scholarly journals Alginate-amphothericin B Nanocomplexes Covered by Nanocrystals From Bacterial Cellulose: Physico-chemical Characterization and in Vitro Toxicity

2020 ◽  
Author(s):  
Victória Soares Soeiro ◽  
Ricardo Silva-Carvalho ◽  
Daniela Martins ◽  
Pier Parpot ◽  
Denise Grotto ◽  
...  
Keyword(s):  
Water Solubility ◽  
Chemical Characterization ◽  
Therapeutic Use ◽  
Water Soluble ◽  
In Vitro Toxicity ◽  
Small Surface ◽  
Nanostructured Systems ◽  
Additional Protection ◽  
Anti Fungal

Abstract Background: Nanostructured systems free of surfactants have pharmacotechnical and biopharmaceutical advantages, in addition to being a green process. Amphotericin B (AmB) is a drug with anti-leishmanial and anti-fungal potential, but its low water solubility and permeability limit its therapeutic use. Therefore, it could profit from being incorporated into nanostructured systems. In the present study, a self-assembled nanocomplex of alginate (Alg), a polysaccharide extracted from natural sources that can be used in the pharmaceutical area, with AmB was produced in order to improve the limited therapeutic use of this drug (Alg-AmB). Further, as a reinforcing component, cellulose nanocrystals (NCC) were ionically adsorbed into the surface of the nanocomplex systems (Alg-AmB + NCC). Results: Despite some polydispersity (0.523 ± 0.073), this straightforward process allowed to obtain water soluble particles with a hydrodynamic size of 258.87 ± 10.41 nm and charge of -62.93 ± 2.02 mV. Furthermore, the ionic adsorption of the NCC into the Alg-AmB nanocomplex surface was confirmed by an increase in the particle size (466.3 ± 17.57 nm) and a small surface charge decrease (-55.75 ± 1.23 mV). The amorphous inclusion complex of AmB into the polysaccharide chain network in both formulations was confirmed by DSC and FTIR. AmB in the nanocomplexes was in supper-aggregated form and showed good biocompatibility, being significantly less cytotoxic in vitro against kidney cells and significantly less hemolytic comparatively to the free-drug. Conclusions: The results were indicated the Alg-AmB nanocomplex can be considered an economical, non-toxic alternative to improve the AmB therapeutic effect. Furthermore, NCC coating of the nanocomplexes brought additional protection to the system without compromised the advantages attributed to the developed formulation.

scholarly journals Alginate-Amphothericin B Nanocomplexes Covered By Nanocrystals From Bacterial Cellulose: Physico-Chemical Characterization And In Vitro Toxicity

2021 ◽  
Author(s):  
Victória Soares Soeiro ◽  
Ricardo Silva-Carvalho ◽  
Daniela Martins ◽  
Pier Parpot ◽  
Denise Grotto ◽  
...  
Keyword(s):  
Water Solubility ◽  
Chemical Characterization ◽  
Water Soluble ◽  
In Vitro Toxicity ◽  
Small Surface ◽  
Physico Chemical ◽  
Nanostructured Systems ◽  
Additional Protection ◽  
Anti Fungal

Abstract Amphotericin B (AmB) is a drug with anti-leishmanial and anti-fungal ability, but it has low water solubility and permeability, limiting its therapeutic use. Therefore, the incorporation of AmB into nanostructured systems could be profit. Nanostructured systems without surfactants have pharmacotechnical advantages such as amplify the water solubility and decrease the toxicity. For this reason, the present study aimed to produce a nanocomplex of alginate (Alg) with AmB covered by NCC in order to decrease the toxicity of AmB. This straightforward process allowed to obtain water soluble particles Furthermore, the ionic adsorption of the NCC into the Alg-AmB nanocomplex surface was confirmed by an increase in the particle size and a small surface charge decrease. The amorphous inclusion of AmB complex into the polysaccharide chain network in both formulations. AmB in the nanocomplexes was in supper-aggregated form and showed good biocompatibility, being significantly less cytotoxic in vitro against kidney cells and significantly less hemolytic compared to the free-drug. The results indicated the Alg-AmB nanocomplex can be considered a non-toxic alternative to improve the AmB therapeutic effect. Furthermore, NCC coating of the nanocomplexes brought additional protection to the system without compromised the advantages attributed to the developed formulation.

