FORMULATION, IN VITRO AND EX VIVO CHARACTERIZATION OF MUCOADHESIVE BUCCAL TABLETS FOR ANTIHYPERTENSIVE DRUG

Himabindu Peddapalli; Vasudha Bakshi; Narender Boggula

doi:10.22159/ajpcr.2018.v11i8.26126

Authors

Himabindu Peddapalli Department of Pharmaceutics, School of Pharmacy, Anurag Group of Institutions, Venkatapur, Ghatkesar- 500 088, Telangana, India.
Vasudha Bakshi Department of Pharmaceutics, School of Pharmacy, Anurag Group of Institutions, Venkatapur, Ghatkesar- 500 088, Telangana, India.
Narender Boggula Department of Pharmaceutics, School of Pharmacy, Anurag Group of Institutions, Venkatapur, Ghatkesar- 500 088, Telangana, India.

DOI:

https://doi.org/10.22159/ajpcr.2018.v11i8.26126

Keywords:

Mucoadhesive buccal tablets, Olmesartan, Direct compression method, ex vivo permeation studies

Abstract

Objective: Olmesartan belongs to a class of angiotensin II receptor blockers. It is used in the treatment of hypertension. However, it undergoes extensive hepatic first-pass metabolism, resulting in low oral bioavailability is about 26%. The aim of this study was to prepare and evaluate the mucoadhesive buccal tablets of olmesartan with a goal to increase the bioavailability and improve the patient compliance.

Methods: Mucoadhesive buccal tablets were prepared by a direct compression technique using mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC K4M), sodium carboxymethylcellulose (SCMC), and Carbopol 934P. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, ex vivo mucoadhesive strength, ex vivo mucoadhesive time, and ex vivo permeation studies. The release kinetics was calculated to determine the drug release mechanism.

Results: The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets F2, F7, and F11 showed satisfactory drug release rates with the diffusion controlled mechanism. Optimized buccal tablets developed for olmesartan possess reasonable mucoadhesive strength, mucoadhesive time, and surface pH was in an acceptable salivary pH 6.76Â±0.28â€“6.89Â±0.34. The ex vivo permeation studies for optimized tablets were shown satisfactory drug permeation and could meet the target flux 0.991 mg hâˆ’1cmâˆ’2.

Conclusion: The obtained results could be used as a platform to develop the buccal delivery of this drug, which bypasses the first-pass metabolism and results in the improvement of bioavailability. Hence, the present study concludes that the olmesartan could be delivered through the buccal route.

Downloads

Download data is not yet available.

References

Patel KV, Patel ND, Dodiya HD, Shelat PK. Buccal bioadhesive drug delivery system: An overview. Indian J Pharma Bioarch 2011;2:275-82.

Satyabrata B, Ellaiah M, Chandan M, Murthy KV, Bibhutibhusan P, Kumar PS. Design and in vitro evaluation of mucoadhesive buccal tablets of Perindopril prepared by sintering technique. Asian J Pharm Clin Res 2010;3:4-10.

Shojaei AH, Zhuo SL, Li X. Transbuccal delivery of acyclovir (II): Feasibility, system design, and in vitro permeation studies. J Pharm Sci 1998;1:66-73.

Zhang H, Zhang J, Streisand JB. Oral mucosal drug delivery: Clinical pharmacokinetics and therapeutic applications. Clin Pharm 2002;41:661-80.

Kadam SS, Yeole DH, Unjavani HK, Ganure AG, Kabra RP. Formulation and evaluation of mucoadhesive buccal tablets containing Carvedilol. Int J Curr Pharm Res 2014;1:67-80.

Senel S, Kremer MJ, Ka SH, Wertz PW, HÄ±ncal AA, Squier CA. Enhancing effect of Chitosan on peptide drug delivery across Buccal mucosa. Biomaterials 2000;21:2067-71.

Peddapalli H, Chinnala KM, Banala N. Design and in vitro characterization of mucoadhesive buccal patches of duloxetine hydrochloride. Int J Pharm Pharm Sci 2017;9:52-9.

Jaffar IS, Maraie NK. Formulation and in vitro evaluation of buccal mucoadhesive tablets of promethazine HCl. Int J Pharm Sci Rev Res 2014;24:61-9.

Patel MC, Patil CC. Formulation and evaluation of mucoadhesive buccal tablets of repaglinide. RGUHS J Pharm Sci 2014;4:34-42.

Roy AK, Kumar V, Basha SJ, Haque R, Karki R. Formulation and evaluation of Mucoadhesive buccal tablets of Valsartan. Int J Drug Dev Res 2013;5:145-58.

