Oral Delivery of Biologics for Precision Medicine

Abstract

Precision medicine has led to the identification of new biological drugs and targets for personalized treatments. A limitation of biological drugs relies on their difficulties for overcoming biological barriers. However, recent developments on drug delivery are opening new avenues that may soon make feasible the oral administration of biologics. In article number 1901935, María José Alonso and co‐workers provide an overview of the current situation, future prospects, barriers to clinical translation, and identified opportunities for advancement in this field.

Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

“…For the local treatment of colonic diseases, colon-targeted drug delivery systems have been actively pursued since conventional non-targeted therapy may have undesirable side-effects and low efficacy due to the systemic absorption of drug before reaching the target site [4,5]. In addition to the topical delivery, colon-targeted drug delivery systems are also applicable to improve the bioavailability of drugs vulnerable to acidic and/or enzymatic destabilization in the upper gastrointestinal (GI) tract, particularly macromolecules such as proteins and peptides due to lower protease activity in the colon [6][7][8]. Although colonic delivery of macromolecules has been explored less extensively compared to small molecules, continuous research may reveal its potential as an effective oral delivery system for macromolecules.…”

Micro and nanoscale technologies in oral drug delivery

“…Among the developed particles for oral drug delivery, some polymer-based particles have been approved in clinical studies, and several liposomal formulations are under clinical investigations [260]. Additionally, other nanoparticle carriers, such as silica nanoparticles and calcium phosphate nanoparticles have been used in oral drug delivery and have begun to see translation into clinical trials [27]. These nanocarriers have been primarily used to deliver insulin, as well as small lipophilic peptides (~1-2 kDa molecular weight) with a cyclic structure, which are resistive to peptidase degradation.…”

“…The oral delivery of biologicals could potentially improve the life of millions of patients and huge efforts are being put to push such solutions to the clinic [27][]. A self-emulsifying system for oral delivery is marketed for delivering immunosuppressing agent cyclosporine A (Sansimmune, CH).…”

“…Improving the standardization of preclinical parameters and procedures, including biodistribution, toxicity, protein adsorption, and device removal [27,269] will enable faster translation of technologies into the clinic. Despite these challenges, the opportunities for improving oral drug delivery using micro and nanoscale technologies is immense, and therefore the field should continue the push for translation into large animal models and eventual clinical trials.…”

“…The small intestine can also account for the digestion of drugs, as digestive enzymes, such as trypsins, chymotrypsins, carboxypeptidases, and elastases are present in high concentrations [ 26 ]. Finally, the colon provides a longer residence time of up to 20 h, low concentrations of digestive enzymes, and relatively neutral pH values of 6–6.7, as well as low fluid volumes to drug ratios [ 27 ].

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