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.

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-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.

Complexation with Hydroxypropyl-gama-Cyclodextrin of Birch Tree Extract Physico-chemical Characterisation of their Binary Products

2008 ◽  
Vol 59 (6) ◽  
Author(s):  
Codruta Soica ◽  
Cristina A. Dehelean ◽  
Valentin Ordodi ◽  
Diana Antal ◽  
Vicentiu Vlaia
Keyword(s):  
Inclusion Complexes ◽  
Water Solubility ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Bark Extract ◽  
Birch Bark ◽  
Preparation Methods ◽  
Birch Tree ◽  
Physico Chemical

Birch bark contains important pentacyclic triterpens that determine an anticancer, anti-inflammatory and antiviral activity. The compounds can be extracted by simple procedures with organic solvents. The major problem of this type of triterpens is their low water solubility which can be increased by physical procedures like cyclodextrin complexation. The aim of present study was to analyse the products between birch bark extract and hydroxypropyl-g -cyclodextrin. Hydroxypropyl-g -cyclodextrin (HPGCD) was used as a host to improve its solubility in water, via inclusion complex formation. In order to obtain the inclusion complexes, 1:2 molar ratio and two preparation methods (physical mixing, kneading) were used. The inclusion complexes were analyzed by in vitro dissolution tests, thermal analysis and X-ray diffraction.

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.

Antibody targeting of lipid nanocapsules for directed drug delivery: physico-chemical characterization and in vitro study

2010 ◽  
Vol 15 (23-24) ◽  
pp. 1105-1105
Author(s):  
P. Sánchez-Moreno ◽  
H. Boulaiz ◽  
J.A. Marchal ◽  
J.L. Ortega-Vinuesa ◽  
J.M. Peula García ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Chemical Characterization ◽  
In Vitro Study ◽  
Vitro Study ◽  
Lipid Nanocapsules ◽  
Physico Chemical ◽  
Antibody Targeting

scholarly journals In Vitro Physico-Chemical Characterization and Standardized In Vivo Evaluation of Biocompatibility of a New Synthetic Membrane for Guided Bone Regeneration

Materials ◽  
2019 ◽  
Vol 12 (7) ◽  
pp. 1186
Author(s):  
Lívia da Costa Pereira ◽  
Carlos Fernando de Almeida Barros Mourão ◽  
Adriana Terezinha Neves Novellino Alves ◽  
Rodrigo Figueiredo de Brito Resende ◽  
Marcelo José Pinheiro Guedes de Uzeda ◽  
...  
Keyword(s):  
Bone Regeneration ◽  
Chemical Properties ◽  
Chemical Characterization ◽  
Guided Bone Regeneration ◽  
Tissue Reaction ◽  
In Vivo Evaluation ◽  
Physico Chemical ◽  
Tissue Reactions

This study’s aim was to evaluate the biocompatibility and bioabsorption of a new membrane for guided bone regeneration (polylactic-co-glycolic acid associated with hydroxyapatite and β-tricalcium phosphate) with three thicknesses (200, 500, and 700 µm) implanted in mice subcutaneously. Scanning electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, and the quantification of carbon, hydrogen and nitrogen were used to characterize the physico-chemical properties. One hundred Balb-C mice were divided into 5 experimental groups: Group 1—Sham (without implantation); Group 2—200 μm; Group 3—500 μm; Group 4—700 μm; and Group 5—Pratix®. Each group was subdivided into four experimental periods (7, 30, 60 and 90 days). Samples were collected and processed for histological and histomorphometrical evaluation. The membranes showed no moderate or severe tissue reactions during the experimental periods studied. The 500-μm membrane showed no tissue reaction during any experimental period. The 200-μm membrane began to exhibit fragmentation after 30 days, while the 500-μm and 700-µm membranes began fragmentation at 90 days. All membranes studied were biocompatible and the 500 µm membrane showed the best results for absorption and tissue reaction, indicating its potential for clinical guided bone regeneration.

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.

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