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Bone infection is a feared complication for patients with surgically fixed bone fractures and local antibiotic delivery is important in prophylaxis and treatment of these infections. Recent studies indicated that Staphylococcus aureus can penetrate bone tissue through micron-sized canaliculi and evade systemic and currently available local antibiotic treatments. Targeting bacteria within the bone requires highly efficient delivery of antimicrobials to the infected bone tissue. In this work, a biodegradable microsphere carrier loaded with antibiotics and with specific affinity to bone mineral was developed. Two widely used antibiotics, i.e., Gentamicin-dioctyl sulfosuccinate (GM-AOT) and Ciprofloxacin (CF) were embedded in poly(ϵ-caprolactone) (PCL) microspheres fabricated by oil-in-water emulsion techniques with carboxylated poly(vinyl alcohol) (cPVA) as surfactant. The carboxylic acid groups present at the Poly(ϵ-caprolactone)/cPVA (PCL-cPVA) microsphere surface were functionalized with aspartic acid oligomers (ASP) granting bone targeting properties. We report on cPVA synthesis, microsphere formulation, and antibiotic loading of PCL/cPVA-ASP microspheres. Antibiotic loaded PCL/cPVA-ASP microspheres show sustained release of its antibiotic load and can inhibit bacterial growth in vitro for up to 6 days. PCL/cPVA-ASP microspheres show enhanced affinity to mineralized substrates compared to non-functionalized PCL/cPVA microspheres. These findings support further development of these bone targeting antibiotic carriers for potential treatment of persistent bone infections. [ABSTRACT FROM AUTHOR]

Poly(aspartic acid) (PASP) is an anionic polypeptide that is a highly versatile, biocompatible, and biodegradable polymer that fulfils key requirements for use in a wide variety of biomedical applications. The derivatives of PASP can be readily tailored via the amine-reactive precursor, poly(succinimide) (PSI), which opens up a large window of opportunity for the design and development of novel biomaterials. PASP also has a strong affinity with calcium ions, resulting in complexation, which has been exploited for bone targeting and biomineralization. In addition, recent studies have further verified the biocompatibility and biodegradability of PASP-based polymers, which is attributed to their protein-like structure. In light of growing interest in PASP and its derivatives, this paper presents a comprehensive review on their synthesis, characterization, modification, biodegradation, biocompatibility, and applications in biomedical areas.

This work provides a simple method to prepare a hydrophilic/oleophobic coating using polyester filter cloth as the substrate, a mixture of three hydrophilic polymers (poly(aspartic acid), poly(acrylic acid), and poly(vinyl alcohol)); SiO 2 with an average particle size of 30 nm is used to improve the surface roughness of the filter cloth. Then, a long fluorocarbon chain of 1 H ,1 H ,2 H ,2 H -perfluorooctyltriethoxysilane is grafted onto the surface by a vacuum silanization coupling reaction to obtain hydrophilic/oleophobic properties. The water and hexadecane contact angles of the treated filter cloth are 3 and 99.8°, respectively. A separation efficiency of 98% was achieved in hexadecane/water separation. The durability test shows that the separation efficiency of toward hexadecane-water mixture remains more than 98% after 20 cycles. The obtained material also presents a strong underwater antipollution property when using hexane, rapeseed oil, mineral oil, and pump oil as model pollutants. For oils with higher viscosity, the separation efficiency remains above 97%. However, the separation efficiency is ∼80% when treating emulsions.

• The hydrogel was designed from PAsp with acylhydrazide and ethoxyl groups. • The hydrogels exhibited good mechanical property and self-healing property. • The hydrogels showed good biocompatibility. • The hydrogels have potential in local drug delivery. Self-healing hydrogels were prepared from hydrazide functionalized poly(aspartic acid) (PAsp). The polymer succinimide (PSI) was reacted with hydrazine and ethanolamine successively to obtain water soluble poly(aspartic acid) derivatives with hydrazide functional groups (PAEH). The hydrogel was prepared by cross-linking PAEH with poly(ethylene glycol) dialdehyde (PEG DA) under mild conditions without addition of catalyst. The rheological property and the self-healing property of the hydrogels were investigated intensively. The in vitro toxicity experiment showed the hydrogels have good bio-compatibility and the doxorubicin (DOX)-loaded hydrogels showed controlled release profile. Importantly, the hydrogel can still be degraded based on poly(aspartic acid) backbone. The bio-degradable poly(amino acid) based on self-healing hydrogel could have great potential application in bioscience including tissue repairing, drug loading and release. [ABSTRACT FROM AUTHOR]

