Evaluation Of Transdermal Patches Research Articles

Fabrication, Optimization, and Evaluation of Transdermal Patch: As an Alternative and Effective Transdermal Delivery System for Nebivolol HCl.

Nebivolol HCl is a unique third-generation beta blocker that has less oral bioavailability and exhibits various adverse effects like gastrointestinal disturbance and abdominal pain. This study aimed to formulate and evaluate nebivolol HCl transferosomal transdermal patches to reduce the problems associated with oral delivery of the drug and enhancement of drug permeation through the skin. Nebivolol HCl loaded transferosomes were prepared by thin film hydration method. Eight formulations were prepared based on the two independent variables, type of surfactant (Tween 80 and Span 80) and Phospholipid: Edge activator ratio and were evaluated for their vesicle size, PDI, and entrapment efficiency. The optimized formulations were incorporated into transdermal patches, which were evaluated for physicochemical properties, in-vitro and ex-vivo permeation, skin irritancy, and stability studies. The vesicle size of the transferosomes ranged from 49nm to 93nm, and EE% varied from 39% to 79%. Vesicles formed with Span 80 as an edge activator showed smaller vesicle size and greater EE% as compared to Tween 80. Based on the results, TW4 and SP4 were selected as the optimized formulations for further incorporation into the transdermal patches. In-vitro and ex-vivo permeation studies showed permeation in the order F2 > F3 > F1, indicating that transferosomal formulations showed superior permeation of the drug compared to plain Nebivolol HCl patches. Span 80 transferosomes showed a slightly better permeation than Tween 80. Stability studies showed that transferosomes and the transdermal patches demonstrated good stability under proper storage conditions. The study concluded that transferosomal patches of Nebivolol HCl could be used as a potential approach with effective transdermal delivery for the management of hypertension.

Formulation and Evaluation of Febuxostat Transdermal Patch for Management of Gout

The present research was aimed to formulate a soft and easy to handle transdermal patch consisting simple and cost effective monolithic polymeric film as an attempt to deliver Febuxostat transdermallyand overcome problems associated with its poor bioavailability and hepatic first pass metabolism. Transdermal patches of Febuxostat were prepared by solvent casting method. Prepared formulations were evaluated for various parameters tensile strength, thickness, folding endurance, % moisture content, % moisture uptake, % drug content, % elongation, In vitro drug release. Based on the evaluation of transdermal patches, concluded that the concept of transdermal drug delivery is a novel, nontoxic as well cost-effective technique for enhancing the aqueous solubility and bioavailability of the drug. It can be concluded that transdermal drug delivery works very simple in which drug is applied inside the patch and it is worn on skin for long period of time. By this constant concentration of drug remain in blood for long time. Thus, overcome the adverse effects caused by oral route.

Formulation and Evaluation of Transdermal Patches Containing BGP-15.

BGP-15 is an active ingredient with many advantages, e.g., beneficial cardiovascular and anti-inflammatory effects. The transdermal administration of BGP-15 has great potential, which has not been investigated yet, despite the fact that it is a non-invasive and safe form of treatment. The aim of our study was to formulate transdermal patches containing BGP-15 and optimize the production with the Box-Behnken design of experiment. The most optimal formulation was further combined with penetration enhancers to improve bioavailability of the active ingredient, and the in vitro drug release and in vitro permeation of BGP-15 from the patches were investigated. FTIR spectra of BGP-15, the formulations and the components were also studied. The most optimal formulation based on the tested parameters was dried for 24 h, with 67% polyvinyl alcohol (PVA) content and low ethanol content. The selected penetration enhancer excipients were not cytotoxic on HaCaT cells. The FTIR measurements and SEM photography proved the compatibility of the active substance and the vehicle; BGP-15 was present in the polymer matrix in dissolved form. The bioavailability of BGP-15 was most significantly enhanced by the combination of Transcutol and Labrasol. The in vitro permeation study confirmed that the formulated patches successfully enabled the transdermal administration of BGP-15.

