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Recent Advances in Drug Delivery and Formulation

Editor-in-Chief

ISSN (Print): 2667-3878
ISSN (Online): 2667-3886

Research Article

Design and Statistical Optimization of Novel Polyelectrolyte Complex Microbeads to Improve Entrapment Efficiency and Release Study of Vildagliptin

Author(s): Ritesh Kumar Tiwari*, Lalit Singh and Mukesh Kr. Singh

Volume 17, Issue 1, 2023

Published on: 27 March, 2023

Page: [71 - 85] Pages: 15

DOI: 10.2174/2667387817666230308113951

Price: $65

Abstract

Background: The current research focused on the improvement of drug entrapment efficiency and release study of hydrophilic drug through polymer complextation.

Objective: Ionotropic gelation technique was utilised for the preparation of Polyelectrolyte complex microbeads of Vildagliptin using Sodium alginate and Eudragit RL100 and their performance was optimized by Central composite design.

Methods: Fourier Transform Infrared Spectroscopy, Scanning Electron Microscope, Differential Scanning Calorimetry, particle size, Drug Entrapment Efficiency, X-ray diffraction and in vitro drug release at 10hr were chosen for evaluating formulated microbeads. The impact of independent variables like concentration of sodium alginate and eudragit RL100 was examined over dependent responses.

Results: The interpretation of XRD, SEM, DSC, and FTIR affirmed no drug excipients interference and confirmed formation of polyelectrolyte complex microbeads. For complex microbeads, the maximum and minimum drug release after 10 hours was obtained as 96.23.5% and 89.45%, respectively. The 32 central composite design was further used to obtain response surface graph and the values for the particle size, DEE and Drug release were retained as 0.197, 76.30 % and 92.15%, respectively for the optimize batch.

Conclusion: The result suggested the combination of two polymers (Sodium alginate and Eudragit RL100) were suitable for improving the entrapment efficiency of hydrophilic drug (Vildagliptin). The central composite design (CCD) technique is an effective tool for obtaining optimal drug delivery systems of Vildagliptin polyelectrolyte complex microbeads.

Keywords: Polyelectrolyte complex, central composite design, Eudragit RL 100, FTIR, vildagliptin, HbA1C.

