Overcoming challenges in the development of oral formulations

Oral delivery of therapeutic agents is one of the preferred administration strategies for patients. However, there are many challenges we may encounter during the development of oral formulations. In Chapter 1, the biological barriers to oral delivery as well as the challenges and benefits of oral delivery were reviewed. The characteristics of drug-containing polymeric nanomedicines as drug delivery systems and the various applications of these systems were discussed. In Chapter 2, we discussed the most relevant analytical characterization techniques and their applications for the evaluation of amorphous solid dispersion, which is a promising formulation approach to improve the solubility, dissolution rate, and bioavailability of poorly water-soluble drugs for oral delivery. In Chapter 3 and 4, we comprehensively investigated the impact of hot melt extrusion processes on amorphous solid dispersions. Hot melt extrusion has been used to prepare solid dispersions, especially molecularly dispersed amorphous solid dispersions for solubility enhancement purposes. The influences of mechanical and thermal energy during hot melt extrusion on the preparation and physical stability of amorphous solid dispersions were investigated in Chapter 3. In Chapter 4, we further investigated the dehydration of drug hydrate and its impact on the preparation of amorphous solid dispersions by hot melt extrusion. In Chapter 5, we discussed the risk of internal tablet defects encountered during the manufacturing for oral formulations. We developed an analysis program that incorporates deep learning convolutional neural networks to fully automate the routine image analysis of oral tablets for internal crack detection with high accuracy, throughput, and adaptability.