scholarly journals Supramolecular Carotenoid Complexes of Enhanced Solubility and Stability—The Way of Bioavailability Improvement

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3947 ◽  
Author(s):  
Focsan ◽  
Polyakov ◽  
Kispert
Keyword(s):  
Food Processing ◽  
Water Solubility ◽  
State Of The Art ◽  
Release Kinetics ◽  
High Sensitivity ◽  
Point Of View ◽  
Water Soluble ◽  
Practical Application ◽  
Bioavailability Enhancement ◽  
Enhanced Solubility

Carotenoids are natural dyes and antioxidants widely used in food processing and in therapeutic formulations. However, their practical application is restricted by their high sensitivity to external factors such as heat, light, oxygen, metal ions and processing conditions, as well as by extremely low water solubility. Various approaches have been developed to overcome these problems. In particular, it was demonstrated that application of supramolecular complexes of “host-guest” type with water-soluble nanoparticles allows minimizing the abovementioned disadvantages. From this point of view, nanoencapsulation of carotenoids is an effective strategy to improve their stability during storage and food processing. Also, nanoencapsulation enhances bioavailability of carotenoids via modulating their release kinetics from the delivery system, influencing the solubility and absorption. In the present paper, we present the state of the art of carotenoid nanoencapsulation and summarize the data obtained during last five years on preparation, analysis and reactivity of carotenoids encapsulated into various nanoparticles. The possible mechanisms of carotenoids bioavailability enhancement by multifunctional delivery systems are also discussed.

scholarly journals Improved Antibacterial Activity of Water-Soluble Nanoformulated Kaempferol and Combretastatin Polyphenolic Compounds

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Y. Santhosh Kumar ◽  
Langeswaran Kulanthaivel ◽  
G. S. Hikku ◽  
R. Saravanan ◽  
Thangavelu Lakshmi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Water Solubility ◽  
Release Kinetics ◽  
Antibacterial Properties ◽  
Polyphenolic Compounds ◽  
Water Soluble ◽  
Aureus Strain ◽  
Significant Activity ◽  
Molecular Vibrations ◽  
Pump System

Kaempferol and combretastatin are polyphenolic compounds derived from plant sources which are known for their antibacterial activity. However, owing to their large size and water insolubility, their antibacterial activity is limited. In this context, the present study focused on the nanoformulation of kaempferol (NF-k) and combretastatin (NF-c) and their influence on water solubility and antibacterial properties. The NF-k and NF-c were prepared using the solvent evaporation method and were thoroughly characterized for evaluating the morphology, molecular vibrations, size, etc. Based on the results, it is observed that the pristine forms of kaempferol and combretastatin drugs get nanoformulated and completely soluble in water. Using particle size analyzer, the particle sizes of NF-k and NF-c were estimated as 334 nm and 260 nm, respectively, which are very fine compared to pristine kaempferol and combretastatin (5193 nm and 1217 nm, respectively). The molecular vibrations that exist in NF-k and NF-c were confirmed by the Fourier transform infrared spectra, where the nanoformulated drug showed lower intensities than the pristine form of kaempferol and combretastatin. The drug release kinetics of the nanoformulated drugs were carried out using the dialysis membrane method and were compared with their pristine forms. Owing to the size effect, the NF-k and NF-c release up to 50% of the drug in a sustained manner till 50 h showing twofold higher concentration than the control where it released 25%. The antibacterial activity was assessed by measuring the optical density at 600 nm using UV-vis spectrophotometer and displayed significant activity against gram-positive Staphylococcus aureus strain. The mechanisms behind the antibacterial activity of NF-k and NF-c were discussed in detail. The activation of ATP-dependent efflux pump system and the blockage of porin channels could be the cause for the bactericidal activity. Our understanding of efflux pumps and their role in antibacterial activity is still in its early stages. No studies have been performed to date using nanoformulations of kaempferol and combretastatin to investigate their roles. This complicates the determination of the exact mechanisms acting against bacterial growth when using nanoformulation drugs. Our increasing knowledge of water-soluble nanoformulation drugs and their roles in reduced bacterial activity will pave the way to developing effective treatments in the future.

