Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo Studies

被引:6
作者
Chen, Jian-Ming [1 ,2 ]
Liu, Kuan-Chieh [2 ]
Yeh, Wen-Ling [1 ]
Chen, Jin-Chung [3 ]
Liu, Shih-Jung [1 ,2 ]
机构
[1] Chang Gung Mem Hosp Linkou, Dept Orthoped Surg, Taoyuan 33305, Taiwan
[2] Chang Gung Univ, Dept Mech Engn, Taoyuan 33302, Taiwan
[3] Chang Gung Univ, Grad Inst Biomed Sci, Taoyuan 33302, Taiwan
关键词
sustained drug release; poly(D; L-lactide-co-glycolide); electrospraying; acemetacin; levobupivacaine; lidocaine; HIP FRACTURE; NONOPERATIVE TREATMENT; PAIN MANAGEMENT; DELIVERY; RELIEF; BLOCK; SCAPULA; REDUCE; PLGA;
D O I
10.3390/ijms21031093
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In this study, we explored the release characteristics of analgesics, namely levobupivacaine, lidocaine, and acemetacin, from electrosprayed poly(D,L-lactide-co-glycolide) (PLGA) microparticles. The drug-loaded particles were prepared using electrospraying techniques and evaluated for their morphology, drug release kinetics, and pain relief activity. The morphology of the produced microparticles elucidated by scanning electron microscopy revealed that the optimal parameters for electrospraying were 9 kV, 1 mL/h, and 10 cm for voltage, flow rate, and travel distance, respectively. Fourier-transform infrared spectrometry indicated that the analgesics had been successfully incorporated into the PLGA microparticles. The analgesic-loaded microparticles possessed low toxicity against human fibroblasts and were able to sustainably elute levobupivacaine, lidocaine, and acemetacin in vitro. Furthermore, electrosprayed microparticles were found to release high levels of lidocaine and acemetacin (well over the minimum therapeutic concentrations) and levobupivacaine at the fracture site of rats for more than 28 days and 12 days, respectively. Analgesic-loaded microparticles demonstrated their effectiveness and sustained performance for pain relief in fracture injuries.
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页数:14
相关论文
共 47 条
[1]   Fracture pain-Traveling unknown pathways [J].
Alves, Cecilia J. ;
Neto, Etrela ;
Sousa, Daniela M. ;
Leitao, Luis ;
Vasconcelos, Daniel M. ;
Ribeiro-Silva, Manuel ;
Alencastre, Ines S. ;
Lamghari, Meriem .
BONE, 2016, 85 :107-114
[2]   Delivery of local anaesthetic via a sternal catheter to reduce the pain caused by sternal fractures: first case series using the new technique [J].
Appelboam, A. ;
McLauchlan, C. A. J. ;
Murdoch, J. ;
MacIntyre, P. A. .
EMERGENCY MEDICINE JOURNAL, 2006, 23 (10) :791-793
[3]   Electrospraying, a Reproducible Method for Production of Polymeric Microspheres for Biomedical Applications [J].
Bock, Nathalie ;
Woodruff, Maria A. ;
Hutmacher, Dietmar W. ;
Dargaville, Tim R. .
POLYMERS, 2011, 3 (01) :131-149
[4]  
Botros JM, 2017, AIN SHAMS J ANAESTHE, V10, P224
[5]   A Lidocaine-Containing Formulation of Large-Gel Particle Hyaluronic Acid Alleviates Pain [J].
Brandt, Fredric ;
Bank, David ;
Cross, Sharon L. ;
Weiss, Robert .
DERMATOLOGIC SURGERY, 2010, 36 (03) :1876-1885
[6]   INTRAVENOUS LIPID EMULSION IN THE EMERGENCY DEPARTMENT: A SYSTEMATIC REVIEW OF RECENT LITERATURE [J].
Cao, Dazhe ;
Heard, Kennon ;
Foran, Mark ;
Koyfman, Alex .
JOURNAL OF EMERGENCY MEDICINE, 2015, 48 (03) :387-397
[7]   Lidocaine Skin Patch (Lidopat® 5%) Is Effective in the Treatment of Traumatic Rib Fractures: A Prospective Double-Blinded and Vehicle-Controlled Study [J].
Cheng, Yu-Jen .
MEDICAL PRINCIPLES AND PRACTICE, 2016, 25 (01) :36-39
[8]   Scapula fractures [J].
Cole P.A. ;
Freeman G. ;
Dubin J.R. .
Current Reviews in Musculoskeletal Medicine, 2013, 6 (1) :79-87
[9]   Electrosprayed poly(vinylidene fluoride) microparticles for tissue engineering applications [J].
Correia, D. M. ;
Goncalves, R. ;
Ribeiro, C. ;
Sencadas, V. ;
Botelho, G. ;
Gomez Ribelles, J. L. ;
Lanceros-Mendez, S. .
RSC ADVANCES, 2014, 4 (62) :33013-33021
[10]   Trends in Operative and Nonoperative Hip Fracture Management 1990-2014: A Longitudinal Analysis of Manitoba Administrative Data [J].
Cram, Peter ;
Yan, Lin ;
Bohm, Eric ;
Kuzyk, Paul ;
Lix, Lisa M. ;
Morin, Suzanne N. ;
Majumdar, Sumit R. ;
Leslie, William D. .
JOURNAL OF THE AMERICAN GERIATRICS SOCIETY, 2017, 65 (01) :27-34