scholarly journals Development of the technology for obtaining new hydrogel materials based on acrylic monomers

2017 ◽  
pp. 20-29
Author(s):  
Nazerke Nurabay ◽  
M. Abutalip ◽  
Raikhan Rakhmetullayeva ◽  
Grigoriy Mun
Keyword(s):  
Acrylic Acid ◽  
Drug Carrier ◽  
Antibacterial Properties ◽  
Homogeneous Solution ◽  
Radical Copolymerization ◽  
Water Soluble ◽  
Effect Of Temperature ◽  
Stimuli Responsive ◽  
Scanning Calorimetry ◽  
Smart Water

Smart water-soluble polymers and hydrogels are capable to reversibly react to insignificant changes of the medium properties (pH, temperature, ionic strength, a presence of some substances, illumination, electric field). The reacting of a system is visible to the naked eye (the formation of a new phase in a homogeneous solution, or compression of the hydrogel). The properties of such polymers and hydrogels are considered. For the first time, the stimuli-responsive polymeric hydrogels based on N-isopropylacrylamide (NIPAAM), 2-hydroxyethyl acrylate (HEA) and acrylic acid (AA) have been synthesized by free initiation of radical copolymerization. The purpose of the research is to obtain stimuli-responsive cross-linked terpolymers based on N-isopropylacrylamide, 2-hydroxyethyl acrylate and acrylic acid and study their physicochemical properties. The physicochemical methods such as scanning electron microscopy, differential scanning calorimetry, infrared spectroscopy, gravimetry, cathetometric and thermogravimetric analyses were used in this study. To determine the thermal and pH – sensitivity of the modified copolymer, the effect of temperature on the NIPAAM-НEA-AA nets (in different pH media) was studied. They are characterized by a thermally induced collapse and a dependence on a medium pH. The interaction of copolymers with drugs such as lincomycin and gentamicin was studied for using the new copolymers as a drug carrier. To study the antibacterial properties and the transportation of physiologically active substances of hydrogel, the elimination of specially prepared bacteria by hydrogels with various medicinal ingredients were conducted.

scholarly journals Development and Characterization of Glimepiride Novel Solid Nanodispersion for Improving Its Oral Bioavailability

2020 ◽  
Vol 88 (4) ◽  
pp. 52
Author(s):  
Mona Qushawy ◽  
Ali Nasr ◽  
Shady Swidan ◽  
Yasmin Mortagi
Keyword(s):  
Solid Dispersion ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Water Soluble ◽  
Production Yield ◽  
Scanning Calorimetry ◽  
Differential Scanning Calorimetry Study ◽  
Drug Content ◽  
Vitro Release

Glimepiride is an antidiabetic drug which is one of the third generation sulfonylureas. It belongs to class II, according to the BCS (Biopharmaceutical Classification System), which is characterized by low solubility and high permeability. The aim of this work was to formulate glimepiride as solid dispersion using water-soluble carriers to enhance its aqueous solubility and thus enhance its bioavailability. Nine formulations of glimepiride solid dispersion were prepared by a solvent evaporation technique using three different carriers (mannitol, polyethylene glycol 6000, and β-cyclodextrin) with three different drug carrier ratio (1:1, 1:3, and 1:6). Formulation variables were optimized using 32 full factorial design. The prepared formulations were evaluated for production yield, drug content, micromeritic properties, thermal analysis, in-vitro release, and in-vivo hypoglycemic effect. All prepared formulations showed high production yield ranged from 98.4 ± 2.8 to 99.8 ± 2.2% and high drug content in the range of 97.2 ± 3.2 to 99.6 ± 2.1%. The micromeritic properties revealed that all prepared glimepiride formulations showed good flowability. The differential scanning calorimetry study revealed the presence of the drug in the more soluble amorphous form. In accordance with the results of in vitro release study, it was found that the solubility of glimepiride was increased by increasing the drug carrier ratio, compared with the pure form of the drug. It was found that F9 showed a high and rapid reduction in blood glucose levels in diabetic rats, which indicated the success of a solid dispersion technique in improving the solubility and hence the bioavailability of glimepiride.

