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.
The rationale of the current work was to evaluate antihypertensive activity ofTimolol maleate nanoparticles loaded transdermal patch. Nanoparticles loaded transdermal patch of timolol maleate was prepared using Compritol 888, Lutrol F68, tween 80 etc. The formulated patches were subjected to skin irritation study and in-vivo antihypertensive activity. Hypertension was induced by dexamethasone in experimental rats. No any marked skin irritation observed before and after applying the patch. Both systolic and diastolic blood pressure in experimental animals was reduced significantly after 7 days treatment with Timolol maleate nanoparticles loaded transdermal patch. So, it was concluded that timolol maleate patch could be formulated into a matrix-type naoparticle loaded transdermal patch for the management of hypertension. Also, this study can be considered as a new report that focuses on the problem of the side-effects associated with the modern medicaments toward hypertension
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