Polylactic acid-glycolic acid (PLGA) is a copolymer of lactic acid (LA) and glycolic acid (GA). Different monomer ratios can be used to prepare different types of PLGA, such as PLGA75:25, which means that the polymer is composed of 75% LA and 25% GA. By adjusting the ratio of LA to GA, the hydrophilicity of the nanoparticles can be affected. Within a certain range, the higher the LA content, the worse the hydrophilicity of the nanoparticles, and the slower the drug release. In addition, the ratio of LA to GA will also affect the crystallinity of PLGA. LA is crystalline, while GA is more amorphous. A higher content of GA will shift the ratio of crystalline and amorphous in the nanoparticles to amorphous, resulting in faster particle hydrolysis. When LA and GA each account for 50%, PLGA degrades fastest. The particle size and surface potential of PLGA will also affect its encapsulation rate and absorption rate. Studies have shown that in the antibacterial test of Gram-positive and Gram-negative bacteria, the diameter of the antibacterial zone of 45nm nanoparticles is greater than that of 114nm nanoparticles. Similar results have been found in cancer treatment, where ultra-small nanoparticles are more conducive to deep tumor penetration and uniform drug distribution.
Figure 1. Poly(lactic-co-glycolic acid)-based composite bone-substitute materials.( Zhao D, et al. 2020)
PLGA nanoparticles are drug carrier polymers that are widely used in the biomedical industry. Targeted delivery of therapeutic agents is an important research direction of PLGA in the biomedical field, involving medicine, biology, optics and other disciplines. PLGA nanoparticles exhibit a series of favorable properties as drug and vaccine delivery systems, such as good bioavailability and compatibility, biodegradable polymer skeleton, and good safety. PLGA nanoparticles can encapsulate drugs or antigens in nanoparticles, which can not only protect drugs or antigens from enzymatic hydrolysis, but also allow the drugs to be released slowly; they can also be coupled to the surface of the particles to play the role of antigen display.
PLGA nanoparticles are representatives of polymer nanoparticles. Immunotherapy mediated by PLGA nanoparticles is a promising tool with a variety of potential applications. Among them, PLGA has been widely used in the study of nanovaccines as a nanodelivery system, which can enhance the uptake of antigen presenting cells (APCs) and induce humoral and cellular immune responses. Soluble antigens such as recombinant proteins have a relatively short half-life, mainly activate the major histocompatibility complex II (MHC-II) class pathway, and have low immunogenicity. Adjuvants are required to enhance the intensity of antigen-specific immune responses. Studies have shown that soluble antigens encapsulated in PLGA nanoparticles can be effectively taken up by antigen presenting cells because the MHC-I pathway increases effective cross-presentation and CD8+ cytotoxic T cell activation. In addition, researchers can also select PLGA with a corresponding monomer ratio (LA and GA) according to the properties of different drug molecules and the rate of drug release. The biodegradable properties of PLGA have led to its extensive research in the field of drug delivery, mainly including the delivery of anticancer drugs, protein or peptide drugs, bacterial or viral DNA, etc.; it can also achieve targeted drug delivery and improve the effect of cellular drug uptake. It is reported that curcumin can show anticancer activity against a variety of tumors, but the body's absorption capacity of curcumin is limited. Encapsulating it in PLGA nanoparticles is an effective strategy for delivering drugs to tumor sites. In addition, PLGA nanoparticles have a targeting effect and can reach specific cancer cells, thereby enhancing the anti-tumor effect of curcumin. The nanoparticles can successfully integrate the complex network of alternative cancer treatment and traditional treatment development. Flamma Fluor FKR648 is a fluorescent dye that emits in the far-red spectrum, typically at around 648 nm. Interestingly, the dye's far-red emission is particularly useful for minimizing background fluorescence from biological tissues, making it very useful in applications that require high sensitivity and specificity. PLGA-FKR648, formed by linking Flamma Fluor FKR648 and PLGA, has great visualization, which can help drug developers track the location of drugs in the body.
Alternate Names:
PLGA-Flamma Fluor FKR648
Poly(lactic-co-glycolic acid)-Flamma Fluor FKR648
PLG-Flamma Fluor FKR648
Poly(lactide-co-glycolide)-FKR648
Poly(lactic acid-co-glycolic acid)-Flamma Fluor FKR648
PLGA-FKR648 Dye Conjugate
Poly(lactide-co-glycolide) conjugated with Flamma Fluor FKR648
References:
1. Zhao D, et al. Poly(lactic-co-glycolic acid)-based composite bone-substitute materials. Bioact Mater. 2020, 6(2):346-360.
2. Rocha CV, et al. PLGA-Based Composites for Various Biomedical Applications. Int J Mol Sci. 2022 Feb 12;23(4):2034.
PLGA-Based Micro/Nanoparticles: An Overview of Their Applications in Respiratory Diseases
Int J Mol Sci.
Authors: Guo X, Zuo X, Zhou Z, Gu Y, Zheng H, Wang X, Wang G, Xu C, Wang F.
Abstract
Respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), are critical areas of medical research, as millions of people are affected worldwide. In fact, more than 9 million deaths worldwide were associated with respiratory diseases in 2016, equivalent to 15% of global deaths, and the prevalence is increasing every year as the population ages. Due to inadequate treatment options, the treatments for many respiratory diseases are limited to relieving symptoms rather than curing the disease. Therefore, new therapeutic strategies for respiratory diseases are urgently needed. Poly (lactic-co-glycolic acid) micro/nanoparticles (PLGA M/NPs) have good biocompatibility, biodegradability and unique physical and chemical properties, making them one of the most popular and effective drug delivery polymers. In this review, we summarized the synthesis and modification methods of PLGA M/NPs and their applications in the treatment of respiratory diseases (asthma, COPD, cystic fibrosis (CF), etc.) and also discussed the research progress and current research status of PLGA M/NPs in respiratory diseases. It was concluded that PLGA M/NPs are the promising drug delivery vehicles for the treatment of respiratory diseases due to their advantages of low toxicity, high bioavailability, high drug loading capacity, plasticity and modifiability. And at the end, we presented an outlook on future research directions, aiming to provide some new ideas for future research directions and hopefully to promote their widespread application in clinical treatment.
Exploiting PLGA-Based Biocompatible Nanoparticles for Next-Generation Tolerogenic Vaccines against Autoimmune Disease
Int J Mol Sci.
Authors: Cappellano G, Comi C, Chiocchetti A, Dianzani U.
Abstract
Tolerogenic vaccines are aimed at inhibiting antigen-specific immune responses. Antigen-loaded nanoparticles (NPs) have been recently emerged as ideal tools for tolerogenic vaccination because their composition, size, and capability of loading immunomodulatory molecules can be readily exploited to induce peripheral tolerance. Among polymeric NPs, poly(lactic-co-glycolic acid) (PLGA) NPs have the advantage of currently holding approval for several applications in drug delivery, diagnostics, and other clinical uses by the Food and Drug Administration (FDA). PLGA-NPs are non-toxic and display excellent biocompatibility and biodegradability properties. Moreover, surface functionalization may improve their interaction with biological materials, thereby optimizing targeting and performance. PLGA-NPs are the most extensively studied in pre-clinical model in the field of tolerogenic vaccination. Thus, this review describes their potential applications in the treatment of autoimmune diseases.
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