Research Article | Volume: 8, Issue: 9, September, 2018

Formulation and Evaluation of Gliclazide in Vegetable Oil-Based Self Emulsifying Delivery System

Gehan F. Balata   

Open Access   

Published:  Sep 30, 2018

DOI: 10.7324/JAPS.2018.8905
Abstract

Objectives: To formulate a poorly water-soluble, antidiabetic drug, gliclazide, in the vegetable oil-based self-emulsifying delivery system (SEDDS), as a trial to improve its dissolution and hence its bioavailability. Material and methods: Solubility of gliclazide was investigated in different vegetable oils, surfactants and co-surfactants. The system was selected and the self-emulsification region was identified. Drug-loaded SEDDS was prepared and evaluated in terms of emulsification time, phase separation, droplet size and rate of drug dissolution. The formulation that showed good self-emulsifying properties, acceptable droplet size and high % drug release was further processed into solid- SEDDS by physical mixing with varying proportions of a mixture (2:1) of microcrystalline cellulose and lactose and characterized for crystalline, droplet size and in vitro drug dissolution properties. Results and Conclusions: Formulation of gliclazide in liquid and solid SEDDS using olive oil resulted in significant (P < 0.05) improvement in its dissolution properties. Both differential scanning calorimetry and x-ray diffraction studies demonstrated the presence of gliclazide in the molecular state in all the prepared solid formulations. Solid SEDDS of gliclazide containing a lower proportion of adsorbent (G1) had comparable dissolution properties with its liquid form. Thus formulation of gliclazide in the solid self-emulsifying system may be a promising strategy to improve its dissolution properties.


Keyword:     Gliclazide solid-SEDDS ternary phase diagram dissolution olive oil.


Citation:

Balata GF. Formulation and Evaluation of Gliclazide in Vegetable Oil-Based Self Emulsifying Delivery System. J App Pharm Sci, 2018; 8(09): 023-033.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Reference

Abdalla A, Klein S, Mäder K. A new self-emulsifying drug delivery system (SEDDS) for poorly soluble drugs: Characterization, dissolution, in vitro digestion and incorporation into solid pellets. Eur J Pharm Sci, 2008; 3(5):457-464.https://doi.org/10.1016/j.ejps.2008.09.006

Aboutaleb HA, Kharshoum RM, Ismail HR. Formulation and optimization of solid self-nanoemulsifying system using porous carriers for oral delivery of cinnarizine. Int J Pharm Pharm Sci, 2016; 8(1):433-438.

ACCU Dyne TestTM. Available at: www.accudynetest.com/visc_ table.html.

Agubata CO, Nzekwe IT, Obitte NC, Ugwu CE, Attama AA, Onunkwo GC. Effect of oil, surfactant and co-surfactant concentrations on the phase behavior, physicochemical properties and drug release from self-emulsifying drug delivery systems. J Drug Discov Develop and Deliv, 2014; 1(1):1-7.

Amemiya T, Mizuno S, Yuasa H, Watanabe J. Emulsion type new vehicle for soft gelatin capsule available for preclinical and clinical trials: stabilization of new vehicle containing vitamin K2 with PEG 6000. Xenobiotics, 1999; 14(5):392-398.https://doi.org/10.2133/dmpk.14.392

Azeem A, Rizwan M, Ahmad FJ, Iqbal Z, Khar RK, Aqil M, Talegaonkar S. Nanoemulsion components screening and selection: A technical note. AAPS Pharm Sci Tech, 2009; 10:69-76.https://doi.org/10.1208/s12249-008-9178-x

Bagwe RP, Kanicky JR, Palla BJ, Patanjali PK, Shah DO. Improved drug delivery using microemulsions: Rationale, recent progress, and new horizons. Crit Rev Ther Drug Carrier Syst, 2001; 18:77-140.

