Subcutaneous drug delivery and the role of the lymphatics
Abstract
Subcutaneous injections are widely utilised as a delivery route for compounds with limited oral bioavailability or as a means to modify or extend the release profile. In this review, factors affecting absorption from the subcutaneous space are discussed with particular emphasis on differential drug absorption into either the underlying blood or lymphatic capillaries. Formulation and targeted delivery approaches, which utilise the subcutaneous administration route, are reviewed with reference to associated technologies and future challenges.:
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The lymphatics provide an alternative absorption pathway into the circulation system for macromolecules.
“therefore, the lymphatics provide an alternative absorption pathway into the circulation system [70, 71].”
From Subcutaneous Administration of Biotherapeutics: An Overview of Current Challenges and Opportunities (2018) · cites this paper as [70]
The absorption pattern of macromolecules into the blood is a consequence of their limited permeability across the vascular endothelia.
“This absorption pattern of macromolecules into the blood is a consequence of their limited permeability across the vascular endothelia”
From Subcutaneous Administration of Biotherapeutics: An Overview of Current Challenges and Opportunities (2018) · cites this paper as [70]
Subcutaneously injected therapeutic proteins typically have a slow absorption rate from the subcutaneous extracellular matrix, with Cmax levels below those achieved with intravenous dosing.
“whereas the pharmacokinetic profile of subcutaneously injected therapeutic proteins is typically characterized by a slow absorption rate from the subcutaneous extracellular matrix with Cmax levels below those achieved with intravenous dosing.”
From Subcutaneous Administration of Biotherapeutics: An Overview of Current Challenges and Opportunities (2018) · cites this paper as [70]
Factors that can contribute to incomplete bioavailability of subcutaneously injected molecules include the composition, volume, pH, and viscosity of the dosing formulation; interactions with interstitial glycosaminoglycans and proteins; and enzymatic degradation.
“Other factors that can contribute to incomplete bioavailability of subcutaneously injected molecules can include the composition, volume, pH, and viscosity of the dosing formulation; interactions with interstitial glycosaminoglycans and proteins; and enzymatic degradation [70, 72, 73].”
From Subcutaneous Administration of Biotherapeutics: An Overview of Current Challenges and Opportunities (2018) · cites this paper as [70]
Absorption via the lymphatics has been described as a barrier for complete uptake of subcutaneously injected molecules.
“However, absorption via the lymphatics has also been described as a barrier for complete uptake of subcutaneously injected molecules.”
From Subcutaneous Administration of Biotherapeutics: An Overview of Current Challenges and Opportunities (2018) · cites this paper as [70]
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References 54 · Cited by 259
- Authors
- McLennan, D. N., Porter, C. J. H., & Charman, S. A.
- Affiliations
- Monash University (AU)
- Corresponding author
- Charman, Susan A.
- Venue
- Drug Discovery Today: Technologies
- Publisher
- Elsevier BV
- Published
- 2005-03
- Volume
- 2
- Issue
- 1
- Pages
- 89-96
- ISSN
- 1740-6749 (ISSN-L)
- OpenAlex
- W1996773895
- Cited by
- 259
- References
- 54
- Citations by year
- 2026: 14 · 2025: 17 · 2024: 28 · 2023: 24 · 2022: 27 · 2021: 18 · 2020: 26 · 2019: 14 · 2018: 14 · 2017: 9 · 2016: 13 · 2015: 15 · 2014: 7 · 2013: 7 · 2012: 5
- FWCI
- 1.48
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drug Discovery Today Technologies (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Emergency Medicine › Intramuscular injections and effects
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Keywords
- subcutaneous drug delivery, subcutaneous injection, lymphatic absorption, lymphatic capillaries, drug absorption, targeted drug delivery, oral bioavailability
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