scholarly journals Alginate-amphotericin B nanocomplexes covered by nanocrystals from bacterial cellulose: physico-chemical characterization and in vitro toxicity

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Victória Soares Soeiro ◽  
Ricardo Silva-Carvalho ◽  
Daniela Martins ◽  
Pier Parpot ◽  
Denise Grotto ◽  
...  
Keyword(s):  
Bacterial Cellulose ◽  
Amphotericin B ◽  
Water Solubility ◽  
Chemical Characterization ◽  
Water Soluble ◽  
In Vitro Toxicity ◽  
Physico Chemical ◽  
Additional Protection ◽  
Anti Fungal

AbstractNanocomplexes systems made up natural poylymers have pharmacotechnical advantages such as increase of water solubility and a decrease of drugs toxicity. Amphotericin B (AmB) is a drug apply as anti-leishmanial and anti-fungal, however it has low water solubility and high toxicity, limiting its therapeutic application. With this in mind, the present study aimed to produce nanocomplexes composed by alginate (Alg), a natural polymer, with AmB covered by nanocrystals from bacterial cellulose (CNC). For this reason, the nanocomplexes were produced utilizing sodium alginate, amphotericin B in a borate buffer (pH 11.0). The CNC was obtained by enzymatic hydrolysis of the bacterial cellulose. To CNC cover the nanocomplexes 1 ml of the nanocomplexes was added into 1 ml of 0.01% CNC suspension. The results showed an ionic adsorption of the CNC into the Alg-AmB nanocomplexes surface. This phenomena was confirmed by an increase in the particle size and PDI decrease. Besides, nanocomplexes samples covered by CNC showed uniformity. The amorphous inclusion of AmB complex into the polysaccharide chain network in both formulations. AmB in the nanocomplexes was in supper-aggregated form and showed good biocompatibility, being significantly less cytotoxic in vitro against kidney cells and significantly less hemolytic compared to the free-drug. The in vitro toxicity results indicated the Alg-AmB nanocomplexes can be considered a non-toxic alternative to improve the AmB therapeutic effect. All process to obtain nanocomplexes and it coat was conduce without organic solvents, can be considered a green process, and allowed to obtain water soluble particles. Furthermore, CNC covering the nanocomplexes brought additional protection to the system can contribut advancement in the pharmaceutical.

Formulation and Evaluation of Benidipine Nanosuspension

2021 ◽  
pp. 4111-4116
Author(s):  
Sejal Patel ◽  
Anita P. Patel
Keyword(s):  
Particle Size ◽  
Water Solubility ◽  
Polymer Concentration ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
Selection Of

In the interest of administration of dosage form oral route is most desirable and preferred method. After oral administration to get maximum therapeutic effect, major challenge is their water solubility. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is poorly water soluble antihypertensive drug has lower bioavailability. To improve bioavailability of Benidipine HCL, BND nanosuspension was formulated using media milling technique. HPMC E5 was used to stabilize nanosuspension. The effect of different important process parameters e.g. selection of polymer concentration X1(1.25 mg), stirring time X2 (800 rpm), selection of zirconium beads size X3 (0.4mm) were investigated by 23 factorial design to accomplish desired particle size and saturation solubility. The optimized batch had 408 nm particle size Y1, and showed in-vitro dissolution Y2 95±0.26 % in 30 mins and Zeta potential was -19.6. Differential scanning calorimetry (DSC) and FT-IR analysis was done to confirm there was no interaction between drug and polymer.

scholarly journals Considerable Improvement of Ursolic Acid Water Solubility by Its Encapsulation in Dendrimer Nanoparticles: Design, Synthesis and Physicochemical Characterization

