scholarly journals Preparation of Curcumin-Liposomes using pH-Driven Method to Enhance Stability and Encapsulation Efficiency

2020 ◽  
pp. 120-129
Author(s):  
Fransiska Christydira Sekaringtyas ◽  
Suwasmi Purwajanti ◽  
Etik Mardliyati ◽  
Sri Ningsih
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Oral Bioavailability ◽  
Encapsulation Efficiency ◽  
Hydrolytic Degradation ◽  
Aqueous Solubility ◽  
Alkaline Condition ◽  
Alkaline Conditions ◽  
The Stability ◽  
Film Method

Curcumin, a hydrophobic polyphenol, derived from turmeric, has numerous pharmacological activities, including hepatoprotective, antioxidant, anti-inflammatory, antimicrobial, and anticarcinogenic. However, the therapeutic efficacy of curcumin is limited due to its poor oral bioavailability and high susceptibility to degradation. The poor oral bioavailability of curcumin has been attributed to its poor aqueous solubility and extensive first past metabolism. Curcumin dissolves in alkaline conditions but it is highly unstable undergoing rapid hydrolytic degradation in neutral or alkaline condition. To solve these problems, liposome-based encapsulation technology is applied to improve the bioavailability of curcumin. The existing method to prepare curcumin-liposome, thin-film method, is complex and usually required the use of organic solvents. In this study, pH-driven method, an organic solvent-free and easily encapsulation technique utilizing the pH-dependent solubility of curcumin was proposed to improve the stability and bioavailability. Curcumin-liposomes were prepared using phospholipon 90 H and soya lecithin as phospholipid sources. The characterizations of curcumin-liposomes include particle size, microstructure, encapsulation efficiency, infrared spectra, salt stability and storage stability. The particle size measured was 77.85 ± 0.39 nm. It was found that curcumin-liposomes prepared by the pH-driven method was stable during storage for 30 days and gave encapsulation efficiency of 60.71 ± 0.20%, higher as compared to the ones prepared by thin-film method. In conclusion, pH-driven is a promising method for the preparation of curcumin-liposomes to enhance stability and encapsulation efficiency

scholarly journals The Effect of the Liposomal Encapsulated Saffron Extract on the Physicochemical Properties of a Functional Ricotta Cheese

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 120
Author(s):  
Zahra Siyar ◽  
Ali Motamedzadegan ◽  
Jafar Mohammadzadeh Milani ◽  
Ali Rashidinejad
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Textural Properties ◽  
Constant Concentration ◽  
Soy Lecithin ◽  
Significant Difference ◽  
Saffron Extract ◽  
The Stability ◽  
Potential Stability

In this study, the encapsulation of saffron extract (SE) was examined at four various concentrations of soy lecithin (0.5%–4% w/v) and constant concentration of SE (0.25% w/v). Particle size and zeta potential of liposomes were in the range of 155.9–208.1 nm and −34.6–43.4 mV, respectively. Encapsulation efficiency was in the range of 50.73%–67.02%, with the stability of nanoliposomes in all treatments being >90%. Encapsulated SE (2% lecithin) was added to ricotta cheese at different concentrations (0%, 0.125%, 1%, and 2% w/v), and physicochemical and textural properties of the cheese were examined. Lecithin concentration significantly (p ≤ 0.05) affected the particle size, zeta potential, stability, and encapsulation efficiency of the manufactured liposomes. In terms of chemical composition and color of the functional cheese, the highest difference was observed between the control cheese and the cheese enriched with 2% liposomal encapsulated SE. Hardness and chewiness increased significantly (p ≤ 0.05) in the cheeses containing encapsulated SE compared to the control cheese. However, there was no significant difference in the case of adhesiveness, cohesiveness, and gumminess among different cheeses. Overall, based on the findings of this research, liposomal encapsulation was an efficient method for the delivery of SE in ricotta cheese as a novel functional food.

