Fabrication and properties of poly（lactic acid））/ibuprofen microspheres through electrostatic spray method

doi:10.19491/j.issn.1001-9278.2022.07.009

Abstract

Abstract:

The ibuprofen （IBU）?loaded poly（lactic acid）（PLA） microspheres were prepared through electrostatic spray using PLA as a skeleton carrier material and IBU as a model drug， and their morphology， microstructure， and properties were investigated using scanning electron microscope， X ray diffractometer， differential scanning calorimeter， infrared spectrophotometer， thermogravimetric analyzer， and UV?Vis spectrophotometer. The obtained PLA/IBU microspheres showed a porous and amorphous structure with good dispersibility. IBU was loaded in PLA in a molecular or random state and without any changes in chemical structure. Their stability was higher than that of pure IBU. Based on the in vitro controlled release test， The PLA/IBU microspheres exhibited a better effect for controlled release than pure IBU. The release rate and cumulative release amount of IBU from the microspheres increased with an increase in the dosage of IBU. The cumulative release amount of IBU reached 52 % at 48 h when the IBU content was 16 wt%. With the bioavailability and dissolution rate of IBU， the PLA/IBU microspheres developed by this work exhibit great application potential in the biomedicine field.

Key words: electrostatic spray, poly（lactic acid）, ibuprofen, amorphousness, release property

CLC Number:

TQ321

SHEN Xuemei, ZHU Xiaolong, HU Yanchao, SONG Renyuan, ZHANG Xianfeng, LI Xi. Fabrication and properties of poly（lactic acid））/ibuprofen microspheres through electrostatic spray method[J]. China Plastics, 2022, 36(7): 61-67.

Figures/Tables 6

Fig.1. SEM images and particle size frequency distribution histograms of PLA/IBU microspheres with different dosages

