scholarly journals Efficient modification of PAMAM G1 dendrimer surface with β-cyclodextrin units by CuAAC: impact on the water solubility and cytotoxicity

RSC Advances ◽  
2020 ◽  
Vol 10 (43) ◽  
pp. 25557-25566
Author(s):  
Kendra Sorroza-Martínez ◽  
Israel González-Méndez ◽  
Ricardo D. Martínez-Serrano ◽  
José D. Solano ◽  
Andrea Ruiu ◽  
...  
Keyword(s):  
Water Solubility ◽  
Drug Carriers ◽  
Clinical Applications ◽  
Amino Groups

The toxicity of the poly(amidoamine) dendrimers (PAMAM) caused by the peripheral amino groups has been a limitation for their use as drug carriers in clinical applications.

scholarly journals Silver Nanocolloids Loaded with Betulinic Acid with Enhanced Antitumor Potential: Physicochemical Characterization and In Vitro Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 152
Author(s):  
Iulia Pinzaru ◽  
Cristian Sarau ◽  
Dorina Coricovac ◽  
Iasmina Marcovici ◽  
Crinela Utescu ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Betulinic Acid ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
A549 Cells ◽  
Drug Carriers ◽  
Biological Evaluation ◽  
Correlation Spectroscopy ◽  
Hydrodynamic Diameter

Betulinic acid (BA), a natural compound with various health benefits including selective antitumor activity, has a limited applicability in vivo due to its poor water solubility and bioavailability. Thus, this study focused on obtaining a BA nano-sized formulation with improved solubility and enhanced antitumor activity using silver nanocolloids (SilCo and PEG_SilCo) as drug carriers. The synthesis was performed using a chemical method and the physicochemical characterization was achieved applying UV-Vis absorption, transmission electron microscopy (TEM), Raman and photon correlation spectroscopy (PCS). The biological evaluation was conducted on two in vitro experimental models—hepatocellular carcinoma (HepG2) and lung cancer (A549) cell lines. The physicochemical characterization showed the following results: an average hydrodynamic diameter of 32 nm for SilCo_BA and 71 nm for PEG_SilCo_BA, a spherical shape, and a loading capacity of 54.1% for SilCo_BA and 61.9% for PEG_SilCo_BA, respectively. The in vitro assessment revealed a cell type- and time-dependent cytotoxic effect characterized by a decrease in cell viability as follows: (i) SilCo_BA (66.44%) < PEG_SilCo_BA (72.05%) < BA_DMSO (75.30%) in HepG2 cells, and (ii) SilCo_BA (75.28%) < PEG_SilCo_BA (86.80%) < BA_DMSO (87.99%) in A549 cells. The novel silver nanocolloids loaded with BA induced an augmented anticancer effect as compared to BA alone.

scholarly journals Competitive Biological Activities of Chitosan and Its Derivatives: Antimicrobial, Antioxidant, Anticancer, and Anti-Inflammatory Activities

2018 ◽  
Vol 2018 ◽  
pp. 1-13 ◽  
Author(s):  
Suyeon Kim
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Biological Properties ◽  
Biomedical Science ◽  
Amino Groups ◽  
Chitosan Oligosaccharides ◽  
Primary Amino ◽  
Anti Inflammatory ◽  
Key Functional Groups ◽  
Application Fields

Chitosan is obtained from alkaline deacetylation of chitin, and acetamide groups are transformed into primary amino groups during the deacetylation. The diverse biological activities of chitosan and its derivatives are extensively studied that allows to widening the application fields in various sectors especially in biomedical science. The biological properties of chitosan are strongly depending on the solubility in water and other solvents. Deacetylation degree (DDA) and molecular weight (MW) are the most decisive parameters on the bioactivities since the primary amino groups are the key functional groups of chitosan where permits to interact with other molecules. Higher DDA and lower MW of chitosan and chitosan derivatives demonstrated higher antimicrobial, antioxidant, and anticancer capacities. Therefore, the chitosan oligosaccharides (COS) with a low polymerization degree are receiving a great attention in medical and pharmaceutical applications as they have higher water solubility and lower viscosity than chitosan. In this review articles, the antimicrobial, antioxidant, anticancer, anti-inflammatory activities of chitosan and its derivatives are highlighted. The influences of physicochemical parameters of chitosan like DDA and MW on bioactivities are also described.

