The present experimental study aimed to design, develop, evaluate and optimize the buccal patch formulations of Venlafaxine hydrochloride using hydrophilic and hydrophobic polymers, having different concentrations. Venlafaxine hydrochloride is an antidepressant with a high first-pass metabolism and a low oral bioavailability of 40%. To increase the bioavailability and to reduce the dosing frequency of the drug, an attempt was made by formulating mucoadhesive patches of Venlafaxine Hydrochloride for buccal delivery. An Optimized buccal patch formulation was prepared by the solvent casting method. Eudragit RS-100 polymer was used as film forming polymer while HPMC E-15 was incorporated to provide the patches with bioadhesive properties and to modify the rate of drug release. A 32 full factorial design was employed to design batches of the formulation. The concentration of Eudragit RS 100 and HPMC E15 was selected as two independent variables while cumulative percent drug release was a dependent variable. Prepared batches of formulation were evaluated for content uniformity, thickness, weight variation, swelling index, surface pH, tensile strength, elongation at break, mucoadhesive strength, mucoadhesion time, in vitro drug release, etc. The optimized batch of the buccal patch has a drug release of 95.29 ± 0.42 %, an ex–vivo residence period of 3782.51 minutes, and a content uniformity of 97.96 0.17 percent to 103.24 0.48 percent. The ex–vivo residence time ranged from 378 ± 2.51 min to 470 ± 2.08 min. Mucoadhesive strength and swelling index were directly proportional to the concentration of hydrophilic polymer. The study suggested that the buccal patch significantly enhanced the bioavailability of Venlafaxine hydrochloride and modified the drug release.
Al-Mogherah AI, Ibrahim MA, Hassan MA. Optimization and evaluation of venlafaxine hydrochloride fast dissolving oral films. Saudi Pharm J. 2020 Nov 1;28(11):1374-82. doi: 10.1016/j.jsps.2020.09.001, PMID 33250644.
Kaur A, Kaur G, Kaur G. Mucoadhesive buccal patches based on interpolymer complexes of chitosan–pectin for delivery of carvedilol. Saudi Pharm J. 2012 Jan 1;20(1):21-7. doi: 10.1016/j.jsps.2011.04.005, PMID 23960773.
Ajeet SB, Juneja R. Recent findings in concern to buccal patches: a review. Int J Curr Pharm Res. 2012;4(1):12-7.
Yamsani MR, Kishan V, Yasmani MR. Development of mucoadhesive patches for buccal administration of prochlorperazine: evaluation of in vitro release and mechanical properties. Int. PharmSci Nanotechnol. 2008;1:64-70. doi: 10.37285/10.37285/ijpsn.2008.1.1.5.
Swain S, Behera A, Dinda SC, Patra CN, Jammula S, Beg S, Rao ME. Formulation design, optimization and pharmacodynamic evaluation of sustained release mucoadhesive microcapsules of venlafaxine HCl. Indian J Pharm Sci. 2014 Jul;76(4):354-63. PMID 25284934. -. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4171873/.
Liu Y, Sun Y, Sun J, Zhao N, Sun M, He Z. Preparation and in vitro/in vivo evaluation of sustained-release venlafaxine hydrochloride pellets. Int J Pharm. 2012 Apr 15;426(1-2):21-8. doi: 10.1016/j.ijpharm.2011.12.053, PMID 22266529.
Choudhary A, Tiwari G, Pandey M, Kymonil KM, Saraf SA. Formulation and characterization of carvedilol buccal mucoadhesive patches. Int J Res Pharm Sci. 2010;1(4):396-401.
Morales JO, McConville JT. Manufacture and characterization of mucoadhesive buccal films. Eur J Pharm Biopharm. 2011 Feb 1;77(2):187-99. doi: 10.1016/j.ejpb.2010.11.023, PMID 21130875.
Yadav VK, Gupta AB, Kumar R, Yadav JS, Kumar B. Mucoadhesive polymers: means of improving the mucoadhesive properties of drug delivery system. J Chem Pharm Res. 2010;2(5):418-32.
Sam AP, Van den Heuij JTM, Tukker JJ. Mucoadhesion of both film-forming and non-film -forming polymeric materials as evaluated with the Wilhelmy plate method. Int J Pharm. 1992 Feb 1;79(1-3):97-105. doi: 10.1016/0378-5173(92)90100-G.
