Formulation and optimization of mucoadhesive buccal patches of losartan potassium by using response surface methodology

Ikram, Md.; Gilhotra, Neeraj; Gilhotra, Ritu Mehra

Formulation and optimization of mucoadhesive buccal patches of losartan potassium by using response surface methodology

Authors

¹ School of Pharmacy, Suresh Gyan Vihar University, Jaipur, Rajasthan, India

² Department of Pharmacy, Maharshi Dayanand University, Rohtak, Haryana, India

Abstract

Background: This study was undertaken with an aim to systematically design a model of factors that would yield an optimized sustained release dosage form of an anti-hypertensive agent, losartan potassium, using response surface methodology (RSM) by employing 3² full factorial design.
Materials and Methods: Mucoadhesive buccal patches were prepared using different grades of hydroxypropyl methylcellulose (HPMC) (K4M and K100M) and polyvinylpyrrolidone-K30 by solvent casting method. The amount of the release retardant polymers – HPMC K4M (X₁) and HPMC K100M (X₂) was taken as an independent variable. The dependent variables were the burst release in 30 min (Y₁), cumulative percentage release of drug after 8 h (Y₂) and swelling index (Y₃) of the patches. In vitro release and swelling studies were carried out and the data were fitted to kinetic equations.
Results: The physicochemical, bioadhesive, and swelling properties of patches were found to vary significantly depending on the viscosity of the polymers and their combination. Patches showed an initial burst release preceding a more gradual sustained release phase following a nonfickian diffusion process.
Discussion: The results indicate that suitable bioadhesive buccal patches with desired permeability could be prepared, facilitated with the RSM.

