Bolaamphiphiles or bolaforms have drawn particular interest in drug and gene delivery, and studies of bolaforms have been growing continuously. Bolaforms, due to their unique structure, exhibit specific self-assembly behavior in water. The present work aims to develop biodegradable cationic bolaforms with a better gene transfection ability. In this work, a novel cationic bolaform (Bola-1) with head groups bearing hydroxyl (OH) functionality was designed and synthesized to investigate self-assembly and gene transfection efficiency. The selfassembly behavior of Bola-1 in water was compared with that of the hydrochloride salt (Bola-2) of its precursor molecule to investigate the effect of the −OH functionality on their solution properties. Several techniques, including surface tension, electrical conductivity, fluorescence probe, calorimetry, dynamic light scattering, and atomic force microscopy, were employed for the physicochemical characterization of Bola-1 and Bola-2. Despite the presence of polar urea groups in the spacer chain, both bolaforms were found to form spherical or elongated micelles above a relatively low critical aggregation concentration (CAC). The presence of the OH group was found to significantly affect the CAC value. The results of calorimetric measurements suggested a thermodynamically favorable aggregate formation in salt-free water. Despite stronger binding efficiency with calf thymus DNA, in vitro gene transfection studies performed using adherent cell Hek 293 suggested that both Bola-1 and Bola-2 have gene transfection efficiency comparable to that of turbofectamine standard. Both bolaforms were found to exhibit significant in vitro cytotoxicity at higher concentrations. Also, the bolaforms showed beneficial antibacterial activity at higher concentrations.
Xanthan-gum-facilitated aspirin-loaded ethyl cellulose microparticles were prepared by multiple-emulsion solvent evaporation technology and the impact on variation in process parameters was investigated systematically. Scanning electron microscopy was performed to determine the surface morphology of the microparticles before and after dissolution study. X-ray diffraction (XRD), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) analysis were performed, and yield value, swelling study, encapsulation efficiency, flow properties and dissolution profiles of the prepared formulations were evaluated. The size of microparticles varied between 247 and 410 μ m, and 58.34 % drug entrapment efficiency was achieved depending on the variation in process parameters. The drug release in acid solutions was slower than in alkaline solution. The microparticles provided extended drug release in alkaline dissolution medium, and the drug release was found to be controlled by Fickian diffusion mechanism. XRD and DSC analyses revealed the amorphous nature of drug in the microparticles. FTIR data indicated the stable character of the encapsulated drug in the microparticles. Thus, variation in process parameters showed a slow and prolonged release of aspirin in simulated intestinal fluid.
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