The development of nanomedicine in oncology reflects a multidisciplinary trajectory integrating materials science, pharmacology, and molecular biology. Over the past six decades, the field has evolved from Feynman's conceptualization of nanotechnology to the practical application of nanoscale drug delivery systems. A pivotal advance emerged in the 1970s and 1980s when studies demonstrated that nanoparticle-encapsulated therapeutics preferentially extravasate into tumor tissues, leading to the formulation of the enhanced permeability and retention (EPR) effect. This foundational principle established a theoretical basis for the design of nanostructures aimed at overcoming the limitations of conventional chemotherapy.
The last fifteen years have witnessed rapid growth in cancer nanomedicine. From the early Doxil (1995) to multi-drug formulations like Vyxeos (2017) and further innovations such as Hensify (2019), nanoparticles have increasingly demonstrated potent therapeutic performance with reduced systemic toxicity. Publication trends mirror this progress, rising from 640 papers in 2012 to 2,487 in 2022, highlighting the expanding research interest and confidence in nanoscale strategies for cancer applications.
Nanoparticle-based delivery systems offer distinct advantages for tumor targeting, primarily derived from their unique physicochemical properties and biological interactions.
Selective Accumulation: Nanocarriers can differentiate between malignant and normal tissues, minimizing off-target effects. This selectivity is achieved via two complementary mechanisms: passive accumulation through the tumor's leaky vasculature and compromised lymphatic drainage, and active targeting through surface functionalization that guides nanoparticles to cells overexpressing specific receptors.
Pharmacokinetic Optimization: Encapsulation enhances drug circulation time, increases local tumor concentrations, and limits off-target distribution. Additionally, nanoparticles protect labile molecules such as mRNA or siRNA from degradation, preserving stability and functional activity, as evidenced by the success of lipid nanoparticle-based vaccines during the COVID-19 pandemic.
Various classes of nanoparticles are utilized in cancer research, each with unique structural features and functional objectives:
Liposomes: Among the earliest nanocarriers, liposomes (e.g., Doxil) exploit EPR-mediated accumulation while mitigating systemic toxicity.
Inorganic Nanoparticles: Gold nanoparticles enable photothermal therapy, while superparamagnetic iron oxide nanoparticles (SPIONs) can serve as imaging contrast agents.
Polymeric Nanocarriers: Polymers such as poly (lactic-co-glycolic acid) (PLGA) and hyaluronic acid nanoparticles offer biocompatibility and tunable drug release profiles.
Mesoporous Silica Nanoparticles: High drug-loading capacity and controlled release properties make them suitable for precision delivery.
Selenium Nanoparticles (SeNPs): Especially when biomimetically modified, SeNPs demonstrate promising antitumor activity.
Hybrid Nanoparticles: Combining multiple materials, hybrid systems provide innovative solutions for complex challenges, including barrier penetration and multi-functional targeting.
Fig.1 Smart nanoparticle delivery system for cancer therapy1,2.
Tumor targeting by nanoparticles relies on two complementary strategies: passive targeting and active targeting, which collectively enhance selective accumulation within tumor tissues.
Passive Targeting: Exploits the structural abnormalities of tumor vasculature. Nanoparticles within the 10–100 nm range extravasate through endothelial gaps and are retained due to impaired lymphatic drainage, in accordance with the EPR effect. Passive targeting does not require specific molecular recognition, relying primarily on nanoparticle size and physical distribution characteristics.
Active Targeting: Involves surface modification with ligands (e.g., antibodies, peptides, small molecules) that bind selectively to overexpressed receptors on tumor cells. Following passive accumulation via EPR, ligand-receptor interactions trigger receptor-mediated endocytosis, enhancing intracellular uptake and improving delivery efficiency.
The EPR effect underlies the selective accumulation of nanoparticles in tumor tissues. Tumor vasculature exhibits enlarged endothelial gaps, structural irregularities, and impaired lymphatic clearance, enabling nanoparticles to extravasate and remain in the tumor interstitium at higher concentrations than in normal tissues.
