Targeting Brain
Creative Biolabs is an undisputed global leader in providing custom targeted delivery services. Since novel brain-specific targeting modules are in urgent needed to increse the efficiency of drugs, Creative Biolabs empolys new targeting moieties to achieve active targeting of drug delivery systems to the brain. The brain-targeting drug delivery holds great promise in curing nervous system degenerative diseases and brain tumors in clinical applications.
Despite the application of aggressive surgery, radiotherapy and chemotherapy in clinics, brain diseases particularly tumors are still a difficult health challenge due to their fast development, poor prognosis and less efficacious treatment. Although the blood-brain barrier (BBB) helps prevent damaging substances from entering the central nervous system (CNS) and the blood, it also results in drugs out of the CNS. The delivery of drug across the BBB can result in an instantaneous and uniform increase in drug concentration throughout the brain once the drug crosses the BBB. Thus, brain-targeted drug delivery systems, which increase drug accumulation in the targeted region and reduce toxicity in normal brain and peripheral tissue, are a promising new approach to brain tumor treatments.
Fig.1 Schematic representation of the BBB and various transport processes across the brain endothelial layer.1
Strategy of Targeted Delivery for Brain
Multiple carriers have been used in brain targeted delivery. Among them, interest has been focused on the peptide, particularly, cell-penetrating peptides (CPPs). Specifically, the combinational use of targeting module which can target the brain and CPP serves as a promising platform for the design of novel drug and gene delivery vectors. Here shows some mainly targeted delivery strategies for the brain.
Fig.2 Schematic diagram of drug transport across the BBB.2
The BBB strictly limits drug transport into the brain by serving as a physical (tight junctions), metabolic (enzymes) as well as an immunological barrier. To tackle this challenge, many kinds of active targeting strategies were adopted for developing effective drug delivery systems to the brain. Active targeting strategies are mainly divided into transporter-mediated transcytosis, absorptive-mediated transcytosis (AMT), and receptor-mediated endocytosis (RMT).
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Blood-brain Tumor Barrier (BBTB) Targeting Strategies
BBTB is located between brain tumor tissues and micro-vessels formed by highly specialized endothelial cells (ECs), limiting the paracellular delivery of most hydrophilic molecules to tumor tissue. Only when the tumor cell clusters grow to a certain volume will BBB be damaged and BBTB is formed. The strategies for BBTB targeting are mainly based on receptors high expressed on the tumor such as epidermal growth factor receptors (EGFR) and integrin.
Fig.3 Uptake of liposomes by cells viaa dual-mechanism involving receptor targeting and cell penetration.1
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EPR Effect-based Strategies
As the brain tumor develops, the enhanced permeability and retention effect (EPR effect) appears. EPR effect enables nano-systems with suitable particle size to enter the brain tumor via endothelial gaps on the micro-vessels of brain tumors.
What Can We Do for You?
Equipped with our well-established module delivery systems, we can provide either individual targeting modules or different kinds of module-payload/carrier conjugates targeting the brain. Numerous moieties have been identified and can be used for specific targeting to the brain. These components could act as single targeting ligands in different forms on multiple carriers to enhance uptake of CNS drugs into the brain. With deep understanding of this, Creative Biolabs offers a wide range of customized services, products and tailored solutions to meet our customers’ specifications. If you are interested in our services, please feel free to contact us for more information.
References
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Sharma, Gitanjali, et al. "The role of cell-penetrating peptide and transferrin on enhanced delivery of drug to brain." International journal of molecular sciences 17.6 (2016): 806.
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Zhao, Yi, et al. "Recent advances in drug delivery systems for targeting brain tumors." Drug Delivery 30.1 (2023): 1-18.
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