PLGA(75:25)(poly(lactic-co-glycolic acid))
(Synonyms: 聚乳酸-羟基乙酸共聚物; poly(lactic-co-glycolic acid) 目录号 : GC30049
PLGA(75:25)(poly(lactic-co-glycolic acid))是一种低毒、生物相容、可生物降解的可控给药载体，可在生物体内实现缓释。
Cas No.:34346-01-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
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Protocol 1 (Synthesis of PLGA@ Icaritin )[1]： |
| 1.PLGA-PEG copolymers (PEG2000) were prepared by melt polymerization under vacuum using stannous octoate [stannous 2-ethylhexanoate] as a catalyst. PLGA and PEG2000 (0.77 g) (45%/w) were heated to 140℃ in a bottleneck flask under a nitrogen atmosphere for complete melting. (The molar ratio of DL-lactide to glycolide was 3:1 in PLGA) 2.Stannous octoate [0.05% (w/w)] was added, and the temperature of the reaction mixture was increased to 180℃. This temperature was maintained for 4 h. Polymerization was performed under vacuum. 3.The copolymer was recovered by dissolution in methylene chloride, followed by precipitation in ice-cold diethyl ether. After 24 h, PLGA-PEG was purified by washing with ethanol and drying under vacuum. 4.Icaritin (0.5 mg) was dissolved in 500 μL dimethyl sulfoxide and mixed with 5 mg of PLGA-PEG in the drug solution. 5.The drug-polymer mixture was added dropwise to 10 mL of deionized water while stirring and stirred for 24 h at room temperature in a beaker. 6.PLGA@Icaritin was obtained, dialyzed to remove the organic solvent, and freeze-dried.
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References: [1]. Xiao Y, Yao W, et,al. Icaritin-loaded PLGA nanoparticles activate immunogenic cell death and facilitate tumor recruitment in mice with gastric cancer. Drug Deliv. 2022 Dec;29(1):1712-1725. doi: 10.1080/10717544.2022.2079769. PMID: 35635307; PMCID: PMC9176696. |
PLGA(poly (lactic-co-glycolic acid)) is made by random polymerization of two monomers: lactic acid and glycolic acid. It is a degradable functional polymer organic compound with good biocompatibility, non-toxic, and good cystforming and film forming properties. It is widely used in pharmaceutical, medical engineering materials and modern industrial fields[1,2].
PLGA@Icaritin nanoparticles (NPs) dramatically suppressed cell growth, induced Lactic dehydrogenase (LDH) leakage, arrested more GC cells at G2 phase, and inhibited the invasion and metastasis of GC cells, compared to free icaritin. In addition, PLGA@Icaritin could help generate dozens of reactive oxygen species (ROS) within GC cells, following by significant mitochondrial membrane potentials (MMPs) loss and excessive production of oxidative-mitochondrial DNA (Ox-mitoDNA)[3].
PLGA. 聚乳酸-羟基乙酸共聚物 (poly (lactic-co-glycolic acid),PLGA)由两种单体——乳酸和羟基乙酸随机聚合而成,是一种可降解的功能高分子有机化合物,具有良好的生物相容性、无毒、良好的成囊和成膜的性能,被广泛应用于制药、医用工程材料和现代化工业领域[1,2]
PLGA@Icaritin NPs与游离Icaritin相比,可以显著抑制细胞生长,诱导乳酸脱氢酶(LDH)渗漏,在G2期阻滞更多的GC细胞,抑制GC细胞的侵袭和转移。此外,PLGA@Icaritin可以帮助在GC细胞内产生数十种活性氧(ROS),造成显著的线粒体膜电位(MMPs)损失和氧化线粒体DNA (Ox-mitoDNA)的过度产生[3]。
References:
[1]. Gentile P, Chiono V, et,al. An overview of poly(lactic-co-glycolic) acid (PLGA)-based biomaterials for bone tissue engineering. Int J Mol Sci. 2014 Feb 28;15(3):3640-59. doi: 10.3390/ijms15033640. PMID: 24590126; PMCID: PMC3975359.
