scholarly journals PEG Grafted Polymethacrylates Bearing Antioxidants as a New Class of Polymer Conjugates for Application in Cosmetology

Materials ◽  
2020 ◽  
Vol 13 (16) ◽  
pp. 3455 ◽  
Author(s):  
Justyna Odrobińska ◽  
Dorota Neugebauer
Keyword(s):  
Release Kinetics ◽  
Amphiphilic Copolymers ◽  
Click Reactions ◽  
Polymer Carriers ◽  
New Class ◽  
Polymer Conjugates ◽  
Poly Ethylene ◽  
Esterification Reactions ◽  
Neutral Conditions

The amphiphilic copolymers of poly(ethylene glycol) methyl ether methacrylate (MPEGMA) and alkyne functionalized 2-hydroxyethyl methacrylate (AlHEMA) were synthesized by controlled atom transfer radical polymerization (ATRP). The reactions were carried out using the standard ATRP initiator ethyl α-bromoisobutyrate, (EiBBr) and the “bio”initiator bromoester derivative of 4-n-butylresorcinol (4nBREBr2). Two substances with antioxidant activity used in cosmetology, (±)-α-lipoic acid (LA) and ferulic acid (FA), were subjected to esterification reactions to introduce azide groups. The “click” reactions between the alkyne contained copolymers and functionalized acids (LA-N3, FA-N3) were performed to obtain polymer-antioxidant conjugates (P((HEMA-click-FA)-co-MPEGMA) and P((HEMA-click-LA)-co-MPEGMA)). The conjugation was performed with an efficiency of 20–75%. In vitro experiments in a phosphate buffer saline (PBS) solution at neutral conditions demonstrated that the sufficient release was reached after 2.5 h for FA and 1 h for LA. The rapid release kinetics as well as the polymer carriers, which were applied to regulate the delivery of antioxidant substances, are beneficial in cosmetology.

scholarly journals Poly(3-Hydroxybutyrate)-Based Nanoparticles for Sorafenib and Doxorubicin Anticancer Drug Delivery

2020 ◽  
Vol 21 (19) ◽  
pp. 7312 ◽  
Author(s):  
György Babos ◽  
Joanna Rydz ◽  
Michal Kawalec ◽  
Magdalena Klim ◽  
Andrea Fodor-Kardos ◽  
...  
Keyword(s):  
Drug Release ◽  
Glycolic Acid ◽  
Release Kinetics ◽  
Solvent Evaporation Method ◽  
Poly Ethylene Glycol ◽  
Anticancer Drug Delivery ◽  
Poly Ethylene ◽  
Average Size ◽  
Dual Drug

Dual drug-loaded nanotherapeutics can play an important role against the drug resistance and side effects of the single drugs. Doxorubicin and sorafenib were efficiently co-encapsulated by tailor-made poly([R,S]-3-hydroxybutyrate) (PHB) using an emulsion–solvent evaporation method. Subsequent poly(ethylene glycol) (PEG) conjugation onto nanoparticles was applied to make the nanocarriers stealth and to improve their drug release characteristics. Monodisperse PHB–sorafenib–doxorubicin nanoparticles had an average size of 199.3 nm, which was increased to 250.5 nm after PEGylation. The nanoparticle yield and encapsulation efficiencies of drugs decreased slightly in consequence of PEG conjugation. The drug release of the doxorubicin was beneficial, since it was liberated faster in a tumor-specific acidic environment than in blood plasma. The PEG attachment decelerated the release of both the doxorubicin and the sorafenib, however, the release of the latter drug remained still significantly faster with increased initial burst compared to doxorubicin. Nevertheless, the PEG–PHB copolymer showed more beneficial drug release kinetics in vitro in comparison with our recently developed PEGylated poly(lactic-co-glycolic acid) nanoparticles loaded with the same drugs.

scholarly journals Micellar Carriers Based on Amphiphilic PEG/PCL Graft Copolymers for Delivery of Active Substances

