The Effect of pH and Sodium Caseinate on the Aqueous Solubility, Stability, and Crystallinity of Rutin towards Concentrated Colloidally Stable Particles for the Incorporation into Functional Foods

Poor water solubility and low bioavailability of hydrophobic flavonoids such as rutin remain as substantial challenges to their oral delivery via functional foods. In this study, the effect of pH and the addition of a protein (sodium caseinate; NaCas) on the aqueous solubility and stability of rutin was studied, from which an efficient delivery system for the incorporation of rutin into functional food products was developed. The aqueous solubility, chemical stability, crystallinity, and morphology of rutin (0.1–5% w/v) under various pH (1–11) and protein concentrations (0.2–8% w/v) were studied. To manufacture the concentrated colloidally stable rutin–NaCas particles, rutin was dissolved and deprotonated in a NaCas solution at alkaline pH before its subsequent neutralisation at pH 7. The excess water was removed using ultrafiltration to improve the loading capacity. Rutin showed the highest solubility at pH 11, while the addition of NaCas resulted in the improvement of both solubility and chemical stability. Critically, to achieve particles with colloidal stability, the NaCas:rutin ratio (w/w) had to be greater than 2.5 and 40 respectively for the lowest (0.2% w/v) and highest (4 to 8% w/v) concentrations of NaCas. The rutin–NaCas particles in the concentrated formulations were physically stable, with a size in the range of 185 to 230 nm and zeta potential of −36.8 to −38.1 mV, depending on the NaCas:rutin ratio. Encapsulation efficiency and loading capacity of rutin in different systems were 76% to 83% and 2% to 22%, respectively. The concentrated formulation containing 5% w/v NaCas and 2% w/v rutin was chosen as the most efficient delivery system due to the ideal protein:flavonoid ratio (2.5:1), which resulted in the highest loading capacity (22%). Taken together, the findings show that the delivery system developed in this study can be a promising method for the incorporation of a high concentration of hydrophobic flavonoids such as rutin into functional foods.

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A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2021.14.4.1 ◽

2021 ◽

Vol 14 (4) ◽

pp. 5519-5228

Author(s):

Sunitha M Reddy ◽

Sravani Baskarla

Keyword(s):

Drug Delivery ◽

Dissolution Rate ◽

Drug Delivery System ◽

Delivery System ◽

Drug Delivery Systems ◽

Water Solubility ◽

Drug Loading ◽

Aqueous Solubility ◽

Delivery Systems ◽

Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.

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Designing Highly Stable Poly(sarcosine)-based Telodendrimer Micelles with High Drug Content Exemplified with Fulvestrant

10.26434/chemrxiv-2021-p3jf5 ◽

2021 ◽

Author(s):

Qing Yu ◽

Richard England ◽

Anders Gunnarsson ◽

Robert Luxenhofer ◽

Kevin Treacher ◽

...

Keyword(s):

Colloidal Stability ◽

Water Solubility ◽

High Efficiency ◽

Polymeric Micelles ◽

Drug Loading ◽

Polymeric Micelle ◽

Chemotherapeutic Agents ◽

Loading Capacity ◽

High Drug ◽

Linear Poly

Polymeric micelles have been extensively used as nanocarriers for the delivery of chemotherapeutic agents aiming to improve their efficacy in cancer treatment. However, poor loading capacity, premature drug release, non-uniformity and reproducibility still remain the major challenges. To create a stable polymeric micelle with high drug loading, a telodendrimer micelle was developed as a nanocarrier for fulvestrant, as an example of a drug that has extremely poor water solubility (sub nanomolar range). Telodendrimers were prepared by synthesis of a hydrophilic linear poly(sarcosine) and growing a lysine dendron from the chain terminal amine by a divergent synthesis. At the periphery of the dendritic block, 4, 8, and 16 fulvestrant molecules were conjugated to the lysine dendron creating a hydrophobic block. Having drug as part of the carrier not only reduces the usage of the inert carrier materials but also prevent the drugs from leakage and premature release by diffusion. The self-assembled telodendrimer micelles demonstrated good colloidal stability (CMC < 2 µM) in buffer and were uniform in size. In addition, these telodendrimer micelles could solubilize additional fulvestrant yielding an excellent overall drug loading capacity of up to 77 wt.% total drug load (summation of conjugated and encapsulated). Importantly, the size of the micelles could be tuned between 25-150 nm by controlling (i) the ratio between hydrophilic and hydrophobic blocks and (ii) the amount of encapsulated fulvestrant. The versatility of these telodendrimer-based micelle systems to both conjugate and encapsulate drug with high efficiency and stability, in addition to possessing other tuneable properties makes it a promising drug delivery system for a range of active pharmaceutical ingredients and therapeutic targets.