Amphiphilic polymers with pH-responsive abilities have been widely used as carriers for intracellular delivery of bioactive substances, while their membrane-disruptive activity exerted on cells is a critical characteristic that determines delivery efficiency. Herein, we present a novel method to prepare amphiphilic and pH-responsive polymers by chemically tethering l-phenylalanine methyl ester and followed by N ε -carbobenzyloxy-l-lysine benzyl ester to the side carboxylic acid groups of poly(aspartic acid). The obtained phenylalanine- and lysine-grafted polymer (PAsp- g-Phe)- g-Lys demonstrated enhanced membrane-disruptive activity at pH 7.4 in comparison with that of PAsp- g-Phe. Moreover, the pH-responsive behavior of the grafted polymers caused by the significantly intensified hydrophobicity could be modulated by the tethered amount of hydrophobic amino acids with phenyl groups. The prepared amphiphilic (PAsp- g-Phe)- g-Lys could facilitate entry of calcein into NIH/3T3 and HeLa cells at physiological pH values, possibly due to local chemical destabilization of cell membranes by the interaction between the polymer and membrane bilayers. Therefore, we have provided a feasible approach to prepare pH-responsive polymers with enhanced membrane-disruptive activity, and the phenylalanine- and lysine-grafted polymers could be a potential candidate for intracellular delivery of bioactive molecules in biomedical applications.

The study presents a novel strategy for obtaining highly ordered interpolymeric complexes based on a protein, bovine serum albumin and a synthetic polymer, poly(aspartic acid). In this approach, experimental tests were carried out in the presence of a magnetic field of different intensities, namely 0.11 T and 0.3 T produced by permanent magnets. The influence of the magnetic force on the complexation process and the resulted self-assembled structures were studied by means of FTIR spectroscopy, X-ray diffraction, DLS, SEM microscopy and in vitro assay. The changes in the FTIR spectra acquired after 24 h of exposure were connected with conformational changes in the secondary structure and increased interactions between polymers, particularly when a higher intensity field was used. Due to a large anisotropy of magnetic susceptibility characteristic to both proteins and polypeptides, the magnetic field generated ordered assemblies consisting in globular structures of nanometric dimensions. This assembly strategy using magnets, along with remote manipulation capability can provide a versatile, contact-free, and inexpensive tool to create new, complex materials with tailorable characteristics., (Copyright © 2018 Elsevier B.V. All rights reserved.)

A novel interpenetrating network hydrogel for drug controlled release, composed of modified poly(aspartic acid) (KPAsp) and carboxymethyl chitosan (CMCTS), was prepared in aqueous system. The surface morphology and composition of hydrogels were characterized by SEM and FTIR. The swelling properties of KPAsp, KPAsp/CMCTS semi-IPN and KPAsp/CMCTS IPN hydrogels were investigated and the swelling dynamics of the hydrogels was analyzed based on the Fickian equation. The pH, temperature and salt sensitivities of hydrogels were further studied, and the prepared hydrogels showed extremely sensitive properties to pH, temperature, the ionic salts kinds and concentration. The results of controlled drug release behaviors of the hydrogels revealed that the introduction of IPN observably improved the drug release properties of hydrogels, the release rate of drug from hydrogels can be controlled by the structure of the hydrogels and pH value of the external environment, a relative large amount of drug released was preferred under simulated intestinal fluid. These results illustrated high potential of the KPAsp/CMCTS IPN hydrogels for application as drug carriers. [ABSTRACT FROM AUTHOR]

Fertilizer is one of the most important elements of modern agriculture. However, conventional fertilizer, when applied to crops, is vulnerable to losses through volatilization, leaching, nitrification, or other means. Such a loss limits crop yields and pollutes the environment. In an effort to enhance nutrient use efficiency and reduce environmental pollution, an environmental smart fertilizer was reported in the current study. Poly(aspartic acid) and a degradable macro-cross-linker based on l-aspartic acid were synthesized and introduced into the fertilizer as a superabsorbent to improve the fertilizer degradability and soil moisture-retention capacity. Sustained release behavior of the fertilizer was achieved in soil. Cumulative release of nitrogen and phosphorus was 79.8% and 64.4% after 30 days, respectively. The water-holding and water-retention capacities of soil with the superabsorbent are obviously higher than those of the control soil without superabsorbent. For the sample of 200 g of soil with 1.5 g of superabsorbent, the water-holding capacity is 81.8%, and the water-retention capacity remains 22.6% after 23 days. All of the current results in this study indicated that the as-prepared fertilizer has a promising application in sustainable modern agriculture.

Platinum based anticancer drugs have revolutionized cancer chemotherapy, and continue to be in widespread clinical use especially for management of tumors of the ovary, testes, and the head and neck. However, several dose limiting toxicities associated with platinum drug use, partial anti-tumor response in most patients, development of drug resistance, tumor relapse, and many other challenges have severely limited the patient quality of life. These limitations have motivated an extensive research effort towards development of new strategies for improving platinum therapy. Nanocarrier-based delivery of platinum compounds is one such area of intense research effort beginning to provide encouraging preclinical and clinical results and may allow the development of the next generation of platinum chemotherapy. This review highlights current understanding on the pharmacology and limitations of platinum compounds in clinical use, and provides a comprehensive analysis of various platinum-polymer complexes, micelles, dendrimers, liposomes and other nanoparticles currently under investigation for delivery of platinum drugs., (© 2013.)