Brain Targeted Liposomal Drug Delivery System Development Service

Introduction to Our Brain Targeted Liposomal Drug Delivery System Development Service

Overcoming the blood-brain barrier (BBB) remains one of the most formidable challenges in central nervous system (CNS) drug development. Liposomal drug delivery systems have emerged as powerful nanocarriers for targeted delivery to the brain, offering superior pharmacokinetics, reduced systemic toxicity, and improved therapeutic index. At BOC Sciences, we specialize in the design and preclinical development of brain-targeted liposomal delivery systems—tailored for precise delivery of small molecules, nucleic acids, peptides, and other biologics to the brain. With over two decades of expertise in liposome contract manufacturing services, surface modification, ligand conjugation, and preclinical evaluation, we offer scientific depth, technical precision, and unmatched reliability in designing advanced delivery systems tailored to CNS targeting.

How to Get Started with Us?

  • Reach Out to Us: Begin by contacting us through our website or directly via email to initiate your project discussion.
  • Schedule a Consultation: Arrange a meeting with our experts to discuss your specific brain-targeted liposomal drug delivery needs, including your research goals and desired outcomes.
  • Feasibility Assessment: Our team will review the details of your project, evaluating its scientific feasibility, and provide initial feedback on the best approach for development.
  • Tailored Development Plan: Based on your requirements, we will provide a comprehensive development plan outlining specific timelines, budget estimates, and key project milestones.
  • Formal Agreement: Once all terms and conditions are agreed upon, we will proceed with a formal contract that officially kicks off the development process.

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What is Brain Targeted Drug Delivery?

Brain targeted drug delivery systems are engineered platforms designed to facilitate the selective and efficient transport of therapeutic agents across the BBB into the brain parenchyma. Leveraging receptor-mediated transcytosis (e.g., transferrin or insulin receptor targeting), adsorptive-mediated transcytosis, and other transport mechanisms, liposomes can be modified with targeting ligands (e.g., peptides, antibodies, aptamers) to navigate and penetrate the BBB. Such systems are particularly beneficial for enhancing the pharmacokinetic profile of CNS-active drugs, reducing systemic exposure, and optimizing therapeutic outcomes in disorders such as glioblastoma, Parkinson's disease, Alzheimer's disease, and epilepsy.

Comprehensive Services for Brain Targeted Liposomal Drug Delivery System Development

BOC Sciences delivers an integrated, technically advanced service portfolio specifically tailored to support the development of brain-targeted liposomal drug delivery systems for preclinical research. Our offerings span from specialized lipid materials to fully customized liposomal formulation services designed to cross the blood-brain barrier and achieve high-precision CNS delivery.

Specialized Lipid Raw Materials for Brain Targeting

To engineer brain-penetrant liposomal systems, BOC Sciences provides a wide array of surface-modifiable and functional lipids suitable for ligand conjugation and BBB transport optimization, for example:

(1) PEGylated Lipids with Reactive Groups

  • DSPE-PEG2000-Maleimide, DSPE-PEG2000-NHS, DSPE-PEG3400-Carboxylic Acid
  • These allow for efficient conjugation of brain-targeting ligands (e.g., peptides, antibodies, aptamers) via thiol, amine, or click chemistry pathways.

(2) Cationic Lipids and Zwitterionic Lipids

  • DOTAP, DODMA, EPC, and others for enhancing electrostatic interaction with the negatively charged BBB interface, especially useful for RNA or DNA delivery.

(3) Target-Specific Ligand-Conjugated Lipids (custom synthesis available)

  • RVG-PEG-DSPE (for neuron-specific rabies virus glycoprotein targeting)
  • Angiopep-2-PEG-DSPE (for LRP1 receptor-mediated transcytosis)
  • T7-peptide, transferrin, lactoferrin, and ApoE-based lipids for active BBB penetration

These tailored lipids are rigorously purified and characterized (NMR, MALDI-TOF, HPLC) and can be delivered in bulk or incorporated into your formulation through our downstream services.

Ligand Screening and Conjugation Strategy Optimization

BOC Sciences offers ligand identification and conjugation optimization as a standalone or integrated service, ensuring the selected targeting moiety maximizes BBB transport. This includes:

  • Comparative screening of multiple ligands for receptor expression compatibility (e.g., LRP1, TfR, insulin receptor)
  • Spacer length and ligand density optimization to balance targeting affinity with systemic circulation
  • Conjugation via DSPE-PEG functional handles using click chemistry, amide bonding, or thiol-maleimide reactions

We also support co-ligand strategies to enhance specificity and brain region selectivity, particularly in disease-specific models such as glioblastoma or Parkinson's disease.