Basalious EB, Shawky N, Badr-Eldin SM. SNEDDS containing bioenhancers for improvement of dissolution and oral absorption of lacidipine. I: development and optimization. Int J Pharm, 2010; 391:203- 211.https://doi.org/10.1016/j.ijpharm.2010.03.008

Berraaouan A, Abid S, Bnouham M. Antidiabetic oils. Current Diabetes Reviews, 2013; 9(6):499-505.https://doi.org/10.2174/15733998113096660081

Bhagwat DA, D'Souza JI. Development of solid self-microemulsifying drug delivery system with neusilin UF-2 for enhanced dissolution rate of telmisartan. Int J Drug Dev & Res, 2012; 4(4):398-407.

Bhandari V, Avachat A. Formulation and characterization of self emulsifing pellets of carvedilol. Braz J Pharm Sci, 2015; 51(3):663-671.https://doi.org/10.1590/S1984-82502015000300018

Bhikshapathi D, Madhukar P, Kumar BD, Kumar GA. Formulation and characterization of pioglitazone HCl self-emulsifying drug delivery system. Pharm Lett, 2013; 5(2):292-305.

Biswal S, Sahoo J, Murthy PN, Giradkar, RP, Avari JG. Enhancement of dissolution rate of gliclazide using solid dispersions with polyethylene glycol 6000. AAPS Pharma Sci Tech, 2008; 9(2):563-570.https://doi.org/10.1208/s12249-008-9079-z

Biswal S, Sahoo J, Murthy PN. Physicochemical properties of solid dispersions of gliclazide in polyvinyl pyrrolidone K-90. AAPS Pharm Sci Tech, 2009; 10(2):329-334.https://doi.org/10.1208/s12249-009-9212-7

Chen ZQ, Liu Y, Zhao JH, Wang L, Feng NP. Improved oral bioavailability of poorly water-soluble indirubin by a supersaturatable selfmicroemulsifying drug delivery system. Int J Nanomed, 2012; 7:1115- 1125.

Cho H, Kang J, Ngo L, Tran P, Lee Y. Preparation and evaluation of solid-self-emulsifying drug delivery system containing paclitaxel for lymphatic delivery. J Nanomater, 2016; Article ID 3642418: 14 pages.

Craig DQM. The use of self-emulsifying systems as a means for improving drug delivery. Bull Tech Gattefossé, 1993; 86:21-31.

Czajkowska-Kośnik A, Szekalska M, Amelian A, Szymańska E, Winnicka K. Development and evaluation of liquid and solid self-emulsifying drug delivery systems for atorvastatin. Molecules, 2015; 20:21010-21022.https://doi.org/10.3390/molecules201219745

Dixit RP, Nagarsenker MS. Self-nanoemulsifying granules of ezetimibe: Design, optimization and evaluation. Eur J Pharm Sci, 2008; 35:183-192.https://doi.org/10.1016/j.ejps.2008.06.013

Dokania S, Joshi AK. Self-microemulsifying drug delivery system (SMEDDS) – challenges and road ahead. Drug Delivery, 2015; 22(6).https://doi.org/10.3109/10717544.2014.896058

El-Laithy HM. Self-nanoemulsifying drug delivery system for enhanced bioavailability and improved hepatoprotective activity of biphenyl dimethyl dicarboxylate. Curr Drug Deliv, 2008; 5:170-176.https://doi.org/10.2174/156720108784911695

Fatouros DG, Deen GR, Arleth L, Bergenstahl B, Nielsen FS, Pedersen JS, Mullertz A. Structural development of self nano emulsifying drug delivery systems (SNEDDS) during in vitro lipid digestion monitored by small-angle X-ray scattering. Pharm Res, 2007; 24:1844-1853.https://doi.org/10.1007/s11095-007-9304-6

Franceschinis E, Bortoletto C, Perissutti B, Dal Zotto M, Voinovich D, Realdon N. Self-emulsifying pellets in a lab-scale high shear mixer: Formulation and production design. Powder Technology, 2011; 207:113-118.https://doi.org/10.1016/j.powtec.2010.10.016