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SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2016.v9s2.13180 ◽

2016 ◽

pp. 33

Author(s):

Sonia Anand ◽

Rishikesh Gupta ◽

Prajapati Sk

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Water Solubility ◽

Oral Absorption ◽

Aqueous Solubility ◽

Class Ii ◽

Oral Route ◽

Oral Drug ◽

Liquid Form

ABSTRACT Oral route is the most convenient route of drug administration in many diseases and till today it is the first way investigated in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility, thereby pretense problems in their formulation. More than 40% of potential drug products suffer from poor water solubility. For the therapeutic delivery of lipophilic active moieties (biopharmaceutical classification system Class II drugs), lipid-based formulations are inviting increasing attention. Currently, a number of technologies are available to deal with the poor solubility, dissolution rate, and bioavailability of insoluble drugs. One of the promising techniques is self-microemulsifying drug delivery systems (SMEDDS). SMEDDS have gained exposure for their ability to increase solubility and bioavailability of poorly soluble drugs. SMEDDS, which are isotropic mixtures of oils, surfactants, solvents, and co-solvents/surfactants can be used for the design of formulations to improve the oral absorption of highly lipophilic drug compounds. Conventional SMEDDS are mostly prepared in a liquid form, which can have some disadvantages. SMEDDS can be orally administered in soft or hard gelatin capsules and form fine relatively stable oil-in-water emulsions. Solid-SMEDDS are prepared by solidification of liquid/semisolid self-micron emulsifying ingredients into powders, have gained popularity. This article gives a complete overview of SMEDDS, but special attention has been paid to formulation, design, evaluation, and little emphasis on application of SMEDDS. Keywords: Self-microemulsifying drug delivery system, Surfactant, Oil, Co-surfactant, Bioavailability, Lipophilic, Biopharmaceutical classification system Class II drugs.

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Self Microemulsifying Nutraceutical and Drug Delivery Systems

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2014.7.3.3 ◽

2014 ◽

Vol 7 (3) ◽

pp. 2520-2528 ◽

Cited By ~ 1

Author(s):

Vikrant P Wankhade ◽

Nivedita S Kale ◽

K.K Tapar

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Ternary Phase Diagram ◽

Aqueous Solubility ◽

Oral Formulation ◽

Water Soluble ◽

Drug Dissolution ◽

The Novel ◽

Peristaltic Movement

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.

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Multi-Walled Carbon Nanotubes Decorated with Guanidinylated Dendritic Molecular Transporters: An Efficient Platform for the Selective Anticancer Activity of Doxorubicin

Pharmaceutics ◽

10.3390/pharmaceutics13060858 ◽

2021 ◽

Vol 13 (6) ◽

pp. 858

Author(s):

Kyriaki-Marina Lyra ◽

Archontia Kaminari ◽

Katerina N. Panagiotaki ◽

Konstantinos Spyrou ◽

Sergios Papageorgiou ◽

...

Keyword(s):

Carbon Nanotubes ◽

Anticancer Activity ◽

Cancer Cells ◽

Delivery System ◽

Colloidal Stability ◽

Triggered Release ◽

Selective Toxicity ◽

Molecular Transporters ◽

Multi Walled Carbon Nanotubes ◽

Walled Carbon Nanotubes

An efficient doxorubicin (DOX) drug delivery system with specificity against tumor cells was developed, based on multi-walled carbon nanotubes (MWCNTs) functionalized with guanidinylated dendritic molecular transporters. Acid-treated MWCNTs (oxCNTs) interacted both electrostatically and through hydrogen bonding and van der Waals attraction forces with guanidinylated derivatives of 5000 and 25,000 Da molecular weight hyperbranched polyethyleneimine (GPEI5K and GPEI25K). Chemical characterization of these GPEI-functionalized oxCNTs revealed successful decoration with GPEIs all over the oxCNTs sidewalls, which, due to the presence of guanidinium groups, gave them aqueous compatibility and, thus, exceptional colloidal stability. These GPEI-functionalized CNTs were subsequently loaded with DOX for selective anticancer activity, yielding systems of high DOX loading, up to 99.5% encapsulation efficiency, while the DOX-loaded systems exhibited pH-triggered release and higher therapeutic efficacy compared to that of free DOX. Most importantly, the oxCNTs@GPEI5K-DOX system caused high and selective toxicity against cancer cells in a non-apoptotic, fast and catastrophic manner that cancer cells cannot recover from. Therefore, the oxCNTs@GPEI5K nanocarrier was found to be a potent and efficient nanoscale DOX delivery system, exhibiting high selectivity against cancerous cells, thus constituting a promising candidate for cancer therapy.

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Fennel essential oil loaded porous starch-based microencapsulation as an efficient delivery system for the quality improvement of ground pork

International Journal of Biological Macromolecules ◽

10.1016/j.ijbiomac.2021.01.090 ◽

2021 ◽

Vol 172 ◽

pp. 464-474

Author(s):

Yanan Sun ◽

Min Zhang ◽

Bhesh Bhandari ◽

Baosong Bai

Keyword(s):

Quality Improvement ◽

Essential Oil ◽

Delivery System ◽

Efficient Delivery ◽

Ground Pork

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Fabrication of 239/238Pu-Zirconolite Ceramic Pellets by Natural Sintering

MRS Proceedings ◽

10.1557/proc-807-267 ◽

2003 ◽

Vol 807 ◽

Cited By ~ 2

Author(s):

T. Advocat ◽

F. Jorion ◽

T. Marcillat ◽

G. Leturcq ◽

X. Deschanels ◽

...

