Shengfeng Peng

Improved in vitro digestion stability of (−)-epigallocatechin gallate through nanoliposome encapsulation

(-)-Epigallocatechin gallate (EGCG) is unstable and degraded in near-neutral or alkaline fluids. To overcome its limitation, EGCG nanoliposome (EN) was prepared by an ethanol injection method combined with dynamic high-pressure microfluidization. EN possessed good physicochemical characterizations (high entrapment efficiency=92.1%, small average particle size=71.7nm, low polydispersity index=0.286 and zeta potential=-10.81mv). EN exhibited a relative good sustained release property. Stability of EGCG in simulated intestinal fluid (SIF) was significantly improved by nanoliposome encapsulation. After 1.5h incubating in SIF without or with pancreatin, the residual EGCG of EN was 31.2% and 47.7% respectively, but the residual EGCG in EGCG solution was only 3.4% and 3.5% respectively. The degenerations of in vitro antioxidant activities of EGCG were effectively slowed by nanoliposome encapsulation. This study expects to provide theories and practice guides for further applications of EN.

The Stability, Sustained Release and Cellular Antioxidant Activity of Curcumin Nanoliposomes.

Curcumin is a multifunctional and natural agent considered to be pharmacologically safe. However, its application in the food and medical industry is greatly limited by its poor water solubility, physicochemical instability and inadequate bioavailability. Nanoliposome encapsulation could significantly enhance the solubility and stability of curcumin. Curcumin nanoliposomes exhibited good physicochemical properties (entrapment efficiency = 57.1, particle size = 68.1 nm, polydispersity index = 0.246, and zeta potential = −3.16 mV). Compared with free curcumin, curcumin nanoliposomes exhibited good stability against alkaline pH and metal ions as well as good storage stability at 4 °C. Curcumin nanoliposomes also showed good sustained release properties. Compared with free curcumin, curcumin nanoliposomes presented an equal cellular antioxidant activity, which is mainly attributed to its lower cellular uptake as detected by fluorescence microscopy and flow cytometry. This study provide theoretical and practical guides for the further application of curcumin nanoliposomes.

Environmental stress stability of microencapsules based on liposomes decorated with chitosan and sodium alginate.

In this study, liposomes (LPs), chitosan (CH) coated LPs, sodium alginate (AL) and CH multilayered LPs (AL-CH-LPs) were developed based on the electrostatic interaction between charged polysaccharides at a certain pH. The increase of polymer layers on LPs led to a monotonic increase in size from ∼600 (LPs) to ∼1810 nm (AL-CH-LPs) and negative charge from -12.5 to -25.2 mV, regarded as a consequence of the formation of gradually expanded structures by cationic CH and anionic AL. The environmental stress including pH, storage and ionic strength (10-200 mM NaCl) had significant impact on the appearance and the particle size of the double-layered liposome (AL-CH-LPs). Furthermore, LPs showed the highest release rate of hydrophilic model ingredient (vitamin C) under gastrointestinal conditions, while the polymers had a capacity to reduce the vitamin C release in simulated intestinal fluid. This work provided useful information on the potential application of CH and AL based delivery systems.

Hybrid liposomes composed of amphiphilic chitosan and phospholipid: Preparation, stability and bioavailability as a carrier for curcumin

Hybrid liposomes, composed of amphiphilic chitosan and phospholipid, were prepared and used to evaluate the effect of amphiphilic polymers on the properties of liposomes. Successful preparation of the hybrid liposomes was confirmed using physicochemical characteristics, including morphology, particle size and zeta potential. Physical stability studies (exposure to solutions of increasing ionic strength and heat treatment) indicated that the hybrid liposomes had better ionic stability than amphiphilic chitosan-based polymeric liposomes and higher thermal stability than traditional phospholipid liposomes. Curcumin was then encapsulated in the hybrid liposomes. Compared with phospholipid liposomes, the hybrid liposomes displayed better storage stability and more sustained curcumin release. Cellular uptake experiments showed that the hybrid liposomes significantly increased the bioavailability of curcumin. The study highlights the potential of well-designed stable hybrid liposomes that increase the stability and bioavailability of lipophilic bioactive, such as curcumin.