Transdermal Patches Approach Towards Self-Nano-Emulsifying Drug Delivery System (SNEDDS) Using Essential Oil as Penetration Enhancer

Abstract: A transdermal patch is a topically applied adhesive patch that delivers a medication dose directly into the blood. The patch allows for the safe delivery of a drug to the targeted site, ideally by a permeable layer covering a reservoir of the drug by melting small patches of drug embedded in the adhesive, which is one benefit of transdermal drug delivery over most types of pharmaceutical deliveries, including oral, topical, intramuscular, intravenous, and several others. This can also help heal a damaged body part, improving patient compliance, treatment efficacy, and dose frequency while minimizing the side effects. This review covers the production, methods of evaluation, quality, use of penetration enhancers, and pros and downsides of transdermal patches, as well as the benefits of essential oil as a penetration enhancer. Compared to chemical enhancers, essential oils have shown the ability to break down the stratum corneum layer, allowing drugs to penetrate deeper into the skin. Essential oils are excellent penetration enhancers for the skin. These penetration enhancers are cost-effective, biocompatible, readily available, non-toxic, chemically modifiable, and possibly biodegradable. In this review, attention has been paid to the formulation and evaluation of transdermal patches with the help of SNEDDS (self-nano-emulsifying drug delivery systems) using essential oil as a penetration enhancer, and their future prospects.

Design, Development, and Evaluation of Transdermal Patches Containing Donepezil Hydrochloride

This study aimed to develop a donepezil hydrochloride (DH) transdermal drug delivery system to address non-compliance due to dementia in Alzheimer’s patients. DH has a low dose, balanced hydrophilicity/lipophilicity, and low toxicity making it suitable for transdermal. DH transdermal patches were prepared using a polymer and plasticizer matrix system via box-Behnken design and evaluated for properties. Formulation B2 containing hydroxy propyl methyl cellulose (HPMC), ethyl cellulose (EC), and xanthan gum was optimal, exhibiting a maximum of ~99.17% in-vitro drug release for 48 hours. In-vivo pharmacokinetic parameters studied in rabbits were superior to commercial DH tablets. The study demonstrates the potential for DH transdermal patches as an alternative to oral medication for Alzheimer’s patients. The patches can provide sustained release for prolonged periods without requiring multiple doses. However, further confirmation is needed via in-vivo pharmacodynamic and human pharmacokinetic studies.

Development and Evaluation of Transdermal patches of Piperine hydrochloride

The fundamentals οf a successful pharmaceutical fοrmulatiοn depend οn the delivery οf the medicament tο the target site at therapeutically relevant level, with negligible οr minimum discοmfοrt and side effects tο the patient. Low dose maintenance therapy of Piperine HCl has the capability to reduce potential side effects and improved patient compliance which are more common with conventional drug delivery. The developed formulation of Piperine HCl is expected to improve the patient compliance, form better dosage regimen and provide maintenance therapy to patients suffering from inflammation and allergy. These promising results showed the feasibility of delivering Piperine HCl through transdermal matrix patch. The developed transdermal patches of Piperine HCl may prove to be a better alternative to conventional dosage forms in allergy as revealed by the results

Formulation and Evaluation of Transdermal patch of Methimazole

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

An Insight into delivery of drug through The Skin: Transdermal Drug Delivery system

In the recent days about 75% of the drugs taken orally are does not show the desired therapeutic effect. Oral conventional dosage forms have several disadvantages such as poor bioavailability due to hepatic first pass metabolism and tendency to produce rapid blood level spikes (Both high and low). Thus, rapid drug levels in the plasma leads to a need of high and/or frequent dosing, which can be both uneconomical and inconvenient. To overcome such disadvantages transdermal drug delivery system was developed. TDDS is such a delivery system which has been explored extensively over the last two decades, with therapeutic success. Transdermal drug delivery systems (TDDS) are the drug delivery systems which involves transportation of drug to epidermal and dermal tissues of the skin for local therapeutic action while major fraction of the drug is transported into the systemic blood circulation. Topical administration of therapeutic agents offers vast advantages over conventional oral and invasive methods of drug delivery. Some of the advantages of transdermal drug delivery include limitation of hepatic first pass metabolism, enhancement of therapeutic efficiency and maintenance of steady state plasma level concentration of the drug. This study includes a brief overview of TDDS, its advantages over conventional dosage forms, drug delivery routes across human skin, permeation enhancers, and classification, formulation, methods of preparation and evaluation of transdermal patches.

