The nervous system's complex structure requires therapies that are highly targeted and biocompatible. Nanoparticles, 1-100 nm carriers, offer a versatile platform for neurological drug delivery. Liposomes, polymeric nanoparticles, dendrimers, and inorganic nanoparticles can encapsulate or bind diverse neuroactive compounds. Modifying size, surface charge, and functional groups allows precise control of drug release and distribution. PLGA nanoparticles, for example, improve stability and prolong circulation for neurotrophic factor delivery. Advances in nanotechnology continue to make nanoparticle-based systems essential for effective neurological therapeutics.
Developing effective therapies for neurological disorders is hindered by multiple biological barriers. The blood-brain barrier (BBB) is a highly selective interface that restricts the entry of most macromolecules and hydrophilic compounds, preventing more than 98% of small-molecule drugs and nearly all biologics from accessing the central nervous system (CNS). Additionally, pathological regions in the CNS, such as tumor microenvironments or sites of neuroinflammation, exhibit pronounced heterogeneity, further complicating targeted delivery. Conventional systemic administration often results in non-specific distribution, leading to peripheral toxicity. Many therapeutic agents also face chemical instability, rapid systemic clearance, and limited CNS retention—illustrated by the low brain accumulation of antibody-based therapeutics in Alzheimer's disease models. These factors collectively represent significant bottlenecks in neurological drug development.
Nanoparticle-based carriers offer distinct advantages for CNS drug delivery. Their core structures protect labile therapeutics from enzymatic and chemical degradation, improving bioavailability. Surface modifications can prolong circulation time while minimizing capture by the liver and spleen. Critically, functionalized nanoparticles can leverage receptor-mediated transport mechanisms to actively cross biological barriers and accumulate selectively in brain regions. Drug-loaded nanoparticles also allow for controlled release, maintaining therapeutic concentrations at the target site and reducing dosing frequency. In Parkinson's disease models, nanoparticles delivering dopamine precursors have demonstrated prolonged striatal coverage compared to free drugs. Moreover, these platforms can co-deliver diagnostic probes alongside therapeutics, enabling real-time monitoring of treatment efficacy.
Innovative strategies have been developed to enhance nanoparticle penetration of the BBB. Receptor-mediated transcytosis is among the most promising approaches, where nanoparticles conjugated with transferrin or low-density lipoprotein receptor ligands exploit endogenous transport mechanisms. For instance, gold nanoparticles functionalized with transferrin exhibit approximately fivefold higher brain accumulation. Cell-penetrating peptides, such as TAT, can further enhance membrane translocation, while charge-neutralization strategies exploit electrostatic interactions between cationic nanoparticles and endothelial cells to facilitate adsorptive-mediated transport. Biodegradable polymeric nanoparticles can transiently modulate tight junctions to improve permeability. Recently, exosome-mimetic nanoparticles have demonstrated inherent tropism for neural tissues, offering unique advantages in BBB traversal. Collectively, these advanced approaches are progressively transforming the efficiency and precision of CNS drug delivery.
Nanocarriers in the nervous system function not only as precise delivery vehicles but also as multi-level biological modulators that promote neuroprotection and regeneration. The core mechanisms include targeted delivery to neurons and glial cells, modulation of oxidative stress and neuroinflammatory microenvironments, and efficient gene or siRNA delivery within neural tissue. The following sections detail the implementation pathways and representative examples for each mechanism.
Due to the diverse cell types in the nervous system, therapeutics must be distributed selectively. Nanoparticles can achieve targeted delivery by modifying their surfaces with specific ligands. For neurons, commonly used ligands include antibodies against neural cell adhesion molecules (NCAM), peptides derived from synaptophysin, and molecules that interact with blood-brain barrier receptors like transferrin receptor.