Recent studies have expanded this concept through the active transport and retention (ATR) principle, suggesting that nanoparticle entry may also involve transcytosis through specialized endothelial cells, vesicular trafficking, or interactions with circulating immune cells. Tumor-associated macrophages may further facilitate intratumoral distribution, while residual lymphatics contribute to partial nanoparticle clearance. Accumulation patterns depend on tumor type and nanoparticle properties, with soft nanoparticles favoring passive mechanisms and harder, rigid nanoparticles more likely to exploit active transcytosis.
Receptor-mediated uptake is a critical mechanism for efficient intracellular delivery, relying on ligand-receptor binding. Nanoparticles decorated with specific ligands bind to overexpressed tumor cell receptors, triggering endocytosis pathways. Common targets include CD44, folate receptor, transferrin receptor, and integrins. This strategy not only enhances cellular specificity but also facilitates intracellular release. Endosomal acidification promotes payload release from nanoparticles, maximizing intracellular availability while limiting exposure to non-target cells. Biomimetic approaches further improve receptor-mediated uptake. For example, selenium nanoparticles encapsulated within tumor-derived extracellular vesicles leverage homotypic targeting to selectively interact with cells of the same origin, substantially improving delivery efficiency and tumor growth inhibition in preclinical models. Nanotechnology thus exploits fundamental features of tumor biology to achieve unprecedented precision in therapeutic delivery. As mechanistic understanding deepens, next-generation nanoparticles promise enhanced targeting specificity, efficient intracellular transport, and innovative solutions for complex tumor environments.
BOC Sciences offers versatile nanoparticles engineered for targeted drug delivery and therapeutic applications. Our customized solutions enhance treatment efficacy and precision.
Lipid-based nanoparticles and liposomes offer distinct advantages as carriers for drug and gene delivery. These vesicular systems, composed of phospholipid bilayers, can encapsulate both hydrophilic and hydrophobic therapeutic agents. In nucleic acid delivery, cationic lipids form stable electrostatic complexes with negatively charged nucleic acids, protecting them from enzymatic degradation and facilitating intracellular release. For instance, siRNA-loaded lipid nanoparticles exploit ionizable lipids that protonate under acidic conditions, promoting endosomal escape and efficient gene silencing.
Surface modification with polyethylene glycol (PEG) prolongs circulation time and reduces clearance by the reticuloendothelial system. Functionalized liposomes can incorporate targeting ligands, such as transferrin or folate, enabling selective recognition of cells with overexpressed receptors and enhancing tumor-specific accumulation. Thermosensitive liposomes undergo phase transitions under localized heating, enabling controlled drug release and higher intratumoral concentrations. These strategies also support dual-drug co-delivery, facilitating precise molar ratios to overcome tumor heterogeneity-induced resistance.
Polymeric nanocarriers provide tunable physicochemical properties that are critical for controlled drug release and nucleic acid delivery. PLGA nanoparticles, for example, allow precise modulation of drug release kinetics by adjusting monomer ratios. Dendritic polymers, with highly branched structures and abundant surface functional groups, can simultaneously load multiple therapeutic agents and undergo surface modification for targeted delivery.
Metal-based nanoparticles exhibit unique optical, magnetic, and structural properties. Gold nanoparticles can convert absorbed light into heat via surface plasmon resonance and allow facile surface functionalization for targeting. Mesoporous silica nanoparticles offer highly ordered pores and large surface area, enabling high-capacity drug loading. Iron oxide nanoparticles can be magnetically guided to specific locations while providing imaging contrast. Some metal-based nanoparticles also respond to tumor microenvironment features, such as elevated reactive oxygen species, to enhance therapeutic effects.
Hybrid nanoparticle systems integrate multiple material advantages to achieve synergistic therapeutic effects. Lipid-polymer hybrid nanoparticles combine the biocompatibility of liposomes with the structural stability of polymers, maintaining integrity during circulation and releasing payloads rapidly upon reaching target sites. Gold nanoshell-liposome composites simultaneously enable photothermal therapy and drug delivery; near-infrared (NIR) irradiation induces localized heating, triggering payload release.
