Development, characterization &amp; invivo evaluation of proniosomal based transdermal delivery system of Atenolol

Ramkanth, S; Chetty, C. Madhusudhana; Sudhakar, Y.; Thiruvengadarajan, V. S.; Anitha, P.; Gopinath, Chakka

doi:10.1016/j.fjps.2017.10.003

Cited by 31 publications

(21 citation statements)

References 46 publications

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“…As shown in Figure 1(A), amount of surfactant has a positive significant effect on EE%, this could be justified by the more number of vesicles formed by the increased amount of surfactant (Thomas & Viswanad, 2012). Also, increasing the amount of surfactant leads to an increase in the hydrophobic domain, hence increases the entrapment of the drug (Ramkanth, 2018). However, further increase in surfactant amount showed a decrease in EE%, this could be due to the formation of mixed micelles together with niosomes, which may lead to lower EE% (Ramkanth, 2018).…”

Section: Resultsmentioning

confidence: 99%

“…Also, increasing the amount of surfactant leads to an increase in the hydrophobic domain, hence increases the entrapment of the drug (Ramkanth, 2018). However, further increase in surfactant amount showed a decrease in EE%, this could be due to the formation of mixed micelles together with niosomes, which may lead to lower EE% (Ramkanth, 2018). Figure 1(A) showed that increasing surfactant:cholesterol ratio leads to a decrease in EE%.…”

Section: Resultsmentioning

confidence: 99%

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Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

2019

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Brimonidine tartrate (BRT) is a hydrophilic a 2 adrenergic agonist used for the treatment of glaucoma. Glaucoma is an ocular disease affecting the anterior segment of the eye requiring lifetime treatment. Owing to the obstacles facing ocular delivery systems and hydrophilicity of BRT, frequent administration of the eye drops is required. Niosomes have been widely used to improve the ocular bioavailability of the topically applied drugs and to enhance the ocular residence time. However, they have drawbacks as physical instability, aggregation, and loss of the entrapped drug. For this reason, BRT proniosomes were prepared to overcome niosomal instability issues. A D-optimal design was utilized to determine the optimum conditions for preparation of the proniosomal gels. Independent variables were amount of surfactant, surfactant:cholesterol ratio, and type of surfactant used. The dependent variables were entrapment efficiency (EE%), particle size, percentage of drug released after 2 h (Q 2h), and percentage of drug released after 24 h (Q 24h). The optimum formula was suggested with desirability 0.732 and the composition of 540 mg Span 60 and 10:1 surfactant:cholesterol ratio. The results obtained after reconstitution were; EE% of 79.23 ± 1.12% particle size of 810.95 ± 16.758 nm, polydispersity index (PDI) 0.6785 ± 0.213, zeta potential 59.1 ± 0.99 mV, Q 2h 40.98 ± 1.29%, Q 8h 63.35 ± 6.07%, and Q 24h ¼ 91.11 ± 1.76%. Transmission electron microscope imaging of the formula showed the typical spherical shape of niosomes. In-vivo pharmacodynamic study assured the improved ocular bioavailability of BRT selected formula when compared with Alphagan V R P with relative AUC 0-24 of 5.024 and 7.90 folds increase in the mean residence time (MRT). Lack of ocular irritation of the formula was assured by Draize test.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

2019

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“…The composition of the proniosomal gel used as a vehicle for rutin was selected based on the results of the previously published studies [ 47 , 48 , 49 , 50 ]. The proniosomal gel contained 0.3% ( w/w ) rutin and excipients, as described in Table 1 .…”

Section: Discussionmentioning

confidence: 99%

Proniosomal Gel for Topical Delivery of Rutin: Preparation, Physicochemical Characterization and In Vitro Toxicological Profile Using 3D Reconstructed Human Epidermis Tissue and 2D Cells

et al. 2021

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Rutin (Rut) is a natural flavonol, well-known for its broad-spectrum of therapeutic effects, including antioxidant and antitumoral activities; still, it has a reduced clinical outcome due to its limited solubility in aqueous solutions. To overcome this drawback, this study proposes a novel formulation for rutin as a proniosomal gel for cutaneous applications. The gel was prepared by coacervation phase-separation method and complies with the standard requirements in terms of particle size (140.5 ± 2.56 nm), zeta potential (−27.33 ± 0.09 mV), encapsulation capacity (> 50%), pH (7.002 ± 0.18) and rheological properties. The results showed high biocompatibility of the gel on the 3D reconstructed human epidermis model characterized by increased viability of the cells and a lack of irritant and phototoxic potential. The evaluations on 2D cells confirm the preferential cytotoxic effect of Rut on melanoma cells (IC50 value = 8.601 µM, nuclear fragmentation) compared to normal keratinocytes. Our data suggest that the proniosomal gel is a promising drug carrier for Rut in the management and prevention of skin disorders.

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“…Then BP was determined from the rat tail at predetermined time intervals up to 24 h using the rat BP instrument (Biopac system, USA) and based on a non-invasive BP measuring method. The device consists of a scanner, a tail-cuff, an animal holder attached to the main instrument having a digital BP display panel [37][38][39].…”

Section: In Vivo Antihypertensive Studiesmentioning

confidence: 99%

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

2020

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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.

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Development, characterization & invivo evaluation of proniosomal based transdermal delivery system of Atenolol

Cited by 31 publications

References 46 publications

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

Proniosomal Gel for Topical Delivery of Rutin: Preparation, Physicochemical Characterization and In Vitro Toxicological Profile Using 3D Reconstructed Human Epidermis Tissue and 2D Cells

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

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