Nanocarriers for oral delivery of biologics: small carriers for big payloads

Biologics have gained immense popularity in the past two decades as new and personalized medicines. Yet, the majority of the approved biologics are administered via the parenteral route (i.e., via injections).

Biologics therapy is usually costly as they require administration by a healthcare professional, cold storage, and pose high risk of injection-site infection, leading to low patient compliance.

Orally administrable biologics hold tremendous potential for making these therapeutics more accessible to the broader patient population and reducing cost, whilst boosting patient compliance.

Nanocarrier-based oral biologics hold a strong promise in achieving efficient systemic uptake of these complex therapeutics, which is generally hindered by barriers such as harsh pH (stomach), digestive enzymes, mucus, and cellular barriers of the gastrointestinal tract.

The lightning-paced development of a range of organic and inorganic nanocarriers for oral biologics delivery has pushed a handful of nanocarrier-based oral biologics to various stages of clinical trials, showing a promising future for nanocarriers in this field.

Macromolecular therapeutics of biological origin, also known as biologics, have become one of the fastest-growing classes of drugs for management of a range of chronic and acute conditions. The majority of approved biologics are administered via the parenteral route and are thus expensive, have low patient compliance, and have high systemic toxicity. Therefore, tremendous efforts have been devoted to the development of carriers for oral delivery of biologics. This review evaluates key chemical (e.g. pH and enzymes) and physiological challenges to oral biologics delivery. We review the conventional formulation strategies and their limitations, followed by a detailed account of the progress on the use of nanocarriers used for oral biologics delivery, covering organic and inorganic nanocarriers. Lastly, we discuss limitations and opportunities presented by these emerging nanomaterials in oral biologics delivery.

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Article information: Yuxue Cao, Prarthana Rewatkar, Ran Wang, Sumaira Z. Hasnain, Amirali Popat, Tushar Kumeria, Nanocarriers for oral delivery of biologics: small carriers for big payloads, Trends in Pharmacological Sciences, 2021. https://doi.org/10.1016/j.tips.2021.08.005.