Release behavior and kinetic evaluation of berberine hydrochloride from ethyl cellulose/chitosan microspheres

Abstract

Novel ethyl cellulose/chitosan microspheres (ECCMs) were prepared by the method of w/o/w emulsion and solvent evaporation. The microspheres were spherical, adhesive, and aggregated loosely with a size not bigger than 5 μm. The drug loading efficiency of berberine hydrochloride (BH) loaded in microspheres were affected by chitosan (CS) concentration, EC concentration and the volume ratio of V(CS)/V(EC). ECCMs prepared had sustained release efficiency on BH which was changed with different preparation parameters. In addition, the pH value of release media had obvious effect on the release character of ECCMs. The release rate of BH from sample B was only a little more than 30% in diluted hydrochloric acid (dHCl) and that was almost 90% in PBS during 24 h. Furthermore, the drug release data were fitted to different kinetic models to analyze the release kinetics and the mechanism from the microspheres. The released results of BH indicated that ECCMs exhibited non-Fickian diffusion mechanism in dHCl and diffusion-controlled drug release based on Fickian diffusion in PBS. So the ECCMs might be an ideal sustained release system especially in dHCl and the drug release was governed by both diffusion of the drug and dissolution of the polymeric network.

Keywords

ethyl cellulose (EC) / chitosan (CS) / microsphere / release in vitro / release kinetics

References

[1] Rinaudo M. Chitin and chitosan: Properties and applications. Progress in Polymer Science, 2006, 31(7): 603–632

[2] Dash M, Chiellini F, Ottenbrite R M, . Chitosan — A versatile semi-synthetic polymer in biomedical applications. Progress in Polymer Science, 2011, 36(8): 981–1014

[3] Mukhopadhyay P, Mishra R, Rana D, . Strategies for effective oral insulin delivery with modified chitosan nanoparticles: A review. Progress in Polymer Science, 2012, 37(11): 1457–1475

[4] Liu W-F, Kang C-Z, Kong M, . Controlled release behaviors of chitosan/α, β-glycerophosphate thermo-sensitive hydrogels. Frontiers of Materials Science, 2012, 6(3): 250–258

[5] Liu Y, Ma L, Gao C. Facile fabrication of the glutaraldehyde cross-linked collagen/chitosan porous scaffold for skin tissue engineering. Materials Science and Engineering C, 2012, 32(8): 2361–2366

[6] Young T-H, Wang I-J, Hu F-R, . Fabrication of a bioengineered corneal endothelial cell sheet using chitosan/polycaprolactone blend membranes. Colloids and Surfaces B: Biointerfaces, 2014, 116: 403–410

[7] Hu H L, Tang C, Yin C H. Folate conjugated trimethyl chitosan/graphene oxide nanocomplexes as potential carriers for drug and gene delivery. Materials Letters, 2014, 125: 82–85

[8] An J, Ji Z, Wang D, . Preparation and characterization of uniform-sized chitosan/silver microspheres with antibacterial activities. Materials Science and Engineering C, 2014, 36: 33–41

[9] Ofokansi K C, Kenechukwu F C, Isah A B, . Formulation and evaluation of glutaraldehyde-crosslinked chitosan microparticles for the delivery of ibuprofen. Tropical Journal of Pharmaceutical Research, 2013, 12: 19–25

[10] Tan S, Gao B, Tao Y, . Antiobese effects of capsaicin–chitosan microsphere (CCMS) in obese rats induced by high fat diet. Journal of Agricultural and Food Chemistry, 2014, 62(8): 1866–1874

[11] Zhang W F, Zhao X T, Zhao Q S, . Biocompatibility and characteristics of theophylline/carboxymethyl chitosan microspheres for pulmonary drug delivery. Polymer International, 2014, 63(6): 1035–1040

[12] Fodor-Kardos A, Toth J, Gyenis J. Preparation of protein loaded chitosan microparticles by combined precipitation and spherical agglomeration. Powder Technology, 2013, 244: 16–25

[13] Zhu N, Cooper D, Chen X-B, . A study on the in vitro degradation of poly(L-lactide)/chitosan microspheres scaffolds. Frontiers of Materials Science, 2013, 7(1): 76–82

[14] Fernandes M, Gonçalves I C, Nardecchia S, . Modulation of stability and mucoadhesive properties of chitosan microspheres for therapeutic gastric application. International Journal of Pharmaceutics, 2013, 454(1): 116–124

[15] Zhou H-Y, Zhou D-J, Zhang W-F, . Biocompatibility and characteristics of chitosan/cellulose acetate microspheres for drug delivery. Frontiers of Materials Science, 2011, 5(4): 367–378