Fig.2. XRD spectrum of PLA/IBU microspheres with different dosages

Fig.3. DSC curves of PLA/IBU microspheres with different dosages

Fig.4. FTIR spectrum of PLA/IBU microspheres with different dosages

Fig.5. TG curves of PLA/IBU microspheres with different dosages

Fig.6. Sustained release curves of PLA/IBU microspheres with different dosages

References 23

1	国家药典委员会. 中华人民共和国药典［ M ］. 二部. 北京：化学工业出版社， 2020：附录211⁃213.
2	BEGUM N， SAILAJA K A. Effect of formulation variables on the preparation of ibuprofen loaded polymeric nanoparticles［J］. Pharmaceutical Nanotechnology， 2015， 3（2）： 111⁃121.
3	OKUNLOLA A， GHOMORAI T. Development of ibuprofen microspheres using acetylated plantain starches as polymer for sustained release［J］. Journal of Pharmaceutical Investigation， 2018， 48（5）： 551⁃564.
4	DAS S K， YUVARAJA K， KHANAM J， et al. Formulation development and statistical optimization of ibuprofen⁃loaded polymethacrylate microspheres using response surface methodology［J］. Chemical Engineering Research and Design， 2015， 96： 1⁃14.
5	黎雁. 基于可生物降解聚合物的微米/纳米结构药物控释体系：制备，表征及体内外评价研究［D］.杭州：浙江大学， 2005.
6	陈歌，曹立冬，许春丽，等. 溶剂蒸发法制备丙硫菌唑微囊及其性能研究［J］. 中国农业科学， 2021， 54（4）： 754⁃767.
	CHEN G， CAO L D， XU C L， et al. Performance study of prothioconazole microcapsules prepared by solvent evaporation method［J］. Scientia Agricultura Sinica， 2021， 54（4）： 754⁃767.
7	WANG S S， YANG X， LU W X， et al. Spray drying encapsulation of CD⁃MOF nanocrystals into Eudragit^® RS microspheres for sustained drug delivery［J］. Journal of Drug Delivery Science and Technology， 2021， 64： 102593.
8	WANG J F， ZHANG Y T， ZHANG W， et al. Research progress of electrostatic spray technology over the last two decades［J］. Journal of Energy Engineering， 2021， 147（4）： 03121003.
9	HADIS R， REZA F S， MAHDI R M， et al. Electrospraying as a novel process for the synthesis of particles/nanoparticles loaded with poorly water⁃soluble bioactive molecules［J］. Advances in Colloid and Interface Science， 2021， 290： 102384.
10	NIU B， SHAO P， LUO Y C， et al. Recent advances of electrosprayed particles as encapsulation systems of bioactives for food application［J］. Food Hydrocolloids， 2020， 99： 105376.
11	NGUYEN D N， CLASEN C， MOOTER G V. Pharmaceutical applications of electrospraying［J］. Journal of Pharmaceutical Sciences， 2016， 105（9）： 2 601⁃2 620.
12	NGUYEN T T， JEONG J H. Development of a single⁃jet electrospray method for producing quercetin⁃loaded poly （lactic⁃co⁃glycolic acid） microspheres with prolonged⁃release patterns［J］. Journal of Drug Delivery Science and Technology， 2018， 47： 268⁃274.
13	HSU M Y， HUANG Y T， WENG C J， et al. Preparation and in vitro/in vivo evaluation of doxorubicin⁃loaded poly［lactic⁃co⁃glycol acid］ microspheres using electrospray method for sustained drug delivery and potential intratumoral injection［J］. Colloids and Surfaces B： Biointerfaces， 2020， 190： 110937.
14	韦宗辰，郗悦玮，翁云宣. 聚乳酸基复合骨组织修复材料的研究现状及进展［J］. 中国塑料， 2021， 35（9）： 136⁃146.
	WEI Z C， XI Y W， WENG Y X. Research progress in poly（lactic acid）⁃based composite materials for bone tissue engineering［J］. China Plastics， 2021， 35（9）： 136⁃146.
15	NARAYANAN G， VERNEKAR V N， KUYINU E L， et al. Poly （lactic acid）⁃based biomaterials for orthopaedic regenerative engineering［J］. Advanced Drug Delivery Reviews， 2016， 107： 247⁃276.
16	周圆圆，薛立伟，毛吉富，等. 静电喷雾法制备聚膦腈微球［J］. 高分子学报， 2010（1）： 125⁃130.
	ZHOU Y Y， XUE L W， MAO J F， et al. Preparation of polyphosphazene microparticles via electrospray［J］. Acta Polymerica Sinica， 2010（1）： 125⁃130.
17	洪雅真，朱利会. 载阿霉素聚乳酸多孔微球的表征及释药性能［J］. 化工进展， 2018， 37（3）： 1 130⁃1 136.
	HONG Y Z， ZHU L H. Synthesis，characterization and in vitro drug release performance of poly⁃L⁃lactide porous microspheres［J］. Chemical Industry and Engineering Pro⁃gress， 2018， 37（3）： 1 130⁃1 136.
18	SUN C K， ZOU L M， XU Y J， et al. Ibuprofen‐loaded poly（lactic acid） electrospun mats： the morphology， physicochemical performance， and in vitro drug release behavior［J］. Macromolecular Materials and Engineering， 2020， 305（12）： 2000457.
19	ANA Ć， ĐORĐE M， BOJAN Č， et al. Effect of ibuprofen entrapment procedure on physicochemical and controlled drug release performances of chitosan/xanthan gum polyelectrolyte complexes［J］. International Journal of Biological Macromolecules， 2021， 167： 547⁃558.
20	陆丽婷，唐珊珊，陈光，等. 电纺制备布洛芬纳米纤维状固体分散体［J］. 功能材料， 2015， 46（17）： 17 149⁃17 152.
	LU L T， TANG S S， CHEN G， et al. Preparation of ibuprofen nanofibers solid dispersion by electrospinning［J］. Journal of Functional Materials， 2015， 46（17）： 17 149⁃17 152.
21	LI D X， OH Y K， LIM S J， et al. Novel gelatin microcapsule with bioavailability enhancement of ibuprofen using spray⁃drying technique［J］. International Journal of Pharmaceutics， 2007， 355（1）： 277⁃284.
22	WANG X H， SU T， ZHAO J， et al. Fabrication of polysaccharides⁃based hydrogel films for transdermal sustained delivery of ibuprofen［J］. Cellulose， 2020， 27： 1⁃16.
23	李贝，乔永生，沈腊珍，等. 介孔SiO₂/PPy复合微球对布洛芬的负载与释放研究［J］. 中北大学学报（自然科学版）， 2018， 39（3）： 322⁃327.
	LI B， QIAO Y S， SHEN L Z， et al. Mesoporous SiO₂/PPy composite microspheres for the loading and release of ibuprofen［J］. Journal of North University of China（Natural Science Edition）， 2018， 39（3）： 322⁃327.

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