Colon targeted drug delivery systems have gained a great deal of attention as potential carriers for the local treatment of colonic diseases with reduced systemic side effects and also for the enhanced oral delivery of various therapeutics vulnerable to acidic and enzymatic degradation in the upper gastrointestinal tract. In recent years, the global pharmaceutical market for biologics has grown, and increasing demand for a more patient-friendly drug administration system highlights the importance of colonic drug delivery as a noninvasive delivery approach for macromolecules. Colon-targeted drug delivery systems for macromolecules can provide therapeutic benefits including better patient compliance (because they are pain-free and can be self-administered) and lower costs. Therefore, to achieve more efficient colonic drug delivery for local or systemic drug effects, various strategies have been explored including pH-dependent systems, enzyme-triggered systems, receptor-mediated systems, and magnetically-driven systems. In this review, recent advancements in various approaches for designing colon targeted drug delivery systems and their pharmaceutical applications are covered with a particular emphasis on formulation technologies.

Conventional chemotherapy lacking target selectivity often leads to severe side effects, limiting the effectiveness of chemotherapy. Therefore, drug delivery systems ensuring both selective drug release and efficient intracellular uptake at the target sites are highly demanded in chemotherapy to improve the quality of life of patients with low toxicity. One of the effective approaches for tumor-selective drug delivery is the adoption of functional ligands that can interact with specific receptors overexpressed in malignant cancer cells. Various functional ligands including folic acid, hyaluronic acid, transferrin, peptides, and antibodies, have been extensively explored to develop tumor-selective drug delivery systems. Furthermore, cell-penetrating peptides or ligands for tight junction opening are also actively pursued to improve the intracellular trafficking of anticancer drugs. Sometimes, multiple ligands with different roles are used in combination to enhance the cellular uptake as well as target selectivity of anticancer drugs. In this review, the current status of various functional ligands applicable to improve the effectiveness of cancer chemotherapy is overviewed with a focus on their roles, characteristics, and preclinical/clinical applications.

Probiotics have demonstrated their high potential to treat and/or prevent various diseases including neurodegenerative disorders, cancers, cardiovascular diseases, and inflammatory diseases. Probiotics are also effective against multidrug-resistant pathogens and help maintain a balanced gut microbiota ecosystem. Accordingly, the global market of probiotics is growing rapidly, and research efforts to develop probiotics into therapeutic adjuvants are gaining momentum. However, because probiotics are living microorganisms, many biological and biopharmaceutical barriers limit their clinical application. Probiotics may lose their activity in the harsh gastric conditions of the stomach or in the presence of bile salts. Moreover, they easily lose their viability under thermal or oxidative stress during their preparation and storage. Therefore, stable formulations of probiotics are required to overcome the various physicochemical, biopharmaceutical, and biological barriers and to maximize their therapeutic effectiveness and clinical applicability. This review provides an overview of the pharmaceutical applications of probiotics and covers recent formulation approaches to optimize the delivery of probiotics with particular emphasis on various dosage forms and formulation technologies.

Advancements in biotechnology and protein engineering expand the availability of various therapeutic proteins including vaccines, antibodies, hormones, and growth factors. In addition, protein drugs hold many therapeutic advantages over small synthetic drugs in terms of high specificity and activity. This has led to further R&D investment in protein-based drug products and an increased number of drug approvals for therapeutic proteins. However, there are many biological and biopharmaceutical obstacles inherent to protein drugs including physicochemical and enzymatic destabilization, which limit their development and clinical application. Therefore, effective formulations of therapeutic proteins are needed to overcome the various physicochemical and biological barriers. In current medical practice, protein drugs are predominantly available in injectable formulations, which have disadvantages including pain, the possibility of infection, high cost, and low patient compliance. Consequently, non-invasive drug delivery systems for therapeutic proteins have gained great attention in the research and development of biomedicines. Therefore, this review covers the various formulation approaches to optimizing the delivery properties of protein drugs with an emphasis on improving bioavailability and patient compliance. It provides a comprehensive update on recent advancements in nanotechnologies with regard to non-invasive protein drug delivery systems, which is also categorized by the route of administrations including oral, nasal, transdermal, pulmonary, ocular, and rectal delivery systems.

Tablet film coating is a common but critical process providing various functionalities to tablets, thereby meeting diverse clinical needs and increasing the value of oral solid dosage forms. Tablet film coating is a technology-driven process and the evolution of coated dosage forms relies on advancements in coating technology, equipment, analytical techniques, and coating materials. Although multiple coating techniques are developed for solvent-based or solvent-free coating processes, each method has advantages and disadvantages that may require continuous technical refinement. In the film coating process, intra- and inter-batch coating uniformity of tablets is critical to ensure the quality of the final product, especially for active film coating containing active pharmaceutical ingredients in the coating layer. In addition to experimental evaluation, computational modeling is also actively pursued to predict the influence of operation parameters on the quality of the final product and optimize process variables of tablet film coating. The concerted efforts of experiments and computational modeling can save time and cost in optimizing the tablet coating process. This review provides a brief overview of tablet film coating technology and modeling approaches with a focus on recent advancements in pharmaceutical applications.