Nanomaterials ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 2196 ◽  
Author(s):  
Silvana Alfei ◽  
Anna Maria Schito ◽  
Guendalina Zuccari
Keyword(s):  
Ursolic Acid ◽  
Water Solubility ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Systemic Toxicity ◽  
Water Soluble ◽  
Design Synthesis ◽  
Pentacyclic Triterpenoid

Ursolic acid (UA) is a pentacyclic triterpenoid found in many medicinal plants and aromas endowed with numerous in vitro pharmacological activities, including antibacterial effects. Unfortunately, UA is poorly administered in vivo, due to its water insolubility, low bioavailability, and residual systemic toxicity, thus making urgent the development of water-soluble UA formulations. Dendrimers are nonpareil macromolecules possessing highly controlled size, shape, and architecture. In dendrimers with cationic surface, the contemporary presence of inner cavities and of hydrophilic peripheral functions, allows to encapsulate hydrophobic non-water-soluble drugs as UA, to enhance their water-solubility and stability, and to promote their protracted release, thus decreasing their systemic toxicity. In this paper, aiming at developing a new UA-based antibacterial agent administrable in vivo, we reported the physical entrapment of UA in a biodegradable not cytotoxic cationic dendrimer (G4K). UA-loaded dendrimer nanoparticles (UA-G4K) were obtained, which showed a drug loading (DL%) much higher than those previously reported, a protracted release profile governed by diffusion mechanisms, and no cytotoxicity. Also, UA-G4K was characterized by principal components analysis (PCA)-processed FTIR spectroscopy, by NMR and elemental analyses, and by dynamic light scattering experiments (DLS). The water solubility of UA-G4K was found to be 1868-fold times higher than that of pristine UA, thus making its clinical application feasible.

scholarly journals Soy Protein-Based Composite Hydrogels: Physico-Chemical Characterization and In Vitro Cytocompatibility

Polymers ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 1159 ◽  
Author(s):  
Samira Tansaz ◽  
Raminder Singh ◽  
Iwona Cicha ◽  
Aldo Boccaccini
Keyword(s):  
Soft Tissue ◽  
Metabolic Activity ◽  
Soy Protein ◽  
Colorimetric Assay ◽  
Umbilical Vein ◽  
Chemical Characterization ◽  
Dermal Fibroblasts ◽  
Water Soluble ◽  
Composite Hydrogels

Novel composite hydrogels based on the combination of alginate (Alg), soy protein isolate (SPI) and bioactive glass (BG) nanoparticles were developed for soft tissue engineering. Human umbilical vein endothelial cells (HUVEC) and normal human dermal fibroblasts were cultivated on hydrogels for 7, 14 and 21 days. Cell morphology was visualized using fluorescent staining at Days 7 and 14 for fibroblast cells and Days 14 and 21 for HUVEC. Metabolic activity of cells was analyzed using a colorimetric assay (water soluble tetrazolium (WST) assay). Compared to pure Alg, Alg/SPI and Alg/SPI/BG provided superior surfaces for both types of cells, supporting their attachment, growth, spreading and metabolic activity. Fibroblasts showed better colonization and growth on Alg/SPI/BG hydrogels compared to Alg/SPI hydrogels. The results indicate that such novel composite hydrogels might find applications in soft tissue regeneration.

Development and Characterization of the Neuroregenerative Xanthohumol C/Hydroxypropyl-β-cyclodextrin Complex Suitable for Parenteral Administration

Planta Medica ◽  
2019 ◽  
Vol 85 (16) ◽  
pp. 1233-1241
Author(s):  
Michael Kirchinger ◽  
Lara Bieler ◽  
Julia Tevini ◽  
Michael Vogl ◽  
Elisabeth Haschke-Becher ◽  
...  
Keyword(s):  
Water Solubility ◽  
Pharmaceutical Research ◽  
Water Soluble ◽  
Complexing Agents ◽  
Cyclodextrin Complex ◽  
Scanning Calorimetry ◽  
In Vivo Experiments ◽  
Strong Candidate