[2]. Sadat Tabatabaei Mirakabad F, Nejati-Koshki K, et,al.PLGA-based nanoparticles as cancer drug delivery systems. Asian Pac J Cancer Prev. 2014;15(2):517-35. doi: 10.7314/apjcp.2014.15.2.517. PMID: 24568455.
[3]. Xiao Y, Yao W, et,al.Icaritin-loaded PLGA nanoparticles activate immunogenic cell death and facilitate tumor recruitment in mice with gastric cancer. Drug Deliv. 2022 Dec;29(1):1712-1725. doi: 10.1080/10717544.2022.2079769. PMID: 35635307; PMCID: PMC9176696.
| Cas No. | 34346-01-5 | SDF | |
| 别名 | 聚乳酸-羟基乙酸共聚物; poly(lactic-co-glycolic acid | ||
| Canonical SMILES | O=C(O)C(C)OC(CO[H])=O.[x].[y] | ||
| 分子式 | (C5H8O5)n | 分子量 | 10000-20000 |
| 溶解度 | DMSO : 100 mg/mL ;chloroform : 16.67 mg/mL ;Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.1 mL | 0.5 mL | 1 mL |
| 5 mM | 0.02 mL | 0.1 mL | 0.2 mL |
| 10 mM | 0.01 mL | 0.05 mL | 0.1 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
PLGA-based biodegradable microspheres in drug delivery: recent advances in research and application
Biodegradable microspheres have been widely used in the field of medicine due to their ability to deliver drug molecules of various properties through multiple pathways and their advantages of low dose and low side effects. Poly (lactic-co-glycolic acid) copolymer (PLGA) is one of the most widely used biodegradable material currently and has good biocompatibility. In application, PLGA with a specific monomer ratio (lactic acid and glycolic acid) can be selected according to the properties of drug molecules and the requirements of the drug release rate. PLGA-based biodegradable microspheres have been studied in the field of drug delivery, including the delivery of various anticancer drugs, protein or peptide drugs, bacterial or viral DNA, etc. This review describes the basic knowledge and current situation of PLGA biodegradable microspheres and discusses the selection of PLGA polymer materials. Then, the preparation methods of PLGA microspheres are introduced, including emulsification, microfluidic technology, electrospray, and spray drying. Finally, this review summarizes the application of PLGA microspheres in drug delivery and the treatment of pulmonary and ocular-related diseases.
Poly-(lactic- co-glycolic) Acid Nanoparticles Entrapping Pterostilbene for Targeting Aspergillus Section Nigri
Poly-(lactic-co-glycolic) acid (PLGA) is a biodegradable, biosafe, and biocompatible copolymer. The Aspergillus section Nigri causes otomycosis localized in the external auditory canal. In this research, Aspergillus brasiliensis, a species belonging to the Nigri section, was tested. Coumarin 6 and pterostilbene loaded in poly-(lactic-co-glycolic) acid nanoparticles (PLGA-coumarin6-NPs and PLGA-PTB-NPs) were tested for fungal cell uptake and antifungal ability against A. brasiliensis biofilm, respectively. Moreover, the activity of PLGA-PTB-NPs in inhibiting the A. brasiliensis infection was tested using Galleria mellonella larvae. The results showed a fluorescence signal, after 50 nm PLGA-coumarin6-NPs treatment, inside A. brasiliensis hyphae and along the entire thickness of the biofilm matrix, which was indicative of an efficient NP uptake. Regarding antifungal activity, a reduction in A. brasiliensis biofilm formation and mature biofilm with PLGA-PTB-NPs has been demonstrated. Moreover, in vivo experiments showed a significant reduction in mortality of infected larvae after injection of PLGA-PTB-NPs compared to free PTB at the same concentration. In conclusion, the PLGA-NPs system can increase the bioavailability of PTB in Aspergillus section Nigri biofilm by overcoming the biofilm matrix barrier and delivering PTB to fungal cells.
