Comparison of PLGA Micron and Nano Drug-loaded Particles for Drug Carrier and Delivery
LIN Yanxia1, BAI Rui1, LIU Zhiqiang2, and LIU Huiliang1
1. Department of Cardiology, Third Medical Center of PLA General Hospital,Beijing 100039,China;
2. Institute of Military Cognition and Brain Science, Institute of Military Medicine, Beijing 100850,China
Objective The surface characteristics, drug delivery capacity, chemical drug delivery ability, nucleic acid sustained release ability and cell phagocytosis of poly (lactic acid-glycolic acid) (polylactic acid-glycolic acid copolymer,PLGA) microparticles (micron particle,MP) and nanoparticles (nanoparticle,NP) were evaluated to compare the application of PLGA nanoparticles and micron particles in cell pretreatment and modification.Methods PLGA nanoparticles and microparticles were prepared and characterized respectively. Then, drug loading capacity was compared and drug release characteristics were determined. Finally, the ability of PLGA nanoparticles to bind to cells or enter cells was evaluated by fluorescence intensity at different time points. Results The particle size of the prepared nanoparticles and microparticles were distributed at 200-300 nm and 2-4 μm, respectively. The loading of the two particles was 14.3% and 14.1%, respectively. In the aspect of drug sustained release, the nanoparticles exhibited significant early burst release; the release of microparticles was slow and sustained release could reach about one week; the relatively small nanoparticles were easier to enter or combine with cells, and incubated for 12 hours. That is to say, the micron particles are relatively slow to reach the maximum value, and the maximum value appears after 24 hours of incubation. Conclusions PLGA nanoparticles are more suitable for acute tissue or cell protection, and microparticles are more suitable for chronic persistent protection.
林彦霞,白睿,刘志强,刘惠亮. PLGA微米与纳米载药颗粒用于药物携带与递送的比较研究[J]. 武警医学, 2019, 30(2): 120-123.
LIN Yanxia, BAI Rui, LIU Zhiqiang, and LIU Huiliang. Comparison of PLGA Micron and Nano Drug-loaded Particles for Drug Carrier and Delivery. Med. J. Chin. Peop. Armed Poli. Forc., 2019, 30(2): 120-123.
Makadia H K, Siegel S J. Poly Lactic-co-glycolic acid (PLGA) as biodegradable controlled drug delivery carrier[J]. Polymers, 2011, 3(3): 1377-1397
[3]
Scott R C , Rosano J M , Ivanov Z , et al. Targeting VEGF-encapsulated immunoliposomes to MI heart improves vascularity and cardiac function[J]. Faseb J, 2009, 23(10):3361-3367.
[4]
Zhang J , Ding L , Zhao Y , et al. Collagen-targeting vascular endothelial growth factor improves cardiac performance after myocardial infarction[J]. Circulation, 2009, 119(13):1776-1784.
[5]
Yu T X, Shuangtao M, Gary T, et al. Uncoupling protein 2 in cardiovascular health and disease[J]. Front Physiol, 2018, 9:1060.
[6]
Mahboob T, Nawaz M, Tan T C, et al. Preparation of poly (dl-Lactide-co-Glycolide) nanoparticles encapsulated with periglaucine a and betulinic acid for in vitro anti-acanthamoeba and cytotoxicity activities[J]. Pathog,2018, 7(3):62.
[7]
Wright L, Rao S, Thomas N, et al. Ramizol encapsulation into extended release PLGA micro- and nanoparticle systems for subcutaneous and intramuscular administration: in vitro and in vivo evaluation[J]. Drug Dev Ind Pharm,2018,44(9):1-19.
[8]
Li P, Asokanathan C, Liu F, et al. PLGA nano/micro particles encapsulated with pertussis toxoid (PTd) enhances Th1/Th17 immune response in a murine model[J]. Int J Pharm, 2016, 513(1-2):183-190.
[9]
Rawat A, Bhardwaj U, Burgess D J. Comparison of in vitro - in vivo, release of Risperdal, Consta, microspheres[J]. Int J Pharm, 2012, 434(1-2):115-121.
[10]
Zhang Z, Wang X, Li B, et al. Development of a novel morphological paclitaxel-loaded PLGA microspheres for effective cancer therapy: in vitro and in vivo evaluations[J]. Drug Deliv, 2018, 25(1):166.
[11]
Lunardi C N, Gomes A J, Palepu S, et al. PLGA nano/microparticles loaded with cresyl violet as a tracer for drug delivery: characterization and in-situ hyperspectral fluorescence and 2-photon localization[J].Mat Sci Eng C-Mater, 2017, 70(Pt 1):505-511.
[12]
Beringhs A O, Santos F A, Machado C A, et al. Association of PLGA microspheres to carrier pellets by fluid bed coating: a novel approach towards improving the flowability of microparticles[J]. J Pharmaceut, 2018, 2018:1-12.
[13]
Ho Y T, Poinard B, Kah J C. Nanoparticle drug delivery systems and their use in cardiac tissue therapy[J].Nanomedicine, 2016, 11(6):693-714.
[14]
Cohen-Sela E, Teitlboim S, Chorny M, et al. Single and double emulsion manufacturing techniques of an amphiphilic drug in PLGA nanoparticles: formulations of mithramycin and bioactivity[J]. J Pharm Sci, 2009, 98(4):1452-1462.
[15]
韩淑贤. 鱼精蛋白包覆的乙肝疫苗PLGA纳米粒载体的制备研究[D]. 华中科技大学, 2015.
[16]
Liu Z, Li X, Xiu B, et al. A novel and simple preparative method for uniform-sized PLGA microspheres: preliminary application in antitubercular drug delivery[J]. Colloid Surface B, 2016, 145:679-687.
[17]
Zhang Liangming, Zhang Jinling, Ling Y, et al. Sustained release of melatonin from poly (lactic-co-glycolic acid) (PLGA) microspheres to induce osteogenesis of human mesenchymal stem cells in vitro[J]. J Pineal Res, 2012, 54(1):24-32.
[18]
Qi F, Wu J, Fan Q, et al. Preparation of uniform-sized exenatide-loaded PLGA microspheres as long-effective release system with high encapsulation efficiency and bio-stability[J]. Colloid Surface B, 2013, 112(12m):492-498.
[19]
Damla C,Alt ndal , Menems'e G. Melatonin releasing PLGA micro/nanoparticles and their effect on osteosarcoma cells[J].J Microencapsul,2015, 33(1):1.
[20]
Wang H, Zhang G, Ma X, et al. Enhanced encapsulation and bioavailability of breviscapine in PLGA microparticles by nanocrystal and water-soluble polymer template techniques[J]. Eer J Pharm Biopharm,2017, 115:177-185.
[21]
Chen L, Mei L, Feng D, et al. Anhydrous reverse micelle lecithin nanoparticles/PLGA composite microspheres for long-term protein delivery with reduced initial burst[J]. Colloid Surface B, 2017, 163:146.
2019, Vol. 30 
