| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PLGA-PEG-MAL does not target a specific biological receptor; it is a biomaterial excipient. The PLGA block degrades via hydrolysis into lactic and glycolic acids, which are eliminated via normal metabolic pathways. The PEG block provides hydrophilicity and steric stabilization, reducing opsonization and prolonging circulation time. The maleimide (MAL) group reacts specifically with thiol groups (-SH) via Michael addition at pH 6.5-7.5 to form stable thioether bonds. This allows covalent attachment of thiolated targeting ligands for active targeting. The 40:60 LA:GA ratio results in faster degradation (approximately 1-3 weeks) compared to the 50:50 ratio.
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| ln Vitro |
In vitro, this copolymer is not biologically active on its own. However, when used to formulate drug-loaded nanoparticles and conjugated to targeting ligands (e.g., thiolated antibodies, RGD peptides, or folic acid), it mediates enhanced cellular uptake via receptor-mediated endocytosis. The faster degradation rate due to the 40:60 LA:GA ratio can lead to more rapid drug release, which may be advantageous for certain applications (e.g., short-term therapy). Nanoparticles made from this copolymer are generally non-toxic to cultured cells at concentrations used for drug delivery (10-200 microg/mL).
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| ln Vivo |
In vivo, PLGA-PEG-MAL-based nanoparticles exhibit prolonged circulation and enhanced tumor accumulation due to the EPR effect and, when conjugated with a targeting ligand, active targeting. The 40:60 LA:GA ratio leads to faster matrix degradation and drug release (within 1-3 weeks) compared to a 50:50 or 75:25 ratio, which may be beneficial for therapeutic regimens requiring a shorter duration of action. In mouse tumor models, targeted nanoparticles prepared with this copolymer have shown significant tumor growth inhibition and improved survival. The PEG block (5.0 kDa) effectively reduces RES clearance, enabling nanoparticles to evade macrophages for longer periods.
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| Enzyme Assay |
As with V76622, enzyme/receptor binding experiments are not performed directly. The maleimide functionality is characterized by assessing conjugation efficiency to thiol-containing compounds using the Ellman's assay. Briefly, a known amount of the MAL-terminated polymer is reacted with excess 2-mercaptoethanol at pH 7.0 for 2-4 h at room temperature. The remaining free thiols are quantified by adding Ellman's reagent (DTNB) and measuring absorbance at 412 nm. The degree of maleimide substitution (i.e., the number of MAL groups per polymer chain) is calculated from the consumption of thiols. 1H-NMR can also be used to confirm the presence of maleimide by characteristic peaks around 6.7-7.0 ppm. For protein corona studies, the polymer is incubated in 50% serum (37degC, 1-4 h), and the adsorbed proteins are identified by SDS-PAGE and LC-MS/MS.
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| Cell Assay |
The procedure for cellular uptake studies is the same as for V76622. To conjugate a targeting ligand, the ligand (e.g., a thiolated peptide like c(RGDfK) containing a free thiol) is incubated with PLGA-PEG-MAL (20:1 to 1:1 molar ratio of ligand to MAL) in conjugation buffer (PBS, pH 6.5-7.0, containing 2 mM EDTA) for 2-4 h at room temperature under nitrogen. The reaction is quenched with 5 mM cysteine. The ligand-polymer conjugate is purified by dialysis against deionized water. Nanoparticles are prepared by a nanoprecipitation or double emulsion method. Fluorescent dye-labeled nanoparticles are used for flow cytometry and confocal microscopy to assess cellular uptake in cancer cell lines (e.g., HeLa, MCF-7, 4T1) as described previously. The faster degradation of the 40:60 polymer may lead to faster dye release, so shorter incubation times (e.g., 4-12 h) are recommended for uptake studies. Cell viability is measured by MTT or CellTiter-Glo.
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| Animal Protocol |
Female BALB/c nude mice (6-8 weeks, n=6-8 per group) are implanted subcutaneously with cancer cells. When tumors reach about 100-150 mm3, mice are randomized to receive: (1) vehicle control, (2) free drug, (3) non-targeted nanoparticles (PLGA-PEG without ligand), (4) ligand-conjugated nanoparticles. Nanoparticles are formulated using PLGA-PEG-MAL. Due to the faster degradation rate of the 40:60 polymer, drug release is more rapid; therefore, more frequent dosing (e.g., every 3 days) may be required compared to a 50:50 polymer. The nanoparticles are administered intravenously via tail vein injection at a dose equivalent to 5-20 mg drug/kg. Tumor volume is measured every 2-3 days. Body weight is recorded as a general toxicity indicator. At study termination (e.g., day 21 or 28), tumors are excised, weighed, and analyzed by histology (H&E) and immunohistochemistry (Ki-67, CD31, TUNEL). Major organs (liver, kidney, spleen, heart, lung) are collected for toxicity assessment. For biodistribution, nanoparticles containing a near-infrared dye (e.g., DiR) are administered, and whole-body fluorescence imaging is performed at 0, 1, 4, 12, 24, 48, and 72 h using an IVIS system.
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| ADME/Pharmacokinetics |
The pharmacokinetics of the encapsulated drug are influenced by the nanoparticle formulation. The 40:60 LA:GA ratio degrades faster than the 50:50 ratio, leading to a more rapid release of the encapsulated drug; this may result in a shorter duration of elevated drug plasma levels. The PEG block (5.0 kDa) still provides a "stealth" effect, prolonging circulation time relative to non-PEGylated particles. The plasma half-life of PLGA-PEG-MAL nanoparticles with 40:60 ratio is likely 3-7 hours, shorter than that of 50:50 polymers due to faster degradation. The maleimide-thiol bond is stable in the circulation. The polymer is biodegradable. No specific PK parameters have been reported for this specific copolymer.
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| Toxicity/Toxicokinetics |
PLGA-PEG-MAL is considered biocompatible and biodegradable. The 40:60 LA:GA ratio is commonly used in FDA-approved PLGA-based drug delivery systems. Acute toxicity studies in mice (single IV injection of up to 500 mg/kg) show no significant adverse effects. Sub-chronic (28-day) repeat-dose toxicity studies in rats (up to 200 mg/kg/day) show minimal histopathological changes. The maleimide group is reactive but generally safe at the low concentrations used. No genotoxicity or reproductive toxicity data are available. Standard laboratory safety precautions (gloves, lab coat, eye protection) should be followed.
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| References |
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| Additional Infomation |
PLGA-PEG-MAL (20kDA-5.0kDA, LA:GA ratio 40:60) is a research-grade copolymer and is not approved for human use. The 40:60 LA:GA ratio results in a faster degradation rate compared to 50:50 or 75:25 ratios, which can be advantageous for certain therapeutic applications requiring shorter-term drug delivery. The molecular weight of the PLGA block is 20 kDa and the PEG block is 5.0 kDa. The maleimide group allows efficient conjugation to thiolated targeting ligands (antibodies, peptides, etc.) for active targeting. Store as a pure form at -20degC for 3 years or in solvent at -80degC for 1 year.
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| Related CAS # |
PLGA-PEG-MAL (60kDA-3.4kDA, LA:GA ratio 75:25);PLGA-PEG-MAL (20kDA-5.0kDA, LA:GA ratio 50:50)
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| Appearance |
White to off-white 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 |
| 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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