Abstract: The novel boron-chelated π-conjugated polymers named as BF2-poly and BPh2-poly were synthesized by a feasible condensation-chelation strategy. First, conjugated polymers bearing Boc group were prepared by using palladium-catalyzed Suzuki–Miyaura coupling reaction. Then, conjugated polymers (poly-1) were obtained with high efficiency by removing the Boc group from Boc-poly. Last, boron trifluoride diethyl etherate (BF3·Et2O) or triphenylboron (BPh3) chelated with poly-1 forming the target polymers. Furthermore, the boron-chelated polymers were characterized by UV−Vis absorption spectroscopy, photoluminescence spectroscopy, cyclic voltammetry and thermogravimetric analysis. As expected, fluorescences peaks at 520 nm and 592 nm were observed in diluted CH2Cl2. In addition, BF2-poly and BPh2-poly showed strong fluorescence at 545 nm and 601 nm in homogeneous solid state. The results coming from thermogravimetric analysis and cyclic voltammetry also revealed that the conjugated polymers have favorable electrochemical and thermostable properties.
Abstract: The ability to control the micelle size of poly(lactic acid) and poly(ethylene glycol) (PLA–PEG) block copolymers is important for controlling their circulation in blood cell recognition, drug release and therapeutic effects. We successfully controlled the micelle size by changing the block number of copolymers (multiblock index). PLA–PEG multiblock copolymers with multiblock indexes ranging from 1.35 to 2.78 were synthesized by direct polycondensation with tin chloride/p-toluenesulfonic acid binary catalysts, using PEG with a molecular weight (Mw) of 3200 Da. The Mw of PLA–PEG copolymers increased with an increase in the multiblock index, while micelle size, measured by dynamic light scattering, decreased greatly from 349 to 28 nm. In addition, the X-ray diffraction peak of the PLA crystal disappeared when the multiblock index was increased. These results indicate that a multiblock structure is useful for controlling micelle size without changing the PLA/PEG composition or PEG molecular weight, which strongly influences other micelle features.
Abstract: The aim of this study was to design, synthesize and optimize chlorpromazine hydrochloride (CPZ)-loaded, poly-ε-caprolactone (PCL) based nanocapsules, intended for site specific delivery to the frontal lobe, using a novel melt-dispersion technique that is non-arduous, inexpensive and devoid of any hazardous organic solvents. Experimental trials using a central composite design were performed on 13 statistically derived formulations of various combinations of PCL (1000–3000 mg) and Polysorbate 80 (2%–5% v/v) on the physicochemical and physicomechanical properties and interactive effects on PCL nanocapsule formulation. Differential scanning calorimetry (DSC), Temperature modulated differential scanning calorimetry (TMDSC) and Fourier transform infrared spectroscopy (FTIR) revealed that there was no thermodegardation of the constituents utilized in the melt dispersion technique. Nanocapsule yields achieved were very high however entrapment of CPZ proved to be relatively low due to the highly hydrophilic nature of CPZ and the processing of the nanocapsules post synthesis. Nanocapsule sizes were in the nanotherapeutic range and varied from 132.7 ± 6.8 nm to 566.6 ± 5.5 nm. Zeta potential ranged from 15.1 ± 0.65 mV to 28.8 ± 0.84 mV revealing capsules that were of incipient to moderate stability. Transmission electron microscopy revealed nanocapsules that were spherical shape, well individualized with a moderate degree of flocculation. In vitro CPZ release was biphasic for all formulations with an initial burst release followed by pseudo-steady controlled release over 30 days. The cytotoxicity of the optimized nanocapsule system on a PC12 neuronal cell line proved to be minimal. Following incorporation of the optimized nanocapsules within a polymeric membrane, in vivo implantation of the device in a New Zealand Albino rabbit model proved the efficacy of the system in achieving prolonged more targeted CPZ levels to the brain. Extensive in vitro testing and optimization and preclinical evaluation supports the application for the use and feasibility of the CPZ-loaded, PCL based nanocapsules for the long-term management of certain psychotropic disorders where the benefits of nanotechnology can be exploited.