Miniemulsion Polymerization Stabilized by a Well-Defined, Amphiphilic Gradient Poly(styrene-co-acrylic acid) Copolymer

2006 ◽  
Vol 59 (8) ◽  
pp. 544 ◽  
Author(s):  
Catherine Lefay ◽  
Maud Save ◽  
Bernadette Charleux ◽  
Stéphanie Magnet
Keyword(s):  
Particle Size ◽  
Acrylic Acid ◽  
Methyl Methacrylate ◽  
Butyl Acrylate ◽  
Miniemulsion Polymerization ◽  
Radical Copolymerization ◽  
Water Soluble ◽  
Size Distributions ◽  
Particle Size Distributions ◽  
Free Radical Copolymerization

The nitroxide-mediated controlled free-radical copolymerization of styrene (St) and acrylic acid (AA) was used to synthesize a well-defined poly(St30%-co-AA70%) amphiphilic gradient copolymer. The latter proved to be an efficient stabilizer in the 45 wt.-% solids content, batch miniemulsion polymerizations of St and of mixtures of methyl methacrylate/n-butyl acrylate (35/65 w/w). With 2,2´-azobisisobutyronitrile as an oil-soluble initiator, polystyrene latexes with a very narrow particle distribution were obtained, whereas the water-soluble initiator, potassium persulfate, led to broad, multimodal particle size distributions. Such results were explained by the contribution of two nucleation mechanisms: droplet nucleation and homogeneous nucleation. In contrast, the poly(methyl methacrylate-co-n-butyl acrylate) latexes exhibited larger particle size and narrower particle size distributions with persulfate initiator, than the polystyrene latexes.

scholarly journals Strong Antimicrobial Activity of Highly Stable Nanocomposite Containing AgNPs Based on Water-Soluble Triazole-Sulfonate Copolymer

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 206
Author(s):  
Alexander Pozdnyakov ◽  
Artem Emel’yanov ◽  
Anastasiya Ivanova ◽  
Nadezhda Kuznetsova ◽  
Tat’yana Semenova ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Chemical Reduction ◽  
Gel Permeation Chromatography ◽  
Radical Copolymerization ◽  
Water Soluble ◽  
Morphological Properties ◽  
Hydrodynamic Diameter ◽  
Scanning Calorimetry ◽  
Free Radical Copolymerization ◽  
Strong Antimicrobial Activity

A new hydrophilic polymeric nanocomposite containing AgNPs was synthesized by chemical reduction of metal ions in an aqueous medium in the presence of the copolymer. A new water-soluble copolymer of 1-vinyl-1,2,4-triazole and vinylsulfonic acid sodium salt (poly(VT-co-Na-VSA)) was obtained by free-radical copolymerization and was used as a stabilizing precursor agent. The structural, dimensional, and morphological properties of the nanocomposite were studied by UV–Vis, FTIR, X-ray diffraction, atomic absorption, transmission and scanning electron microscopy, dynamic and electrophoretic light scattering, gel permeation chromatography, thermogravimetric analysis, and differential scanning calorimetry. Hydrodynamic diameter of macroclubs for the copolymer was 171 nm, and for the nanocomposite it was 694 nm. Zeta potential for the copolymer was −63.8 mV, and for the nanocomposite it was −70.4 mV. The nanocomposite had strong antimicrobial activity towards Gram-negative and Gram-positive microorganisms: MIC and MBC values were in the range of 0.25–4.0 and 0.5–8.0 μg/mL, respectively.

scholarly journals Wrinkling on Stimuli-Responsive Functional Polymer Surfaces as a Promising Strategy for the Preparation of Effective Antibacterial/Antibiofouling Surfaces

Polymers ◽  
2021 ◽  
Vol 13 (23) ◽  
pp. 4262
Author(s):  
Carmen M. González-Henríquez ◽  
Fernando E. Rodríguez-Umanzor ◽  
Matías N. Alegría-Gómez ◽  
Claudio A. Terraza-Inostroza ◽  
Enrique Martínez-Campos ◽  
...  
Keyword(s):  
Methylene Blue ◽  
Acrylic Acid ◽  
Antibacterial Properties ◽  
Chemical Properties ◽  
Stimuli Responsive ◽  
Release Capacity ◽  
Carboxylic Groups ◽  
Wrinkled Surface ◽  
Surface Patterns ◽  
Adsorption Desorption