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2876 ◽  
Author(s):  
Justyna Odrobińska ◽  
Dorota Neugebauer
Keyword(s):  
Molecular Weight ◽  
Graft Copolymers ◽  
Drug Loading ◽  
Polymer System ◽  
Amphiphilic Copolymers ◽  
Bioactive Substances ◽  
Click Reactions ◽  
Micellar Systems ◽  
Active Substances

Amphiphilic copolymers of alkyne functionalized 2-hydroxyethyl methacrylate (AlHEMA) and poly(ethylene glycol) methyl ether methacrylate (MPEGMA) with graft or V-shaped graft topologies were synthesized. The functionalization of poly(ε-caprolactone) (PCL) with azide group enabled attachment to P(AlHEMA-co-MPEGMA) copolymers via a “click” alkyne-azide reaction. The introduction of PCL as a second side chain type in addition to PEG resulted in heterografted copolymers with modified properties such as biodegradability. “Click” reactions were carried out with efficiencies between 17–70% or 32–50% (for lower molecular weight PCL, 4000 g/mol, or higher molecular weight PCL, 9000 g/mol, respectively) depending on the PEG grafting density. The graft copolymers were self-assembled into micellar superstructures with the ability to encapsulate active substances, such as vitamin C (VitC), arbutin (ARB) or 4-n-butylresorcinol (4nBRE). Drug loading contents (DLC) were obtained in the range of 5–55% (VitC), 39–91% (ARB) and 42–98% (4nBRE). In vitro studies carried out in a phosphate buffer saline (PBS) solution (at pH 7.4 or 5.5) gave the maximum release levels of active substances after 10–240 min depending on the polymer system. Permeation tests in Franz chambers indicated that the bioactive substances after release by micellar systems penetrated through the artificial skin membrane in small amounts, and a majority of the bioactive substances remained inside the membrane, which is satisfactory for most cosmetic applications.

scholarly journals 4-n-Butylresorcinol-Based Linear and Graft Polymethacrylates for Arbutin and Vitamins Delivery by Micellar Systems

Polymers ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 330 ◽  
Author(s):  
Justyna Odrobińska ◽  
Łukasz Mielańczyk ◽  
Dorota Neugebauer
Keyword(s):  
Click Reaction ◽  
Skin Condition ◽  
Amphiphilic Copolymers ◽  
Solution Ph ◽  
Polymeric Systems ◽  
Micellar Systems ◽  
Poly Ethylene ◽  
Positive Effect ◽  
Active Substances

A novel initiator, bromoester modified 4-n-butylresorcinol (4nBREBr2), was prepared and utilized in controlled atom transfer radical polymerization (ATRP) to obtain three series of amphiphilic copolymers. The V-shaped copolymers of methyl methacrylate (MMA), 2-hydroxyethyl methacrylate (HEMA), and poly(ethylene glycol) methyl ether methacrylate (MPEGMA), abbreviated to P(HEMA–co–MMA), P(HEMA–co–MPEGMA), and P(MMA–co–MPEGMA), were synthesized. Moreover, P((HEMA–graft–PEG)–co–MMA) graft copolymers were prepared by combining the pre-polymerization modification of HEMA and a “click” reaction using a “grafting onto” approach. All copolymers could form micelles with encapsulated active substances (vitamin C (VitC), vitamin E (VitE), arbutin (ARB)), which are used in cosmetology. In vitro studies carried out in a PBS solution (pH 7.4) demonstrates that in most cases the maximum release of active substance was after 1 h. The polymeric systems presenting satisfactory encapsulation characteristics and release profiles are attractive micellar carriers of cosmetic substances, which show a positive effect on the skin condition.

scholarly journals Microfluidic encapsulation of SN-38 in block copolymer nanoparticles: effect of hydrophobic block composition on loading and release properties