Optical properties of hemicyanines with terminal amino groups and their applications in near-infrared fluorescent imaging of nucleoli

2014 ◽  
Vol 2 (40) ◽  
pp. 7065-7072 ◽  
Author(s):  
Jia-Tao Miao ◽  
Chen Fan ◽  
Ru Sun ◽  
Yu-Jie Xu ◽  
Jian-Feng Ge
Keyword(s):  
Optical Properties ◽  
Near Infrared ◽  
Water Solubility ◽  
Stokes Shift ◽  
Fluorescent Imaging ◽  
Amino Groups ◽  
Long Wave ◽  
Terminal Amino ◽  
Wave Emission ◽  
Low Cytotoxicity

A cellular dye with properties of long-wave emission, large Stokes shift, water solubility, low cytotoxicity, and good photostability is reported.

Automated Determination of Free Amino Groups in Serum and Plasma Using 2,4,6-Trinitrobenzene Sulfonate

1969 ◽  
Vol 15 (9) ◽  
pp. 891-901 ◽  
Author(s):  
D W Palmer ◽  
T Peters
Keyword(s):  
Amino Acids ◽  
Free Amino Acids ◽  
Free Amino ◽  
Clinical Applications ◽  
Amino Groups ◽  
Automated Method ◽  
Total Free Amino Acids ◽  
Colored Complexes ◽  
Automated Determination

Abstract A simple automated method is described for determining the level of total free amino acids in the blood. The method utilizes the AutoAnalyzer, and is based on the formation of colored complexes by uniting free amino groups with 2,4,6-trinitrobenzene sulfonate (TNBS). Proteins do not interfere because the free amino acids are first separated by dialysis. Characteristics of the reaction and potential clinical applications of the procedure are discussed.

scholarly journals Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer

2011 ◽  
Vol 61 (4) ◽  
pp. 465-472 ◽  
Author(s):  
Marijana Končič ◽  
Branka Zorc ◽  
Predrag Novak
Keyword(s):  
Drug Delivery ◽  
Water Solubility ◽  
The Other ◽  
Amino Groups ◽  
Chemically Modified ◽  
Drug Conjugates ◽  
17Β Estradiol ◽  
Macromolecular Prodrugs ◽  
Polymer Drug Conjugates ◽  
Estradiol 17Β

Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymerTwo hydrosoluble conjugates of 17β-estradiol (ED) and estradiol-17β-valerate (EV) with polyaspartamide polymer were prepared and characterized. ED and EV were first chemically modified and bound to poly[α,β-(N-2-hydroxyethyl-DL-aspartamide)]-poly[α,β-(N-2-aminoethyl-DL-aspartamide)] (PAHA), a hydrosoluble polyaspartamide-type copolymer bearing both hydroxyl and amino groups. ED was first converted to 17-hemisuccinate (EDS) and then bound to PAHA. In the resulting conjugate PAHA-EDS, the estradiol moiety was linked to the polymer through a 2-aminoethylhemisuccinamide spacer. On the other hand, EV was first converted to estradiol-17β-valerate-3-(benzotriazole-1-carboxylate), which readily reacted with amino groups in PAHA affording the polymer-drug conjugate PAHA-EV. In the prepared conjugate PAHA-EV, the estradiol moiety was covalently bound to the polyaspartamide backbone by carbamate linkage, through an ethylenediamine spacer. The polymer-drug conjugates were designed and prepared with the aim to increase water-solubility, bioavailability and to improve drug delivery of the lipophilic estrogen hormone.

scholarly journals Comparison of triblock copolymeric micelles based on α- and ε-poly(L-lysine): a Cornelian choice

2021 ◽  
Author(s):  
Franck Marquet ◽  
Viorica Patrulea ◽  
Gerrit Borchard
Keyword(s):  
Triblock Copolymer ◽  
Colloidal Stability ◽  
Solid Phase ◽  
Clinical Applications ◽  
Poly Ethylene Glycol ◽  
Amino Groups ◽  
Molecular Weights ◽  
Hydrophobic Compounds ◽  
Poly Ethylene ◽  
Interfering Rna