Poly(lactic-co-glycolic acid) microsphere production based on quality by design: a review
Poly(lactic-co-glycolic acid) (PLGA) has garnered increasing attention as a candidate drug delivery polymer owing to its favorable properties, including its excellent biocompatibility, biodegradability, non-toxicity, non-immunogenicity, and mechanical strength. PLAG are specifically used as microspheres for the sustained/controlled and targeted delivery of hydrophilic or hydrophobic drugs, as well as biological therapeutic macromolecules, including peptide and protein drugs. PLGAs with different molecular weights, lactic acid (LA)/glycolic acid (GA) ratios, and end groups exhibit unique release characteristics, which is beneficial for obtaining diverse therapeutic effects. This review aims to analyze the composition of PLGA microspheres, and understand the manufacturing process involved in their production, from a quality by design perspective. Additionally, the key factors affecting PLGA microsphere development are explored as well as the principles involved in the synthesis and degradation of PLGA and its interaction with active drugs. Further, the effects elicited by microcosmic conditions on PLGA macroscopic properties, are analyzed. These conditions include variations in the organic phase (organic solvent, PLGA, and drug concentration), continuous phase (emulsifying ability), emulsifying stage (organic phase and continuous phase interaction, homogenization parameters), and solidification process (relationship between solvent volatilization rate and curing conditions). The challenges in achieving consistency between batches during manufacturing are addressed, and continuous production is discussed as a potential solution. Finally, potential critical quality attributes are introduced, which may facilitate the optimization of process parameters.
FDA's Poly (Lactic-Co-Glycolic Acid) Research Program and Regulatory Outcomes
Poly (lactic-co-glycolic acid) (PLGA) has been used in many long-acting drug formulations which have been approved by the US Food and Drug Administration (FDA). However, generic counterparts for PLGA products have yet to gain FDA approval due to many complexities in formulation, characterization, and evaluation of test products. To address the challenges of generic development of PLGA-based products, the FDA has established an extensive research program to investigate novel methods and tools to aid both product development and regulatory review. The research focus have been: (1) analytical tools for characterization of PLGA polymers; (2) impacts of PLGA characteristics and manufacturing conditions on product performance; (3) in vitro drug release testing and in vitro-in vivo correlation of PLGA-based products, and (4) modeling tools to facilitate formulation design and bioequivalence study design of PLGA-based drugs. This article provides an overview of FDA's PLGA research program and highlights scientific accomplishments as well as regulatory outcomes that have resulted from successful research investigations.
Customizing poly(lactic-co-glycolic acid) particles for biomedical applications
Nano- and microparticles have increasingly widespread applications in nanomedicine, ranging from drug delivery to imaging. Poly(lactic-co-glycolic acid) (PLGA) particles are the most widely-applied type of particles due to their biocompatibility and biodegradability. Here, we discuss the preparation of PLGA particles, and various modifications to tailor particles for applications in biological systems. We highlight new preparation approaches, including microfluidics and PRINT method, and modifications of PLGA particles resulting in novel or responsive properties, such as Janus or upconversion particles. Finally, we describe how the preparation methods can- and should-be adapted to tailor the properties of particles for the desired biomedical application. Our aim is to enable researchers who work with PLGA particles to better appreciate the effects of the selected preparation procedure on the final properties of the particles and its biological implications.
Statement of significance: Nanoparticles are increasingly important in the field of biomedicine. Particles made of polymers are in the spotlight, due to their biodegradability, biocompatibility, versatility. In this review, we aim to discuss the range of formulation techniques, manipulations, and applications of poly(lactic-co-glycolic acid) (PLGA) particles, to enable a researcher to effectively select or design the optimal particles for their application. We describe the various techniques of PLGA particle synthesis and their impact on possible applications. We focus on recent developments in the field of PLGA particles, and new synthesis techniques that have emerged over the past years. Overall, we show how the chemistry of PLGA particles can be adapted to solve pressing biological needs.