Characterisation of Preformulation Parameters to Design, Develop and Formulate Silymarin loaded PLGA Nanoparticles for Liver Targeted Drug Delivery

2021 ◽  
pp. 5508-5514
Author(s):  
Senthila S ◽  
Manojkumar P. ◽  
Venkatesan P.
Keyword(s):  
Water Solubility ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Chemical Properties ◽  
Water Soluble ◽  
Angle Of Repose ◽  
Effect Of Temperature ◽  
Pharmacokinetic Studies ◽  
Bioavailability Enhancement ◽  
Water Soluble Compound

Silymarin, a flavonolignan,derived from Silybum marianum, family Asteraceae has long been used as a hepatoprotective remedy. Silymarin has cytoprotective activities due to its antioxidant property and free radical scavenging activity. It inhibits the binding of hepatotoxins to receptor sites, protects hepatocyte membranes, enhances liver parenchyma regeneration and increases glutathione levels. The pharmacokinetic studies of past three decades revealed that Silymarin has poor absorption, rapid metabolism especially by Phase II metabolism and ultimately poor oral bioavailability. Typical oral adult dose of Silymarin is 240-800mg /day .It is a non-lipophilic and poorly water soluble compound with water solubility of 0.04mg/ml. Only 20-30% of oral Silymarin is absorbed from gastrointestinal tract where it undergoes extensive entero-hepatic circulation. The advanced type of formulation like polymeric nanoparticles (PNPs) can be successfully utilised for bioavailability enhancement and targeting the Silymarin to hepatocytes. A controlled release PNP of Silymarin was prepared by solvent evaporation method using Poly Lactic-co-Glycolic Acid (PLGA) as biodegradable polymer. Prior to the development of this novel dosage form, it is very important to identify fundamental physical and chemical properties of the drug molecule and other divided properties of the drug powder. This data helps in many of the subsequent events and approaches towards the development of a better formulation. Preformulation studies included determination of solubility, moisture content, partition coefficient, melting point , powder properties like tapped density, bulk density, compressibility index, flow properties like angle of repose, excipient compatibility, entrapment efficiency, release profile of nanoparticles like dissolution, stability studies like effect of temperature and humidity and analysis by scanning Electron Microscopy.

A water soluble ratiometric fluorescent probe for targeting SO2 in mitochondria based on conjugated biquinolines

2020 ◽  
Vol 44 (46) ◽  
pp. 20235-20240
Author(s):  
Jialu Yang ◽  
Caixia Yin ◽  
Kaiqing Ma ◽  
Yongkang Yue ◽  
Fangjun Huo
Keyword(s):  
Fluorescent Probe ◽  
Fluorescent Probes ◽  
Water Solubility ◽  
Water Soluble ◽  
Practical Application ◽  
The Past ◽  
Ratiometric Fluorescent Probe

Despite the unprecedented development of SO2 fluorescent probes in the past five years, the water-solubility of these probes is still an important factor related to their practical application.

scholarly journals SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUGS BY VARIOUS TECHNIQUES

2019 ◽  
Vol 8 (1) ◽  
Author(s):  
Sakshi Minocha ◽  
Dr. Shilpa Pahwa ◽  
Dr. Vandana Arora
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Formulation Development ◽  
Particle Size Reduction ◽  
Bioavailability Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Poor Water Solubility

Solubility is not the ability to dissolve or thaw a substance; it may happen not only due to dissolution but also because of a chemical reaction. Solubility is the phenomenon of dissolution of solid in liquid phase to provide a homogenous system. Solubility is one of the vital factors for accomplishing desired concentration of drug in systemic circulation for pharmacological response. Low aqueous solubility is the major problem seen with formulation development of new chemical entities as well as for the generic development. With all new discovered chemical entities about 40% drugs are lipophilic and doesn’t shown therapeutic range due to their poor water solubility. Drug with poor water solubility shows slow dissolution rates, incomplete absorption and low bioavailability when taken orally. Drug solubility and bioavailability enhancement are the important in the formulation of pharmaceuticals. The Biopharmaceutics Classification System shows that Class II and IV drugs have low water solubility, poor dissolution, and low bioavailability. This review mentions different approaches used for the enhancement of the solubility of poorly water-soluble drugs that includes particle size reduction, pH adjustment, and solid dispersion. This describes the techniques of solubilizaton for the attainment of effective absorption and improved bioavailability. Keywords: Solubility, BCS classification, Bioavailability, Solid-dispersion.

scholarly journals Formulation and Evaluation of Silymarin Microcrystals by In- Situ Micronization Technique

2019 ◽  
Vol 28 (1) ◽  
pp. 1-16
Author(s):  
Ala'a Dheia Noor ◽  
Eman B.H. Al-Khedairy
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Water Solubility ◽  
Ultrasonic Method ◽  
Volume Ratio ◽  
Water Soluble ◽  
Particle Size Reduction ◽  
Enhanced Solubility ◽  
Water Soluble Drugs

