Design and Development of Propranolol Hydrochloride Transdermal Patches: In Vitro and Ex Vivo Characterization

2020 ◽  
Vol 3 (1) ◽  
pp. 01-08
Author(s):  
Chinthakindi Shravya
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Diffusion Mechanism ◽  
Propranolol Hydrochloride ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Percent Moisture

The main aim of this investigation is to design and develop matrix type transdermal patches of Propranolol Hydrochloride which is an anti-hypertensive drug. These matrix type transdermal patches were prepared by “Solvent Casting Technique” using drug, HPMC E15 and Eudragit L 100 in the ratio of 1:6, 1:6.5, 1:7, 1:7.5, 1:8, 1:8.5, 1:9, 1:9.5. All formulations carried 20%v/w of PEG-600 as plasticizer. The prepared patches were characterized for various physicochemical parameters like weight, thickness, folding endurance, drug content, percent moisture content, percent moisture absorption, in vitro drug release and ex vivo permeation. Among this 1:9 ratio was found to be an Optimized formulation and patches were prepared by using permeation enhancers (lemon grass oil, Eucalyptus oil, and clove oil). The cumulative amount of drug release in 12hrs for F7 formulation showed maximum and used for that formulation skin permeation on Goat abdominal skin. FTIR studies show no interaction between drug, polymer and other excipients. The drug permeation kinetics followed “First order” and “zero order” profile with diffusion mechanism.

scholarly journals Formulation and Evaluation of Matrix Type Transdermal Patches of Glibenclamide

2009 ◽  
Vol 1 (01) ◽  
Author(s):  
J. R. D. Gupta ◽  
R. Irchhiaya ◽  
N. Garud ◽  
Priyanka Tripathi ◽  
Prashant Dubey ◽  
...  
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Skin Permeation ◽  
Moisture Loss ◽  
In Vitro Drug Release ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Weight Variation ◽  
Cumulative Amount

Matrix type transdermal patches containing Glibenclamide were prepared using three different polymers by solvent evaporation technique. Aluminium foil cup method was used as a substrate. Polyethylene glycol (PEG) 400 was used as plasticizer and Dimethyl sulfoxide (DMSO) was used as penetration enhancer. The physicochemical parameters like weight variation, thickness, folding endurance, drug content, % moisture absorption and % moisture loss were evaluated. In vitro drug release studies and skin permeation studies were carried out using Franz diffusion cell. Cumulative amount of drug released in 12 hours from the six formulations were 55.467, 52.633, 47.157, 53.394, 49.139 and 45.597 %, respectively. The corresponding values for cumulative amount of drug permeated for the said formulation were 43.013, 40.429, 37.793, 41.522, 37.450 and 34.656 %, respectively. On the basis of in vitro drug release and skin permeation performance, formulation HP-1 was found to be better than other formulations and it was selected as the optimized formulation.

scholarly journals Ethyl Cellulose and Hydroxypropyl Methyl Cellulose Blended Methotrexate-Loaded Transdermal Patches: In Vitro and Ex Vivo

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3455
Author(s):  
Muhammad Shahid Latif ◽  
Abul Kalam Azad ◽  
Asif Nawaz ◽  
Sheikh Abdur Rashid ◽  
Md. Habibur Rahman ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Transdermal Patches ◽  
Percent Moisture ◽  
Vitro Release

