Delivery of Orally Administered Digestible Antibodies Using Nanoparticles

Oral administration of medications is highly preferred in healthcare owing to its simplicity and convenience; however, problems of drug membrane permeability can arise with any administration method in drug discovery and development. In particular, commonly used monoclonal antibody (mAb) drugs are d...

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Main Author: Toshihiko Tashima
Format: Article
Language:English
Published: MDPI AG 2021-03-01
Series:International Journal of Molecular Sciences
Subjects:
Online Access:https://www.mdpi.com/1422-0067/22/7/3349
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author Toshihiko Tashima
author_facet Toshihiko Tashima
author_sort Toshihiko Tashima
collection DOAJ
description Oral administration of medications is highly preferred in healthcare owing to its simplicity and convenience; however, problems of drug membrane permeability can arise with any administration method in drug discovery and development. In particular, commonly used monoclonal antibody (mAb) drugs are directly injected through intravenous or subcutaneous routes across physical barriers such as the cell membrane, including the epithelium and endothelium. However, intravenous administration has disadvantages such as pain, discomfort, and stress. Oral administration is an ideal route for mAbs. Nonetheless, proteolysis and denaturation, in addition to membrane impermeability, pose serious challenges in delivering peroral mAbs to the systemic circulation, biologically, through enzymatic and acidic blocks and, physically, through the small intestinal epithelium barrier. A number of clinical trials have been performed using oral mAbs for the local treatment of gastrointestinal diseases, some of which have adopted capsules or tablets as formulations. Surprisingly, no oral mAbs have been approved clinically. An enteric nanodelivery system can protect cargos from proteolysis and denaturation. Moreover, mAb cargos released in the small intestine may be delivered to the systemic circulation across the intestinal epithelium through receptor-mediated transcytosis. Oral Abs in milk are transported by neonatal Fc receptors to the systemic circulation in neonates. Thus, well-designed approaches can establish oral mAb delivery. In this review, I will introduce the implementation and possibility of delivering orally administered mAbs with or without nanoparticles not only to the local gastrointestinal tract but also to the systemic circulation.
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spelling doaj.art-62bfc7ac87a44e97ae082f0893e6618d2023-11-21T11:56:12ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-03-01227334910.3390/ijms22073349Delivery of Orally Administered Digestible Antibodies Using NanoparticlesToshihiko Tashima0Tashima Laboratories of Arts and Sciences, 1239-5 Toriyama-cho, Kohoku-ku, Yokohama, Kanagawa 222-0035, JapanOral administration of medications is highly preferred in healthcare owing to its simplicity and convenience; however, problems of drug membrane permeability can arise with any administration method in drug discovery and development. In particular, commonly used monoclonal antibody (mAb) drugs are directly injected through intravenous or subcutaneous routes across physical barriers such as the cell membrane, including the epithelium and endothelium. However, intravenous administration has disadvantages such as pain, discomfort, and stress. Oral administration is an ideal route for mAbs. Nonetheless, proteolysis and denaturation, in addition to membrane impermeability, pose serious challenges in delivering peroral mAbs to the systemic circulation, biologically, through enzymatic and acidic blocks and, physically, through the small intestinal epithelium barrier. A number of clinical trials have been performed using oral mAbs for the local treatment of gastrointestinal diseases, some of which have adopted capsules or tablets as formulations. Surprisingly, no oral mAbs have been approved clinically. An enteric nanodelivery system can protect cargos from proteolysis and denaturation. Moreover, mAb cargos released in the small intestine may be delivered to the systemic circulation across the intestinal epithelium through receptor-mediated transcytosis. Oral Abs in milk are transported by neonatal Fc receptors to the systemic circulation in neonates. Thus, well-designed approaches can establish oral mAb delivery. In this review, I will introduce the implementation and possibility of delivering orally administered mAbs with or without nanoparticles not only to the local gastrointestinal tract but also to the systemic circulation.https://www.mdpi.com/1422-0067/22/7/3349orally administered monoclonal antibodiesmouth-to-systemic circulation monoclonal antibody deliverydrug delivery systemneonatal Fc receptor-mediated transcytosisoral immunotherapynanodelivery
spellingShingle Toshihiko Tashima
Delivery of Orally Administered Digestible Antibodies Using Nanoparticles
International Journal of Molecular Sciences
orally administered monoclonal antibodies
mouth-to-systemic circulation monoclonal antibody delivery
drug delivery system
neonatal Fc receptor-mediated transcytosis
oral immunotherapy
nanodelivery
title Delivery of Orally Administered Digestible Antibodies Using Nanoparticles
title_full Delivery of Orally Administered Digestible Antibodies Using Nanoparticles
title_fullStr Delivery of Orally Administered Digestible Antibodies Using Nanoparticles
title_full_unstemmed Delivery of Orally Administered Digestible Antibodies Using Nanoparticles
title_short Delivery of Orally Administered Digestible Antibodies Using Nanoparticles
title_sort delivery of orally administered digestible antibodies using nanoparticles
topic orally administered monoclonal antibodies
mouth-to-systemic circulation monoclonal antibody delivery
drug delivery system
neonatal Fc receptor-mediated transcytosis
oral immunotherapy
nanodelivery
url https://www.mdpi.com/1422-0067/22/7/3349
work_keys_str_mv AT toshihikotashima deliveryoforallyadministereddigestibleantibodiesusingnanoparticles