| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PLGA-PEG-NH2 does not target a specific biological receptor; it is a biomaterial excipient rather than a drug molecule. The PLGA block is hydrophobic and degrades via hydrolysis into lactic and glycolic acids, while the PEG block provides hydrophilicity and steric stabilization. The terminal amine (-NH2) group serves as a conjugation handle for attaching targeting moieties (e.g., antibodies, peptides, folate) that can actively target specific cell surface receptors. Thus, PLGA-PEG-NH2 itself has no intrinsic biological activity, but it is a versatile platform for constructing targeted drug delivery systems.
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| ln Vitro |
In vitro, PLGA-PEG-NH2 is not pharmacologically active in cell-based assays when used alone. However, when used to formulate nanoparticles encapsulating a therapeutic agent (e.g., a drug, siRNA, or protein), these nanoparticles are taken up by cells via endocytosis. The amine group can be used to conjugate fluorescent dyes for cellular uptake studies. For example, FITC-labeled PLGA-PEG-NH2 nanoparticles are incubated with cancer cells, and internalization is quantified by flow cytometry or confocal microscopy. The nanoparticles are non-toxic to most cell lines at concentrations used for drug delivery (e.g., 10-200 microg/mL).
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| ln Vivo |
In vivo, PLGA-PEG-NH2 itself is not administered as an active pharmaceutical ingredient. Instead, it is used as a nanoparticle-forming material to encapsulate therapeutic agents for targeted delivery. In animal models (e.g., tumor-bearing mice), PLGA-PEG-NH2 nanoparticles loaded with an anti-cancer drug show improved pharmacokinetics and enhanced tumor accumulation compared to free drug, due to the enhanced permeability and retention (EPR) effect. The PEGylation reduces opsonization and clearance by the reticuloendothelial system (RES). The terminal NH2 group can be conjugated to a targeting ligand to achieve active tumor targeting, further improving efficacy and reducing off-target toxicity.
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| Enzyme Assay |
In vitro enzyme/receptor binding experiments are not applicable to this copolymer, as it is not designed to bind specific enzymes or receptors. However, binding studies can be performed to characterize the conjugation efficiency. For example, to confirm successful conjugation of a ligand to the NH2 group, FTIR (Fourier-transform infrared spectroscopy) or 1H-NMR is used to verify the disappearance of the primary amine peak and the appearance of new functional groups. The amount of free NH2 groups can be quantified by the ninhydrin assay or fluorescamine assay. For adsorption studies, the binding of proteins (e.g., bovine serum albumin, BSA) to PLGA-PEG-NH2 nanoparticles can be assessed by incubating nanoparticles in protein solution at 37degC for 1-2 h, then centrifuging to pellet the particles and measuring unbound protein in the supernatant using a BCA assay.
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| Cell Assay |
A standard protocol for evaluating cellular uptake of PLGA-PEG-NH2 nanoparticles is provided. PLGA-PEG-NH2 nanoparticles are prepared by a double emulsion solvent evaporation or nanoprecipitation method. A fluorescent dye (e.g., Nile red, DiD, or FITC) is encapsulated or conjugated to the NH2 group via a crosslinker (e.g., sulfo-SMCC). Cancer cells (e.g., HeLa, MCF-7, 4T1) are seeded in 96-well plates (1×10⁴ cells/well) in DMEM + 10% FBS and allowed to attach overnight. The medium is replaced with fresh medium containing fluorescently labeled nanoparticles (10-200 microg/mL in terms of polymer concentration). Cells are incubated for 2-24 h at 37degC. After incubation, cells are washed 3 times with PBS, trypsinized, and analyzed by flow cytometry (488 nm excitation, 520 nm emission for FITC). For confocal microscopy, cells are grown on coverslips, treated similarly, fixed with 4% paraformaldehyde, and stained with DAPI for nuclei. Images are acquired with a 60X or 100X objective. Cell viability is assessed using MTT or CellTiter-Glo to ensure the nanoparticles are not cytotoxic at the concentrations used.