Transdermal drug delivery systems (TDDSs) have become innovative, fascinating drug delivery methods intended for skin application to achieve systemic effects. TDDSs overcome the drawbacks associated with oral and parenteral routes of drug administration. The current investigation aimed to design, evaluate and optimize methotrexate (MTX)-loaded transdermal-type patches having ethyl cellulose (EC) and hydroxypropyl methyl cellulose (HPMC) at different concentrations for the local management of psoriasis. In vitro release and ex vivo permeation studies were carried out for the formulated patches. Various formulations (F1–F9) were developed using different concentrations of HPMC and EC. The F1 formulation having a 1:1 polymer concentration ratio served as the control formulation. ATR–FTIR analysis was performed to study drug–polymer interactions, and it was found that the drug and polymers were compatible with each other. The formulated patches were further investigated for their physicochemical parameters, in vitro release and ex vivo diffusion characteristics. Different parameters, such as surface pH, physical appearance, thickness, weight uniformity, percent moisture absorption, percent moisture loss, folding endurance, skin irritation, stability and drug content uniformity, were studied. From the hydrophilic mixture, it was observed that viscosity has a direct influence on drug release. Among all formulated patches, the F5 formulation exhibited 82.71% drug release in a sustained-release fashion and followed an anomalous non-Fickian diffusion. The permeation data of the F5 formulation exhibited about a 36.55% cumulative amount of percent drug permeated. The skin showed high retention for the F5 formulation (15.1%). The stability study indicated that all prepared formulations had very good stability for a period of 180 days. Therefore, it was concluded from the present study that methotrexate-loaded transdermal patches with EC and HPMC as polymers at different concentrations suit TDDSs ideally and improve patient compliance for the local management of psoriasis.

scholarly journals DESIGN, FORMULATION AND IN VITRO DRUG RELEASE FROM TRANSDERMAL PATCHES CONTAINING IMIPRAMINE HYDROCHLORIDE AS MODEL DRUG

2017 ◽  
Vol 9 (6) ◽  
pp. 220 ◽  
Author(s):  
Swati Hardainiyan ◽  
Krishan Kumar ◽  
Bankim Chandra Nandy ◽  
Richa Saxena
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Skin Permeation ◽  
Solvent Evaporation ◽  
Hydrophilic Polymer ◽  
In Vitro Drug Release ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Imipramine Hydrochloride

Objective: The aim of the present investigation was to form matrix type transdermal patches containing imipramine hydrochloride were prepared using two polymers by solvent evaporation technique to minimise the dose of the drug for lesser side effect and increase the bioavailability of a drug.Methods: In the present study, drug loaded matrix type transdermal films of imipramine hydrochloride were prepared by the solvent evaporation method with the help of polymers along with polyethene glycol (PEG) 400 was used as plasticizer and dimethyl sulfoxide (DMSO) was used as penetration enhancer. Drug-polymer interactions determine by FTIR and a standard calibration curve of imipramine hydrochloride was determined by using UV estimation.Results: The formulated transdermal patch by using PVP K-30, HPMC K100M showed good physical properties. All prepared formulations indicated good physical stability. The formulation F-1 gave the most suitable transdermal film with all desirable physicochemical properties. The thickness of the patches was varied from 0.263±0.67 mm to 0.301±0.61 mm, uniformity of patches showed that patches prepared by solvent evaporation while low standard deviation values ensued by thickness measurements of the film, and weights ranged between 50.5±0.75 mg and 52.15±2.15 mg, which indicates that different batches patch weights, were comparatively similar. Folding endurance was found to be>200 that is satisfactory for the patches, drug content was found to be 5.33±0.14 mg to 5.57±0.095 mg. In vitro, drug permeation studies of formulations were performed by using K-C diffusion cells using abdomen skin of the albino rat. The results were best in in-vitro skin permeation through rat skin as compared to all other formulations prepared with a hydrophilic polymer containing permeation enhancer. The formulation, F1 is considered as the best formulation, since it shows maximum in vitro drug release as 84.71±3.07 % at 24 h. The drug release kinetics studies showed that the majority of formulations were governed by Higuchi model and mechanism of release was non-Fickian mediated.Conclusion: In conclusion, controlled release transdermal drug delivery system (TDDS) patches of imipramine hydrochloride can be prepared using the polymer combinations, with plasticizer and enhancer. The release rate of drug through patched increased simultaneously as the concentration of hydrophilic polymer was increased. However, the mechanism of drug release of all formulations was non-Fickian. The properties of a film did not change during the period of study.

scholarly journals DESIGN AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PHENFORMIN HYDROCHLORIDE