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

Liposomal Mediated Carriers of α Lipoic Acid for the Treatment of Acute Lung Injury: Preclinical Study in Rat Model

2020 ◽  
Vol 10 (1) ◽  
pp. 53-57
Author(s):  
Yu Cao ◽  
Yanling Chai ◽  
Xiaoqun Niu ◽  
Bing Hai ◽  
Xiaojie He ◽  
...  
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Pulmonary Fibrosis ◽  
Lung Injury ◽  
Lipoic Acid ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Preclinical Study ◽  
Liposomal Formulation ◽  
Experimental Animals

The present investigation deals with formulation of lipoic acid as liposomal formulation and to evaluate its efficacy in Lung injury (Pulmonary Fibrosis). The liposomal formulation of Lipoic acid (LA-liposomes) was successfully prepared by thin film hydration method. Such prepared liposomes were characterized for particle size, encapsulation efficiency, drug loading etc. characteristic. An Pulmonary fibrosis was induced using Bleomycin experimental animals rats. The effect of LA liposomal formulation on pulmonary fibrosis was observed. The histopathological finding confirms the efficiency of formulation in attenuation of pulmonary fibrosis.

Degradation Behavior of Poly(ethylene glycol) Diblock and Multiblock Polymers with Hydrolytically Degradable Ester Linkages

2004 ◽  
Vol 69 (8) ◽  
pp. 1643-1656 ◽  
Author(s):  
Alena Braunová ◽  
Michal Pechar ◽  
Karel Ulbrich
Keyword(s):  
Ethylene Glycol ◽  
Hydrolytic Degradation ◽  
Dicarboxylic Acids ◽  
Drug Carriers ◽  
Poly Ethylene Glycol ◽  
Model Study ◽  
Alkaline Conditions ◽  
Rate Of Hydrolysis ◽  
Poly Ethylene ◽  
The Stability

Diblock and multiblock polymers of poly(ethylene glycol) containing degradable ester bonds between the blocks were synthesized and characterized. Monofunctional poly(ethylene glycol) (PEG 2000) was modified by aliphatic dicarboxylic acids (malonic, succinic, glutaric, maleic) to obtain monocarboxylic polymers PEG-COOH containing ester bonds. Diblock polymers (4000) were prepared by polycondensation of a diamine (ethane-1,2-diamine, L-lysine) and the semitelechelic PEG-COOH. The relationship between the structure of the linkage connecting two PEG blocks and the rate of its hydrolytic degradation was studied at pH 5.5, 7.4 and 8.0. The rate of hydrolysis of all polymers was significant already under mild alkaline conditions (pH 7.4 and 8.0) and increased with increasing pH. The ester bonds of polymers with saturated dicarboxylic acid moieties were stable at pH 5.5. However, the presence of double bond in the acid moiety substantially decreased the stability of the polymer not only in alkaline but also in acid medium. The results of this model study can be utilized in the design of biodegradable high-molecular-weight drug carriers and polymers for preparation of "stealth" systems intended for therapeutic application.

Dissolution Improvement of Itraconazole by a Nanoparticulate System Containing Lecithin-Pectin Complexes

2013 ◽  
Vol 747 ◽  
pp. 162-165 ◽  
Author(s):  
Pornsak Sriamornsak ◽  
Sontaya Limmatvapirat ◽  
Kamonrak Cheewatanakornkool
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Zeta Potential ◽  
Surface Charge ◽  
Low Cost ◽  
Drug Carriers ◽  
Drug Dissolution ◽  
Lipophilic Drug ◽  
Dissolution Apparatus ◽  
Film Method

Nanoparticulate system composing of polymeric or lipid materials have been proposed as drug carriers for improving efficacy of encapsulated drugs. Different materials, e.g. phospholipids and polysaccharides, have been proposed for the production of these systems due to their biocompatibility, biodegradability, low cost and safety. In this study, we report a novel particulate system containing lecithin-pectin complexes loaded with a lipophilic drug, itraconazole. The effect of pectin concentration on particle formation and drug dissolution was also investigated. The lecithin-pectin complexes were prepared by thin film method using soya lecithin and then hydrated with different concentration of pectin solution. The surface charge (zeta potential) and particle size of complex particles were characterized. The drug dissolution was determined by using USP dissolution apparatus. The results demonstrated that the particle size of complex particles were in nanometer range. When concentration of pectin increased, the size increased slightly while the surface charge of complex particles was less negative. The drug dissolution from complex particles containing lecithin and pectin was higher than those containing only pectin.

scholarly journals Preparation of Rutin Phytosome Complex

2018 ◽  
Vol 34 (2) ◽  
Author(s):  
Khanh Nguyễn
Keyword(s):  
Particle Size ◽  
Spray Drying ◽  
Oral Bioavailability ◽  
Encapsulation Efficiency ◽  
X Ray Diffraction ◽  
Phospholipid Complex ◽  
Scanning Calorimetry ◽  
Molar Ratios ◽  
Radiation Induced ◽  
Ft Ir