AbstractThe chroman-like chalcone Xanthohumol C, originally found in hops, was demonstrated to be a potent neuroregenerative and neuroprotective natural product and therefore constitutes a strong candidate for further pharmaceutical research. The bottleneck for in vivo experiments is the low water solubility of this chalcone. Consequently, we developed and validated a suitable formulation enabling in vivo administration. Cyclodextrins were used as water-soluble and nontoxic complexing agents, and the complex of Xanthohumol C and 2-hydroxypropyl-β-cyclodextrin was characterized using HPLC, HPLC-MS, NMR, and differential scanning calorimetry. The water solubility of Xanthohumol C increases with increasing concentrations of cyclodextrin. Using 50 mM 2-hydroxypropyl-β-cyclodextrin, solubility was increased 650-fold. Furthermore, in vitro bioactivity of Xanthohumol C in free and complexed form did not significantly differ, suggesting the release of Xanthohumol C from 2-hydroxypropyl-β-cyclodextrin. Finally, a small-scaled in vivo experiment in a rat model showed that after i. p. administration of the complex, Xanthohumol C can be detected in serum, the brain, and the cerebrospinal fluid at 1 and 6 h post-administration. Mean (± SD) Xanthohumol C serum concentrations after 1, 6, and 12 h were determined as 463.5 (± 120.9), 61.9 (± 13.4), and 9.3 (± 0.8) ng/mL upon i. v., and 294.3 (± 22.4), 45.5 (± 0.7), and 13 (± 1.0) ng/mL after i. p. application, respectively. Accordingly, the formulation of Xanthohumol C/2-hydroxypropyl-β-cyclodextrin is suitable for further in vivo experiments and further pharmaceutical research aiming for the determination of its neuroregenerative potential in animal disease models.

Exploration on the adsorption mechanism of aminopyrimidines and quinazoline compounds on graphene oxide: Hydrophobicity and structure-controlled release process

2019 ◽  
Vol 9 (5) ◽  
pp. 419-428
Author(s):  
Li Li ◽  
Chunjiao Pan ◽  
Zhongqiu Guo ◽  
Bingmi Liu ◽  
Hao Pan ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
Computer Simulations ◽  
Water Solubility ◽  
High Water ◽  
Water Soluble ◽  
Release Process ◽  
Adsorption Mechanisms ◽  
Mechanical Stirring

In this study, graphene oxide was synthesized using the Hummers method, and stable and homogeneous graphene oxide aqueous solutions were obtained through mechanical stirring and ultrasonic stripping. In conjunction with our previous studies, graphene oxide-loaded insoluble compound delivery systems were prepared to verify the in vivo release profiles of the graphene oxide delivery system. Several insoluble compounds including imatinib, nilotinib, erlotinib, gefitinib, and afatinib were selected for loading and in vitro graphene oxide release assays to study the non-covalent adsorption mechanisms. Computer simulations were employed for validation processes. For in vivo release assays, the T1/2 values of the poorly water soluble groups were 1.104 ± 0.18 h and the Cmax was 2.600 ± 2.06 mg/L. In previous assays, compounds with high water solubility supported by graphene oxide were released and detected in vivo. The solubility of the compound and its binding force with the carrier played a crucial role in release. The results of graphene oxide loading experiments showed that the maximum loading and entrapment efficiencies of the insoluble model compounds with similar aromatic rings were comparable. Under basic conditions, the in vitro release rates and maximum release levels of amino pyrimidine were elevated. In contrast, quinazoline release declined. Combined with computer simulations, π–π stacking was identified as the dominant mechanism for adsorption onto graphene oxide. Both hydrogen bonding and cation-π bonds played an auxiliary reinforcing role, and the two were regarded as antagonistic.

scholarly journals Formulation and In-Vitro Evaluation of Meloxicam Solid Dispersion using Natural Polymers.