Upconversion nanoparticle-mesoporous silica composites convert NIR light into visible light, activating photosensitizers to produce singlet oxygen for deep-tissue photodynamic therapy. Iron oxide-gold core-shell nanoparticles combine magnetic targeting and photothermal effects, allowing externally guided tumor accumulation and localized heat generation under NIR illumination. Such multifunctional systems provide versatile platforms for combinatorial cancer therapies.
Light-activated nanoparticles exert therapeutic effects through specific photophysical and photochemical processes. Photothermal nanoparticles absorb photons at specific wavelengths via surface plasmon resonance or electronic transitions and convert this energy into heat through non-radiative relaxation, elevating local temperatures. Gold nanorods in the NIR region, for example, generate temperatures of 42–45℃ upon irradiation, inducing apoptosis in tumor cells.
Photodynamic nanoparticles function as photosensitizers, transferring energy to surrounding oxygen molecules upon excitation to produce reactive oxygen species (ROS). Singlet oxygen and other ROS oxidize critical biomolecules, damaging cell membranes and organelles. Titanium dioxide nanoparticles, under UV irradiation, generate electron-hole pairs that react with water and oxygen to produce hydroxyl radicals and superoxide, leading to programmed cell death.
Gold nanostructures are ideal photothermal agents due to their tunable optical properties. Nanorods allow precise control of surface plasmon resonance peaks in the NIR window, enabling deep tissue penetration. Nanoshells, with controlled silica core and gold shell dimensions, strongly absorb NIR light, making them suitable for solid tumor ablation. Gold nanostars, with branched morphologies, enhance local electromagnetic fields, improving photothermal conversion efficiency.
Carbon-based agents, including carbon nanotubes and graphene derivatives, provide broad NIR absorption and high photothermal efficiency. Single-walled carbon nanotubes penetrate deeper tissue regions, while PEGylated graphene oxide improves solubility and biocompatibility, producing efficient heat under 808 nm irradiation. Carbon quantum dots exhibit photostability and low cytotoxicity, enabling simultaneous photothermal therapy and imaging.
Nanoparticle platforms enable spatially and temporally controlled combinatorial therapies, integrating phototherapy with chemotherapy. In photothermal-chemotherapy systems, nanoparticles co-deliver chemotherapeutics and photothermal agents; laser irradiation produces heat that directly damages tumor cells while enhancing vascular permeability and drug release, increasing intracellular drug accumulation. For instance, gold nanorod-doxorubicin composites under NIR irradiation induce simultaneous thermal and chemotherapeutic effects, significantly improving tumor inhibition.
Photodynamic-chemotherapy strategies utilize ROS to sensitize cells to chemotherapeutic agents. Mesoporous silica nanoparticles co-loading photosensitizers and chemotherapeutics generate ROS under light exposure, disrupting cellular defense mechanisms and enhancing intracellular drug retention. Zinc phthalocyanine-doxorubicin composites, upon light activation, produce singlet oxygen and promote drug release from endosomes into the nucleus, achieving synergistic anti-tumor effects. Such multi-modal approaches reduce required drug doses, minimize off-target toxicity, and enhance overall treatment efficiency.
Effective penetration of nanoparticles within tumor tissue remains a significant challenge. The tumor microenvironment is often characterized by high cellular density, irregular vascular architecture, and a dense extracellular matrix, all of which restrict nanoparticle distribution and deep tissue diffusion. Even when nanoparticles accumulate at the tumor site via passive targeting (enhanced permeability and retention effect) or active ligand-receptor-mediated mechanisms, their intratumoral dispersal is frequently hindered by these physical barriers.
Recent studies have highlighted strategies to improve nanoparticle penetration by tuning particle size, surface charge, and structural flexibility. Soft or compressible nanoparticles can navigate dense cellular networks more effectively than rigid particles, while interactions with tumor-associated stromal and immune cells can further enhance intratumoral distribution. Multifunctional nanoparticles integrating enzymatic or microenvironment-responsive elements can locally modulate matrix density, facilitating deeper tissue penetration and more uniform therapeutic agent delivery.