AbstractDue to the lack of safe carriers for the delivery of small interfering RNA (siRNA), clinical applications of nucleotide-based therapeutics have been limited. In this study, biodegradable amphiphilic triblock copolymers with tailored molecular weights for each block composed of methoxy poly(ethylene glycol) (2000 g/mol), poly(L-lysine) (1300 g/mol) and poly(D,L-lactic acid) (1800 g/mol) (mPEG45-α-PLL10-PLA25) were synthesized and fully characterized. The peptide synthesis was carried out on a solid phase to limit the presence of cationic charges. The arrangement and availability of cationic amino groups within a micellar vector were investigated to determine the colloidal stability as well as the predisposition of these systems to vectorize siRNAs in addition to their already known ability to improve the solubility of hydrophobic compounds. For this purpose, a triblock copolymer containing an epsilon poly(L-lysine) was synthesized similarly. Accordingly, the arrangement of the cationic segment modifies the rigidity involving a complexation constraint due to limited cationic charges available on the surface, which can compromise the efficiency of delivery into cells. In addition, the two vectors were biocompatible in different human cell lines.

scholarly journals Extracellular Vesicles as an Efficient and Versatile System for Drug Delivery

Cells ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 2191 ◽  
Author(s):  
Xuan T. T. Dang ◽  
Jayasinghe Migara Kavishka ◽  
Daniel Xin Zhang ◽  
Marco Pirisinu ◽  
Minh T. N. Le
Keyword(s):  
Extracellular Vesicles ◽  
Drug Carriers ◽  
Clinical Applications ◽  
Clinical Translation ◽  
Future Perspective ◽  
Target Specificity ◽  
Intrinsic Properties ◽  
Isolation Methods ◽  
Promising Solution ◽  
Major Factors

Despite the recent advances in drug development, the majority of novel therapeutics have not been successfully translated into clinical applications. One of the major factors hindering their clinical translation is the lack of a safe, non-immunogenic delivery system with high target specificity upon systemic administration. In this respect, extracellular vesicles (EVs), as natural carriers of bioactive cargo, have emerged as a promising solution and can be further modified to improve their therapeutic efficacy. In this review, we provide an overview of the biogenesis pathways, biochemical features, and isolation methods of EVs with an emphasis on their many intrinsic properties that make them desirable as drug carriers. We then describe in detail the current advances in EV therapeutics, focusing on how EVs can be engineered to achieve improved target specificity, better circulation kinetics, and efficient encapsulation of therapeutic payloads. We also identify the challenges and obstacles ahead for clinical translation and provide an outlook on the future perspective of EV-based therapeutics.

Quercetin Loaded Nanoparticles in Targeting Cancer: Recent Development

2019 ◽  
Vol 19 (13) ◽  
pp. 1560-1576 ◽  
Author(s):  
Manjula Vinayak ◽  
Akhilendra K. Maurya
Keyword(s):  
Silver Nanoparticles ◽  
Clinical Application ◽  
Glycolic Acid ◽  
Water Solubility ◽  
Polymeric Micelles ◽  
Metastatic Cancer ◽  
Chitosan Nanoparticles ◽  
Drug Carriers

:The spread of metastatic cancer cell is the main cause of death worldwide. Cellular and molecular basis of the action of phytochemicals in the modulation of metastatic cancer highlights the importance of fruits and vegetables. Quercetin is a natural bioflavonoid present in fruits, vegetables, seeds, berries, and tea. The cancer-preventive activity of quercetin is well documented due to its anti-inflammatory, anti-proliferative and anti-angiogenic activities. However, poor water solubility and delivery, chemical instability, short half-life, and low-bioavailability of quercetin limit its clinical application in cancer chemoprevention. A better understanding of the molecular mechanism of controlled and regulated drug delivery is essential for the development of novel and effective therapies. To overcome the limitations of accessibility by quercetin, it can be delivered as nanoconjugated quercetin. Nanoconjugated quercetin has attracted much attention due to its controlled drug release, long retention in tumor, enhanced anticancer potential, and promising clinical application. The pharmacological effect of quercetin conjugated nanoparticles typically depends on drug carriers used such as liposomes, silver nanoparticles, silica nanoparticles, PLGA (Poly lactic-co-glycolic acid), PLA (poly(D,L-lactic acid)) nanoparticles, polymeric micelles, chitosan nanoparticles, etc.:In this review, we described various delivery systems of nanoconjugated quercetin like liposomes, silver nanoparticles, PLGA (Poly lactic-co-glycolic acid), and polymeric micelles including DOX conjugated micelles, metal conjugated micelles, nucleic acid conjugated micelles, and antibody-conjugated micelles on in vitro and in vivo tumor models; as well as validated their potential as promising onco-therapeutic agents in light of recent updates.