Abstract: Few changes have occurred in the use of various stabilizers over recent years. In the current literature, phosphate derivatives are used as anti-ageing additives in polymers, and the most popular of these are sterically hindering cyclic amines. However, most of these compounds are carcinogenic. Synthetic phenols have been increasingly used as antioxidants in food and in polymers. Ecological standards encourage the elimination of harmful additives in polymeric products that come in contact with food or with the human body. This article presents application of flavonoid (silymarin/flavonoligand) for polymer stabilization and use of natural phytocompounds such as color indicators of polymers ageing time. In this research, I propose two ways of application: traditional, during processing; and the new one, by using impregnation method. Based on the change of deformation energy (ageing coefficient K), FTIR, oxidative induction time (OIT) evaluated by differential scanning calorimetry (OIT), thermogravimetry analysis (TG), spectrophotometric color measurements in terms of CIE-Lab color space values, I confirmed the high antioxidant activity of flavonoids in EPM. They provide coloration of the polymeric materials that changes cyclically as a function of aging time. Additionally, the use of phytocompounds in polymers provides similar stabilizing effect to those of synthetic antioxidants.
Abstract: The use of starch based films as a potential alternative choice to petroleum derived plastics is imperative for environmental waste management. This study presents a new biopolymer (sugar palm starch) for the preparation of biodegradable packaging films using a solution casting technique. The effect of different plasticizer types (glycerol (G), sorbitol (S) and glycerol-sorbitol (GS) combination) with varying concentrations (0, 15, 30 and 45, w/w%) on the tensile, thermal and barrier properties of sugar palm starch (SPS) films was evaluated. Regardless of plasticizer types, the tensile strength of plasticized SPS films decreased, whereas their elongation at break (E%) increased as the plasticizer concentrations were raised. However, the E% for G and GS-plasticized films significantly decreased at a higher plasticizer concentration (45% w/w) due to the anti-plasticization effect of plasticizers. Change in plasticizer concentration showed an insignificant effect on the thermal properties of S-plasticized films. The glass transition temperature of SPS films slightly decreased as the plasticizer concentration increased from 15% to 45%. The plasticized films exhibited increased water vapor permeability values from 4.855 × 10−10 to 8.70 × 10−10 g·m−1·s−1·Pa−1, irrespective of plasticizer types. Overall, the current study manifested that plasticized sugar palm starch can be regarded as a promising biopolymer for biodegradable films.
Abstract: In the present work, we report for the first time the complex coacervation of carboxymethyl sago pulp (CMSP) with gelatine for sustained drug delivery. Toluene saturated with glutaraldehyde and aqueous aluminum chloride was employed as cross-linkers. Measurements of zeta potential confirm neutralization of two oppositely charged colloids due to complexation, which was further supported by infrared spectroscopy. The coacervates encapsulated a model drug ibuprofen and formed microcapsules with a loading of 29%–56% w/w and an entrapment efficiency of 85%–93% w/w. Fresh coacervates loaded with drug had an average diameter of 10.8 ± 1.93 µm (n = 3 ± s.d.). The coacervates could encapsulate only the micronized form of ibuprofen in the absence of surfactant. Analysis through an optical microscope evidenced the encapsulation of the drug in wet spherical coacervates. Scanning electron microscopy revealed the non-spherical geometry and surface roughness of dried drug-loaded microcapsules. X-ray diffraction, differential scanning calorimetry and thermal analysis confirmed intact and crystalline ibuprofen in the coacervates. Gas chromatography indicated the absence of residual glutaraldehyde in the microcapsules. Dual cross-linked microcapsules exhibited a slower release than mono-cross-linked microcapsules and could sustain the drug release over the period of 6 h following Fickian diffusion.