Factors affecting liposomes particle size prepared by ethanol injection method

Shaker, Sherif; Gardouh, Ahmed; Ghorab, Mostafa M.

doi:10.4103/1735-5362.213979

Cited by 142 publications

(77 citation statements)

References 15 publications

(20 reference statements)

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“…The particle size of liposomal preparation of B 12 (C5) (13.50 mM, PC) was in the range of 139‐151 nm with an average polydespersity index (PDI) of ∼ 38% and average molecular weight of ∼ 310 MDa (Figure left panel). It was found that the variation in lipid content results in variation in the size of liposomes as observed by previous workers …”

Section: Resultssupporting

confidence: 69%

The kinetics of photostabilization of cyanocobalamin in liposomal preparations

Arsalan

Ahmad

Ali

et al. 2020

Int J of Chemical Kinetics

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Cyanocobalamin (B 12 ) is a photosensitive vitamin, and its photodegradation to hydroxocobalamin (B 12b ) in liposomes has been investigated. The values of apparent first-order rate constants (k obs ) for the photodegradation of B 12 in liposomes (nine preparations) are in the range of (0.52-2.24) × 10 -3 min -1 , compared to 3.21 × 10 -3 min -1 for B 12 in aqueous solution (pH 5.0). The entrapment efficiency of B 12 in liposomes is 26.4-38.8%. The values of k obs show a linear relation with phosphatidylcholine (PC) content in liposomes, indicating the influence of PC in inhibiting the rate of photolysis of B 12 . The value of the bimolecular rate constant for photochemical interaction of B 12 and PC is 0.32 M -1 min -1 , indicating the stabilizing effect of PC on the photolysis of B 12 . The ratio of B 12 stabilization in liposomal preparations is in the range 2-6 compared to that of the unentrapped vitamin The stabilization of B 12 is mediated by a photoinduced charge-transfer B 12 -PC complex that leads to the reduction of B 12 to B 12r , which is then oxidized to B 12b that has low susceptibility to photolysis. The extent of stabilization of B 12 probably depends on the degree of interaction between the two compounds under the reaction conditions, indicated by the loss of B 12 fluorescence.

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Section: Resultssupporting

confidence: 69%

The kinetics of photostabilization of cyanocobalamin in liposomal preparations

Arsalan

Ahmad

Ali

et al. 2020

Int J of Chemical Kinetics

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“…Two cholesterol: non-ionic surfactant molar ratios were tested (1:1 and 2:1) to study their effect on the physicochemical properties of niosomes. Ethanol injection technique was adopted due to its well-ascribed simplicity and safety [37]. Among different utilized organic solvents, ethanol was found to be a good solvent for niosomes components, including quercetin, avoiding any aggregation during preparation.…”

Section: Resultsmentioning

confidence: 99%

Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

et al. 2020

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Flavonoids possess different interesting biological properties, including antibacterial, antiviral, anti-inflammatory and antioxidant activities. However, unfortunately, these molecules present different bottlenecks, such as low aqueous solubility, photo and oxidative degradability, high first-pass effect, poor intestinal absorption and, hence, low systemic bioavailability. A variety of delivery systems have been developed to circumvent these drawbacks, and among them, in this work niosomes have been selected to encapsulate the hepatoprotective natural flavonoid quercetin. The aim of this study was to prepare nanosized quercetin-loaded niosomes, formulated with different monolaurate sugar esters (i.e., sorbitan C12; glucose C12; trehalose C12; sucrose C12) that act as non-ionic surfactants and with cholesterol as stabilizer (1:1 and 2:1 ratio). Niosomes were characterized under the physicochemical, thermal and morphological points of view. Moreover, after the analyses of the in vitro biocompatibility and the drug-release profile, the hepatoprotective activity of the selected niosomes was evaluated in vivo, using the carbon tetrachloride (CCl 4 )-induced hepatotoxicity in rats. Furthermore, the levels of glutathione and glutathione peroxidase (GSH and GPX) were measured. Based on results, the best formulation selected was glucose laurate/cholesterol at molar ratio of 1:1, presenting spherical shape and a particle size (PS) of 161 ± 4.6 nm, with a drug encapsulation efficiency (EE%) as high as 83.6 ± 3.7% and sustained quercetin release. These niosomes showed higher hepatoprotective effect compared to free quercetin in vivo, measuring serum biomarker enzymes (i.e., alanine and aspartate transaminases (ALT and AST)) and serum biochemical parameters (i.e., alkaline phosphatase (ALP) and total proteins), while following the histopathological investigation. This study confirms the ability of quercetin loaded niosomes to reverse CCl 4 intoxication and to carry out an antioxidant effect.Pharmaceutics 2020, 12, 143 2 of 18 and anticancer activities [1][2][3]. These intrinsic properties, together with their biocompatibility and remarkable antioxidant activity, have attracted researchers' attention to explore potential therapeutic applications [4,5].Quercetin (3, 30, 4, 5, 7-pentahydroxyflavone) is probably the most studied bioflavonoid, belonging to the family of flavonols; its therapeutic applications include hepatoprotection [6], prevention of neural cell apoptosis [7] and cancer chemo-prevention and treatment [8].Quercetin acts as strong antioxidant by scavenging free radicals and transition metal ions, thus decreasing the process of lipid peroxidation, which is responsible for the development of many diseases, e.g., cardiovascular and neurodegenerative diseases, as well as liver damage [9][10][11].However, quercetin therapeutic applications present challenges due to (i) low aqueous solubility, (ii) photo and oxidative degradability, (iii) high first-pass effect, (iv) poor intestinal absorption and, hence, low systemic...

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“…From the DLS measurements, the mean hydrodynamic diameter of the nanoparticles was estimated to be 150 nm for Hep-Chl-1 prodrug, 210 nm for Hep-Chl-2 prodrug, and 300 nm for Hep-Chl-3 prodrug (Figure 4c). As the concentration of Chl increased, more Chl molecules were distributed in the prodrug bilayer, resulting in an increase in the particle size [34]. The size of each prodrug nanoparticle determined from AFM data was smaller than that from the DLS data [21,35].…”

Section: Formation Of the Self-assembled Prodrugmentioning

confidence: 86%

Redox-Responsive Heparin–Chlorambucil Conjugate Polymeric Prodrug for Improved Anti-Tumor Activity

et al. 2019

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Polymeric prodrug-based delivery systems have been extensively studied to find a better solution for the limitations of a single drug and to improve the therapeutic and pharmacodynamics properties of chemotherapeutic agents, which can lead to efficient therapy. In this study, redox-responsive disulfide bond-containing amphiphilic heparin–chlorambucil conjugated polymeric prodrugs were designed and synthesized to enhance anti-tumor activities of chlorambucil. The conjugated prodrug could be self-assembled to form spherical vesicles with 61.33% chlorambucil grafting efficiency. The cell viability test results showed that the prodrug was biocompatible with normal cells (HaCaT) and that it selectively killed tumor cells (HeLa cells). The uptake of prodrugs by HeLa cells increased with time. Therefore, the designed prodrugs can be a better alternative as delivery vehicles for the chlorambucil controlled release in cancer cells.

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Factors affecting liposomes particle size prepared by ethanol injection method

Cited by 142 publications

References 15 publications

The kinetics of photostabilization of cyanocobalamin in liposomal preparations

The kinetics of photostabilization of cyanocobalamin in liposomal preparations

Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

Redox-Responsive Heparin–Chlorambucil Conjugate Polymeric Prodrug for Improved Anti-Tumor Activity

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