Liposome Encapsulation - CNS-Targeted Payloads

Our team develops fully customized liposomal drug delivery systems optimized for a wide spectrum of brain-targeted applications, for example:

(1) Small Molecules Drug Encapsulation

  • Hydrophilic neuroprotectants (e.g., edaravone, memantine)
  • Lipophilic CNS-acting drugs (e.g., cannabinoids, curcumin analogs, antipsychotics)

(2) Macromolecular Therapeutics

  • Peptides and proteins requiring protection from enzymatic degradation
  • Monoclonal antibodies or antibody fragments targeting brain-specific receptors

(3) Genetic and Nucleic Acid Cargo

  • siRNA, miRNA, antisense oligonucleotides (ASOs)
  • mRNA and CRISPR-Cas components for CNS gene modulation
  • DNA plasmids for neural expression studies

Our formulations are available as:

  • Stealth liposomes for prolonged systemic circulation
  • Stimuli-responsive liposomes (pH, enzyme, redox) for controlled release in inflammatory or tumor microenvironments in the brain
  • Intranasal-adapted liposomes for nose-to-brain delivery pathways

With a robust infrastructure, high-purity lipid inventory, and deep formulation expertise, BOC Sciences is positioned as a premier partner for developing next-generation brain-targeted liposomal therapeutics for preclinical use. Whether your payload is a synthetic small molecule, a biologic, or a gene-modifying agent, we offer the tools and technical know-how to bring it across the BBB—effectively and precisely.

Step-by-Step Process of Brain Targeted Liposomal Drug Delivery System Development

1. Project Consultation and Feasibility Analysis

  • We start by reviewing your compound, indication, and targeting requirements to define an optimal liposomal strategy.

2. Target Ligand Selection and Conjugation Strategy

  • Based on BBB biology, we select and conjugate the appropriate ligand to the liposome surface to ensure active targeting.
  • Surface modification with brain-targeting ligands (peptides, antibodies, aptamers)
  • Controlled size and charge tuning for optimal BBB penetration
  • Dual and multi-drug encapsulation strategies

3. Formulation Design and Optimization

  • Through iterative formulation, we balance encapsulation efficiency, particle size, surface charge, and stability.

4. In Vitro Evaluation & In Vivo Preclinical Assessment

  • Using BBB-mimicking models, we assess transport efficiency, cytotoxicity, and cellular uptake.
  • Biodistribution and brain uptake studies validate targeting efficacy, while PK/PD data support dose strategy design.

5. Stability and Scalability Testing

  • Accelerated and long-term stability studies under ICH guidelines
  • Liposome batch reproducibility and process scale-up evaluation

Benefits of Our Brain Targeted Liposomal Drug Delivery System Development

BOC Sciences offers unparalleled expertise in self-adjuvanting liposomal vaccine development. Our advantages include:

Applications of Our Brain Targeted Liposomal Drug Delivery System Development

The ability to deliver therapeutic agents precisely to the brain is revolutionizing preclinical research and the development of treatments for central nervous system (CNS) disorders. Brain-targeted liposomal delivery systems offer unique advantages in increasing drug solubility, improving pharmacokinetics, and reducing systemic toxicity—all essential for addressing the complex pathophysiology of neurological diseases.

Neurodegenerative Disorders

Diseases such as Alzheimer's, Parkinson's, and Huntington's are marked by progressive neuronal loss, often localized to specific brain regions. Liposomes functionalized with BBB-penetrating ligands can deliver neuroprotective compounds, anti-amyloid agents, or mitochondrial stabilizers directly to affected tissues. For example, transferrin- or lactoferrin-modified liposomes have been employed to facilitate the delivery of acetylcholinesterase inhibitors or anti-aggregative peptides in preclinical Alzheimer's models, resulting in improved cognitive function and reduced plaque burden.

Brain Tumors and Gliomas

Malignant gliomas are among the most aggressive and drug-resistant brain cancers due to their infiltrative nature and the restrictive BBB. Liposomes engineered with ligands such as angiopep-2 or RGD peptides can selectively home in on tumor vasculature or integrin-overexpressing glioma cells. Encapsulation of chemotherapeutics like doxorubicin or temozolomide in PEGylated liposomes has shown significantly enhanced tumor accumulation and reduced systemic side effects in orthotopic glioblastoma models. Our liposomal systems can be tailored for co-delivery strategies, combining cytotoxic agents and siRNA for synergistic tumor inhibition.

Neuroinflammation and Ischemic Stroke

Liposomes carrying anti-inflammatory agents such as dexamethasone, minocycline, or antioxidants can be directed to sites of neuroinflammation associated with stroke, multiple sclerosis, or traumatic brain injury. Liposomes modified with cell-penetrating peptides or macrophage-homing ligands can cross the BBB and accumulate in inflamed tissues, promoting neuronal survival and functional recovery. In ischemia-reperfusion models, such systems have shown reductions in infarct size and inflammatory cytokine expression.

