scholarly journals Development and Evaluation of Flupirtine Maleate Transdermal Patch Containing Different Permeation Enhancers

2021 ◽  
Vol 11 (5) ◽  
Keyword(s):  
Polyethylene Glycol ◽  
Polyvinyl Alcohol ◽  
Dimethyl Sulfoxide ◽  
Release Profile ◽  
Transdermal Patch ◽  
Permeation Enhancers ◽  
Peg 400 ◽  
Transdermal Patches ◽  
In Vitro Permeation

The present study was aimed at the formulation of transdermal patches of flupirtine maleate containing different permeation enhancers. It acts indirectly as N-methyl-D-aspartate (NMDA) receptor antagonist and activates the K+ channels; thereby acts as a skeletal muscle relaxant. Flupirtine maleate transdermal patches are intended to provide localized effect. The patches were prepared by solvent evaporation technique, using polyvinyl alcohol (PVA) as the polymer whereas dimethyl sulfoxide (DMSO) and polyethylene glycol (PEG-400) as the permeation enhancers. Methanol was used as a solvent to dissolve the drug and glycerol was used as the plasticizer. These patches were evaluated for in vitro permeation, tensile strength, percent moisture absorption, drug content uniformity, film thickness, weight variation and folding endurance. All the patches showed extended release properties. Formulation FDD8 containing 8% polymer and 2% DMSO was found to be the optimized formulation on the basis of evaluation parameters. In vitro permeation release was found to be 95.71 ± 0.01% at the end of 12 h. As the concentration of DMSO increased, the release profile of drug was enhanced. This indicated that DMSO improved the release profile of flupirtine maleate when compared to PEG-400. The release kinetics of the transdermal patches followed Higuchi matrix model. The stability studies showed that all the optimized patches were stable during their study period. From the present study, it can be concluded that addition of DMSO yields good result to enhance the permeation of the drug. Keywords: flupirtine maleate, transdermal patch, permeation enhancers, dimethyl sulfoxide DMSO, polyethylene glycol PEG-400, polyvinyl alcohol PVA.

scholarly journals EVALUASI IN VITRO-IN VIVO FILM TRANDERMAL DILTIAZEM HCL DENGAN PENINGKAT PENETRASI PEG 400 SEBAGAI ANTIHIPERTENSI

2019 ◽  
Vol 16 (01) ◽  
pp. 1
Author(s):  
Yulias Ninik Windriyati ◽  
Risha Fillah Fithria ◽  
Fitria Dwi Kurniawati ◽  
Ulfa Risalatul Mukaromah
Keyword(s):  
Blood Pressure ◽  
Physicochemical Characteristics ◽  
Penetration Enhancer ◽  
Transdermal Patch ◽  
In Vivo Evaluation ◽  
Peg 400 ◽  
Transdermal Patches ◽  
Diltiazem Hcl

ABSTRACTDiltiazem HCL is an antihypertensive that low oral bioavailability of 40%, so developed to transdermal preparations. A matrix type of transdermal patch of diltiazem HCl was prepared using polyvinyl alcohol and ethyl cellulose with PEG 400 as penetration enhancer. In vitro-in vivo evaluation were conducted to asses drug permeation through the skin and determine the effectiveness of transdermal film as an antihypertensive drug. Transdermal patches of diltiazem HCl were evaluated for physicochemical characteristics weight variation, thickness, folding endurance, moisture uptake, and drug content. In vitro permeation study was conducted using commercial semi permeable membrane in Franz diffusion cell. In vivo activity study was evaluated on male rat Wistar that induced NaCl with CODA non-invasive blood pressure method. Transdermal patches of diltiazem HCl were found no significant differences in terms of physicochemical characteristics. The in vitro skin permeation profiles showed increased flux values with the increase of PEG 400 as a penetration enhancer. The in vivo evaluation showed a reduction in systolic and diastolic blood pressure within one hour after the drug administration. Diltiazem HCl was able penetration into skin, absorbed in blood circulation and effective as antihypertensive via transdermal route.Keywords : antihypertension, diltiazem HCl, PEG 400, transdermal patch

scholarly journals Sustained Release of Linezolid from Prepared Hydrogels with Polyvinyl Alcohol and Aliphatic Dicarboxylic Acids of Variable Chain Lengths

