wang ◽  
Guru Betageri
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Antimicrobial Agents ◽  
Preparation Method ◽  
Physical Stability ◽  
Liposomal Formulations ◽  
Promising Strategy ◽  
Activity Variable ◽  
Distribution Studies

A promising strategy to improve the therapeutic efficiency of antimicrobial agents is targeted therapy. Although vancomycin has been considered a gold standard for the therapy of MRSA pneumonia, clinical failure rates have also been reported owing to its slow, time-dependent bactericidal activity, variable lung tissue penetration and poor intracellular penetration into macrophages. Liposomal encapsulation has been established as an alternative for antimicrobial delivery to infected tissue macrophages and offers enhanced pharmacodynamics, pharmacokinetics and decreased toxicity compared to standard preparations. The aim of the present work is to prepare vancomycin in two different liposomal formulations, conventional and PEGylated liposomes using different methods. The prepared formulations were optimized for their particle size, encapsulation efficiency and physical stability. The dehydration-rehydration was found to be the best preparation method. Both the conventional and PEGylated liposomal formulations were successfully formulated with a narrow particle size and size distribution and % encapsulation efficiency of and , respectively. Both the formulations were stable at C for 3 months. These formulations were successfully used to evaluate for their intracellular killing of MRSA and in vivo pharmacokinetic and bio-distribution studies.

Simultaneous Incorporation of 5-Fluorouracil and Leucovorin into Chitosan Nanoparticle as Drug Carrier and Its Characterization

2010 ◽  
Vol 654-656 ◽  
pp. 2265-2268
Author(s):  
Pu Wang Li ◽  
Yi Chao Wang ◽  
Zheng Peng ◽  
Ling Xue Kong
Keyword(s):  
Particle Size ◽  
Strong Interaction ◽  
Encapsulation Efficiency ◽  
Drug Carrier ◽  
Drug Loading ◽  
Anti Cancer ◽  
Chitosan Nanoparticle ◽  
Combined Drugs ◽  
Drug Encapsulation Efficiency ◽  
Interaction Between Drugs

A combined drug loaded system containing two most common anti-cancer drugs 5-fluorouracil (5-FU) and leucovorin (LV) was designed and prepared by ion crosslinking technology. The resulted nanoparticles are spherical in shape, and the particle size becomes larger when drug combination are loaded. Efficient drug encapsulation efficiency (EE) and drug loading (LC) are obtained due to the strong interaction between drugs and polymer. The combined drugs are distributed in the particles in amorpholous state which are demonstrated by the XRD results.

scholarly journals Development of oil-in-water microemulsion encapsulating Vitamin E for thermal and hydrolysis degradation study

2020 ◽  
Vol 16 (3) ◽  
pp. 277-280
Author(s):  
Khairun Nisa Abdul Rahman ◽  
Vicit Rizal Eh Suk ◽  
Khalisanni Khalid ◽  
Nurhazirah Mohd Ihsan ◽  
Zainurin Md Dom ◽  
...  
Keyword(s):  
Particle Size ◽  
Vitamin E ◽  
Encapsulation Efficiency ◽  
Low Cost ◽  
Bioactive Compound ◽  
Small Particle Size ◽  
Degradation Study ◽  
Oil In Water ◽  
The Mean ◽  
Vitamin E Homologs

Vitamin E is widely used for medicinal and cosmeceuticals purposes. However, it is easy to degrade by the environment. In this study, the degradation of Gold Tri.E™ was studied and determined. Gold Tri.E™ is a mixture of Vitamin E homologs (tocotrienol and tocopherol) extracted from palm oil (Elais Guineensis). A nanocarrier system has been optimized to encapsulate Gold Tri.E™ from degrading and increasing its stability as a bioactive compound. An oil-in-water (o/w) microemulsion was formulated and optimized as the best carrier to encapsulate Gold Tri.E™ with the mean particle size of 32.60±3.60 nm and 99.99±0.01% encapsulation efficiency (EE). Degradation of the Gold Tri.E™ in o/w microemulsion was significantly reduced as compared to the bare Gold Tri.ETM. This suggested that the system could protect Gold Tri.E™ from thermal and hydrolysis degradation. Thus, the ease of preparation, low-cost production, and small particle size obtained when Gold Tri.E™ encapsulated in this system give promising drug delivery system to encapsulate, protect, and increase the shelf life of Gold Tri.E™.

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