OPTIMIZATION AND PREPARATION OF SOLID LIPID NANOPARTICLE INCORPORATED TRANSDERMAL PATCH OF TIMOLOL MALEATE USING FACTORIAL DESIGN
Keywords:Transdermal Patch, Optimization, Drug release, Tensile strength, ANOVA
Objective: Transdermal patch of timolol maleate was prepared in order to increase the permeability of the drug topically.
Methods: The timolol maleate (TM) loaded solid lipid nanoparticles (SLN) were prepared by the solvent evaporation method. For the optimization process full factorial (three-factor and three-level), hydroxypropyl methylcellulose (HPMC) range from 100 to 300 mg, ethylcellulose 100 to 200 gm and almond oil 3 to 4 ml. The response noted in form of tensile strength and percent drug release. These transdermal patches were evaluated for physical characterization like weight variation, thickness, percentage moisture absorption, percentage moisture loss, water vapor transmission rate, folding endurance, tensile strength, and content uniformity.
Results: Solid lipid nanoparticles of TM were optimized and prepared, the data presented that drug release percent ranged from 66.12 to 91.75. 2FI model was observed to fit for response % drug permeation with a p and F value of 0.0271 and 4.50. The tensile strength varies from 0.358 to 0.508. The linear model was observed to fit for the tensile strength response with a p-value and F-value of<0.0001 and 52.41.
Conclusion: The controlled release formulation of Timolol Maleate was successfully optimized and prepared, a study conducted to investigate the effect of different polymers and type of permeation time profiles from Timolol Maleate patches.
Strasser T. Addressing the entire risk profile. J Hum Hypertens 1990;4:51-3.
Kannel WB. Blood pressure as a cardiovascular risk factor: prevention and treatment. JAMA 1996;275:1571-6.
Lalji V, Gupta MM. Oral disintegrating tablet of antihypertensive drug. J Drug Delivery Ther 2013;3:85-92.
Peto R, Darby S, Deo SH, Silcocks P, Whitley E, Doll R. Smoking, smoking cessation, and lung cancer in the UK since 1950: combination of national statistics with two case-control studies. Br Med J 2000;321:323-9.
Kreatsoulas C, Anand SS. The impact of social determinants on cardiovascular disease. Can J Cardiol 2010;26:8C-13C.
Staessen JA, Fagard R, Thijs L, Celis H, Arabidze GG, Birkenhäger WH, et al. Randomised double-blind comparison of placebo and active treatment for older patients with isolated systolic hypertension. Lancet 1997;350:757-64.
Gillman MW, Kannel WB, Belanger A, D'Agostino RB. Influence of heart rate on mortality among persons with hypertension: the framingham study. Am Heart J 1993;125:1148-54.
Jong WHD, Borm PAJ. Drug delivery and nanoparticles: applications and hazards. Int J Nanomed 2008;3:133-49.
Kumar P. Solid lipid nanoparticles incorporated cream of clobetasol-17-propionate: development and in vitro evaluation. Int J Pharm Sci Res 2018;9:5444-8.
Anitha P, Ramkanth S, Saleem MT, Umasankari K, Reddy BP, Chetty M. Preparation, in vitro and in vivo characterization of transdermal patch containing glibenclamide and atenolol: a combinational approach. Pak J Pharm Sci 2011;24:155-63.
Ren C, Fang L, Ling L, Wang Q, Liu S, Zhao L, et al. Design and in vivo evaluation of an indapamide transdermal patch. Int J Pharm 2009;370:129-35.
Nesseem DI, Eid SF, El-Houseny SS. Development of novel transdermal self-adhesive films for tenoxicam, an anti-inflammatory drug. Life Sci 2011;89:430-8.
Saoji SD, Atram SC, Dhore PW, Deole PS, Raut NA, Dave VS. Influence of the component excipients on the quality and functionality of a transdermal film formulation. AAPS PharmSciTech 2015;16:1344-56.
Ahmed TA, Khalid M. Transdermal film-loaded finasteride microplates to enhance drug skin permeation: two-step optimization study. Eur J Pharm Sci 2016;88:246-56.
Kumar M, Trivedi V, Shukla AK, Dev SK. Effect of polymers on the physicochemical and drug release properties of transdermal patches of atenolol. Int J Appl Pharm 2018;10:68-3.
Fayez SM, Shadeed SG, Khafagy E-sayed A, Jaleel GAA, Ghorab MM, El-nahhas SA. Formulation and evaluation of etodolac lecithin organogel transdermal delivery systems. Int J Pharm Pharm Sci 2015;7:325-34.
Suksaeree J, Monton C, Charoonratana T. Morphology study of plai patch by the scanning electron microscope. Part I: chitosan and hydroxypropylmethylcellulose blends. Int J Pharm Pharm Sci 2014;6:576-7.
Jalhan S, Kaur K, Kaur P, K Jain U. Formulation and in vitro evaluation of transdermal matrix patches of doxophylline. Asian J Pharm Clin Res 2016;9:140-5.
Kibria G, Roni MA, Absar MS, Jalil RU. Effect of plasticizer on the release kinetics of diclofenac sodium pellets coated with Eudragit RS 30 D. AAPS PharmSciTech 2008;9:1240-6.