The aim of this investigation was to screen and understand the product variability due to important factors affecting the characteristics CyA-PLGA nanoparticles prepared by O/W emulsification-solvent evaporation method. Independent variables studied were cyclosporine A (CyA) (X1), PLGA (X2), and emulsifier concentration namely SLS (X3), stirring rate (X4), type of organic solvent employed (chloroform or dichloromethane, X5) and organic to aqueous phase ratio (X6). The nanoparticles properties considered were encapsulation efficiency (Y1), mean particle size (Y2), zeta potential (Y3), burst effect (Y4) and dissolution efficiency (Y5). The statistical analysis of the results allowed determining the most influent factors. The nanoparticles were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy. The factors combination showed variability of entrapment efficiency (Y1), mean particle size (Y2) and zeta potential (Y3) from 10.17% to 93.01%, 41.60 to 372.80nm and 29.60 to 34.90 mV, respectively. Initially, nanoparticles showed burst effect followed by sustained release during the 7-day in vitro release study period. The dissolution efficiency (Y5) varied from 52.67% to 84.11%. The nanoparticles revealed Higuchi release pattern and release occurred by coupling of diffusion and erosion. In conclusion, this study revealed the potential of QbD in understanding the effect of formulation and process variables on the characteristics on CyA-PLGA nanoparticles.

As of 21st century, cancer is arguably the most complex and challenging disease known to mankind and an inevitable public health concern of this millennium. Nanotechnology, suitably amalgamated with cancer research, has ushered an era of highly personalized and safer medicines which can improve cancer diagnosis and therapy. A wide variety of nanomedicines are currently under investigation, including polymeric/non-polymeric nanoparticles, dendrimers, quantum dots, carbon nanotubes, lipid- and micelle-based nanoparticles. The bases of these nanomedicines in reducing toxicity associated with cancer therapy are their ability to carry a large payload and multivalent-ligand targeting. This imparts specificity for targeting the tissues as well as bypass resistance mechanisms. The major hurdles on these future medicines are potential toxicity of nanoparticles, which imposes the need of extensive regulatory evaluation before nanomedicines could be utilized as cancer therapeutics. This review highlights nanopharmaceuticals that have been investigated in oncology for various applications (diagnosis, therapeutic delivery and theranostics). It also discusses the effects of nano-sized materials on tissues/organ functions, the possibility of overcoming multi-drug resistance by using nanomedicines and their current clinical status.

Abstract. The focus of this investigation was to prepare the cocrystal of carbamazepine (CBZ) using nicotinamide as a coformer and to compare its preformulation properties and stability profile with CBZ. The cocrystal was prepared by solution cooling crystallization, solvent evaporation, and melting and cryomilling methods. They were characterized for solubility, intrinsic dissolution rate, chemical identification by Fourier transform infrared spectroscopy, crystallinity by differential scanning calorimetry, powder X-ray diffraction, and morphology by scanning electron microscopy. Additionally, mechanical properties were evaluated by tensile strength and Heckel analysis of compacts. The cocrystal and CBZ were stored at 40°C/94% RH, 40°C/75% RH, 25°C/60% RH, and 60°C to determine their stability behavior. The cocrystals were fluffy, with a needle-shaped crystal, and were less dense than CBZ. The solubility profiles of the cocrystals were similar to CBZ, but its intrinsic dissolution rate was lower due to the high tensile strength of its compacts. Unlike CBZ, the cocrystals were resistant to hydrate transformation, as revealed by the stability studies. Plastic deformation started at a higher compression pressure in the cocrystals than CBZ, as indicated by the high yield pressure. In conclusion, the preformulation profile of the cocrystals was similar to CBZ, except that it had an advantageous resistance to hydrate transformation.

No abstract