2017 ◽  
Vol 9 (6) ◽  
pp. 90
Author(s):  
Pratik Swarup Das ◽  
Puja Saha
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Chemical Properties ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Transdermal Patches ◽  
The Matrix

Objective: In present work was designed to develop suitable transdermal matrix patches of Phenformin hydrochloride using various hydrophilic (HPMC) and hydrophobic (EUDRAGID) polymers as matrix formers.Methods: Transdermal patches containing Phenformin hydrochloride were prepared by the solvent casting evaporation technique.Results: Revealed that prepared patches showed good physical characteristics, no drug-polymer interaction and no skin irritation was observed. The in vitro release study revealed that F3 formulation showed maximum release in 24 h. Formulation F3 was subjected for accelerated stability studies. The F3 formulation was found to be stable as there was no drastic change in the Physico-chemical properties of the patches, which was also confirmed by FTIR.Conclusion: Thus conclusion can be made that stable transdermal patches of Phenformin hydrochloride has been developed. F1, F2, F3, F4 formulations showed highest cumulative percentage drug release of 98.13%, 95.50%, 98.65%, 97.21% were obtained during in vitro drug release studies after 24 h. The release of Phenformin hydrochloride appears to be dependent on lipophilicity of the matrix. Moderately lipophillic matrices showed best release. The predominant release mechanism of drug through the fabricated matrices was believed to be by diffusion mechanism. Based upon the in vitro dissolution data the F3 formulation was concluded as optimized formulation.

scholarly journals DEVELOPMENT AND EVALUATION OF TRANSDERMAL FILM CONTAINING SOLID LIPID NANOPARTICLES OF RIVASTIGMINE TARTRATE

2017 ◽  
Vol 9 (6) ◽  
pp. 85
Author(s):  
G. Ravi ◽  
N. Vishal Gupta
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Cost Effective ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Study Results ◽  
Transdermal Film

Objective: The objective of present investigation was to develop rivastigmine tartrate transdermal film employing factorial design.Methods: The formulations were designed by Design-Expert software-version10. A series of films were prepared by solvent casting method using polymers, plasticizer, permeation enhancer and other solvents. Transdermal films were evaluated for flatness, drug content, tensile strength, in vitro drug release and ex vivo skin permeation study.Results: The flatness was found 100% (percentage) for all film formulations. The drug content of transdermal film was found in the range of 96.51±0.2 to 98.81±0.3%. The tensile strength of transdermal film was found in the range of 6.28±0.06 to 11.56±0.03 N/mm2 (newton/millimeter2) and in vitro drug release at 24th h (hour) was found in the range of 86.24±0.25 to 96.1±0.48%% for various formulations and ex vivo skin permeation study results at 24th h was found in the range of 85.83±0.74 to 97.36±0.93%.Conclusion: These results support the feasibility of developing transdermal film of rivastigmine tartrate for human applications. Thus, transdermal delivery of rivastigmine tartrate film is a safe, painless and cost effective drug delivery system for Alzheimer’s patients.

Development of Acrylic Matrix Type Ketoprofen Patch

2012 ◽  
Vol 506 ◽  
pp. 533-536
Author(s):  
Nanthida Wonglertnirant ◽  
S. Tipwichai ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Suwannee Panomsuk ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Pressure Sensitive Adhesive ◽  
Drug Release Rate ◽  
Matrix Type ◽  
Adhesive Matrix ◽  
Pressure Sensitive ◽  
Transdermal Patches ◽  
Significant Difference

Ketoprofen transdermal patches (KTPs) were fabricated using an acrylic pressure sensitive adhesive (PSA) polymer. The influence of different factors (amount of PSA, drug content, and pressure applying on the backing membrane during preparation) on the characteristics of ketoprofen patch (thickness, W/A ratio, and adhesiveness of matrix film) and in vitro drug release behavior were investigated. The results revealed the successful fabrication and a good physical appearance of KTPs using acrylic PSA. Microscopic observations, FTIR spectra, and DSC thermograms were permitted to demonstrate that the drug was dispersed molecularly in the polymer. As the amount of PSA in the adhesive matrix was increased, the release rate of ketoprofen was decreased. Contrarily, the drug release rate was increased corresponding to the increase of ketoprofen content in the adhesive matrix. There was no significant difference in the release rate when the pressure applying on the backing membrane was varied. The kinetic of ketoprofen release from acrylic matrix type transdermal patches followed the Higuchis diffusion model.