scholarly journals A novel dual-adhesive and bioactive hydrogel activated by bioglass for wound healing

2019 ◽  
Vol 11 (1) ◽  
Author(s):  
Long Gao ◽  
Yanling Zhou ◽  
Jinliang Peng ◽  
Chen Xu ◽  
Qing Xu ◽  
...  
Keyword(s):  
Wound Healing ◽  
Tissue Regeneration ◽  
Bond Formation ◽  
Clinical Applications ◽  
Cross Linking ◽  
Polyglutamic Acid ◽  
Amino Groups ◽  
Bioactive Properties ◽  
Good Potential ◽  
Ca Ions

AbstractDual adhesiveness to tissue and implant biomaterials and bioactivity to stimulate tissue regeneration are interesting properties for developing new generations of tissue-repairing hydrogels with potential new clinical applications. In this study, we developed a unique bioglass (BG)/oxidized sodium alginate (OSA) composite hydrogel with adipic acid dihydrazide (ADH)-modified γ-polyglutamic acid (γ-PGA) as the cross-linking agent, in which the BG plays a multifunctional role to endow the hydrogel‍ with both dual-adhesive and bioactive properties. On one hand, the BG could improve the tissue-bonding strength by providing an alkaline microenvironment to stimulate the bond formation between OSA and the amino groups on the surrounding tissues. On the other hand, BG endows the hydrogel‍ with adhesiveness to implantable materials by releasing Ca ions, which might chelate with the carboxyl groups of the hydrogel‍ matrix. In addition, the composite hydrogel‍ showed excellent bioactivity to promote vascularization and accelerate tissue regeneration. This study demonstrates that a multifunctional hydrogel‍ can be designed by utilizing the multifunctional ions released from silicate BG, and the BG/OSA hydrogel shows good potential as an adhesive and bioactive material for wound-healing applications.

scholarly journals The Role of Exosomes in Pancreatic Cancer From Bench to Clinical Application: An Updated Review

2021 ◽  
Vol 11 ◽  
Author(s):  
Kai Chen ◽  
Qi Wang ◽  
Marko Kornmann ◽  
Xiaodong Tian ◽  
Yinmo Yang
Keyword(s):  
Pancreatic Cancer ◽  
Tumor Heterogeneity ◽  
Cell Communication ◽  
Treatment Strategies ◽  
Drug Carriers ◽  
Clinical Applications ◽  
Ductal Adenocarcinoma ◽  
Gastrointestinal Malignancies ◽  
Growing Body

Pancreatic ductal adenocarcinoma (PDAC) remains one of the most dismal gastrointestinal malignancies with an overall 5-year survival rate of 8%–9%. The intra-tumor heterogeneity and special tumor microenvironment in PDAC make it challenging to develop effective treatment strategies. Exosomes are extracellular vesicles that originate from the endosomes and have a diameter of 40–160 nm. A growing body of evidence has shown that exosomes play vital roles in tumor initiation and development. Recently, extensive application of exosomes as biomarkers and drug carriers has rendered them attractive in the field of PDAC. This review summarizes the latest progress in the methodologies for isolation, modification, and tracking of exosomes, exosome-mediated cell-to-cell communication, clinical applications of exosome as minimally invasive liquid biopsy and drugs carriers, as well as their involvement in the angiogenic regulation in PDAC. In spite of these advancements, some obstacles are still required to be overcome to use the exosome-based technologies for early diagnosis or improvement of prognosis of patients with PDAC.

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