Graphical Abstract
[1]
Muchtaridi M, Belali N, Wathoni N. Advances in orally targeted drug delivery to colon. J Adv Pharm Technol Res 2019; 10(3): 100-6.
[http://dx.doi.org/10.4103/japtr.JAPTR_26_19] [PMID: 31334090]
[2]
Philipp B, Dautzenberg H, Linow KJ, Kötz J, Dawydoff W. Polyelectrolyte complexes - recent developments and open problems. Prog Polym Sci 1989; 14(1): 91-172.
[http://dx.doi.org/10.1016/0079-6700(89)90018-X]
[3]
Lankalapalli S, Kolapalli VRM. Polyelectrolyte complexes: A review of their applicability in drug delivery technology. Indian J Pharm Sci 2009; 71(5): 481-7.
[http://dx.doi.org/10.4103/0250-474X.58165] [PMID: 20502564]
[4]
Srivastava P, Visht S. Application and advancement of microsphere as controlled delivery system: a review. Int J Pharm Life Sci 2013; 4(4): 2583-94.
[5]
Pawar SN, Edgar KJ. Alginate derivatization: A review of chemistry, properties and applications. Biomaterials 2012; 33(11): 3279-305.
[http://dx.doi.org/10.1016/j.biomaterials.2012.01.007] [PMID: 22281421]
[6]
Ulery BD, Nair LS, Laurencin CT. Biomedical applications of biodegradable polymers. J Polym Sci, B, Polym Phys 2011; 49(12): 832-64.
[http://dx.doi.org/10.1002/polb.22259] [PMID: 21769165]
[7]
Bajpai SK, Sharma S. Investigation of swelling/degradation behaviour of alginate beads crosslinked with Ca2+ and Ba2+ ions. React Funct Polym 2004; 59(2): 129-40.
[http://dx.doi.org/10.1016/j.reactfunctpolym.2004.01.002]
[8]
Abdul BK, Fahmy SA. Development of coated beads for oral controlled delivery of cefaclor: In vitro evaluation. Acta Pharm 2013; 63(1): 31-44.
[http://dx.doi.org/10.2478/acph-2013-0003] [PMID: 23482311]
[9]
Mohima T, Dewan I, Islam SMA, Rana S, Hossain A. Encapsulation of zidovudine in different cellulosic acrylic and methacrylic polymers loaded microspheres: in vitro characterization and compatibility studies. Int J Pharm Pharm Sci 2015; 7(1): 486-95.
[10]
Moustafine RI, Kemenova VA, Van den Mooter G. Characteristics of interpolyelectrolyte complexes of Eudragit E 100 with sodium alginate. Int J Pharm 2005; 294(1-2): 113-20.
[http://dx.doi.org/10.1016/j.ijpharm.2005.01.029] [PMID: 15814235]
[11]
Motwani SK, Chopra S, Talegaonkar S, Kohli K, Ahmad FJ, Khar RK. Chitosan-sodium alginate nanoparticles as submicroscopic reservoirs for ocular delivery: formulation, optimisation and in vitro characterisation. Eur J Pharm Biopharm 2008; 68(3): 513-25.
[PMID: 17983737]
[12]
Naik JB, Lokhande AB, Mishra S, Kulkarni RD. Development of sustained release micro/nano particles using different solvent emulsification technique: a review. Int J Pharma Bio Sci 2012; 3(4): 573-90.
[13]
Yaacob B, Amin MCIM, Hashim K, Bakar BA. Optimization of reaction conditions for carboxymethylated sago starch. Iran Polym J 2011; 20(3): 195-204.
[14]
Balpande HM, Raut NS, Umekar MJ, Kotagale NR. Compatibility study of metformin with pharmaceutical excipients. Int J Chemtech Res 2013; 5: 1684-93.
[15]
Chikukwa MTR, Walker RB, Khamanga SMM, Sandile M, Khamanga M. Formulation and characterisation of a combination captopril and hydrochlorothiazide microparticulate dosage form. Pharmaceutics 2020; 12(8): 712.
[http://dx.doi.org/10.3390/pharmaceutics12080712] [PMID: 32751409]
[16]
Adhyapak AA, Desai B. Formulation and evaluation of liposomal transdermal patch for targeted drug delivery of tamoxifen citrate for breast cancer. Indian J Health Sci 2016; 9(1): 40-8.
[http://dx.doi.org/10.4103/2349-5006.183677]
[17]
Tejraj MA, Anandro RK, Kumaresh SS. Controlled release of Diclofenac sodium from sodium alginate beads cross-linked with gluteraldehyde. Pharm Acta Helv 1999; 74(9): 29-6.
[18]
Shabaraya AR, Narayanacharyulu R. Design and characterization of mucoadhesive microspheres of novel NSAID drug using algino-eudragit RS100 system. Indian J Pharm Sci 2003; 65: 250-2.
[19]
Shaheen O, Othman S, Jalal I, Awidi A, Alturk W. Comparison of pharmacokinetics and pharmacodynamics of a conventional and a new rapidly dissolving glibenclamide preparation. Int J Pharm 1987; 38(1-3): 123-31.
[http://dx.doi.org/10.1016/0378-5173(87)90107-4]
[20]
Gonzalez-Mira E, Egea MA, Souto EB, Calpena AC, García ML. Optimizing flurbiprofen-loaded NLC by central composite factorial design for ocular delivery. Nanotechnology 2011; 22(4): 045101.
[http://dx.doi.org/10.1088/0957-4484/22/4/045101] [PMID: 21169662]
[21]
Sester C, Ofridam F, Lebaz N, Gagnière E, Mangin D, Elaissari A. ph-sensitive methacrylic acid–methyl methacrylate copolymer eudragit L100 and dimethylaminoethyl methacrylate, butyl methacrylate, and methyl methacrylate tri-copolymer eudragit E100. Polym Adv Technol 2019; 31(3): 440-50.
[http://dx.doi.org/10.1002/pat.4780]
[22]
Szekalska M. Puciłowska A, Szymańska E, Ciosek P, Winnicka K. Alginate: current use and future perspectives in pharmaceutical and biomedical applications. Int J Polym Sci 2016; 2016: 1-17.
[http://dx.doi.org/10.1155/2016/7697031]
[23]
Venkateshwarlu K, Ravi Shankar K, Ramana Murthy KV, Koteswara Rao GS. Applicability of natural gums for the development of controlled release vancomycin hydrochloride tablets in site specific colon region using statistical optimization. Asian J Pharm Sci 2019; 13(4): 385.
[24]
Bhumkar DR, Pokharkar VB. Studies on effect of pH on cross-linking of chitosan with sodium tripolyphosphate: A technical note. AAPS PharmSciTech 2006; 7(2): E138-43.
[http://dx.doi.org/10.1208/pt070250] [PMID: 16796367]

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