Improvement of oral bioavailability of poorly water-soluble drugs remains one of the most challenging aspects of drug development. Solid dispersions seem to be a viable technique for overcoming this problem. However, the practical applicability of these systems has remained limited because of difficulties in conventional methods of preparation, poor reproducibility of physicochemical properties, difficulties in dosage form development, and lack of feasibility for scale-up of manufacturing processes. This review addresses various aspects of solid dispersions and compiles some of the recent technology transfers from various fields such as the chemical, food, and polymer industries for the preparation of solid dispersions that can lead to highly efficient and controlled large-scale manufacturing. Some of the practical aspects to be considered for the preparation of solid dispersions, such as selection of carrier and methods of physicochemical characterization, along with an insight into the release mechanism of drugs are also discussed. Finally, an in-depth rationale for limited commercialization of solid dispersions and recent revival has been considered.
This work reports the targeting of the near infrared (NIR) dye indocyanine green (ICG) to the brain using composite nanoparticles. Thermal decomposition of iron pentacarbonyl was used to synthesize monodisperse oleic acid coated magnetic nanoparticles (OAMNP). Synthesized OAMNP and ICG were encapsulated in a poly (lactide-co-glycolide) matrix using an emulsion evaporation method. Different batches containing OAMNP:PLGA ratios (1:4, 1:2 and 3:4) were prepared with ICG (group B-1, 2, 3) and without ICG (group A-1, 2, 3) loading. All the formulations were characterized in terms of morphology, particle size, zeta potential, magnetic content, ICG encapsulation efficiency and the spectral properties of ICG. The optimized formulation showed an encapsulation efficiency of 56 +/- 4.6% for ICG and 57 +/- 1.37% for OAMNP. The biodistribution and brain targeting study involved three groups of six animals, each with 0.4 mg kg(-1) equivalent of ICG, given as neat ICG solution, composite nanoparticles without the aid of a magnetic field, and composite nanoparticles under the influence of a magnetic field (8000 G) to groups 1, 2 and 3 respectively. The tissue analysis and microscopy images revealed a significantly higher brain concentration of ICG (p < 0.05) for group 3 than the two control groups. These results are encouraging for the brain delivery of hydrophilic dyes/drugs using this method for biomedical applications.
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