2019 ◽  
Vol 97 (5) ◽  
pp. 337-343
Author(s):  
Danica Jensen ◽  
Yimeng Cao ◽  
Changhai Lu ◽  
Jeremy E. Wulff ◽  
Matthew G. Moffitt
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
Polymer Nanoparticles ◽  
Amphiphilic Block Copolymers ◽  
Poly Ethylene Oxide ◽  
Rigid Rod ◽  
Poly Ethylene ◽  
20 Nm ◽  
Vitro Release

A gas–liquid microfluidic reactor was used to prepare polymer nanoparticles (PNPs) containing the drug 7-ethyl-10-hydroxy camptothecin (SN-38) from a series of poly(methyl caprolactone-co-caprolactone)-b-poly(ethylene oxide) (P(MCL-co-CL)-b-PEO) amphiphilic block copolymers with variable MCL content in the hydrophobic block. All three copolymers formed spheres with ∼20 nm core diameters by TEM, although some rigid rod-like aggregates were also formed by the PMCL-50 and PMCL-75 copolymers. SN-38 encapsulation efficiencies (EE = 2.7%–3.0%) and loading levels (DL = 2.0%–2.9%) were similar for the three copolymers. In vitro release kinetics became significantly slower as the MCL content increased, with release half times increasing monotonically from 3.4 to 6.2 h as the MCL content of the hydrophobic block increased from 50% to 100%. The ability to systematically tune release half times via controlled variation in the hydrophobic block composition, while maintaining constant PNP size and loading levels, represents an intriguing chemical handle for the optimization of SN-38 nanomedicines.

A comparison of covalent and noncovalent strategies for paclitaxel release using poly(ester amide) graft copolymer micelles

2015 ◽  
Vol 93 (4) ◽  
pp. 399-405 ◽  
Author(s):  
Abdolrasoul Soleimani ◽  
Mahmoud M. Abd Rabo Moustafa ◽  
Aneta Borecki ◽  
Elizabeth R. Gillies
Keyword(s):  
Ethylene Oxide ◽  
Graft Copolymer ◽  
Drug Carriers ◽  
Prolonged Release ◽  
Amphiphilic Copolymers ◽  
Release Rates ◽  
Drug Molecules ◽  
Poly Ethylene Oxide ◽  
Poly Ethylene

Micelles formed from amphiphilic copolymers are promising for the delivery of drug molecules, potentially leading to enhanced properties and efficacies. Critical aspects of these systems include the use of biocompatible, biodegradable polymer backbones as well as the ability to control the incorporation of drugs and their release rates. In this work, a poly(ester amide)–poly(ethylene oxide) graft copolymer with paclitaxel conjugated via ester linkages was prepared and assembled into micelles. For comparison, micelles with physically encapsulated paclitaxel were also prepared. The release rates of these two systems were studied, and the micelles with covalently conjugated paclitaxel exhibited a prolonged release of the drug in comparison to the noncovalent system, which rapidly released the payload. In vitro studies suggested that the poly(ester amide)–poly(ethylene oxide) copolymers were nontoxic, whereas the toxicities of the drug-loaded micelles were dependent on their release rates. Overall, these systems are promising for further development as anticancer drug carriers.

scholarly journals Amphiphilic drug–peptide–polymer conjugates based on poly(ethylene glycol) and hyperbranched polyglycerol for epidermal growth factor receptor targeting: the effect of conjugate aggregation on in vitro activity

Soft Matter ◽  
2020 ◽  
Vol 16 (24) ◽  
pp. 5759-5769 ◽  
Author(s):  
Lilla Pethő ◽  
György Kasza ◽  
Eszter Lajkó ◽  
Orsolya Láng ◽  
László Kőhidai ◽  
...  
Keyword(s):  
Growth Factor Receptor ◽  
In Vitro Activity ◽  
Poly Ethylene Glycol ◽  
Polymer Conjugates ◽  
Amphiphilic Drug ◽  
Enhanced Solubility ◽  
Epidermal Growth ◽  
Poly Ethylene ◽  
Self Aggregation

EGFR targeting drug–polymer–peptide conjugates have enhanced solubility wherein in vitro biological activity highly depends on the structure of conjugates due to their amphiphilic character and self-aggregation properties.