Keyword(s):

Grain Size ◽

Radioactive Waste ◽

Nuclear Waste ◽

Chemical Stability ◽

Minor Actinides ◽

Loading Capacity ◽

X Ray Diffraction ◽

X Ray ◽

Physical And Chemical ◽

Inorganic Matrix

ABSTRACTZirconolite is a potential inorganic matrix that is currently investigated in France, in the framework of the 1991 radioactive waste management law, with a view to provide durable containment of the trivalent and tetravalent minor actinides like neptunium, curium, americium and small quantities of unrecyclable plutonium separated from other nuclear waste. To confirm the actinide loading capacity of the zirconolite calcium site and to study the physical and chemical stability of this type of ceramic when subjected to alpha self-irradiation, zirconolite ceramic pellets were fabricated with 10 wt% plutonium oxide (isotope 239 or 238). The 55 pellets are dense (> 93.3% of the theoretical density on average) and free of cracks. They are characterized by a grain size of between 10 and 20 micrometers. X-ray diffraction analyses confirmed the presence of the zirconolite 2M crystalline structure.

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The Effect of pH and Viscosity on Magnetophoretic Separation of Iron Oxide Nanoparticles

Magnetochemistry ◽

10.3390/magnetochemistry7060080 ◽

2021 ◽

Vol 7 (6) ◽

pp. 80

Author(s):

Leonie Wittmann ◽

Chiara Turrina ◽

Sebastian P. Schwaminger

Keyword(s):

Iron Oxide ◽

Iron Oxide Nanoparticles ◽

Colloidal Stability ◽

Downstream Processing ◽

Physicochemical Characteristics ◽

Particle Migration ◽

Aggregation Behavior ◽

Oxide Nanoparticles ◽

Separation Processes ◽

Effect Of Ph

Magnetic nanoparticles (MNPs) are used for magnetophoresis-based separation processes in various biomedical and engineering applications. Essential requirements are the colloidal stability of the MNPs and the ability to be separated even in low magnetic field gradients. Bare iron oxide nanoparticles (BIONs) with a diameter of 9.2 nm are synthesized via coprecipitation, exhibiting a high saturation magnetization of 70.84 Am2 kg−1 and no remanence. In our study, zeta potential, dynamic light scattering (DLS), and sedimentation analysis show that the aggregation behavior of BIONs is influenced by pH and viscosity. Small aggregate clusters are formed with either low or high pH values or increased viscosity. Regarding magnetophoresis-based separation, a higher viscosity leads to lower magnetophoretic velocities, similar to how small aggregates do. Additionally, cooperative magnetophoresis, the joint motion of strongly interacting particles, affects the separation of the BIONs, too. Our study emphasizes the effect of pH and viscosity on the physicochemical characteristics of MNPs, resulting in different aggregation behavior. Particularly, for high viscous working media in downstream processing and medicine, respectively, the viscosity should be taken into account, as it will affect particle migration.

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The Emerging Role of Nanosuspensions for Drug Delivery and Stability

Current Nanomedicine ◽

10.2174/2468187312666211222123307 ◽

2021 ◽

Vol 12 ◽

Author(s):

Hitesh Kumar Dewangan

Keyword(s):

Water Solubility ◽

Size Range ◽

Aqueous Solubility ◽

Active Surface ◽

Water Soluble ◽

Active Surface Area ◽

Specific Interest ◽

Advanced Therapies ◽

Processing Techniques

: Poor solubility of some medicinal compounds is a serious challenge that can be addressed by using a nano-suspension for improved delivery. The nanoparticles enhance the bioavailability along with the aqueous solubility of the drug, which is accomplished by increasing the active surface area of the drug. The gained attention of the nanosuspension is due to its stabilization facility, which is achieved by polymers, such as polyethylene glycol (PEG), having a particular size range of 10 - 100 nm. Hence, these nanoparticles have the capacity of binding to the targeted with very low damage to the healthy tissues. These are prepared by various methods, such as milling, high-pressure homogenization, and emulsification, along with melt emulsification. Moreover, surface modification and solidification have been used to add specific properties to the advanced therapies as post-processing techniques. For many decades, it has been known that water solubility hampers the bioavailability and not all drugs are water-soluble. In order to combat this obstacle, nanotechnology has been found to be of specific interest. For elevating the bioavailability by increasing the dissolution rate, the methodology of reduction of the associated drug particles into their subsequent submicron range is incorporated. For oral and non-oral administration, these nanosuspension formulations are used for the delivery of drugs.

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