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| Animal Protocol |
Female BALB/c nude mice (6-8 weeks, 18-22 g, n=6-8 per group) are implanted subcutaneously with 1-5×10⁶ cancer cells (e.g., 4T1 breast cancer, HeLa cervical cancer) in 100 microL PBS. When tumors reach approximately 100-200 mm3, mice are randomized into treatment groups. PLGA-PEG-NH2 nanoparticles encapsulating an anticancer drug (e.g., paclitaxel, doxorubicin, or a fluorescent probe) are prepared and characterized for size (by DLS) and zeta potential. The nanoparticles are resuspended in sterile PBS or 5% glucose. Mice are administered the nanoparticle formulation via intravenous (tail vein) injection at a dose equivalent to 5-20 mg drug/kg, or 50-200 mg polymer/kg. Control groups receive free drug, empty nanoparticles, or vehicle. Tumor volume is measured every 2 days using a digital caliper: volume = (length × width2)/2. Body weight is monitored as a toxicity indicator. At the end of the study (14-28 days), mice are euthanized, and tumors are excised, weighed, and processed for histology (H&E) and immunohistochemistry (e.g., CD31 for angiogenesis, Ki-67 for proliferation). Major organs (liver, kidney, spleen, heart, lung) are also collected for toxicity assessment. For biodistribution studies, fluorescently labeled nanoparticles are administered, and mice are imaged using an in vivo imaging system (IVIS) at various time points (0, 1, 4, 12, 24, 48 h). Alternatively, organs are homogenized and the concentration of the encapsulated drug is measured by HPLC or LC-MS.
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| ADME/Pharmacokinetics |
PLGA-PEG-NH2 is a polymer with molecular weights ranging from 2 kDa to 20 kDa for the PLGA block and 1-5 kDa for the PEG block. The pharmacokinetics of PLGA-PEG-NH2 itself are not typically characterized; instead, the pharmacokinetics of the encapsulated drug are measured. However, the PEGylation (PEG chain) significantly prolongs the circulation half-life of PLGA nanoparticles compared to non-PEGylated PLGA nanoparticles, reducing macrophage uptake in the liver and spleen. The elimination half-life of PEGylated PLGA nanoparticles in rodents is typically 4-12 hours. The polymer is biodegradable; the PLGA block undergoes hydrolysis to lactic and glycolic acid, which enter the tricarboxylic acid cycle and are eliminated as CO2 and water. The PEG block is excreted renally if the molecular weight is below the renal filtration threshold (ca. 30-50 kDa). The NH2 terminus can be used to attach targeting moieties (e.g., antibody fragments, peptides) to achieve active targeting and further improve pharmacokinetic properties.
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| Toxicity/Toxicokinetics |
PLGA-PEG-NH2 is generally regarded as a biocompatible and biodegradable polymer. The US FDA has approved PLGA and PEG for use in various drug delivery systems and medical devices. Acute toxicity studies in rodents (single IV injection up to 1000 mg/kg) show no significant adverse effects. Sub-chronic (28-day repeat dose) studies at doses up to 200 mg/kg/day show minimal histopathological changes in the liver, spleen, or kidneys. The polymer is non-hemolytic and does not activate the complement system to a significant degree. The amine group can cause mild irritation if injected at high concentrations into sensitive tissues, but this is not observed at standard doses used for drug delivery. Genotoxicity and reproductive toxicity studies have not been performed on this specific copolymer; but based on the safety profile of PLGA and PEG individually, the copolymer is expected to have low toxicity.
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| References | |
| Additional Infomation |
PLGA-PEG-NH2 is a research-grade polymer and is not approved for human use as a finished drug product. It is widely used in the field of nanomedicine for the development of nanoparticle-based drug delivery systems, including those for cancer therapy, gene delivery, and vaccine delivery. The PEG block improves circulation time, while the NH2 group enables conjugation of targeting ligands, drugs, or imaging agents via amide bond formation using carbodiimide chemistry (e.g., EDC/NHS coupling). The copolymer is supplied as a white to off-white solid powder with a purity of ≥95%. The LA:GA ratio and molecular weights can be customized; typical molecular weights are PLGA 15-30 kDa and PEG 2-5 kDa. The product is stable for at least 2 years when stored at -20degC, protected from light and moisture.
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| Appearance |
Off-white to light yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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