Rutin is a flavonol glycoside, which has been reported to have antioxidant, anti-inflammatory,  antithrombotic, antineoplastic, inhibit ultraviolet radiation-induced cutaneous oxidative stress  and inflammation. The oral bioavailability of Rutin is very low. Phyto-phospholipid complex (phytosomes) is helpful in enhancing oral bioavailability and transdermal permeation of Rutin. Rutin phytosomes were prepared by using phosphatidylcholine (PC) and cholesterol by solvent evaporation and spray drying method. The physicochemical properties of phytosomes were  evaluated using particle size analyses, polydispersity index, Zeta potential, encapsulation efficiency, furrier transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffraction (XRD). Phytosomes with the rutin: PC: cholesterol molar ratios of 1:1:0.2 were prepared by spray drying showed the lowest particle size (266.4 nm), the highest encapsulation efficiency (95.61%). Results of the FT-IR, DSC and XRD studies confirmed the  phyto-phospholipid complex formation.

The complexing characteristics of insoluble selenides. 1. Silver selenide

1970 ◽  
Vol 48 (22) ◽  
pp. 3491-3497 ◽  
Author(s):  
M. C. Mehra ◽  
A. O. Gubeli
Keyword(s):  
Ionic Strength ◽  
Acidic Medium ◽  
Aqueous Solubility ◽  
Inert Atmosphere ◽  
Mathematical Treatment ◽  
Silver Selenide ◽  
Heterogeneous Equilibrium ◽  
Alkaline Conditions ◽  
The Stability ◽  
Aqueous Species

The aqueous solubility of the system silver selenide has been investigated in an inert atmosphere of nitrogen at a unit molar ionic strength and constant temperature of 25° C. The experimental evidence indicates the formation of two aqueous species [Ag2(HSe)(OH)], and [Ag(Se)2(OH)]4− in contact with the precipitated selenide in different regions of acidity. The former exists in acidic medium and has a pβ value of 48.49 ± 0.10 while the latter is stable only in alkaline conditions and has a pβ value of 24.07 ± 0.19. A mathematical treatment has been elaborated to identify and calculate the stability constants of such selenide complexes formed through a heterogeneous equilibrium.

Design and Development of Solid Dispersion of Valsartan by a Lyophilization Technique: A 3^2 Factorial Design Approach

2020 ◽  
Vol 12 ◽  
Author(s):  
Nitin Rajendra Shirsath ◽  
Ajaygiri Kamalgiri Goswami
Keyword(s):  
Particle Size ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Butyl Alcohol ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Onset Of Action ◽  
Tertiary Butyl ◽  
Water As Solvent

Background: Valsartan is a poorly water-soluble drug having limited oral bioavailability. Its absorption and onset of action are mostly depending on solubility, it needs to enhance their solubility for maximum therapeutic action. Objective: The aim of this work is to formulate valsartan-mannitol solid dispersions (SDs) by bottom-up process based-freeze drying (lyophilization) techniques for solubility enhancement of valsartan. Methods: Valsartan is BCS class II drug having low aqueous solubility and low oral bioavailability. It needs to improve its solubility for the fastest onset of action. The SDs were prepared using water as solvent and tertiary butyl alcohol (TBA) as anti-solvent. A 3^2 (three level-two factors) response surface methodology was used to detect the effect of independent variables such as the amount of valsartan (X_1) and the amount of mannitol (X_2) on dependent variables such as solubility (Y_1) and particle size (Y_2). Results: Prepared SDs were characterized by employing solubility, particle size determination, differential scanning calorimetry (DSC), X-ray diffraction (XRD), zeta potential, fourier transform infrared spectroscopy (FTIR) and field emission scanning electron microscopy (FESEM). The optimum values of solubility and particle size were 115.14µg/L and 242.5 nm respectively. Conclusions:: Solid dispersions of valsartan-mannitol were successfully prepared by simple lyophilization techniques and seem to be promising for enhancing dissolution rate (solubility) and oral bioavailability of valsartan.

scholarly journals Development and In Vitro Evaluation of Liposomes Using Soy Lecithin to Encapsulate Paclitaxel