Improved bioavailability of curcumin in liposomes prepared using a pH-driven, organic solvent-free, easily scalable process

The poor water solubility and bioavailability of curcumin can be improved by encapsulating it into liposomes. However, the existing encapsulation technologies, such as the thin film method and the ethanol injection method, are complex and require the use of organic solvents. In this study, an organic solvent-free and easily scalable encapsulation technique was studied by utilizing the pH-dependent solubility properties of curcumin. Phospholipid was dissolved in water to form liposomes. Curcumin was deprotonated and dissolved under alkaline conditions and then encapsulated into the liposomes after acidification. Morphological observation and X-ray diffraction analysis confirmed that curcumin liposomes had been successfully prepared. Curcumin liposomes prepared by the pH-driven method were stable during storage. During in vitro digestion, curcumin liposomes prepared by the pH-driven method showed similar bioaccessibility to those prepared by the thin film method and higher bioaccessibility than those prepared by the ethanol injection method. The pH-driven method, which is organic solvent-free and easily scalable for industrial production, is thus a promising method for the preparation of curcumin liposomes.

Storage Stability and Antibacterial Activity of Eugenol Nanoliposomes Prepared by an Ethanol Injection-Dynamic High-Pressure Microfluidization Method

Eugenol is a major phenolic component with diverse biological activities. However, it is difficult to formulate into an aqueous solution due to poor water solubility, and this limits its application. In the present study, eugenol nanoliposomes (EN) were prepared by combining the ethanol injection method with the dynamic high-pressure microfluidization method. Good physicochemical characterizations of EN were obtained. The successful encapsulation of eugenol in nanoliposomes was confirmed by Fourier transform infrared spectroscopy. A good storage stability of EN was confirmed by its low variation of average particle diameter and encapsulation efficiency after 8 weeks of storage. No oil drops were found in EN after 8 weeks of storage at 4°C and at room temperature, which suggested that the poor water solubility of eugenol was overcome by nanoliposome encapsulation. Compared with that of eugenol solution, a relatively good sustained release property was observed in EN. The antibacterial activity of EN against four common foodborne pathogenic bacteria (Staphylococcus aureus, Escherichia coli, Salmonella enterica serovar Typhimurium, and Listeria monocytogenes) was evaluated in both Luria broth and milk medium.

Pluronics modified liposomes for curcumin encapsulation: Sustained release, stability and bioaccessibility

The present work evaluated the feasibility of different pluronics (F127, F87 and P85) utilized as modifiers to improve the stability and bioaccessibility of curcumin liposomes (cur-Lps). Pluronics modified curcumin liposomes (cur-pluronic-Lps) were prepared by thin film evaporation combined with dynamic high pressure microfluidization. The particle size and polydispersity index of cur-pluronic-Lps was significantly lower than cur-Lps. Fourier transform infrared spectroscopy analysis revealed that curcumin was loaded in liposomes successfully and X-ray diffraction suggested that curcumin in the liposomes was in an amorphous state. In vitro release studies demonstrated that 73.4%, 63.9%, 66.7% and 58.9% curcumin released from cur-Lps, cur-F127-Lps, cur-F87-Lps and cur-P85-Lps, respectively. Compared with cur-Lps, cur-pluronic-Lps showed a slower release rate and lower cumulative release percentage for curcumin. Non-Fickian transport was the main release mechanism for cur-Lps, cur-F127-Lps and cur-F87-Lps, and typically the first-order model fitted cur-P85-Lps release. Stability studies (exposure to solutions of different pH and heat treatment) indicated that pluronics modification could enhance their pH stability and thermal stability. In vitro simulated gastrointestinal tract studies suggested that pluronics modification could significantly improve the absorption of cur-Lps. Bioaccessibility of curcumin liposomes increased in the following order: cur-Lps < cur-F87-Lps < cur-P85-Lps < cur-F127-Lps. These results may guide the potential application of pluronics modified liposomes as carriers of curcumin in nutraceutical and functional foods.