2021 ◽  
Vol 30 (1) ◽  
pp. 169-178
Author(s):  
Hiba Radhi ALhassani ◽  
Eman B. H. Al-Khedairy
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Oral Absorption ◽  
Chemical Interaction ◽  
Water Soluble ◽  
Natural Polymers ◽  
Drug Content ◽  
Percentage Yield

Meloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug.     The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers. Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content,  water solubility,  dissolution, crystal lattice using powder X-ray diffraction (PXRD) and studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-polymer interaction. All the prepared showed improvement of drug solubility except that prepared with HA. The best result was obtained with formula SD1 (MLX: SA 1:1) that showed a high percentage yield (97), high drug content (97.4±0.05) and increase in solubility compared to solubility of pure MLX with improved dissolution rate. the PXRD study revealed the conversion of the drug to amorphous form without chemical interaction according to FTIR results

scholarly journals Combretastatins: An Overview of Structure, Probable Mechanisms of Action and Potential Applications

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2560 ◽  
Author(s):  
Gökçe Şeker Karatoprak ◽  
Esra Küpeli Akkol ◽  
Yasin Genç ◽  
Hilal Bardakcı ◽  
Çiğdem Yücel ◽  
...  
Keyword(s):  
South African ◽  
Water Solubility ◽  
The Body ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Lead Compounds ◽  
Combretastatin A4 ◽  
Potential Applications

Combretastatins are a class of closely related stilbenes (combretastatins A), dihydrostilbenes (combretastatins B), phenanthrenes (combretastatins C) and macrocyclic lactones (combretastatins D) found in the bark of Combretum caffrum (Eckl. & Zeyh.) Kuntze, commonly known as the South African bush willow. Some of the compounds in this series have been shown to be among the most potent antitubulin agents known. Due to their structural simplicity many analogs have also been synthesized. Combretastatin A4 phosphate is the most frequently tested compounds in preclinical and clinical trials. It is a water-soluble prodrug that the body can rapidly metabolize to combretastatin A4, which exhibits anti-tumor properties. In addition, in vitro and in vivo studies on combretastatins have determined that these compounds also have antioxidant, anti-inflammatory and antimicrobial effects. Nano-based formulations of natural or synthetic active agents such as combretastatin A4 phosphate exhibit several clear advantages, including improved low water solubility, prolonged circulation, drug targeting properties, enhanced efficiency, as well as fewer side effects. In this review, a synopsis of the recent literature exploring the combretastatins, their potential effects and nanoformulations as lead compounds in clinical applications is provided.

Synthesis and Antibacterial Evaluation of Novel Water-Soluble Organic Peroxides

1998 ◽  
Vol 42 (4) ◽  
pp. 911-915 ◽  
Author(s):  
Wenqiu Liu ◽  
Xuejun Liu ◽  
David Knaebel ◽  
Linda Luck ◽  
Yuzhou Li
Keyword(s):  
Antibacterial Agents ◽  
Water Solubility ◽  
Acne Vulgaris ◽  
Antibacterial Activities ◽  
Water Soluble ◽  
Gram Negative Bacteria ◽  
Organic Peroxides ◽  
Quaternary Ammonium Group ◽  
In Vitro Antibacterial Activity

ABSTRACT A set of new water-soluble organic peroxides has been synthesized and evaluated for in vitro antibacterial activity as part of an effort to develop new antibacterial agents for the treatment of acne vulgaris. The water solubility of these new dialkyl peroxides and peroxyesters was achieved by incorporating either a quaternary ammonium group or a polyethylene glycol moiety. These peroxides are effective against both gram-positive and gram-negative bacteria and have a prolonged activity compared to that of benzoyl peroxide and other peroxide-type antiseptic agents. Among them 4-[[(tert-butylperoxy)carbonyl]benzyl]triethylammonium chloride and [10-(tert-butylperoxy)decyl]trimethylammonium bromide have the broadest antimicrobial spectrums. We have shown that the oxidizing properties of the dioxy group of these compounds are responsible for their antibacterial activities.

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