scholarly journals Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1218
Author(s):  
Mohammad A. Altamimi ◽  
Afzal Hussain ◽  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Usamah Abdulrahman Alnemer
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Oral Drug ◽  
In Vitro Drug Release ◽  
Drug Deposition ◽  
Drug Content

Introduction: Luteolin (LUT) is natural flavonoid with multiple therapeutic potentials and is explored for transdermal delivery using a nanocarrier system. LUT loaded cationic nanoemulsions (CNE1–CNE9) using bergamot oil (BO) were developed, optimized, and characterized in terms of in vitro and ex vivo parameters for improved permeation. Materials and methods: The solubility study of LUT was carried out in selected excipients, namely BO, cremophor EL (CEL as surfactant), labrasol (LAB), and oleylamine (OA as cationic charge inducer). Formulations were characterized with globular size, polydispersity index (PDI), zeta potential, pH, and thermodynamic stability studies. The optimized formulation (CNE4) was selected for comparative investigations (% transmittance as %T, morphology, chemical compatibility, drug content, in vitro % drug release, ex vivo skin permeation, and drug deposition, DD) against ANE4 (anionic nanoemulsion for comparison) and drug suspension (DS). Results: Formulations such as CNE1–CNE9 and ANE4 (except CNE6 and CNE8) were found to be stable. The optimized CNE4 based on the lowest value of globular size (112 nm), minimum PDI (0.15), and optimum zeta potential (+26 mV) was selected for comparative assessment against ANE4 and DS. The %T values of CNE1–CNE9 were found to be ˃95% and CEL content slightly improved the %T value. The spherical CNE4 was compatible with excipients and showed % total drug content in the range of 97.9–99.7%. In vitro drug release values from CNE4 and ANE4 were significantly higher than DS. Moreover, permeation flux (138.82 ± 8.4 µg/cm2·h), enhancement ratio (8.23), and DD (10.98%) were remarkably higher than DS. Thus, ex vivo parameters were relatively high as compared to DS which may be attributed to nanonization, surfactant-mediated reversible changes in skin lipid matrix, and electrostatic interaction of nanoglobules with the cellular surface. Conclusion: Transdermal delivery of LUT can be a suitable alternative to oral drug delivery for augmented skin permeation and drug deposition.

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 Comparative study for optimization of folic acid nanoparticles

2020 ◽  
Vol 10 (2) ◽  
pp. 5156-5160
Keyword(s):  
Drug Release ◽  
Comparative Study ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Liquid Paraffin ◽  
Amorphous Structure ◽  
Long Term Stability ◽  
Refrigerator Temperature ◽  
The Stability

The present comparative study aims at studying the effect of several adjuvents on enhancing the stability and sustainability of FA NLCs which previously showed very promising results. The problem was encountered in the high drug release, high skin permeation, low deposition and low stability. In the present study, propylene glycol was added to all preparations as a stabilizer and coemulsifier. Plurol® stearique was utilized as solid lipid and stabilizer instead of apifil®. Soft paraffin was used as a softening additional lipid to Plurol® stearique to ensure the amorphous structure of NLCs. Liquid paraffin was used for its emollient effect instead of capryol ™ 90 with Apifil®. The in vitro drug release, ex vivo drug permeation and skin deposition were analyzed. Selection of the most optimum formulation is achieved to investigate its photostability, long term stability. Also, it was photographed under TEM. The selected formulation was stable after six hours of irradiation. The optimized selected formulation was successfully stable in refrigerator temperature throughout 9 months of the study. The TEM photograph reveals the formation of rounded nano vesicles. The present study was successful in development of more stable, more sustained means for topical delivery of FA for future cosmoceutical benefits.

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