Gastroretentive System of Fluvastatin Sodium by Using Natural Mucilage and Synthetic Polymer

2014 ◽  
Vol 4 (2) ◽  
Author(s):  
Umamaheswara G. ◽  
Anudeep D.
Keyword(s):  
Half Life ◽  
Release Kinetics ◽  
Kinetic Studies ◽  
Diffusion Path ◽  
Synthetic Polymer ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Drug Content ◽  
Biological Half Life

Fluvastatin sodium is a novel compound used as cholesterol lowering agent which acts through the inhibition of 3- hydroxyl-3- methyl glutaryl- coenzyme A (HMG-Co A) reductase. It has short biological half life (1-3h) in humans required a dosing frequency of 20 to 40mg twice a day. Due to its short variable biological half life it has been developed to a sustained gastroretentive system with a natural and synthetic polymer and to study how far the natural mucilage improves the sustained activity. Floating tablets were prepared by direct compression method using in combination of natural mucilage and synthetic polymer. Prior to the preparation of tablets the physical mixtures were subjected to FT IR studies and pre compression parameters. After preparation of tablets they were subjected to various tests like swollen index, drug content, In vitro dissolution and release kinetics with pcp disso software etc. The tablets prepared by direct compression shown good in thickness, hardness and uniformity in drug content, the prepared tablets floated more than 12h except FS1 and FS2 shows 9 and 11h. Swollen index studies shows with increase in concentration of polymer the swelling increases the diffusion path length by which the drug molecule may have to travel and cause lag time. In vitro results shows that on increasing the amount of hibiscus polymer the sustain activity is increased because of its integrity and forms a thick swollen mass and reduces the erosion property of the HypromelloseK100M, kinetic studies shows that FS 1, FS2, FS3 followed the Korsmeyer peppas model and the rest FS 4, FS 5, FS6 follows the zero order respectively. Based on n value indicating that the drug release followed super case II transport mechanism due to the erosion of the polymer.

Conjugates of Classical DNA/RNA Binder with Nucleobase: Chemical, Biochemical and Biomedical Applications

2019 ◽  
Vol 26 (30) ◽  
pp. 5609-5624
Author(s):  
Dijana Saftić ◽  
Željka Ban ◽  
Josipa Matić ◽  
Lidija-Marija Tumirv ◽  
Ivo Piantanida
Keyword(s):  
Molecular Weight ◽  
Small Molecules ◽  
Biomedical Applications ◽  
Protein Targets ◽  
New Class ◽  
Rna Targets ◽  
Covalently Linked ◽  
Structural Aspects

: Among the most intensively studied classes of small molecules (molecular weight < 650) in biomedical research are small molecules that non-covalently bind to DNA/RNA, and another intensively studied class is nucleobase derivatives. Both classes have been intensively elaborated in many books and reviews. However, conjugates consisting of DNA/RNA binder covalently linked to nucleobase are much less studied and have not been reviewed in the last two decades. Therefore, this review summarized reports on the design of classical DNA/RNA binder – nucleobase conjugates, as well as data about their interactions with various DNA or RNA targets, and even in some cases protein targets are involved. According to these data, the most important structural aspects of selective or even specific recognition between small molecule and target are proposed, and where possible related biochemical and biomedical aspects were discussed. The general conclusion is that this, rather new class of molecules showed an amazing set of recognition tools for numerous DNA or RNA targets in the last two decades, as well as few intriguing in vitro and in vivo selectivities. Several lead research lines show promising advancements toward either novel, highly selective markers or bioactive, potentially druggable molecules.

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