Preparation and evaluation of electrospun nanofibers containing pectin and time-dependent polymers aimed for colonic drug delivery of celecoxib

Document Type: Research Paper

Authors

1 Nanotechnology Research Center , School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran

2 Targeted Drug Delivery Research Center, School of Pharmauy, Mashhad University of Medical Sciences, Mashhad, Iran

10.7508/nmj.2016.01.005

Abstract

Objective(s):The aim of this study was to prepare electrospun nanofibers of celecoxib using combination of time-dependent polymers with pectin to achieve a colon-specific drug delivery system for celecoxib.
Materials and Methods:Formulations were produced based on two multilevel 22 full factorial designs. The independent variables were the ratio of drug:time-dependent polymer (X1) and the amount of pec‌tin in formulations (X2). Electrospinning process was used for preparation of nanofibers. The spinning solutions were loaded in 5 mL syringes. The feeding rate was fixed by a syringe pump at 2.0 mL/h and a high voltage supply at range 10-18 kV was applied for electrospinning. Electrospun nanofibers were collected and evaluated by scanning electron microscopy and drug release in the acid and buffer with pH 6.8 with and without pectinase.
Results:Electrospun nanofibers of celecoxib with appropriate morphological properties were produced via electrospinning process. Drug release from electrospun nanofibers was very low in the acidic media; while, drug release in the simulated colonic media was the highest from formulations containing pectin.
Conclusion: Formulation F2 (containing drug:ERS with the ratio of 1:2 and 10% pectin) exhibited acceptable morphological characteristics and protection of drug in the upper GI tract and could be a good candidate as a colonic drug delivery system for celecoxib.  

Keywords


[1]  Luong-Van E, Grondahl L, Chua KN, Leong KW, Nurcombe V, Cool SM. Controlled release of heparin from poly ([-caprolactone) electrospun fibers. Biomaterials. 2006; 27: 2042-2050.

[2]  Liang D, Hsiao BS, Chu B. Functional electrospun nanofibers scaffold for biomedical applications. Adv Drug Deliver Rev. 2007; 59: 1392-1412.

[3] Wu SH, Qin XH. Uniaxially aligned polyacrylonitrile nanofiber yarns prepared by a novel modified electrospinning method. Mater Lett. 2013; 106: 204-207.

[4]  Abdal-Hay A, Tijing LD, Lim JK. Characterization of the surface biocompatibility of an electrospun nylon 6/CaP nanofiber scaffold using osteoblasts. Chem Eng J. 2013; 215-216: 57-64. 

[5]  Unnithan AR, Barakat NAM, Pichiah PBT, Gnanasekaran G, Nirmala R, Cha YS, Hung CH, El-Newehy M, Kim HY. Wound-dressing materials with antibacterial activity from electrospun polyurethane-dextran nanofiber mats containing ciprofloxacin HCl. Carbohyd Polym. 2012; 90(4): 1786-1793.

[6]  Bhardwaj N, Kundu SC. Electrospinning: a fascinating fiber fabrication technique. Biotechnol Adv. 2010; 28(3): 325-347.

[7]  Wang Y, Hsieh YL. Enzyme immobilization to ultra-fine cellulose fibers via amphiphilic polyethylene glycol spacers. J. Polym. Sci. Part A, Polymer Chemistry. 2004; 42: 4289-4299.

[8] Wu L, Yuan X, Sheng J. Immobilization of cellulose in nanofibrous PVA membranes by electrospinning. J Membrane Sci. 2005; 250: 167-173.  

[9]  Yu DG, Yang JM, Branford-White C, Lu P, Zhang L, Zhu LM. Third generation solid dispersions of ferulic acid in electrospun composite nanofibers. Int J Pharm. 2010; 400: 158-164.

[10] Okuda T, Tominaga K, Kidoaki S. Time-programmed dual release formulation by multilayered drug-loaded nanofiber meshes. J Control Release. 2010; 143(2): 258-264.

[11] Yoo HS, Kim TG, Park TG. Surface-functionalized electrospun nanofibers for tissue engineering and drug delivery. Adv Drug Deliver Rev. 2009; 61(12): 1033-1042.

[12] Maretschek S, Greiner A, Kissel T. Electrospun biodegradable nanofiber nonwovens for controlled release of proteins. J Control Release. 2008; 127(2): 180-187.

[13] Maroni A, Del Curto MD, Zema L, Foppoli A, Gazzaniga A. Film coatings for oral colon delivery. Int J Pharm. 2013; 457(2): 372-394.

[14] Ashford M, Fell JT, Attwood D, Sharma H, Woodhead PJ. An in vitro investigation into the suitability of pH dependent polymers for colonic targeting. Int J Pharm. 1993; 95: 193–199.

[15] Shen X, Yu D, Zhu L, Brandford-White C, White K, Chatterton NP. Electrospun diclofenac sodium loaded eudragit L 100-55 nanofibers for colon-targeted drug delivery. Int J Pharm. 2011; 408: 200-207.

[16] Setia S, Nehru B, Sanial SN. Celecoxib prevents colitis associated carcinogenesis: an upregulation of apoptosis. Pharmacol Rep. 2014; 66(6): 1083-1091.

[17] Liu Y, Ma G, Fang D, Xu J, Zhang H, Nie J. Effects of solution properties and electric field on the electrospinning of hyaluronic acid. Carbohyd Polym. 2011; 83(2): 1011-5.

[18] Shukla RK, Tiwari A. Carbohydrate polymers: Applications and recent advances in delivering drugs to the colon. Carbohyd Polym. 2012; 88(2): 399-416.

[19] Akhgari A, Abbaspour M, Moradkhanizadeh M. Combination of pectin and eudragit RS and eudragit RL in the matrix of pellets prepared by extrusion-spheronization for possible colonic delivery of 5-amino salicylic acid. Jundishapur J Nat Pharm Prod. 2013; 8(2): 86-92.

[20] McDonald PF, Lyons JG, Geever LM, Higginbotham CL. In vitro degradation and drug release from polymer blends based on poly(DL-lactide), poly(L-lactideglycolide) and poly(e-caprolactone). J Mater Sci. 2010; 45: 1284-1292.

[21] Chou SF, Carson D, Woodrow KA. Current strategies for sustaining drug release from electrospun nanofibers. J Control Release. 2015; In Press.

[22] Rao PR, Diwan PV. Formulation and in vitro evaluation of polymeric films of diltiazem hydrochloride and indomethacin for transdermal administration. Drug Dev Ind Pharm. 1998; 4: 327-333.

[23] Akhgari A, Farahmand F, Afrasiabi Garekani H, Sadeghi F, Vandamme T. The effect of pectin on swelling and permeability characteristics of free films containing eudragit RL and/or RS as a coating formulation aimed for colonic drug delivery. DARU. 2010; 18(2): 91-96.