The Emerging Role of Nanosuspensions for Drug Delivery and Stability

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.

Review: Emerging role of nanosuspensions for drug delivery and stability

2021 ◽  
Vol 06 ◽  
Author(s):  
Hitesh Kumar Dewangan ◽  
Brijesh Yadav ◽  
Manas Kumar Jha
Keyword(s):  
Drug Delivery ◽  
Size Range ◽  
Aqueous Solubility ◽  
Active Surface ◽  
Active Surface Area ◽  
Drug Molecules ◽  
Media Milling ◽  
Advanced Therapies ◽  
Processing Techniques

: Poor aqueous solubility of some of the drug molecules are of a major concern, which can be emerged in the nano-suspension for better delivery. Coming up to the nanoparticles, it enhances 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 done by polymers such as polyethylene glycol (PEG) having a particular size range of 10-100 nm. Hence, to our notice, these nanoparticles have the capacity of binding in the targeted parts with a very low damage to the healthy tissues. These are seen to be prepared by various methods such as media milling, high pressure homogenization, and emulsification along with melt emulsification. Apart it can also be seen that surface modification and solidification have been used to add specific properties to the advanced therapies as post-processing techniques. These days, it is very evident that the drugs are water insoluble and thus have a poor bioavailability which have been developed from the drug delivery programmes and in order to combat this obstacle, nanotechnology have been found to be of specific interest. In order to elevate the bioavailability by increasing the dissolution rate, the methodology of reduction of the associated drug particles into its subsequent submicron range is incorporated. For oral and non-oral administration, these nanosuspensions formulations are used for delivering of the drugs.

scholarly journals Nanosuspension Technologies for Delivery of Poorly Soluble Drugs

2015 ◽  
Vol 2015 ◽  
pp. 1-13 ◽  
Author(s):  
Roya Yadollahi ◽  
Krasimir Vasilev ◽  
Spomenka Simovic
Keyword(s):  
Aqueous Solubility ◽  
Drug Formulation ◽  
Preparation Methods ◽  
Administration Routes ◽  
Drug Molecules ◽  
Advanced Therapies ◽  
Poorly Soluble ◽  
Minimal Damage ◽  
Processing Techniques ◽  
Cancer Tissues

Poor aqueous solubility of some drug molecules is a major problem in drug formulation. Drug nanosuspensions emerged as one solution to delivering such hydrophobic drugs. Scaling down to nanoparticles enhances drug aqueous solubility and bioavailability by increasing drug surface area that comes into contact with biological media. Nanosuspensions that have attracted particular attention are those sterically stabilised by steric polymers such as polyethylene glycol (PEG) with a typical size range of 10–100 nm. These nanoparticles are capable of accumulating in targeted areas such as cancer tissues and infarct zones with minimal damage to healthy tissues. Nanosuspensions are often prepared by commercially available methods such as high pressure homogenization, media milling, emulsification, and melt emulsification. Solidification and surface modification methods are post-processing techniques used to add particular properties for advanced therapies. In this review, we firstly describe preparation methods for nanosuspensions. Secondly, we highlight typical characterization techniques. Finally, we describe several practical application of applications for drug delivery design and different administration routes such as parenteral, pulmonary, oral, and ocular.

Role of Surfactant in Peritoneal Dialysis

2000 ◽  
Vol 20 (5) ◽  
pp. 503-515 ◽  
Author(s):  
Brian A. Hills
Keyword(s):  
Peritoneal Dialysis ◽  
Water Solubility ◽  
Adhesion Formation ◽  
Mesothelial Cell ◽  
Water Soluble ◽  
Cell Junctions ◽  
Pathogen Invasion ◽  
Water Transmission ◽  
Future Direction

