Challenges & References

oral
drug delivery

• Oral drug delivery is the most preferred and convenient route of drug administration due to high patient compliance, cost-effectiveness, least sterility constraints, flexibility in the design of dosage form and ease of production.
• The use of modern drug discovery approaches, such as combinatorial chemistry and high-throughput screening as well as structural understanding of drug-target binding by X-ray diffraction and molecular modelling, has resulted in an increasing percentage of highly potent lead compounds.
• These compounds present increasing issues for formulation development as they often have high-melting points (Tm) and high octanol–water partition coefficients (logP).
• While Tm is a characteristic of crystal lattice energy, logP, as a partition coefficient, denotes a solvation tendency
• These properties are in the chemical space of poorly water soluble drugs often associated with hydrophobicity and lipophilicity, respectively.
• Drug delivery and the drug modalities in the discovery and development pipelines of the Pharmaceutical and Biotechnology Industries have changed significantly over the last 25 years.
• Drug delivery was traditionally used primarily to enhance oral exposure or prolong exposure of small molecules and the early peptide drugs formulated as Immediate Release or Sustained Release.
• The world is rapidly changing; the drug modalities are diversifying, and drug delivery scientists must play a more prominent role and are core to the genesis of innovative medicines of the future.
• It is sometimes forgotten within the drug discovery community that bio-enabling drug delivery systems also have a significant role to play in addressing poorly water soluble compounds.
• Drug delivery science will play a critical role in treating diseases of the future.
• New skills, capabilities and behaviors will be critical for the success of the next generation of medicines.
• Drug delivery science will be required at the inception of projects in discovery as well as in development where until recently this wasn’t predominantly been the case.
• Formulation design and selection in drug product development has historically been centered on empirical testing, specifically laboratory experimentation and preclinical evaluation in animal models. Indeed, trials and errors approaches are still currently used in pharmaceutical development.
• There is a lack of systematic and rational approaches as well as formulation modelisation mimicking the drug discovery and including in vivo fate are still needed.
• There is, however, a growing need from the industry to accelerate this process in order to save time, resource and improve competitive position i.e., 1st to market.