Biocompatible smart interfaces play a crucial role in biomedical or tissue engineering applications, where their ability to actively change their conformation or physico-chemical properties permits finely tuning their surface attributes. Polyelectrolytes, such as acrylic acid, are a particular type of smart polymers that present pH responsiveness. This work aims to fabricate stable hydrogel films with reversible pH responsiveness that could spontaneously form wrinkled surface patterns. For this purpose, the photosensitive reaction mixtures were deposited via spin-coating over functionalized glasses. Following vacuum, UV, or either plasma treatments, it is possible to spontaneously form wrinkles, which could increase cell adherence. The pH responsiveness of the material was evaluated, observing an abrupt variation in the film thickness as a function of the environmental pH. Moreover, the presence of the carboxylic acid functional groups at the interface was evidenced by analyzing the adsorption/desorption capacity using methylene blue as a cationic dye model. The results demonstrated that increasing the acrylic acid in the microwrinkled hydrogel effectively improved the adsorption and release capacity and the ability of the carboxylic groups to establish ionic interactions with methylene blue. Finally, the role of the acrylic acid groups and the surface topography (smooth or wrinkled) on the final antibacterial properties were investigated, demonstrating their efficacy against both gram-positive and gram-negative bacteria model strains (E. coli and S. Aureus). According to our findings, microwrinkled hydrogels presented excellent antibacterial properties improving the results obtained for planar (smooth) hydrogels.

scholarly journals Formulation, Development, Evaluation and Solubility Enhancement of Lercanidipine Hydrochloride by Solid Dispersion Techniques

2021 ◽  
pp. 195-213
Author(s):  
S. D. Mankar ◽  
Punit R. Rachh
Keyword(s):  
Solid State ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Onset Of Action ◽  
Drug Molecules ◽  
Lercanidipine Hydrochloride

Background: Solid dispersions (SDs) are the dispersion of hydrophobic drugs in an inert hydrophilic carrier. SDs are prepared to improve the dissolution properties and bioavailability of slightly water-soluble drug molecules by dispersing them into an inert hydrophilic carrier. Aims and Objective: Evaluate the dissolution and solubility of Solid Dispersion of Lercanidipine Hydrochloride (LER). Materials and Methods: To study the effect of polymer, dissolution and solubility studies were carried out. Solid state characterizations of prepared solid dispersions were performed by differential scanning calorimetry (DSC).Drug- carrier interactions were studied by FT-IR spectroscopy, whereas X-ray diffraction of powder was done to demonstrate the crystal structure of the dispersions. Results: The prepared solid dispersion exhibited 94% drug release at 30 minutes which is higher than both LER pure and LER MKT. Better dissolution characteristic of solid dispersion was confirmed by 9.86 min MDT and 63.12% DE30 which is higher than that of LER MKT (13.64 MDT, 46.92 % DE30) Solid state characterization revealed that enhancement of dissolution is the result of conversion of crystalline form of LER to less crystalline and/or amorphous form. Conclusion: Solid dispersion of LER can successfully be prepared with the PEG6000 in the ratio of 1:6 using solvent evaporation technique. It is a successful and easy approach for the increase in onset of action of drug after administration and facilitates treatment of cardiovascular diseases.

scholarly journals Thermal Behaviour of Microgels Composed of Interpenetrating Polymer Networks of Poly(N-isopropylacrylamide) and Poly(Acrylic Acid): A Calorimetric Study

Polymers ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 115
Author(s):  
Silvia Franco ◽  
Elena Buratti ◽  
Valentina Nigro ◽  
Monica Bertoldo ◽  
Barbara Ruzicka ◽  
...  
Keyword(s):  
Transition Temperature ◽  
Acrylic Acid ◽  
Polymer Networks ◽  
State Diagram ◽  
Interpenetrating Polymer Networks ◽  
Phase Behaviour ◽  
Calorimetric Study ◽  
Stimuli Responsive ◽  
Scanning Calorimetry ◽  
Poly Acrylic Acid