Franceschinis E, Voinovich D, Grassi M, Perissutti B, Filipovic- Grcic J, Martinac A, Meriani-Merlo F. Self-emulsifying pellets prepared by wet granulation in high-shear mixer: influence of formulation variables and preliminary study on the in vitro absorption. Int J Pharm, 2005; 291:87-97.https://doi.org/10.1016/j.ijpharm.2004.07.046

Gershanik T, Benita S. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur J Pharm Biopharm; 2000; 50:179-188.https://doi.org/10.1016/S0939-6411(00)00089-8

Gurram AK, Deshpande PB, Kar SS, Nayak YU, Udupa N, Reddy MS. Role of components in the formation of self-microemulsifying drug delivery systems. Indian J Pharm Sci, 2015; 77(3):249-257.https://doi.org/10.4103/0250-474X.159596

Harrower AD. Comparison of efficacy, secondary failure rate and complications of sulfonylurea. J Diabetes Complicat, 1994; 8:201-203.https://doi.org/10.1016/1056-8727(94)90044-2

Harshal M, Tanvir S, Dheera B, Rajendra WD. Design and development of solid self-micro-emulsifying drug delivery system (SMEDDS) of fenofibrate. Int J Pharm Pharm Sci, 2011; 3(4):163-166.

Hegazi R, El-Gamal M, Abdel-Hady N, Hamdy O. Epidemiology of and risk factors for type 2 diabetes in Egypt. Annals of Global Health, 81(6):814-820.https://doi.org/10.1016/j.aogh.2015.12.011

Iosio T, Voinovich D, Grassi M, Pinto JF, Perissutti B, Zacchigna M, Quintavalle U, Serdoz F. Bi-layered self-emulsifying pellets prepared by co-extrusion and spheronization: Influence of formulation variables and preliminary study on the in vivo absorption. Eur J Pharm Biopharm, 2008; 69:686-697.https://doi.org/10.1016/j.ejpb.2007.11.014

Jaiswal P, Aggarwal G, Harikumar SL, Singh K. Development of self-microemulsifying drug delivery system and solid-self-microemulsifying drug delivery system of telmisartan. Int J Pharm Investig, 2014; 4(4):195- 206.https://doi.org/10.4103/2230-973X.143123

Jung YJ, Dong YS, Lee SH, Kim KH, Yoon DS, Lee KH. Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique. Int J Pharm, 1999; 187:209-218.https://doi.org/10.1016/S0378-5173(99)00191-X

Kaithwas G, Majumdar DK. In vitro antioxidant and in vivo antidiabetic, antihyperlipidemic activity of linseed oil against streptozotocin-induced toxicity in albino rats. Eur J Lipid Sci Technol, 2012; 114:1237-1245.https://doi.org/10.1002/ejlt.201100263

Kallakunta VR, Bandari S, Jukanti R, Veerareddy PR. Oral self-emulsifying powder of lercanidipine hydrochloride: Formulation and evaluation. Powder Technology, 2012; 221:375-382.https://doi.org/10.1016/j.powtec.2012.01.032

Kallakunta VR, Eedara BB, Jukanti R, Ajmeera RK, Suresh Bandari SA. Gelucire 44/14 and labrasol based solid self-emulsifying drug delivery system: formulation and evaluation. J Pharm Invest, 2013; 43:185- 196.https://doi.org/10.1007/s40005-013-0060-9

Khan KA. The concept of dissolution efficiency. J Pharm Pharmacol, 1975; 27:48-49.https://doi.org/10.1111/j.2042-7158.1975.tb09378.x

Khedekar K, Mittal S. Self emulsifying drug delivery system: A review. Int J Pharm Sci Res, 2013; 4(12):4494-4497.

Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev, 2009; 45:89-121.https://doi.org/10.1016/S0169-409X(00)00103-4

Levy MY, Benita S. Drug release from submicronized O/W emulsion: a new in vitro kinetic evaluation model. Int J Pharm, 1990; 66(1- 3):29-37.

Li L, Yi T, Wai-Kei Lam C. Effects of spray-drying and choice of solid carriers on concentrations of labrasol® and transcutol® in solid self-microemulsifying drug delivery systems (SMEDDS). Molecules, 2013; 18:545-560.https://doi.org/10.3390/molecules18010545

Mahajan HS, Girnar GA, Nerkar P. Dissolution and bioavailability enhancement of gliclazide by surface solid dispersion using spray drying technique. Indian J Novel Drug Deliv, 2012; 4(2):115-124.

Mehrnia MA, Jafari SM, Zadeh BS, Maghsoudlou Y. Crocin loaded nano-emulsions: factors affecting emulsion properties in spontaneous emulsification. Int J Biol Macromol, 2016; 84:261-267.https://doi.org/10.1016/j.ijbiomac.2015.12.029

Miryala V, Kurakula M. Self-nano emulsifying drug delivery system (SEDDS) for oral delivery of atorvastatin—Formulation and bioavailability studies. JDDT, 2013; 3:131-142.

Mohanvarma SK, Padavala MV. Oral lipid-based drug delivery systems – an overview. Acta Pharm Sin B, 2013; 3(6):361-372.https://doi.org/10.1016/j.apsb.2013.10.001

Mosca M, Cuomo F, Lopez, F, Ceglie A. Role of emulsifier layer, antioxidants and radical initiators in the oxidation of olive oil-in-water emulsions. Food Res Int, 2013; 50:377-383.https://doi.org/10.1016/j.foodres.2012.10.046

Nepal PR, Han HK, Choi HK. Preparation and in vitro-in vivo evaluation of Witepsol_ H35 based selfnanoemulsifying drug delivery systems (SNEDDS) of coenzyme Q10. European J Pharm Sci, 2010; 39(4), 224-232.https://doi.org/10.1016/j.ejps.2009.12.004

Nigade PM, Patil S, Shradha S. Self emulsifying drug delivery system (sedds): a review. IJPBS, 2012; 2(2):42-52.

Nikolakakis I, Panagopoulou A, Salis A, Malamataris S. Relationships between the properties of self-emulsifying pellets and of the emulsions used as massing liquids for their preparation. AAPS Pharm Sci Tech, 2015; 16(1):129-139.https://doi.org/10.1208/s12249-014-0214-8

Nipun TS, Ashraful Islam SM. SEDDS of gliclazide: Preparation and characterization by in-vitro, ex-vivo and in-vivo techniques. Saudi Pharm Journal, 2014; 22(4):343-348.https://doi.org/10.1016/j.jsps.2013.06.001

Ostertag F, Weiss J, McClements DJ. Low-energy formation of edible nanoemulsions: factors influencing droplet size produced by emulsion phase inversion. J Colloid Interface Sci, 2012; 388:95-102.https://doi.org/10.1016/j.jcis.2012.07.089

Palmer KJ, Brogden RN. Gliclazide, an update of its pharmacological properties and therapeutic efficacy. Drugs, 1993; 46:92- 125.https://doi.org/10.2165/00003495-199346010-00007

Parekh VJ, Desai ND, Shaikh MS, Shinde UA. Self nanoemulsifying granules (SNEGs) of meloxicam: preparation, characterization, molecular modeling and evaluation of in vivo anti-inflammatory activity. Drug Dev Ind Pharm, 2017; 43(4).https://doi.org/10.1080/03639045.2016.1275665

Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur J Pharm Sci, 2000; 11:S93-S98.https://doi.org/10.1016/S0928-0987(00)00167-6

Pouton CW. Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system. Eur J Pharm Sci, 2006; 29:278-287.https://doi.org/10.1016/j.ejps.2006.04.016

Saifee M, Zarekar S, Rao VU, Zaheer Z, Soni R, Burande S. Formulation and In vitro evaluation of solid-self- emulsifying drug delivery system (SEDDS) of Glibenclamide. AJADD, 2013; 1(3):323-340.