Yadav AV, Urade MN. Preparation and evaluation of chitosan containing mucoadhesive buccal films of venlafaxine hydrochloride. Res J Pharm Technol. 2010 Dec 28;3:1213-7.
Raza SN, Kar AH, Wani TU, Khan NA. Formulation and evaluation of mouth dissolving films of losartan potassium using 32 factorial design. Int J Pharm Sci Res. 2019;10(3):1402-11. doi: 10.13040/IJPSR.0975-8232.10(3).1402-11.
Hardenia S, Darwhekar G. Formulation and optimization of fast dissolving tablets of promethazine theoclate using 32 factorial design. J Drug Deliv Ther. 2017 Dec 21;7(7):12-4. doi: 10.22270/jddt.v7i7.1571.
Senthil A, Chauhan N, Siroya R, Patel J, Vantoor N. Formulation and evaluation of venlafaxine hydrochloride buccal patch. Int Res J Pharm. 2012;3(3):282-6.
Choudhury A, Das S, Dhangar S, Kapasiya S, Kanango A. Development and characterization buccoadhesive film of ciprofloxacin hydrochloride. Int J Pharm Tech Res. 2010 Apr;2(2):1050-7.
Khairnar A, Jain P, Baviskar D, Jain D. Developmement of mucoadhesive buccal patch containing aceclofenac: in vitro evaluations. Int. J. Pharmtech Res.2009 Oct;1(4):978-81.
Gupta B, Chaurasia U, Chakraborty P. Design and development of oral transmucosal film for delivery of salbutamol sulphate. J Pharm Chem Biol Sci. 2014;2(2):118-29.
Patel VM, Prajapati BG, Patel MM. Effect of hydrophilic polymers on buccoadhesive Eudragit patches of propranolol hydrochloride using factorial design. AAPS PharmSciTech. 2007 Jun;8(2):Article 45. doi: 10.1208/pt0802045, PMID 17622120.
Peh KK, Wong CF. Polymeric films as vehicle for buccal delivery: swelling, mechanical, and bioadhesive properties. J Pharm Pharm Sci. 1999 Aug;2(2):53-61. PMID 10952770.
Ikram M, Gilhotra N, Gilhotra RM. Formulation and optimization of mucoadhesive buccal patches of losartan potassium by using response surface methodology. Adv Biomed Res. 2015 Jan 1;4(1):239. doi: 10.4103/2277-9175.168606, PMID 26682205.
Asif HM, Rao TR, Ayesha N, Anjum M, Rahman MA. Design and evaluation of mucoadhesive buccal patches of venlafaxine. J Pharm Res Int. 2015 Feb 23;6(2):96-106. doi: 10.9734/BJPR/2015/12637.
Alagusundaram M, Chengaiah B, Ramkanth S, Parameswari SA, Chetty CM, Dhachinamoorthi D. Formulation and evaluation of mucoadhesive buccal films of ranitidine. Int J PharmTech Res. 2009 Jul;1(3):557-63.
Lohani A, Prasad N, Arya RK. Formulation and characterization of mucoadhesive buccal films of ranitidine hydrochloride. Int J Pharm Sci Res. 2011 Sep 1;2(9):2457.
Al-Mogherah AI, Ibrahim MA, Hassan MA. Optimization and evaluation of venlafaxine hydrochloride fast dissolving oral films. Saudi Pharm J. 2020 Nov;28(11):1374-82. doi: 10.1016/j.jsps.2020.09.001, PMID 33250644.
Deshmane SV, Channawar MA, Chandewar AV, Joshi UM, Biyani KR. Chitosan based sustained release mucoadhesive buccal patches containing verapamil HCl. Int J Pharm Pharm Sci. 2009 Nov;1(1):216-29.
Senthilnathan B, Rupenagunta A. Formulation development and evaluation of venlafaxine hydrochloride orodispersible tablets. Int J Pharm Sci Res. 2011 Apr 1;2(4):913.
Galkina MA, Galkin OM, Kochetkov KA. Crystallization and quality examination of pharmaceutical substance venlafaxine. Pharm Chem J. 2012 Apr 1;46(1):60-3. doi: 10.1007/s11094-012-0734-z.