Evidence is reviewed that demonstrates how the mesothelial cell in the normal peritoneum and comparable serosal cavities secretes surface-active phospholipid (SAPL) as a means of protecting itself and the membrane it forms with its neighbors. It is shown how SAPL, if adsorbed (reversibly bound) to mesothelium, can impart excellent lubricity, antiwear and release (antistick) properties, while impeding surgical adhesion formation. More-speculative benefits include acting as a deterrent to fibrosis and as a barrier to both protein leakage and pathogen invasion by spanning cell junctions. Such spanning would also “pin down” cell corners, impeding peeling as the first step in exfoliation encountered in prolonged continuous ambulatory peritoneal dialysis (CAPD). The molecular mechanism underlying each of these possible functions is adsorption. Morphological and hydrophobicity studies are discussed as validation for such an adsorbed lining and how it can be fortified by administering exogenous SAPL. Any role for SAPL in ultrafiltration is much more controversial. However, a surfactant lining can explain the very high permeability of the membrane to lipid-soluble drugs, implying that it is a barrier to water-soluble solutes. The clinical and animal evidence is conflicting but would seem to be best explained by a role for the barrier in promoting semipermeability, and hence the osmotic driving force for water transmission. Thus, adsorption of exogenous SAPL in CAPD patients with low ultrafiltration seems to restore this barrier function. The future direction for surfactant in CAPD would seem to rest with the physical chemists in producing formulations that optimize adsorption, probably involving a compromise between water solubility and surface activity of the phospholipids selected. It might even warrant using the interdialytic interval for re-adsorbing SAPL without the problem of dilution by a large volume of dialysate.

scholarly journals CD Oxyanions as a Tool for Synthesis of Highly Anionic Cyclodextrin Polymers

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2845
Author(s):  
Tomasz Girek ◽  
Kinga Koziel ◽  
Beata Girek ◽  
Wojciech Ciesielski
Keyword(s):  
Metal Ion ◽  
Water Solubility ◽  
Polymer Network ◽  
Synthesis Method ◽  
Molecular Size ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Alkaline Media ◽  
Hydroxyl Groups ◽  
Wide Range

Water soluble highly anionic β-cyclodextrin-based polymers were synthesized by reaction between cyclodextrin oxyanion and pyromellitic anhydride. The synthesis method utilizes activation hydroxyl groups in anhydrous glucopyranosyl units (AGU) in the DMF solution with the use of NaH. In these conditions, like in the case of the cyclodextrin reactions in the highly alkaline media, there is a nucleophilic substitution of difunctional compounds, which develops a polymer network with various cyclodextrin substitution. Different molar ratios of the reagents were investigated in terms of molecular size, chemical structure and water solubility of the polymers. The separation of the polymer due to particle size by ultrafiltration process and HPSEC-MALLS-RI and MALDI-TOF MS measurements for molecular mass analysis were employed. The IR, H NMR, SEM, DSC and TG measurements were taken for the structural characterization of the polymers. Additionally, the solubility test and metal ion complexation processes were also investigated in a wide range of pH. These polymers could be used in several areas such as: improving the aqueous solubility of poor water-soluble molecules, removing heavy metals from waste water, protecting degradable substances or synthesizing new drug delivery systems.

scholarly journals The Dissolution Study For Sodium Selenite Tablets Using Atomic Absorption Spectrophotometer

2012 ◽  
Vol 9 (4) ◽  
pp. 663-667
Author(s):  
Baghdad Science Journal
Keyword(s):  
Atomic Absorption ◽  
Sodium Selenite ◽  
Water Solubility ◽  
Generic Drugs ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Atomic Absorption Spectrophotometer ◽  
Drug Products ◽  
Mechanical Methods

The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to both the pharmaceutical industry and the agencies that regulate them. Natural surfactants aid in the dissolution and subsequent absorption of drugs with limited aqueous solubility. In vitro, various techniques have been used to achieve adequate dissolution of the sparingly water – soluble or water insoluble drug products such as the use of mechanical methods (i.e., increased agitation and the disintegration method) or hydro alcoholic medium or large volumes of medium. The necessity of assuring the quality of drugs , especially those with low aqueous solubility and in vivo absorption , has led to the development and evaluation of new techniques that can reduce the time and cost of analysis. This study has been examines the efficiency and accuracy of an automated dissolution system, fitted with a simple, integrated, for analysis of generic drugs. Sodium Selenite 200 ?g tablets was chosen as model drugs for this study and comparison was made with a conventional analysis based on flameless atomic absorption spectrophotometer (AAS). The analytical system under study gave reproducible and accurate results. Low instrumentation cost was demonstrated which is provide satisfactory elemental drugs analysis to a standard at least as good as that achieved using AAS.

scholarly journals Anesthetic Related Advances with Cyclodextrins

2007 ◽  
Vol 7 ◽  
pp. 364-371 ◽  
Author(s):  
Mark Welliver ◽  
John P. McDonough
Keyword(s):  
Drug Delivery ◽  
Supramolecular Chemistry ◽  
Water Solubility ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Component Part ◽  
Recent Advances ◽  
Unique Ability

Cyclodextrins encapsulate and electrostatically bind to lipophilic molecules. The exterior of cyclodextrins are water-soluble and maintain aqueous solubility despite encapsulation of non-aqueous soluble molecules. This unique ability to encapsulate lipophilic molecules and maintain water solubility confers numerous pharmacologic advantages for both drug delivery and removal. Cyclodextrins, a component part of supramolecular chemistry, may be in its infancy of anesthetic application but recent advances have been described as novel and revolutionary. A review of current research coupled with an understanding of cyclodextrin properties is necessary to fully appreciate the current uses and future potentials of these unique molecules.