Silymarin (SM) is a plant extract obtained from Silybum marianum( milk thistle) . It is class II type drug according to  Biopharmaceutics Classification System with low bioavailability due to its low solubility. Micro/nanonization during crystallization, surface modification and crystal structure modification may improve the dissolution rate of poorly water-soluble drugs. The aim of this study was to increase the water solubility and dissolution rate of SM by in-situ micronization using solvent change either by stirring or ultrasonic method. Stabilizers like Gelatin, PVP-K30, HPMC15, Pulullan were used to stabilize the prepared ultrafine crystals. Effect of type and concentration of hydrophilic polymer, solvent: antisolvent volume ratio and the effect of ultrasonic irradiation were studied. The prepared  microcrystals were evaluated for their %yield,  water solubility, crystals structure by XRD,DSC, and SEM. Particle size and  dissolution rate were also tested . Silymarin microcrystals prepared by ultrasonic method and stabilized by 0.1%gelatin using 1:2 solvent: anti-solvent volume ratio showed the best results with particle size reduction from mean diameter of 1.5µm (untrated silymarin) to 0.43µm with uniform morphology and enhanced solubility and  dissolution.

BIOAVAILABILITY ENHANCEMENT OF POORLY-WATER SOLUBLE DRUGS BY SOLID DISPERSION

2012 ◽  
pp. 5-11
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Van Toi Vo
Keyword(s):  
Pharmaceutical Industry ◽  
Solid Dispersion ◽  
State Of The Art ◽  
Water Soluble ◽  
Bioavailability Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Drug Candidates ◽  
Water Soluble Drugs ◽  
Insoluble Drugs ◽  
Poorly Water Soluble

Solubilization of poorly-water soluble drugs is most interesting field in pharmaceutical industry. Currently, up to 40% of new drug candidates have been discovered are water-insoluble drugs. Hence, they have low absorption and bioavailability. Solid dispersion, a popular technique that is currently gaining much attention from pharmaceutical scientists known to improve the solubility and dissolution rate of poorly water-soluble drugs. A number of key references that describe state-of-the-art technologies have been collected in this review, which addresses various pharmaceutical strategies for the solubilization of poorly water-soluble drugs using solid dispersion. Keywords: solid dispersion; poorly water-soluble drugs; dissolution. Key words: Solid dispersion; poorly water-soluble drugs; dissolution

Development of L-lysine amino acid-based cocrystal of Telmisartan using crystal engineering approach to improve solubility, dissolution and micrometric properties

2020 ◽  
Vol 17 ◽  
Author(s):  
Nitin Kumar Bhatt ◽  
Jamshed Haneef ◽  
Manish Vyas ◽  
Gopal L. Khatik
Keyword(s):  
Physical Properties ◽  
Dissolution Rate ◽  
Intermolecular Interaction ◽  
Crystal Engineering ◽  
Water Solubility ◽  
Crystal Packing ◽  
Water Soluble ◽  
Specific Chemical ◽  
Enhanced Solubility ◽  
Water Soluble Drugs

Aim: To develop cocrytsal of telmisartan for enhancing its solubility in water. Background: Intermolecular interaction happens in crystal packing; it utilizes and helps us to understand the design of new solid with their respective chemical and physical properties called that crystal engineering. It is a blueprint of molecular solids with specific chemical and physical properties through an understanding and handling of intermolecular interaction for increasing solubility if poor water-soluble drugs. Objectives: The study was taken under consideration with an aim to generate and synthesize a cocrystal form of telmisartan (TEL) with L-lysine to improve its water solubility, dissolution, and micrometric properties. Methods: A dry grinding technique, solvent evaporation & cooling crystallization, the results revealed a generation of cocrystals with enhanced solubility by liquid drop grinding method. Hence, this process was further explored to investigate various formulation and process parameters that could significantly affect the crystal solubility, dissolution, and micrometric properties. Results: The solubility of TEL cocrystals was enhanced by L-lysine. Further, the optimized batch was subjected to its micrometric evaluation & physiochemical characterization like FT-IR, NMR, PXRD. The result of the micrometric evaluation showed better results as compared to standards. The dissolution studies also showed a better dissolution rate for TEL cocrystal tablets than TEL tablets formulation. Conclusion: Cocrystals of TEL with L-lysine showed better solubility and dissolution rate.

scholarly journals Development, characterization and solubility enhancement of poorly water soluble drug telmisartan by polymer enriched bridging liquid technique using peg 4000 as hydrophilic polymer