Shayeda, Ramesh G, Reddy PC, Rao YM. Development of novel bioadhesive buccal formulation of diltiazem: In vitro and in vivo characterization. PDA J Pharm Sci Tech 2009;63:1-9.

Vishnu YV, Sekhar KC, Rao ME, Rao YM. Development and in vitro evaluation of buccoadhesive Carvedilol tablets. Acta Pharm 2007;57:185-97.

Patil P, Kulkarni SV, Rao BS, Ammanage A, Surpur C, Basavaraj. Formulation and in vitro evaluation of mucoadhesive tablets of ofloxacin using natural gums. Int J Curr Pharm Res 2011;3:93-8.

Ishida M, Nambu N, Nagai T. Ointment-type oral mucosal dosage form of carbopol containing Prednisolone for treatment of aphtha. Chem Pharm Bull (Tokyo) 1983;31:1010-14.

Ahuja A, Khar RK, Ali J. Mucoadhesive drug delivery systems. Drug Dev Ind Pharm 1997;23:489-17.

Bromberg LE, Buxton DK, Friden PM. Novel periodontal drug delivery system for treatment of periodontitis. Control Release 2001;71:251-9.

Dortunc B, Ozer L, Uyanik N. Development and in vitro evaluation of a Buccoadhesive pindolol tablet formulation. Drug Dev Ind Pharm 1998;24:281-8.

Sudhakar Y, Kuotsu K, Bandyopadhya AK. Buccal bioadhesive drug delivery. A promising option for orally less efficient drugs. J Control Rel 2006;114:15-40.

Reddy PC, Rao YM. Buccal Drug Delivery Systems. In: Advances in Drug Delivery. Vol. 01. India: Published by Pharma Book Syndicate; 2010. p. 139-210.

Kumar V, Zakir F, Agarwal G, Choudhary A. Formulation and evaluation of buccal patches of venlafaxine. Int J Pharm Biosci 2011;1:170-82.

Warner GT, Jarvis B. Olmesartan medoxomil. Drugs 2002;62:1345-53.

Nakagomi-Hagihara R, Nakai D, Kawai K, Yoshigae Y, Tokui T, Abe T, et al. OATP1B1, OATP1B3, and Mrp2 are involved in hepatobiliary transport of olmesartan, a novel angiotensin II blocker. Drug Metab Disposition 2006;34:862-9.

Gupta A, Garg S, Khar RK. Measurements of bioadhesive strength of buccal tablets: Design of an in vitro assembly. Indian Drugs 1993;30:152-55.

Patel DM, Shah PM, Patel CN. Formulation and evaluation of bioadhesive buccal drug delivery of repaglinide tablets. Asian J Pharm 2012;6:171-9.

Channawar MA, Bakde BV, Gawnde SR, Chandewar AV, Kshirsagar MD. Development and in vitro characterization of diltiazem buccal tablets. J Pharm Res 2012;5:908-12.

Velmurugan S, Srinivas P. Formulation and in vitro evaluation of losartan potassium mucoadhesive buccal tablets. Asian J Pharm Clin Res 2013;6:125-30.

Bottenberg P, Cleymaet R, Muynek CD, Remon JP, Coomans D, Slop D. Development and testing of bioadhesive, fluoride-containing slow-release tablets for oral use. J Pharm Pharmacol 1991;43:457-64.

Shaik K, Shanmugam V, Angilicam A, Rao SS, Shaik K. Formulation and evaluation of famotidine buccal tablets. Int J Curr Pharm Res 2014;5:410-7.

Patel VM, Prajapati BG, Patel HV, Patel KM. Mucoadhesive bilayer tablets of propranolol hydrochloride. AAPS Pharm Sci Tech 2007;8:1 6.

Kumar BP, Kavitha P, Devi KJ. Formulation design and evaluation of mucoadhesive buccal tablets of nitroglycerin. Int J Pharm Pharm Sci 2014;6:251-9.

Nagaraju K, Velmurugan S, Deepika B, Vinushitha S. Formulation and in vitro evaluation of buccal tablets of metoprolol tartrate. Int J Pharm Pharm Sci 2011;3:239-46.

Patel VM, Prajapati BG. Design and in vitro characterization of Eudragit containing mucoadhesive buccal patches. Int J Pharma Pharm Sci 2011;3:783-9.

Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanism of solute release from porous hydro-matrices and other factors may be responsible. Int J Pharm 1983;15:25-35.