Nanoparticle stability and biocompatibility are critical determinants of delivery efficiency. Unmodified nanoparticles may aggregate or prematurely release their payloads, resulting in inconsistent dosing and off-target distribution. Additionally, nanoparticle materials may elicit immune responses or produce potentially toxic degradation byproducts, compromising safety and efficacy.
To address these challenges, surface modifications and material optimizations are commonly employed. PEGylation, natural polymer coatings, and biomimetic membrane cloaking extend circulation time, reduce immune clearance, and maintain drug stability. Controlled release mechanisms, including pH-sensitive, temperature-responsive, or light-triggered systems, allow precise spatial and temporal release of therapeutic agents, maximizing local efficacy while minimizing systemic exposure.
BOC Sciences possesses extensive expertise in the custom design and synthesis of nanoparticles, allowing researchers to generate nanomaterials with precise chemical structures and functionalities tailored to specific experimental needs.
Precision Synthesis Techniques: The company utilizes advanced chemical strategies, including click chemistry and sol-gel methods, to construct nanoparticles with defined architectures. For instance, BOC Sciences has synthesized periodic mesoporous organosilica nanoparticles (PMONPs) protected with tert-butoxycarbonyl (BOC) groups. These nanoparticles can release CO2 under specific conditions, such as acidic environments or elevated temperatures, providing opportunities for responsive applications in integrated experimental settings.
Surface Engineering and Functionalization: Surface modification plays a critical role in optimizing nanoparticle performance. BOC Sciences leverages techniques such as PEG grafting to enhance circulation stability and the conjugation of targeting ligands, including folate, peptides, or antibodies, to achieve active targeting toward specific cell populations.
Advanced Material Design: In polymeric nanoparticle development, the company employs block copolymer self-assembly to spatially arrange functional groups, such as benzophenone or ferrocene, within discrete nanoparticle domains. This precise spatial control facilitates the creation of multifunctional nanoparticles capable of photoreactivity, shape transformation, or subsequent chemical functionalization.
Table 1. Functional Nanoparticles for Cancer Research Applications.
| Product Name | Features & Functions | Typical Applications | Inquiry |
| Targeted Liposomes | Encapsulate hydrophilic and hydrophobic drugs; PEGylated for prolonged circulation; surface can be modified with targeting ligands (e.g., folate, transferrin) | Tumor drug delivery, siRNA/mRNA delivery, enhanced tumor-specific accumulation | Inquiry |
| Thermosensitive Liposomes | Sensitive to localized heating, enabling controlled drug release | Localized tumor drug release, dual-drug combination therapy | Inquiry |
| PLGA Nanoparticles | Adjustable monomer ratios control drug release kinetics; surface functionalizable | Controlled release of anticancer drugs, tumor-targeted delivery | Inquiry |
| Dendrimers | Highly branched structures with abundant surface functional groups; can load multiple therapeutic agents | Combination drug delivery, gene delivery applications | Inquiry |
| Gold Nanoparticles | Strong photothermal conversion; easily functionalized | Photothermal therapy combined with drug delivery, tumor-targeted hyperthermia | Inquiry |
| Mesoporous Silica Nanoparticles (MSNs) | High surface area and ordered pores; high drug loading capacity | High-capacity drug carriers, controlled release of anticancer agents | Inquiry |
| Iron Oxide Nanoparticles | Magnetically guided; can serve as imaging contrast agents | Magnetic-targeted drug delivery, image-guided studies | Inquiry |
| Hybrid Nanoparticles | Integrate lipid, polymer, and metal advantages for multifunctional synergy | Combined drug + photothermal/photodynamic therapy, stimulus-responsive tumor delivery | Inquiry |
BOC Sciences offers a broad spectrum of delivery solutions to improve the transport, stability, and targeted release of both small-molecule therapeutics and genetic materials.