2019 ◽  
Vol 10 (3) ◽  
pp. 2234-2241
Author(s):  
Manoj K ◽  
Seenivasan P ◽  
Arul K ◽  
Senthil kumar M
Keyword(s):  
Water Solubility ◽  
Chemical Interaction ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Hydrophilic Polymer ◽  
Formulation Development ◽  
Flow Properties ◽  
Bioavailability Enhancement ◽  
Poorly Water Soluble

The solubility and bioavailability enhancement of poorly water soluble drugs has been a foremost challenge in formulation development. Telmisartan belonging to Angiotension II receptor antagonist, extensively used candidate for the treatment of hypertension possess poor water solubility and bioavailability. Polymer Enriched Bridging Liquid (PEBL) method was adopted here for enhancing the flow properties and solubility of Telmisartan. The techniques involve the incorporation of a hydrophilic polymer, PEG4000 into the bridging liquid during the crystallisation process. The drug content determination suggested the better incorporation of polymer into the crystal aggregates. The FTIR analysis showed the absence of any chemical interaction. The DSC analysis showed a significant reduction in the enthalpy and melting point. The crystallinity of Telmisartan was reduced from 50.789 to 34.655% indicated by the reduction in peak intensity analysis and peak area calculation by X-Ray diffraction. The SEM analysis revealed the spherical nature of crystals resulting in the improvement of flow properties. The saturation solubility analysis revealed that the formulation STPG03 has shown 25.86 fold increase in the solubility in water and 24.217 folds in pH7.5 Phosphate buffer. The in vitro dissolution data also supported the results of solubility analysis. Hence PEBL technique provided a better alternative to enhance the flow characteristics, solubility, dissolution and bioavailability of Telmisartan.

A Facile Synthesis of Nido-Carborane Polymers via Dynamic Self-Assembly by Poly(carboxybetaine methacrylate)

2021 ◽  
Vol 21 (11) ◽  
pp. 5681-5687
Author(s):  
Zhou Wang
Keyword(s):  
Self Assembly ◽  
Water Solubility ◽  
Point Of View ◽  
Water Soluble ◽  
Boron Uptake ◽  
One Pot ◽  
Boron Neutron Capture ◽  
Transmission Electron ◽  
Carborane Polymers ◽  
Harsh Conditions

Carborane are widely applied in boron neutron capture therapy (BNCT) field, but it is difficult to perform biocompatibility with cells due to its own water solubility differences, so how to solve the water solubility problem has always been the focus of research. A simple, inexpensive and effective method was used to study the synthesis of nido-carborane azaspirodecanium poly(carboxybetaine methacrylate) by one-pot cyclization of nido-carborane azaspirodecanium under the synergistic effect of inorganic bases and conventional organic solvents. Its characterization is mainly to use 1H-NMR nuclear magnetic resonance spectrum and infrared spectroscopy to determine the characteristic peak and range of borane. Through transmission electron microscope (TEM), it can be observed that the white nanoparticles, namely carborane, are completely contained by polymer ions, which not only increases the surface area but also the concentration of boron uptake in the cell is 100 times that of borono-phenylalanine (BPA). Based on the successful synthesis of N-CB5-4 and N-CB6-5 without harsh conditions, a feasibility point of view was put forward, namely, super water-soluble carborane polymer.

scholarly journals Novel Delivery System Used for Oral Bioavailability Enhancement of Poorly Water Soluble Drugs

2020 ◽  
Vol 10 (6-s) ◽  
pp. 139-144
Author(s):  
Sunil Kumar Lakavath
Keyword(s):  
Delivery System ◽  
Oral Bioavailability ◽  
Water Solubility ◽  
Delivery Systems ◽  
Water Soluble ◽  
Bioavailability Enhancement ◽  
Major Drawback ◽  
The Poor ◽  
Poorly Water Soluble ◽  
Novel Delivery Systems

Majority of the drugs used for the treatment of various diseases are administered by oral route using conventional delivery. The major drawback of the oral administration is the poor bioavailability due to the poor water solubility, chemical stability and pre-systemic metabolism. Numerous researches are going on for the improvement of oral bioavailability of drugs using novel drug delivery systems as an alternative to conventional delivery systems. Majority of the novel delivery system includes; solid dispersion, sustained, controlled buccal, gastro retentive, nano carrier delivery systems such as lipid nanoparticles, and self-emulsifying systems. The oral bioavailability improvement by these delivery systems might be due to the increased particle size, improved dissolution and/or permeation and subsequently bioavailability of the drugs. In this review, we attempt to discuss the various novel delivery systems developed for the enhancement of oral bioavailability of poorly water soluble therapeutics. Keywords: Oral bioavailability, poor solubility, stability, metabolism, novel delivery systems, nano carriers.

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