Stimuli-responsive microgels have recently attracted great attention in fundamental research as their soft particles can be deformed and compressed at high packing fractions resulting in singular phase behaviours. Moreover, they are also well suited for a wide variety of applications such as drug delivery, tissue engineering, organ-on-chip devices, microlenses fabrication and cultural heritage. Here, thermoresponsive and pH-sensitive cross-linked microgels, composed of interpenetrating polymer networks of poly(N-isopropylacrylamide) (PNIPAM) and poly(acrylic acid) (PAAc), are synthesized by a precipitation polymerization method in water and investigated through differential scanning calorimetry in a temperature range across the volume phase transition temperature of PNIPAM microgels. The phase behaviour is studied as a function of heating/cooling rate, concentration, pH and PAAc content. At low concentrations and PAAc contents, the network interpenetration does not affect the transition temperature typical of PNIPAM microgel in agreement with previous studies; on the contrary, we show that it induces a marked decrease at higher concentrations. DSC analysis also reveals an increase of the overall calorimetric enthalpy with increasing concentration and a decrease with increasing PAAc content. These findings are discussed and explained as related to emerging aggregation processes that can be finely controlled by properly changing concentration, PAAc content an pH. A deep analysis of the thermodynamic parameters allows to draw a temperature– concentration state diagram in the investigated concentration range.

Smart Polymers and their Applications: A Review

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Gore S. A. ◽  
Gholve S. B. ◽  
Savalsure S. M. ◽  
Ghodake K. B. ◽  
Bhusnure O. G. ◽  
...  
Keyword(s):  
Oil Recovery ◽  
Water Soluble ◽  
Solution Temperature ◽  
Smart Polymers ◽  
Stimuli Responsive ◽  
Responsive Materials ◽  
Water Soluble Polymers ◽  
Commercial Applications ◽  
Stimuli Sensitive ◽  
External Stimuli

Smart polymers are materials that respond to small external stimuli. These are also referred as stimuli responsive materials or intelligent materials. Smart polymers that can exhibit stimuli-sensitive properties are becoming important in many commercial applications. These polymers can change shape, strength and pore size based on external factors such as temperature, pH and stress. The stimuli include salt, UV irradiation, temperature, pH, magnetic or electric field, ionic factors etc. Smart polymers are very promising applicants in drug delivery, tissue engineering, cell culture, gene carriers, textile engineering, oil recovery, radioactive wastage and protein purification. The study is focused on the entire features of smart polymers and their most recent and relevant applications. Water soluble polymers with tunable lower critical solution temperature (LCST) are of increasing interest for biological applications such as cell patterning, smart drug release, DNA sequencing etc.

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.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

Amorphous and Crystalline Particulates: Challenges and Perspectives in Drug Delivery

2017 ◽  
Vol 23 (3) ◽  
pp. 350-361 ◽  
Author(s):  
Hisham Al-Obaidi ◽  
Mridul Majumder ◽  
Fiza Bari
Keyword(s):  
Crystal Engineering ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Chemical Properties ◽  
Pharmaceutical Product ◽  
Water Soluble ◽  
Amorphous Form ◽  
Physico Chemical ◽  
Water Soluble Drugs ◽  
Amorphous Drug

Crystalline and amorphous dispersions have been the focus of academic and industrial research due to their potential role in formulating poorly water-soluble drugs. This review looks at the progress made starting with crystalline carriers in the form of eutectics moving towards more complex crystalline mixtures. It also covers using glassy polymers to maintain the drug as amorphous exhibiting higher energy and entropy. However, the amorphous form tends to recrystallize on storage, which limits the benefits of this approach. Specific interactions between the drug and the polymer may retard this spontaneous conversion of the amorphous drug. Some studies have shown that it is possible to maintain the drug in the amorphous form for extended periods of time. For the drug and the polymer to form a stable mixture they have to be miscible on a molecular basis. Another form of solid dispersions is pharmaceutical co-crystals, for which research has focused on understanding the chemistry, crystal engineering and physico-chemical properties. USFDA has issued a guidance in April 2013 suggesting that the co-crystals as a pharmaceutical product may be a reality; but just not yet! While some of the research is still oriented towards application of these carriers, understanding the mechanism by which drug-carrier miscibility occurs is also covered. Within this context is the use of thermodynamic models such as Flory-Huggins model with some examples of studies used to predict miscibility.

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