A Novel Vesicular Approach for Transdermal Administration of Enalapril Maleate Loaded Nanoproniosomal Gel: Formulation, Ex Vivo Evaluation and in Vivo Antihypertensive Study

Abstract

Objective: The objective of the study was to formulate and evaluate the nanoproniosomal gel of Enalapril maleate (EM) for the treatment of hypertension through the transdermal administration and to provide better bioavailability.
 Methods: The nanoproniosomal gel of the EM was formulated by Lecithin, Cholesterol, Non-ionic surfactants using the Coacervation-phase separation method. The prepared nanoproniosomal gels were evaluated for pH and viscosity, vesicle size analysis, rate of spontaneity, entrapment efficiency, zeta potential, ex vivo skin permeation studies, skin irritation test, stability studies and in vivo antihypertensive studies.
 Results: Physical characterization was found to be within acceptable limits. The ex vivo skin permeation studies showed the cumulative permeation of 58.75 % to 89.72 % through the albino rat skin in 24 h for all the formulations, which indicate the zero-order drug permeation with diffusion, non-fickian release. Among all formulations, EMNP7 was selected as best formulation because it showed better characteristics than other formulations in several aspects like physicochemical characterization, ex vivo skin permeation studies, permeation kinetics, and other evaluation parameters. The skin irritation study revealed that there was no irritation after topical application and it was found to be safer to use. The In vivo antihypertensive study revealed that the formulation of EMNP7 was successful to regress the rat blood pressure (BP) to normal values in experimental hypertensive rats.
 Conclusion: The nanoproniosomal gel is an efficient transdermal therapeutic system for the delivery of EM for the treatment of hypertension. It is suitable for once a day controlled release formulation.

Proniosomal Gel Mediated Transdermal Delivery of Glibenclamide and Atenolol Combination: Exvivo and Pharmacodynamic Studies

“…According to the Korsmeyer-peppas model, the calculated n-values were greater than 0.45 but less than 0.89, indicating non-Fickian or anomalous release, which refers to a combination of both diffusion and erosion controlled-drug release mechanism. These results are in good agreement with previous work for a combination of drugs that have been loaded with a transdermal delivery system [45,48].…”

“…An adhesive tape was rolled over the gel formulation to fix it securely to the site of application. SBP levels were measured just before and at 0, 2, 4, 6, 8, 12, and 24h using the tail-cuff system [44,45].…”

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“…Gellan was attributed as a consequence of increasing the chain interaction with polymer concentration. [24,25] The solution to gel time…”

Test title

“…In vitro studies helps in identifying the mechanism of skin permeation of the drug and later it can be formulated into a transdermal therapeutic system [9].…”