Modulating drug release from poly(lactic-co-glycolic) acid microparticles by the addition of alginate and pectin

The aim of the present work is the characterization of PLGA microparticles including biopolymers for the controlled release of tilmicosin, a broad-spectrum antibiotic. Microparticles were prepared using the double-emulsion solvent evaporation technique. The effect of alginate and pectin incorporation over particle size and porosity, encapsulation efficiency (EE) and pH-responsive drug release was evaluated. Formulations presented a mean particle size of 5.5 μm approximately and a drug EE ranged from 22%–57%. PLGA-Alginate particles showed an increased porosity. Tilmicosin release profiles from PLGA and PLGA-biopolymer microparticles were affected by the particular combination of polymers and the pH of the release medium. The experimental data was simulated using a mathematical model, which takes into account the autocatalytic polymer degradation and the different mechanisms of drug transport. The combination of PLGA and biopolymers strongly influenced the morphology of the particles, offering the possibility of controlling the drug release profiles according to the therapy.     

A polyphenolic biomacromolecule prepared from a flavonoid: Catechin as degradable microparticles

Catechin (CAT) was crosslinked with trimethylolpropane triglycidyl ether (TMPTGE) to obtain degradable poly(CAT) particles in a single step. Spherical p(CAT) particles with tens of micrometer size range and an isoelectronic point at pH 1.2 were obtained. The hydrolytic degradation of p(CAT) particles provided sustainable and extended release with 264 mg/g CAT release within 10 days at pH 7.4. The antioxidant capacity of 55.0 ± 0.9 μg/ml gallic acid equivalent in terms of total phenol content, and 0.88 ± 0.3 μmol/g trolox equivalent were estimated for p(CAT) particles displaying strong radical scavenging capability. Blood clotting and hemolysis assays demonstrated dose-dependent blood compatibility revealing higher blood compatibility for p(CAT) particles up to 10 μg/ml concentration. The cytotoxicity results show that p(CAT) particles have almost no toxicity for CCD841 normal colon cells at 250 μg/ml concentration in 24 h incubation time giving ~97% cell viability, whereas CAT molecules only provide ~34% cell viability.     

Synthesis,characterization, and cell viability of bifunctional medical-grade polyurethane nanofiber: Functionalization by bone inducing and bacteria ablating materials

There is an extensive possibility of improving characteristics of fibers used in hard tissue engineering, being hydrophobic and less osteoconductive, resulting in the dynamic growth of new tissues. The current work focuses on the fabrication of nanofibers incorporated with titanium dioxide (TiO₂) ''as osteoconductive'' and silver (Ag) ''as self-healing'' nanoparticles (NPs). The incorporation of AgNO₃ by in situ method not only helped to impart the antibacterial activity but also changed the contact angle from 81 ± 03° in the case of pristine nanofibers to 74 ± 03°, 61 ± 03°, 50 ± 08°, and 39 ± 1.1°, in the composite scaffolds containing 0.01, 0.03, 0.05, and 0.07 M of Ag salts. The incubation in simulated body fluid at 37°C to induce mineralization on nanofiber scaffolds indicated Ca and P crystals' formation. The antibacterial activity showed significantly more toxicity toward E. coli (8.3 ± 0.9 mm) than S. aureus (1.2 ± 0.1 mm). Biocompatibility studies using MTT assay on the pre-osteoblasts showed that both TiO₂ and Ag NPs present in the nanofibers are non-toxic to the bone-like cells. However, results show that a higher concentration of Ag NPs (i.e., 0.07 M) is toxic to cells growing. Finally, all the results suggest that the nanofiber scaffolds have considerable scope for future bone tissue engineering materials.     

Reinforcing effect of nanocrystalline cellulose and office waste paper fibers on mechanical and thermal properties of poly (lactic acid) composites

Nanocrystalline cellulose (NCC) was prepared from office waste paper (OWP) by sulfuric acid hydrolysis method in this paper and it was used to prepare a series of poly (lactic acid) PLA/NCC composites by using a dissolution method in solvent N, N-dimethylformamide solution. The results indicated that with the addition of only 3 wt% NCC, the composites exhibited outstanding mechanical property. The tensile, bending and impact properties of the PLA/3NCC composite were improved by 8.2%, 13.1%, and 35.9% than those of pure PLA, respectively. On this basis, office waste paper fibers (OWF) were also used as a physical blended filler to enhance PLA/NCC composites to reduce the preparation cost of PLA composites and the perfect PLA/NCC/OWF sample was easily manufactured by melting–blending and injection molding. According to the crystallization and melting performance table, both NCC and OWF can act as nucleating agent to promote the crystallization properties on composites, while the blends did not have positive effect on thermal stability. Furthermore, the water absorption and degradation properties of PLA composites were also studied. This work not only provided a novel idea for the utilization of office waste paper but also successfully produced environment friendly composites with favorable mechanical properties and crystallization performance.     

Great enhancement of mechanical features in PLA based composites containing aligned few layer graphene (FLG), the effect of FLG loading,size, and dispersion on mechanical and thermal properties

Four series of polylactide (PLA) based composite films containing horizontally aligned few layer graphene (FLG) flakes of high aspect ratio and adsorbed albumin are prepared. The mechanical and thermal properties varies with percentage, dispersion degree and size of FLG flakes. Great improvement up to 290% and 360% of tensile modulus and strength respectively were obtained for the composite containing high lateral size of FLG at 0.17% wt, and up to 60% and 80% for the composite with very well dispersed 0.02% wt FLG. The composites of PLA and PEG-PLLA containing very well dispersed FLG flakes at 0.07% wt are ductile showing enhancement of elongation at break up to respectively 80% and 88%. Relatively high electrical conductivity, 5 × 10⁻³ S/cm, is measured for PLA film charged with 3% of FLG.     