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 982
Author(s):  
Gustavo Carreño ◽  
Adolfo Marican ◽  
Sekar Vijayakumar ◽  
Oscar Valdés ◽  
Gustavo Cabrera-Barjas ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Polyvinyl Alcohol ◽  
Sustained Release ◽  
Release Kinetics ◽  
Dicarboxylic Acids ◽  
Release Profile ◽  
Significant Activity ◽  
Crosslinking Degree ◽  
Aliphatic Dicarboxylic Acids

A series of hydrogels with a specific release profile of linezolid was successfully synthesized. The hydrogels were synthesized by cross-linking polyvinyl alcohol (PVA) and aliphatic dicarboxylic acids, which include succinic acid (SA), glutaric acid (GA), and adipic acid (AA). The three crosslinked hydrogels were prepared by esterification and characterized by equilibrium swelling ratio, infrared spectroscopy, thermogravimetric analysis, mechanical properties, and scanning electron microscopy. The release kinetics studies of the linezolid from prepared hydrogels were investigated by cumulative drug release and quantified by chromatographic techniques. Mathematical models were carried out to understand the behavior of the linezolid release. These data revealed that the sustained release of linezolid depends on the aliphatic dicarboxylic acid chain length, their polarity, as well as the hydrogel crosslinking degree and mechanical properties. The in vitro antibacterial assay of hydrogel formulations was assessed in an Enterococcus faecium bacterial strain, showing a significant activity over time. The antibacterial results were consistent with cumulative release assays. Thus, these results demonstrated that the aliphatic dicarboxylic acids used as crosslinkers in the PVA hydrogels were a determining factor in the antibiotic release profile.

scholarly journals Pengaruh Kombinasi Polimer Polivinil Pirolidon dan Etil Selulosa terhadap Karakteristik dan Uji Penetrasi Formulasi Transdermal Patch Ekstrak Bawang Dayak (Eleutherine palmifolia (L)

2021 ◽  
Vol 7 (1) ◽  
pp. 173-184
Author(s):  
Novia Novia ◽  
Noval Noval
Keyword(s):  
Active Substance ◽  
Ethyl Cellulose ◽  
Transdermal Patch ◽  
Onion Extract ◽  
Physical Evaluation ◽  
Transdermal Patches ◽  
Franz Diffusion Cells ◽  
Penetration Tests ◽  
Pvp K30

The transdermal patch can deliver the active substance with good bioavailability, then made formulations of such preparations from dayak onion extract, which has a compound content of flavonoids, with a combination of polymer PVP K30 and ethyl cellulose to produce transdermal patches with good physical evaluation and penetration. The research aims to carry out the effect and ideal formulation of transdermal patches of dayak onion extract with a combination of polymers PVP K30 and ethyl cellulose based on physical evaluation and penetration—manufacture of transdermal patches using the solvent evaporation method. Physical evaluation includes organoleptic testing, weight uniformity, thickness, folding resistance, and moisture testing. Then evaluate the penetration of the active substance using Franz diffusion cells. Analyze data with One Way ANOVA. The physical evaluation results of weight uniformity, patch thickness, folding resistance, and moisture test of transdermal patches on F1, F2, F3, and F4 meet the requirements. As for the results of penetration tests, F1, F2, F3, and F4 can be penetrated from 120 minutes to 180 minutes with the concentration of active substances that are linearly penetrated. The combination of polymers PVP K30 and ethylcellulose has affected the physical evaluation of transdermal patches of dayak onion extract. Based on the physical evaluation and penetration test in vitro obtained, the most optimal formula results are F3 with comparison PVP K30 and ethyl cellulose (100:300).

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN

2019 ◽  
pp. 317-323
Author(s):  
SHIKHA BAGHEL CHAUHAN ◽  
SUSHILA SAINI
Keyword(s):  
Moisture Absorption ◽  
Skin Permeation ◽  
Penetration Enhancers ◽  
Moisture Loss ◽  
Metoprolol Tartrate ◽  
Peg 400 ◽  
Transdermal Patches ◽  
Weight Variation ◽  
Basil Oil

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers. Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin. Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability. Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

scholarly journals COMPARISON OF EFFECT OF PENETRATION ENHANCER ON DIFFERENT POLYMERS FOR DRUG DELIVERY

2019 ◽  
Vol 11 (1) ◽  
pp. 89
Author(s):  
Bhawana Sethi ◽  
Rupa Mazumder
Keyword(s):  
Oleic Acid ◽  
Permeation Enhancers ◽  
In Vitro Drug Release ◽  
Franz Diffusion Cell ◽  
In Vitro Permeation ◽  
Treatment Of Hypertension ◽  
Permeation Studies ◽  
Evaporation Technique ◽  
Polymer Interaction