Experimental data show that PLGA nanoparticles functionalized with transferrin receptor ligands achieve approximately threefold higher neuronal uptake in mouse brains compared to unmodified nanoparticles, substantially increasing local concentrations of neuroprotective agents. Similarly, chitosan nanoparticles targeting GFAP preferentially accumulate in reactive astrocytes in brain injury models, suppressing excessive glial proliferation and facilitating restoration of neural network function.
Oxidative stress and chronic inflammation are common pathological features in neurodegenerative contexts. Nanocarriers intervene via two main mechanisms: direct delivery of antioxidants or anti-inflammatory agents, and utilization of intrinsic material properties to scavenge reactive species or modulate inflammatory cell activity.
Metal oxide nanoparticles, such as CeO2, possess enzyme-mimetic activity capable of simulating superoxide dismutase (SOD) and catalase (CAT) functions, continuously eliminating superoxide and hydrogen peroxide to reduce oxidative damage. When CeO2 nanoparticles are co-encapsulated with anti-inflammatory small molecules in liposomes, dopaminergic neuron survival in Parkinson's disease models increases by approximately 40%.
Polymeric nanoparticles maintain sustained concentrations of anti-inflammatory drugs in microglia, inhibiting NF κB signaling and reducing pro-inflammatory cytokines such as TNF α and IL 1β. In cerebral ischemia–reperfusion models, this approach significantly alleviates tissue edema and improves neural function.
Gene editing and RNA interference offer precise molecular tools for neural regeneration but face challenges from nucleic acid negative charge, enzymatic degradation, and blood-brain barrier restrictions. Nanocarriers overcome these obstacles via charge neutralization, protective encapsulation, and controlled intracellular release.
Cationic polymers, such as polyethyleneimine or chitosan, form 80-120 nm complexes with siRNA, enabling receptor-mediated endocytosis across the BBB into neurons. For example, PEG-modified gold nanoparticles carrying siRNA targeting α-synuclein achieve approximately 70% gene knockdown in α-synuclein overexpressing transgenic mice, improving motor behavior.
Similarly, gene-editing delivery can be facilitated using lipid or polymeric nanoparticles. Lipid nanoparticles containing gene-editing mRNA and specific sgRNA successfully knocked out PTEN in inhibitory neurons of the mouse hippocampus, promoting axonal regeneration and enhancing synaptic plasticity, demonstrating an effective molecular strategy for neuroregeneration.
Fig.1 Overview of Nanoparticle Types in Neurological Treatment1,2.
BOC Sciences offers versatile nanoparticles engineered for targeted drug delivery and therapeutic applications. Our customized solutions enhance treatment efficacy and precision.
The blood-brain barrier presents a formidable obstacle to effective drug delivery in the nervous system. Nanoparticles, with their tunable size, surface properties, and multifunctional carrier capabilities, offer new avenues for the precise delivery of neuroactive molecules. Based on material composition and functional design, commonly used nanoparticles for neurological applications can be categorized into three major types: lipid-based, polymer-based, and metallic/magnetic nanoparticles. Each class exhibits unique advantages in drug encapsulation, controlled release, and imaging applications.
Lipid-based nanoparticles include liposomes, solid lipid nanoparticles (SLNs), and nanoemulsions. Their lipidic core enables encapsulation of both hydrophilic and lipophilic drugs, providing a protective barrier against enzymatic degradation while enhancing BBB permeability. Literature reports indicate that liposomes can deliver neuroprotective agents to affected regions in models of neurodegeneration, increasing brain drug concentrations and reducing systemic exposure. SLNs, with particle sizes typically below 100 nm, achieved through lipid composition optimization, further enhance uptake by brain endothelial cells. Nanoemulsions, leveraging oil phases to solubilize poorly water-soluble neuroactive compounds, exhibit rapid initial release followed by sustained delivery, making them suitable for conditions requiring immediate therapeutic action. Moreover, surface functionalization with ligands such as transferrin or brain-targeting peptides allows for selective accumulation in specific brain regions, improving delivery efficiency while minimizing off-target exposure.