Targeted Liposomal Platforms: The company provides liposome bio-conjugation services to functionalize lipid surfaces with specific targeting moieties. By attaching ligands that recognize overexpressed cellular receptors, such as folate or transferrin receptors, liposomes achieve enhanced cellular uptake and preferential localization within tumor-like environments, improving therapeutic specificity.
Intelligent Drug Precursors and Carriers: BOC Sciences develops chemically modified drug derivatives, such as BOC-NH-DOX (tert-butoxycarbonyl-protected doxorubicin). The BOC modification increases molecular stability during nanoparticle formulation and enables controlled activation in response to environmental cues, such as acidic pH, facilitating localized drug release.
Gene Delivery Platforms: The company also provides nanoparticle-based solutions for nucleic acid delivery, including siRNA and mRNA. These systems commonly utilize ionizable lipids or cationic polymers to encapsulate and protect fragile genetic materials, promoting cellular internalization and endosomal escape for efficient cytoplasmic delivery and functional gene modulation.
To support the development of high-quality, well-defined nanomaterials, BOC Sciences offers comprehensive analytical and characterization services.
Composition and Structural Analysis: The company employs techniques such as mass spectrometry (MS), UV-Vis spectroscopy, infrared spectroscopy (IR), nuclear magnetic resonance (NMR), and chromatographic methods (GC, LC) to determine chemical composition, molecular structures, and purity of nanomaterials.
Morphology and Physical Property Characterization: Nanoparticle size, shape, and surface features are analyzed through scanning electron microscopy (SEM) and transmission electron microscopy (TEM), while X-ray diffraction (XRD) is used to assess crystalline structures.
In-Depth Characterization of Biotherapeutics: For complex biologics such as proteins and antibodies, BOC Sciences provides peptide mapping, glycosylation profiling, and high-resolution LC/Q-TOF mass spectrometry for precise molecular weight determination and structural analysis, supporting the rational design and optimization of bioactive nanoparticle systems.
Table 2. Nanoparticle-Related Services for Cancer Therapy Research at BOC Sciences.
| Service Name | Service Description | Inquiry |
| Custom Nanoparticle Synthesis | Design and synthesize lipid, polymer, metal, and hybrid nanoparticles tailored for cancer research, providing precise structures and functional capabilities | Inquiry |
| Nanoparticle Functionalization | Surface PEGylation or conjugation with targeting ligands for prolonged circulation and active tumor targeting | Inquiry |
| Drug and Gene Delivery Development | Provide chemically modified drug derivatives, siRNA/mRNA encapsulation, and stimulus-responsive delivery strategies to optimize intracellular delivery | Inquiry |
| Nanomaterial Analysis & Characterization | Assess nanoparticle size, morphology, chemical composition, crystalline structure, and drug loading to ensure high-quality research materials | Inquiry |
| Hybrid & Multifunctional Nanoparticle Development | Develop multifunctional platforms combining multiple materials for synergistic therapies and complex experimental designs | Inquiry |
| Stimuli-Responsive Nanoparticle Development | Construct intelligent nanoparticles responsive to ROS, acidic pH, or external triggers (heat, light) for tumor microenvironment-targeted drug release | Inquiry |
Recognizing the challenges of sophisticated cancer-targeted strategies, BOC Sciences focuses on developing hybrid and multifunctional nanoparticles to enable synergistic effects and integrated experimental approaches.
Multifunctional Hybrid Systems: The company designs nanoparticles that combine materials such as lipids, polymers, and inorganic components. For example, lipid-polymer hybrid nanoparticles merge the biocompatibility of liposomes with the mechanical stability and controlled release capabilities of polymeric carriers.
Stimuli-Responsive Nanoparticles: BOC Sciences engineers nanoparticles that respond to specific environmental stimuli, such as ROS, acidic pH, or external triggers like heat or light. This enables the smart release of encapsulated molecules in target environments. For instance, ROS-responsive lipid-based nanoparticles can selectively release cargo in areas with elevated oxidative stress.
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