Enzymatic degradability and release properties of graphene oxide/silk fibroin nanocomposite films

The structure evolution of silk fibroin (SF) in the nanocomposite films with graphene oxide (GO) was investigated and related to the enzymatic degradability and release property. The interaction with GO was found to induce conformation transition of SF from random coil to β-sheet. However, the surface binding constrained the rearrangement of the silk chains, leading to a decrease of β-sheet when GO content was more than 1.0%. The crystal structure of SF played a key role in the degradation of GO/SF composites. The preferential degradation of the hydrophilic blocks resulted in a faster degradation of SF films with higher β-sheet content. The addition of GO to SF matrix led to a slower release and a reduction of the burst release of RhB, the model compound. The release profile was well fitted to the Rigter–Peppas equation, from which the characteristic constant decreased and the diffusional exponent increased with increasing GO content but quickly leveled off when GO content was more than 1.0%. Degradation of the composites had little influence on the characteristic constant of RhB release, however, led to an increased diffusional exponent, which was more evident for the composites with higher β-sheet content.     

Poly (vinyl alcohol)/polylactic acid blend film with enhanced processability,compatibility, and mechanical property fabricated via melt processing

Poly (vinyl alcohol)/polylactic acid (PVA/PLA) blend film, which is environment friendly and has potential applications in food and electronic packaging fields, was fabricated by melt extrusion casting. Fourier transform infrared spectroscopy analysis confirmed the formation of the hydrogen bonding between PLA and PVA, which improved the compatibility of PLA with PVA, making PLA uniformly dispersed in PVA matrix as small spheres, even when PLA content increase to 15 wt%. In this way, the original hydrogen bond network among PVA was disturbed and the chain mobility of PVA was activated, endowing PVA/PLA blends with lower melt viscosity than bot modified PVA and PLA, and the blend films with the increased crystallinity, mechanical property, and water resistance. Compared with PVA film, the crystallinity, tensile strength and Young's modulus of the blend film with 15 wt% PLA, respectively, increased by 15.1%, 9 and 51 MPa, and the water contact angle enlarged from 23° to 60°.     

生物降解材料在水环境中降解性能的研究进展

综述了目前典型生物降解材料在水环境中降解性能的研究现状,详细介绍了聚乳酸（PLA）高分子材料（PLA、PLA共聚物、PLA复合材料等）、聚羟基烷酸酯（PHA）、聚己内酯（PCL）、聚丁二酸丁二醇酯（PBS）、聚（己二酸丁二醇酯?对苯二甲酸乙二醇酯）（PBAT）和CO₂共聚物等在不同水环境中的降解性能;最后总结了生物降解材料未来需要关注的问题和发展方向。     

Biodegradable Microparticles for Simultaneous Detection of Counterfeit and Deteriorated Edible Products

In an era of globalized trade relations where food and pharmaceutical products cross borders effortlessly, consumers face counterfeit and deteriorated products at elevated rates. This paper presents multifunctional, biodegradable hydrogel microparticles that can provide information on the authenticity and the potential deterioration of the tagged food or pharmaceutical formulations. These microparticles integrate spatially patterned authenticity code with two sensors—the first one detects possible presence of pathogenic microbes through monitoring pH while the second one identifies products stored above optimal temperatures via optical monitoring of the microparticle degradation. Particles are synthesized from a biocompatible polymer and a photoinitiator, dextran modified with 2‐hydroxyethylmethacrylate and riboflavin, respectively, using a continuous, high throughput method stop‐flow lithography. The proposed synthesis approach also enables crosslinking with visible light bringing about additional flexibility to flow lithography. Model liquid and solid food and pharmaceutical products are successfully labeled with microparticles and the functionality of the sensors in aqueous solutions is demonstrated.     

Microfluidic Production of Biodegradable Microcapsules for Sustained Release of Hydrophilic Actives

Biodegradable microcapsules with a large aqueous lumen and ultrathin membrane are microfluidically designed for sustained release of hydrophilic bioactives using water‐in‐oil‐in‐water double‐emulsion drops as a template. As a shell phase, an organic solution of poly(lactic‐co‐glycolic acid) is used, which is consolidated to form a biodegradable membrane. The encapsulants stored in the lumen are released over a long period of time as the membranes degrade. The period can be controlled in a range of —three to five months at neutral pH condition by adjusting membrane thickness, providing highly sustained release and potentially enabling the programed release of multiple drugs. At acidic or basic condition, the degradation is accelerated, leading to the release in the period of approximately two months. As the membrane is semipermeable, the microcapsules respond to the osmotic pressure difference across the membrane. The microcapsules are inflated in hypotonic condition and deflated in hypertonic condition. Both conditions cause cracks on the membrane, resulting in the fast release of encapsulants in a day. The microcapsules implanted in mice also show sustained release, despite the period is decreased to a month. It is believed that the microcapsules are promising for the in vivo sustained release of drugs for high and long‐term efficacy.