Objective: Aliskiren hemifumarate is used for the treatment of hypertension. The aim of this research to study the effect on the delivery of drug using natural and synthetic permeation enhancers like limonene, cineol, β-cyclodextrin, and oleic acid by using different polymers. As different penetration acts differently with polymers.Methods: Transdermal patches were prepared by the solvent evaporation technique. The controlled release polymers were used for the preparation of patches. The patches were prepared with different polymers and different plasticizer. The drug and polymer interaction study was performed by Fourier transform infrared spectra. In vitro permeation studies were conducted using pretreated cellophane membrane using franz diffusion cell. Results: The prepared patches were evaluated for in vitro drug release, and the release profile was varied from 52.32% PGH (oleic acid) to 87.63% B (cineol). The permeability coefficient was found in the range of 5.82 to 8.32 cm/h, and corresponding flux was found between 281.61 to 729.08 µg/cm2/h on the prepared patches and statistical analysis performed using t-test (p<0.005).Conclusion: On the basis of the obtained results, it was concluded that patch prepared using methocel k 15 m as a polymer, glycerin as plasticizer and cineol as a permeation enhancer shows the maximum release. The increase in the release due to increase in the flux.

scholarly journals Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1650
Author(s):  
Jun Soo Park ◽  
Jeong Soo Kim ◽  
Myoung Jin Ho ◽  
Dong Woo Park ◽  
Eun A. Kim ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Penetration Enhancers ◽  
Ambient Conditions ◽  
Permeation Enhancers ◽  
Drug Degradation ◽  
Franz Diffusion Cell ◽  
Promising Tool ◽  
In Vitro Permeation ◽  
Topical Solution

The incorporation of permeation enhancers in topical preparations has been recognized as a simple and valuable approach to improve the penetration of antifungal agents into toenails. In this study, to improve the toenail delivery of efinaconazole (EFN), a triazole derivative for onychomycosis treatment, topical solutions containing different penetration enhancers were designed, and the permeation profiles were evaluated using bovine hoof models. In an in vitro permeation study in a Franz diffusion cell, hydroalcoholic solutions (HSs) containing lipophilic enhancers, particularly prepared with propylene glycol dicaprylocaprate (Labrafac PG), had 41% higher penetration than the HS base. Moreover, the combination of hydroxypropyl-β-cyclodextrin with Labrafac PG further facilitated the penetration of EFN across the hoof membrane. In addition, this novel topical solution prepared with both lipophilic and hydrophilic enhancers was physicochemically stable, with no drug degradation under ambient conditions (25 °C, for 10 months). Therefore, this HS system can be a promising tool for enhancing the toenail permeability and therapeutic efficacy of EFN.

scholarly journals In vitro evaluation of Transdermal Patch of Palonosetron for Antiemetic Therapy

2018 ◽  
Vol 9 (4) ◽  
pp. 119 ◽  
Author(s):  
Atul Tripathi ◽  
Piyush Tyagi ◽  
Amber Vyas ◽  
Beena Gidwani ◽  
Amol Chandekar ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Antiemetic Therapy ◽  
Transdermal Patch ◽  
Barrier Membrane ◽  
Permeation Study ◽  
In Vitro Permeation

<p>Skin is one of the routes for systemic delivery of drugs through various drug delivery system. A transdermal Drug Delivery System (TDDS) is one of the most reliable and useful system to deliver drug systemically through skin. Generally medicated patch is placed on skin for delivery of medication through it into the blood stream. The aim of present study was to formulate and evaluate Palonosetron transdermal patch in vitro that could be used for antiemetic therapy. The incorporation ofPalonosetron a serotonin 5-HT<sub>3</sub> antagonist drug was envisaged. The TDDS was prepared by solvent evaporation technique and was evaluated for organoleptic characteristics and other physicochemical properties Thickness, Weight variation, Drug content uniformity, Tensile strength, % Elongation, Folding endurance &amp; Moisture content. The in vitro permeation study of the patch was carried out through KesaryChein diffusion cell as barrier membrane. Phosphate buffer pH 7.4 was used as dissolution medium and the temperature was maintained at 37 ± 1<sup>0</sup>C. The in vitro permeation study of the prepared patch indicated a time dependent increase in drug release throughout the study. The percentage of cumulative drug release was found to be 76.25% in 24 hours.The study shows a new approach to work in with Palonosetron.<strong></strong></p>

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