Psychiatric and Behavioral Disorders

Emerging studies suggest that liposomal delivery of neuromodulatory compounds (e.g., serotonin or dopamine analogs, NMDA receptor modulators) can enhance therapeutic responses in disorders such as depression, schizophrenia, or anxiety. By targeting specific brain regions, these systems can minimize peripheral side effects and improve CNS bioavailability—crucial for drugs with poor BBB permeability or narrow therapeutic windows.

Genetic and Rare Neurological Disorders

Liposomal carriers can serve as efficient vectors for gene editing tools (e.g., CRISPR/Cas9) or RNA therapeutics (e.g., antisense oligonucleotides, siRNA) in treating inherited CNS disorders. Conditions such as spinal muscular atrophy, lysosomal storage diseases, and leukodystrophies may benefit from CNS-targeted delivery of therapeutic nucleic acids. Our systems can be engineered for sustained release, endosomal escape, and region-specific targeting—essential for long-term genetic correction and disease modification.

CNS Infectious Diseases

In conditions like HIV-associated neurocognitive disorders (HAND) or neurotuberculosis, liposomal systems enable the delivery of antiviral or antibacterial agents across the BBB—often a limiting factor in standard treatments. Liposomes help achieve therapeutic concentrations in the brain parenchyma without systemic toxicity, opening new preclinical research directions for CNS-targeted anti-infective strategies.

FAQs – Insights about Our Brain Targeted Liposomal Drug Delivery System Development

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How do you ensure that liposomes effectively cross the blood-brain barrier (BBB)?

We employ ligand-mediated targeting strategies such as transferrin, RVG peptide, angiopep-2, and antibody conjugation to facilitate receptor-mediated transcytosis across the BBB. Additionally, our in vitro BBB models simulate tight junction integrity, and all candidate formulations are screened in preclinical in vivo models for brain uptake efficiency.

What is the typical size range of your brain-targeted liposomes, and why does it matter?

Our liposomes are typically engineered within the 80–150 nm range, which balances prolonged systemic circulation and efficient BBB penetration. Size is tightly controlled using dynamic light scattering (DLS) and extrusion methods to ensure optimal biodistribution and targeting efficiency.

What is the advantage of using liposomal carriers for CNS drug delivery compared to other nanoparticle systems?

Liposomal systems are biocompatible, biodegradable, and less immunogenic than many synthetic nanocarriers. Their lipid-based composition mimics biological membranes, allowing for superior BBB interaction and minimal systemic toxicity. Surface functionalization further enhances their targeting specificity and pharmacokinetics.

Can you develop dual-targeted liposomes (e.g., BBB + tumor-specific)?

Yes. We have experience in dual-ligand surface engineering for complex targeting scenarios, such as liposomes designed to first cross the BBB and then target glioblastoma or metastatic lesions via tumor-specific ligands (e.g., folate, EGFR antibodies).

Can you support projects requiring targeted delivery of nucleic acids or gene editing tools to the brain?

Absolutely. We provide liposomal encapsulation and delivery systems for siRNA, miRNA, mRNA, and CRISPR-Cas components, with a focus on achieving brain-specific uptake and expression. We validate cellular uptake, endosomal escape, and gene silencing efficacy in relevant neuronal models.

To accelerate your brain-targeted therapeutic programs, contact BOC Sciences today and explore how our liposomal innovation can deliver your molecule—where it matters most.

Supplementary Knowledges: Brain-targeted Drug Delivery

What is the brain specific drug delivery system?

A brain-specific drug delivery system is an engineered platform designed to transport therapeutic agents directly to the brain while minimizing exposure to peripheral tissues. These systems typically incorporate targeting strategies—such as ligand-functionalized nanocarriers (e.g., liposomes)—that exploit receptor-mediated transport mechanisms at the blood-brain barrier (BBB). The goal is to enhance drug accumulation in brain tissue, improve therapeutic efficacy, and reduce systemic side effects, especially for neurological or neurodegenerative conditions.

What is the blood - brain barrier(BBB) and what does it do?

The blood-brain barrier (BBB) is a highly selective, semipermeable barrier formed by endothelial cells lining cerebral microvessels. It functions to protect the brain from harmful substances in the bloodstream while tightly regulating the transport of essential nutrients and signaling molecules. While crucial for maintaining brain homeostasis, the BBB also poses a significant obstacle to drug delivery, as it restricts the passage of most therapeutics—especially large, hydrophilic, or charged molecules—into the central nervous system.

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