Polymeric nanoparticles are composed of synthetic polymers (e.g., PLGA, PLA) or natural polymers (e.g., chitosan, alginate). PLGA nanoparticles are widely used for long-term neurodrug delivery due to their biodegradability and tunable release profiles. Studies show that PLGA carriers can sustain the release of neuroprotective agents over several weeks, effectively maintaining therapeutic concentrations in the CNS. Chitosan-based nanoparticles utilize electrostatic interactions between their positive surface charge and the negatively charged brain endothelium to improve BBB transport, and surface PEGylation can prolong circulation time while reducing liver and spleen uptake. Dendrimers, with their highly branched three-dimensional architecture, offer abundant surface functional groups for high drug loading and multi-ligand targeting, demonstrating promising results in neurological drug delivery applications. The controllable degradation of polymeric nanoparticles allows precise modulation of drug release kinetics, enabling "on-demand" delivery aligned with disease progression.
Metallic nanoparticles, such as gold, silver, and silica, provide dual capabilities for drug delivery and real-time imaging due to their distinctive optical and plasmonic properties. Gold nanoparticles can be conjugated with antibodies or peptides for high-affinity targeting of specific neural cells, and their photothermal response to near-infrared light can enhance localized drug release or induce direct ablation of pathological tissue. Magnetic nanoparticles, primarily composed of iron oxide, can be directed to target brain regions under an external magnetic field, achieving localized high-concentration drug deposition while minimizing systemic exposure. Magnetic resonance imaging (MRI) enables sensitive tracking of these nanoparticles, integrating therapeutic delivery with diagnostic monitoring. Surface modification of metallic and metal oxide nanoparticles with PEG or other biocompatible polymers enhances circulation stability and reduces immune recognition, providing a feasible approach for sustained delivery in long-term neurological interventions.
At BOC Sciences, we enhance the delivery efficiency of neurological nanomedicines through systematic formulation optimization processes. Applying the principle of "Quality by Design" (QbD), we perform detailed analysis of critical quality attributes (CQAs) of nanoparticle formulations, such as particle size distribution, surface charge, drug loading capacity, and release kinetics. Through experimental design, our researchers precisely evaluate the impact of various formulation parameters on the nanoparticles' ability to cross the BBB, enabling us to develop reliable predictive models.
In the optimization of lipid-based nanoparticles, BOC Sciences has pioneered microfluidic-based preparation techniques, achieving precise control over particle size and polydispersity. By adjusting factors such as the ratio of phospholipids to cholesterol and the type and concentration of surfactants, we significantly enhance the stability of nanoparticles in systemic circulation. For polymeric nanoparticles, our optimization efforts focus on fine-tuning molecular weight, crystallinity, and degradation rate to ensure sustained drug release at the targeted neural site. These systematic formulation optimization activities provide a solid foundation for the industrialization of neurological nanomedicines.
Table 1. Nanoparticle Development and Characterization Services for CNS Applications.