[16] Calejo M T, Kjøniksen A L, Pinazo A, . Thermoresponsive hydrogels with low toxicity from mixtures of ethyl(hydroxyethyl) cellulose and arginine-based surfactants. International Journal of Pharmaceutics, 2012, 436(1–2): 454–462

[17] Feczkó T, Kovács M, Voncina B. Improvement of fatigue resistance of spirooxazine in ethyl cellulose and poly(methyl methacrylate) nanoparticles using a hindered amine light stabilizer. Journal of Photochemistry and Photobiology A: Chemistry, 2012, 247: 1–7

[18] Larsson M, Hjärtstam J, Berndtsson J, . Effect of ethanol on the water permeability of controlled release films composed of ethyl cellulose and hydroxypropyl cellulose. European Journal of Pharmaceutics and Biopharmaceutics, 2010, 76(3): 428–432

[19] Feng H, Zhang L, Zhu C. Genipin crosslinked ethyl cellulose–chitosan complex microspheres for anti-tuberculosis delivery. Colloids and Surfaces B: Biointerfaces, 2013, 103: 530–537

[20] Mirabedini S M, Dutil I, Farnood R R. Preparation and characterization of ethyl cellulose-based core–shell microcapsules containing plant oils. Colloids and Surfaces A: Physicochemical and Engineering Aspects, 2012, 394: 74–84

[21] Es-haghi H, Mirabedini S M, Imani M, . Preparation and characterization of pre-silane modified ethyl cellulose-based microcapsules containing linseed oil. Colloids and Surfaces A: Physicochemical and Engineering Aspects, 2014, 447: 71–80

[22] Li Y, Cao R, Wu X, . Hypercrosslinked poly(styrene-co-divinylbenzene) resin as a specific polymeric adsorbent for purification of berberine hydrochloride from aqueous solutions. Journal of Colloid and Interface Science, 2013, 400: 78–87

[23] Li H, Li Y, Li Z, . Preparation and adsorption behavior of berberine hydrochloride imprinted polymers by using silica gel as sacrificed support material. Applied Surface Science, 2012, 258(10): 4314–4321

[24] Ashjari M, Khoee S, Mahdavian A R. Controlling the morphology and surface property of magnetic/cisplatin-loaded nanocapsules via W/O/W double emulsion method. Colloids and Surfaces A: Physicochemical and Engineering Aspects, 2012, 408: 87–96

[25] Lee Y S, Johnson P J, Robbins P T, . Production of nanoparticles-in-microparticles by a double emulsion method: a comprehensive study. European Journal of Pharmaceutics and Biopharmaceutics, 2013, 83(2): 168–173

[26] Remuñán-López C, Lorenzo-Lamosa M L, Vila-Jato J L, . Development of new chitosan-cellulose multicore microparticles for controlled drug delivery. European Journal of Pharmaceutics and Biopharmaceutics, 1998, 45(1): 49–56

[27] Gui R, Wang Y, Sun J. Encapsulating magnetic and fluorescent mesoporous silica into thermosensitive chitosan microspheres for cell imaging and controlled drug release in vitro. Colloids and Surfaces B: Biointerfaces, 2014, 113: 1–9

[28] Zhou H Y, Chen X G, Kong M, . Preparation of chitosan-based thermosensitive hydrogels for drug delivery. Journal of Applied Polymer Science, 2009, 112(3): 1509–1515

[29] Malana M A, Zohra R. The release behavior and kinetic evaluation of tramadol HCl from chemically cross linked Ter polymeric hydrogels. DARU Journal of Pharmaceutical Sciences, 2013, 21(1): 10 (10 pages)

[30] Wahab A, Khan G M, Akhlaq M, . Pre-formulation investigation and in vitro evaluation of directly compressed ibuprofen-ethocel oral controlled release matrix tablets: A kinetic approach. African Journal of Pharmacy and Pharmacology, 2011, 5: 2118–2127

[31] Higuchi T. Mechanism of sustained-action medication. theoretical analysis of rate of release of solid drugs dispersed in solid matrices. Journal of Pharmaceutical Sciences, 1963, 52(12): 1145–1149

[32] Siepmann J, Peppas N A. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Advanced Drug Delivery Reviews, 2001, 48(2–3): 139–157

[33] Zhou H-Y, Jiang L-J, Zhang Y-P, . β-Cyclodextrin inclusion complex: preparation, characterization, and its aspirin release in vitro. Frontiers of Materials Science, 2012, 6(3): 259–267

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