Keywords

References

1.	Adhikari SN, Nayak BS, Nayak AK, Mohanty B. Formulation and evaluation of buccal patches for delivery of atenolol. AAPS Pharm Sci Tech 2010;11:1038-44.
2.	Yamsani VV, Gannu R, Kolli C, Rao ME, Yamsani MR. Development and in vitro evaluation of buccoadhesive carvedilol tablets. Acta Pharm 2007;57:185-97.
3.	Puratchikody A, Prasanth VV, Mathew ST, Kumar BA. Development and characterization of mucoadhesive patches of salbutamol sulfate for unidirectional buccal drug delivery. Acta Pharm 2011;61:157-70.
4.	Morales JO, McConville JT. Manufacture and characterization of mucoadhesive buccal films. Eur J Pharm Biopharm 2011;77:187-99.
5.	Koland M, Charyulu RN, Prabhu P. Mucoadhesive films of losartan potassium for buccal delivery: Design and characterization. Indian J Pharm Educ Res 2010;44:315-23.
6.	Chopra S, Patil GV, Motwani SK. Release modulating hydrophilic matrix systems of losartan potassium: Optimization of formulation using statistical experimental design. Eur J Pharm Biopharm 2007;66:73-82.
7.	Singh B, Chakkal SK, Ahuja N. Formulation and optimization of controlled release mucoadhesive tablets of atenolol using response surface methodology. AAPS Pharm Sci Tech 2006;7:E3.
8.	Chaudhary R, Qureshi MS, Patel J, Panigrahi UP, Giri IC. Formulation, development and in-vitro evaluation of mucoadhesive buccal patches of methotrexate. Int J Pharma Sci Res 2010;1:357-65.
9.	Vasantha PV, Puratchikody A, Mathew ST, Balaraman AK. Development and characterization of Eudragit based mucoadhesive buccal patches of salbutamol sulfate. Saudi Pharm J 2011;19:207-14.
10.	Patel VM, Prajapati BG, Patel MM. Effect of hydrophilic polymers on buccoadhesive eudragit patches of propranolol hydrochloride using factorial design. AAPS Pharm Sci Tech 2007;8:E119-26.
11.	Shidhaye SS, Saindane NS, Sutar S, Kadam V. Mucoadhesive bilayered patches for administration of sumatriptan succinate. AAPS Pharm SciTech 2008;9:909-16.
12.	Koland M, Sandeep V, Charyulu N. Fast Dissolving sublingual films of ondansetron hydrochloride: Effect of additives on in vitro drug release and mucosal permeation. J Young Pharm 2010;2:216-22.
13.	Semalty M, Semalty A, Kumar G. Formulation and characterization of mucoadhesive buccal films of glipizide. Indian J Pharm Sci 2008;70:43-8. [PUBMED]
14.	Giannola LI, De Caro V, Giandalia G, Siragusa MG, Tripodo C, Florena AM, et al. Release of naltrexone on buccal mucosa: Permeation studies, histological aspects and matrix system design. Eur J Pharm Biopharm 2007;67:425-33.
15.	Gilhotra RM, Mathurm M. Glycerogelatin-based ocular inserts of aceclofenac: Physicochemical, drug release studies and efficacy against prostaglandin E2-induced ocular inflammation. Drug Deliv 2011;18:54-64.
16.	Kaur A, Kaur G. Mucoadhesive buccal patches based on interpolymer complexes of chitosan-pectin for delivery of carvedilol. Saudi Pharm J 2012;20:21-7.
17.	Gilhotra RM, Gilhotra N, Mishra DN. Piroxicam bioadhesive ocular inserts: Physicochemical characterization and evaluation in prostaglandin-induced inflammation. Curr Eye Res 2009;34:1065-73.
18.	Verma N, Chattopadhyay P. Preparation of mucoadhesive buccal patches of carvedilol and evaluation for in-vitro drug permeation through porcine buccal membrane. Afr J Pharm Pharmacol 2011;5:1228-33.
19.	Alanazi FK, Rahman AA, Mahrous GM, Alsarra IA. Formulation and physicochemical characterization of buccoadhesive films containing ketorolac. J Drug Deliv Sci 2007;17:183-92.
20.	Patel VM, Prajapati BG, Patel MM. Design and characterization of chitosan-containing mucoadhesive buccal patches of propranolol hydrochloride. Acta Pharm 2007;57:61-72.
21.	Prajapati ST, Patel CG, Patel CN. Formulation and evaluation of transdermal patch of repaglinide. ISRN Pharm 2011;2011:651909.
22.	Dash S, Murthy PD, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm Drug Res 2010;67:217-23.
23.	Korsmeyer RW, Gurny R, Doelker EM, Buri P, Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25-35.
24.	Ritger PL, Peppas NA. Simple equation for solute release part 1. Fickian and nonfickian release from non-swellable devices in the form of slabs, spheres, cylinders or disks. J Control Release 1987;5:37-42.
25.	Hogan J. Hydroxypropyl methylcellulose sustained release technology. Drug Dev Ind Pharm 1989;15:975-99.
26.	Karavas E, Georgarakis E, Bikiaris D. Application of PVP/HPMC miscible blends with enhanced mucoadhesive properties for adjusting drug release in predictable pulsatile chronotherapeutics. Eur J Pharm Biopharm 2006;64:115-26.
27.	Perioli L, Ambrogi V, Angelici F, Ricci M, Giovagnoli S, Capuccella M, et al. Development of mucoadhesive patches for buccal administration of ibuprofen. J Control Release 2004;99:73-82.
28.	Sakarkar DM, Kshirsagar RV, Deshbhratar RM. Studies on formulation and in vitro evaluation of gastroretentive drug delivery system of carbamazepine. Int J Chem Tech Res 2010;2:108-13.
29.	Conti S, Maggi L, Segale L, Ochoa Machiste E, Conte U, Grenier P, et al. Matrices containing NaCMC and HPMC 2. Swelling and release mechanism study. Int J Pharm 2007;333:143-51.
30.	Li S, Lin S, Daggy BP, Mirchandani HL, Chien YW. Effect of HPMC and Carbopol on the release and floating properties of gastric floating drug Delivery system using factorial design. Int J Pharm 2003;253:13-22.
31.	Islam MR, Ahmed I, Quadir MA, Rahman MH. Once daily sustained-release matrix tablet of naproxen: Formulation and in vitro evaluation. Dhaka Univ J Pharm Sci 2010;9:47-52.
32.	Rahman MM, Roy S, Das SC, Jha MK, Begum T, Ahsan MQ, et al. Evaluation of various grades of hydroxypropylmethylcellulose matrix systems as oral sustained release drug delivery systems. J Pharm Sci Res 2011;3:930-8.
33.	Siepmann J, Peppas NA. Higuchi equation: Derivation, applications, use and misuse. Int J Pharm 2011;418:6-12.
34.	Tran HT, Park JB, Hong KH, Choi HG, Han HK, Lee J, et al. Preparation and characterization of pH-independent sustained release tablet containing solid dispersion granules of a poorly water-soluble drug. Int J Pharm 2011;415:83-8.

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