| Service Category | Description | Inquiry |
| Custom Nanoparticle Synthesis | Design and fabrication of LNPs, polymeric, or metallic/magnetic nanoparticles with tunable size, surface charge, and physicochemical properties, enabling tailored CNS-targeted therapeutic solutions. | Inquiry |
| Nanoparticle Characterization & Quality Control | Comprehensive analysis of particle size, polydispersity, surface charge, and endotoxin levels using advanced techniques, ensuring reproducible preparation and reliable quality for research and scale-up. | Inquiry |
| Scale-Up & Manufacturing | Scalable nanoparticle production from laboratory to pilot scale, maintaining consistent particle properties and formulation performance for advanced research and translational applications. | Inquiry |
| Surface Functionalization Services | PEGylation, transferrin conjugation, or brain-targeting peptide modification to tune nanoparticle surface properties, enhance circulation stability, and improve CNS targeting efficiency. | Inquiry |
| Nanoparticle Stability Evaluation | Assessment of thermal, pH, and freeze-drying stability to ensure long-term storage, formulation robustness, and performance in CNS therapeutic applications. | Inquiry |
| Drug Loading & Release Optimization | Encapsulation, quantification, and in vitro release profiling of therapeutic agents, allowing controlled release kinetics to maximize efficacy and reduce dosing frequency. | Inquiry |
| Physicochemical Analysis | Comprehensive evaluation of nanoparticle morphology, surface charge, and crystalline structure, providing critical data for formulation development product characterization. | Inquiry |
BOC Sciences tailors nanoparticle solutions to address the specific pathophysiological features of various CNS diseases. For neurodegenerative diseases, we have developed composite nanoparticle systems capable of co-loading multiple neuroprotective agents. These systems are designed to concurrently intervene in the multiple pathological mechanisms of Alzheimer's disease, such as β-amyloid deposition and tau hyperphosphorylation. For brain tumor treatment, BOC Sciences has engineered nanoparticles that are responsive to the tumor microenvironment, capable of releasing chemotherapeutic drugs rapidly under acidic pH or high matrix metalloproteinase (MMP) concentrations, thereby enhancing drug uptake by tumor cells. In the field of stroke therapy, we have developed nanoparticles targeting the ischemic penumbra, functionalized with antibodies that recognize vascular cell adhesion molecules to achieve selective accumulation in ischemic regions.
Additionally, for neuropsychiatric disorders, BOC Sciences has developed nanoparticle carriers capable of crossing the blood-brain barrier to deliver traditionally brain-penetrating molecules, such as neuroregulatory agents. These customized solutions embody the latest advancements in precision neuropharmacology, highlighting the significant strides in creating therapies with enhanced targeting and efficacy.
Table 2. Nanoparticle Products for CNS Drug Delivery.
| Product Category | Description | Inquiry |
| Lipid Nanoparticles | Lipid-based carriers including liposomes, solid lipid nanoparticles, and nanoemulsions, designed for high drug-loading, protecting cargo stability, and enhancing blood-brain barrier penetration for neuroactive agents and RNA therapeutics. | Inquiry |
| Polymeric Nanoparticles | Biodegradable or natural polymer carriers such as PLGA, PLA, chitosan, and dendrimers, offering controlled drug release, surface functionalization, and prolonged circulation for sustained neuroprotective and regenerative factor delivery. | Inquiry |
| Magnetic Nanoparticles | Gold, silver, and iron oxide nanoparticles enabling dual functions of drug delivery and imaging, with magnetic guidance capability, allowing precise targeting of brain regions while supporting diagnostic tracking. | Inquiry |
| Functionalized Nanoparticles | Nanoparticles modified with transferrin, brain-targeting peptides, or PEG to enhance selective uptake by neurons or glial cells, improving bioavailability and enabling precise delivery of neuroprotective or gene-editing molecules. | Inquiry |
These research activities and technological innovations are at the forefront of the rapidly advancing field of neurological nanomedicines. Through our expertise in nanoparticle development and optimization, BOC Sciences is making critical contributions to the next generation of therapies for CNS diseases. Our comprehensive platform, from formulation design and molecular engineering to customized delivery solutions, positions us as a key partner in the evolving landscape of neurological drug development.
Nanoparticles offer significant potential in neurological disorder research through their ability to deliver targeted, sustained-release therapies with high precision. By modifying particle size, surface charge, and functional groups, nanoparticles can achieve controlled drug delivery and targeted treatment. BOC Sciences provides a comprehensive range of custom nanoparticle products and services, including lipid nanoparticles, polymeric nanoparticles, and magnetic nanoparticles, tailored to meet the specific needs of neurological research. Our services cover the entire process from nanoparticle design and synthesis to surface functionalization, quality control, and stability testing, ensuring that each batch meets the highest standards. Additionally, we offer scalable production capabilities, supporting smooth transitions from laboratory-scale development to pilot and industrial-scale manufacturing.
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