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Thi Lan Nguyen ◽  
Thi Hiep Nguyen ◽  
Dai Hai Nguyen
Keyword(s):  
Thin Film ◽  
Cell Proliferation ◽  
Particle Size ◽  
Light Scattering ◽  
Delivery System ◽  
Drug Loading ◽  
Soy Lecithin ◽  
Physiochemical Properties ◽  
Film Method

The formulation of a potential delivery system based on liposomes (Lips) formulated from soy lecithin (SL) for paclitaxel (PTX) was achieved (PTX-Lips). At first, PTX-Lips were prepared by thin film method using SL and cholesterol and then were characterized for their physiochemical properties (particle size, polydispersity index, zeta potential, and morphology). The results indicated that PTX-Lips were spherical in shape with a dynamic light scattering (DLS) particle size of 131±30.5 nm. Besides, PTX was efficiently encapsulated in Lips, 94.5±3.2% for drug loading efficiency, and slowly released up to 96 h, compared with free PTX. More importantly, cell proliferation kit I (MTT) assay data showed that Lips were biocompatible nanocarriers, and in addition the incorporation of PTX into Lips has been proven successful in reducing the toxicity of PTX. As a result, development of Lips using SL may offer a stable delivery system and promising properties for loading and sustained release of PTX in cancer therapy.

scholarly journals The Anti-obesity Effects of Direct Delivery of Resveratrol-encapsulated Liposomes to Inguinal White Adipose Tissue in Male APOE*3Leiden.CETP Transgenic Mice (P21-006-19)

2019 ◽  
Vol 3 (Supplement_1) ◽  
Author(s):  
Md Shahjalal Hossain Khan ◽  
Lei Hao ◽  
Shu Wang
Keyword(s):  
Particle Size ◽  
Body Weight ◽  
Adipose Tissue ◽  
Food Intake ◽  
High Fat Diet ◽  
Encapsulation Efficiency ◽  
Aqueous Solubility ◽  
Body Temperatures ◽  
High Fat ◽  
Core Body

Abstract Objectives Browning of white adipose tissue (WAT) is a promising strategy for preventing and treating obesity. Trans-resveratrol (R) has the potential to increase the energy expenditure via inducing WAT browning, but its application in obesity is limited by a low level of aqueous solubility, a high level of hepatic metabolism and toxicity. We have successfully synthesized biocompatible and biodegradable R encapsulated liposomes (Rlipo). The objective of this project is to deliver Rlipo directly to the inguinal WAT (iWAT) in mice with the goal of maximizing anti-obesity efficacy while minimizing side effects and toxicity. Methods Rlipo were prepared using R and soy phosphatidylcholine (soy-PC) dissolved in ethanol. After mixing and drying them under nitrogen, deionized water was added followed by sonication. Unencapsulated R was removed by ultrafiltration. The void liposomes (Vlipo) were prepared using only soy-PC. The particle size and polydispersity index (PI) of Rlipo and Vlipo were measured using a Brookhaven BI-MAS particle size analyzer. R’s encapsulation efficiency and solubility were measured using a liquid chromatography-mass spectrometry. Male APOE*3Leiden.CETP mice having human-like lipoprotein metabolism were fed with a high-fat diet (45% of calorie from fat) for 10 weeks. After treating the high-fat diet for 4 weeks, mice received iWAT injection of Rlipo, Vlipo, free R and saline (control) once a week. R concentration was 17.5 mg/kg body weight/week. Body weight and food intake were measured weekly. Body composition of mice was measured using an EchoMRITM every other week. Core body temperatures of mice were determined using a Type T thermometer. Glucose tolerance test (GTT) was performed at the 4th week of treatment. Results Rlipo increased the aqueous solubility of R by more than 100 times. The size of Rlipo and Vlipo was 170 ± 6 nm and 140 ± 7 nm, respectively. Their PI values were less than 0.2. The encapsulation efficiency of Rlipo was 99.8%. The post-treatment core body temperatures for control, free R, Vlipo and Rlipo groups were 36.2°C, 36.2°C, 36.6°C, and 37.0°C, respectively. Food intake was similar among 4 groups. Compared to other groups, the Rlipo-treated mice had the lowest body weight, body fat mass, and body fat percentage. The Rlipo group had the lowest area under the curve in the GTT among 4 groups. Conclusions Nanoencapsulation increased R’s solubility and enhanced its anti-obesity efficacy. Funding Sources NIH/NCCIH (Grant R15AT008733).

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