BODIPY Fluorophores for Membrane Potential Imaging

2019 ◽  
Author(s):  
Jenna Franke ◽  
Benjamin Raliski ◽  
Steven Boggess ◽  
Divya Natesan ◽  
Evan Koretsky ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Water Solubility ◽  
Water Soluble ◽  
Voltage Sensitivity ◽  
Chemical Transformations ◽  
Direct Modification ◽  
Biological Compatibility ◽  
Meso Position ◽  
Ionizable Groups ◽  
Boron Center

Fluorophores based on the BODIPY scaffold are prized for their tunable excitation and emission profiles, mild syntheses, and biological compatibility. Improving the water-solubility of BODIPY dyes remains an outstanding challenge. The development of water-soluble BODIPY dyes usually involves direct modification of the BODIPY fluorophore core with ionizable groups or substitution at the boron center. While these strategies are effective for the generation of water-soluble fluorophores, they are challenging to implement when developing BODIPY-based indicators: direct modification of BODIPY core can disrupt the electronics of the dye, complicating the design of functional indicators; and substitution at the boron center often renders the resultant BODIPY incompatible with the chemical transformations required to generate fluorescent sensors. In this study, we show that BODIPYs bearing a sulfonated aromatic group at the meso position provide a general solution for water-soluble BODIPYs. We outline the route to a suite of 5 new sulfonated BODIPYs with 2,6-disubstitution patterns spanning a range of electron-donating and -withdrawing propensities. To highlight the utility of these new, sulfonated BODIPYs, we further functionalize them to access 13 new, BODIPY-based voltage-sensitive fluorophores. The most sensitive of these BODIPY VF dyes displays a 48% ΔF/F per 100 mV in mammalian cells. Two additional BODIPY VFs show good voltage sensitivity (≥24% ΔF/F) and excellent brightness in cells. These compounds can report on action potential dynamics in both mammalian neurons and human stem cell-derived cardiomyocytes. Accessing a range of substituents in the context of a water soluble BODIPY fluorophore provides opportunities to tune the electronic properties of water-soluble BODIPY dyes for functional indicators.

Tenacious Mass Transfer Limitations Drive Catalytic Selectivity during Electrochemical Carbon Dioxide Reduction

2019 ◽  
Author(s):  
Kailun Yang ◽  
Recep Kas ◽  
Wilson A. Smith
Keyword(s):  
Surface Area ◽  
High Surface ◽  
High Surface Area ◽  
Catalyst Layer ◽  
Active Surface ◽  
Active Surface Area ◽  
High Concentration ◽  
Copper Electrodes ◽  
Surface Enhanced ◽  
Local Current

<p>This study evaluated the performance of the commonly used strong buffer electrolytes, i.e. phosphate buffers, during CO<sub>2</sub> electroreduction in neutral pH conditions by using in-situ surface enhanced infrared absorption spectroscopy (SEIRAS). Unfortunately, the buffers break down a lot faster than anticipated which has serious implications on many studies in the literature such as selectivity and kinetic analysis of the electrocatalysts. Increasing electrolyte concentration, surprisingly, did not extend the potential window of the phosphate buffers due to dramatic increase in hydrogen evolution reaction. Even high concentration phosphate buffers (1 M) break down within the potentials (-1 V vs RHE) where hydrocarbons are formed on copper electrodes. We have extended the discussion to high surface area electrodes by evaluating electrodes composed of copper nanowires. We would like highlight that it is not possible to cope with high local current densities on these high surface area electrodes by using high buffer capacity solutions and the CO<sub>2</sub> electrocatalysts are needed to be evaluated by casting thin nanoparticle films onto inert substrates as commonly employed in fuel cell reactions and up to now scarcely employed in CO<sub>2</sub> electroreduction. In addition, we underscore that normalization of the electrocatalytic activity to the electrochemical active surface area is not the ultimate solution due to concentration gradient along the catalyst layer.This will “underestimate” the activity of high surface electrocatalyst and the degree of underestimation will depend on the thickness, porosity and morphology of the catalyst layer. </p> <p> </p>

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

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