Samarji R, Balbaa M. Anti-diabetic activity of different oils through their effect on arylsulfatases. J Diabetes Metab Disord, 2014; 13:116.https://doi.org/10.1186/s40200-014-0116-z

Sapkal NP, Kilor VA, Bhusari KP, Daud AS. Evaluation of some methods for preparation of gliclazide-®-cyclodextrin inclusion complexes. Trop J Pharm Res, 2007; 6(4):833-840.https://doi.org/10.4314/tjpr.v6i4.14667

Seo YG, Kim DH, Ramasamy T, Kim JH, Marasini N, Oh YK, Kim DW, Kim JK, Yong CS, Kim JO, Choi HG. Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect. Int J Pharm, 2013; 452:412-420.https://doi.org/10.1016/j.ijpharm.2013.05.034

Shahavia MH, Hosseinia M, Jahanshahia M, Meyer RL, Najafpour G. Evaluation of critical parameters for preparation of stable clove oil nanoemulsion. Arabian Journal of Chemistry, 2015.https://doi.org/10.1016/j.arabjc.2015.08.024

Shavi GV, Kumar AR, Usha YN, Armugam K, Ranjan O, Ginjupalli K, Pandey S, Udupa N. Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques. Int J Drug Deliv, 2010; 2:49-57.https://doi.org/10.5138/ijdd.2010.0975.0215.02011

Suresh PK, Sharma S. Formulation and in-vitro characterization of self-nanoemulsifying drug delivery system of cinnarizine. Pharmacie Globale (IJCP), 2011; 9(8):1-6.

Talegaonkar S, Azeem A, Ahmad FJ, Khar RK, Pathan SK, Khan ZI. Microemulsions: a novel approach to enhanced drug delivery. Recent Pat Drug Deliv Formul, 2008; 2:238-257.https://doi.org/10.2174/187221108786241679

Tuleu C, Newton M, Rose MJ, Euler D, Saklatvala R, Clarke A, Booth S. Comparative bioavailability study in dogs of a self-emulsifying formulation of progesterone presented in a pellet and liquid form compared with an aqueous suspension of progesterone. J Pharm Sci, 2004; 93:1495- 1502.https://doi.org/10.1002/jps.20068

Yi T, Wan J, Xu H, Yang X. New solid self-microemulsifying formulation prepared by spray-drying to improve the oral bioavailability of poorly water soluble drugs. Eur J Pharm Biopharm, 2008; 70:439-444.https://doi.org/10.1016/j.ejpb.2008.05.001

Wankhade VP, Atram SC, Nishan N Bobade NN, Pande SD, Tapar KK. Formulation and optimization of SNEDDS of gliclazide using response surface methodology. Asian J Pharm, 2012; 6(4):289.https://doi.org/10.4103/0973-8398.107565

Yin YM, Cui FD, Mu CF, Choi MK, Kim JS, Chung SJ, Shim CK, Kim DD. Docetaxel microemulsion for enhanced oral bioavailability: preparation and in vitro and in vivo evaluation. J Controlled Release, 2009; 140:86-94.https://doi.org/10.1016/j.jconrel.2009.08.015

Zambiazi RC, Przybylski R, Zambiazi MW, Mendonca CB. Fatty acid composition of vegetable oils and fats. Curitiba, 2007; 25(1):111-120.

Zeing L, Xin X, Zhang Y. Development and characterization of promising Cremophor EL-stabilized o/w nanoemulsions containing short-chain alcohols as a cosurfactant. RSC Adv, 2017; 7:19815-19827.https://doi.org/10.1039/C6RA27096D

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