Enhancement of curcumin bioavailability by encapsulation in Sophorolipid-coated nanoparticles: An in vitro and in vivo study

There is great interest in developing colloidal delivery systems to enhance the water solubility and oral bioavailability of curcumin, which is a hydrophobic nutraceutical claimed to have several health benefits. In this study, a natural emulsifier was used to form sophorolipid-coated curcumin nanoparticles. The curcumin was loaded into sophorolipid micelles using a pH-driven mechanism based on the decrease in curcumin solubility at lower pH values. The sophorolipid-coated curcumin nanoparticles formed using this mechanism were relatively small (61 nm) and negatively charged (-41 mV). The nanoparticles also had a relatively high encapsulation efficiency (82%) and loading capacity (14%) for curcumin, which was present in an amorphous state. Both in vitro and in vivo studies showed that the curcumin nanoparticles had an appreciably higher bioavailability than that of free curcumin crystals (2.7-3.6-fold), which was mainly attributed to their higher bioaccessibility. These results may facilitate the development of natural colloidal systems that enhance the oral bioavailability and bioactivity of curcumin in food, dietary supplements, and pharmaceutical products.

Effect of dynamic high pressure microfluidization on structure and stability of pluronic F127 modified liposomes

Abstract Pluronics modified liposomes have been prepared and shown to enhance stability of liposomes in our previous reports. In this study, we intended to evaluate the effect of dynamic high pressure microfluidization (DHPM) on the structure and stability of pluronic F127 modified liposomes. The results indicated that the particle size of F127 modified liposomes was decreased from 1180.6 nm to 73.5 nm after DHPM treatment. Meanwhile, the morphology was changed from irregularly multilamellar vesicle to spherically unilamellar structure. Structural characteristics were examined by fourier transformed infrared spectrometer, differential scanning calorimetry and X-ray powder diffraction. The subtle difference of structure might be attributed to the incorporation of PPO chains into the bilayer caused by DHPM treatment. Stability studies indicated that DHPM treatment could enhance the storage and membrane stability of F127 modified liposomes. This study may provide more insight to understand the effect of preparation method on the structure and stability of F127 modified liposomes. GRAPHICAL ABSTRACT

Impact of Delivery System Type on Curcumin Bioaccessibility: Comparison of Curcumin-Loaded Nanoemulsions with Commercial Curcumin Supplements

In this study, nanoemulsion-based delivery systems fabricated using three different methods were compared with three commercially available curcumin supplements. Powdered curcumin was dispersed into the oil-in-water nanoemulsions using three methods: the conventional oil-loading method, the heat-driven method, and the pH-driven method. The conventional method involved dissolving powdered curcumin in the oil phase (60 °C, 2 h) and then forming a nanoemulsion. The heat-driven method involved forming a nanoemulsion and then adding powdered curcumin and incubating at an elevated temperature (100 °C, 15 min). The pH-driven method involved dissolving curcumin in an alkaline solution (pH 12.5) and then adding this solution to an acidified nanoemulsion (pH 6.0). The three commercial curcumin products were capsules or tablets purchased from an online supplier: Nature Made, Full Spectrum, and CurcuWin. Initially, the encapsulation efficiency of the curcumin in the three nanoemulsions was determined and decreased in the following order: pH-driven (93%) > heat-driven (76%) > conventional (56%) method. The different curcumin formulations were then subjected to a simulated gastrointestinal tract (GIT) model consisting of mouth, stomach, and small intestine phases. All three nanoemulsions had fairly similar curcumin bioaccessibility values (74-79%) but the absolute amount of curcumin in the mixed micelle phase was highest for the pH-driven method. A comparison of these nanoemulsions and commercial products indicated that the curcumin concentration in the mixed micelles decreased in the following order: CurcuWin ≈ pH-driven method > heat-driven method > conventional method ≫ Full spectrum > Nature Made. This study provides valuable information about the impact of the delivery system type on curcumin bioavailability. It suggests that encapsulating curcumin within small lipid particles may be advantageous for improving its absorption form the GIT.