Formulation and evaluation of transdermal patch of stiripentol for treatment of seizures

Formulation and evaluation of transdermal patch of stiripentol for treatment of seizures

Formulation and evaluation of transdermal patches containing dexketoprofen trometamol

Dexketoprofen Trometamol is a NSAID, used as an analgesic and anti-inflammatory drug. It works by blocking the action of cyclo-oxygenase in the body. Conventional route of delivery has many drawbacks such as hepatic first-pass metabolism, reduced bioavailability, and fluctuating drug concentrations in the blood. These problems can be overcome by development of transdermal drug delivery system. The objective of this study was to develop and evaluate the transdermal patches of the drug Dexketoprofen Trometamol. The patches were prepared by solvent casting method using polymers; Ethyl cellulose, HPMC and ERS 100 in different ratios.The prepared formulations were uniform in their physical characteristicsThe formulation F6, combination of polymer (HPMC: EC in ratio 4:1) showed maximum release of 85.77% in 24 hours. The resultant data was fitted in to zero, first, Higuchi and Peppas model. The results specify that Dexketoprofen Trometamol transdermal patch can be designed for obtaining better therapeutic benefits.

A REVIEW ON DESIGN AND EVALUATION OF TRANSDERMAL PATCHES

A REVIEW ON DESIGN AND EVALUATION OF TRANSDERMAL PATCHES

Invitro evaluation of transdermal patch for edivoxetine hydrochloride

Invitro evaluation of transdermal patch for edivoxetine hydrochloride

Formulation and Evaluation of Transdermal Patches Containing Glimipiride

The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Glimepride with different ratios of hydrophilic and hydrophobic polymeric systems by the solvent evaporation technique. Different concentrations of oleic acid and isopropyle myristate were used to enhance the transdermal permeation of glimipride. Matrix type transdermal patches prepared by using different ratio of Eudragit RS100, HPMC100M, by using solvent evaporation techniques. All the prepared formulation were subjected to evaluation studies i.e., weight variation, thickness, drug content, moisture content, moisture uptake, flatness and in-vitro drug release. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Compatibility study between drug and polymer can be done by FTIR. From the all formulation batch F3 was optimized formula. Shows linear zero order release for 24 hrs with cumulative % drug diffusion of 88.34% from 4cm2 patches. It is concluded that concentration of polymer (HPMC100M) when increases into primary layer, then In-vitro diffusion rate also increases and concentration of Eudragit Rs100 when increases, the drug diffusion decreases. It provides better controlled drug release for patch.

Formulation optimization and Evaluation of Transdermal patch of losartan potassium containing DMSO as permeation enhancer

The present investigation focused on the formulation optimization and evaluation of transdermal patch of losartan potassium containing DMSO as permeation enhancer. Transdermal patches were prepared by solvent evaporation method by taking different ratios of polymers such as HPMC K100M and Eudragit RS 100, along with the DMSO as permeation enhancer and PEG-400 as plasticizer. Two factor three levels central composite design applied to optimize the formulation variables. In this study, amount of HPMC K100 M (X1) and amount of Eudragit RS 100 (X2) were selected as independent variables. The percentage losartan potassium permeated at 3 hrs (Y1), percentage losartan potassium permeated at 6 hrs (Y2) and permeation flux (Y3) were selected as dependent variables. The FTIR studies confirmed that there is no interaction between losartan potassium and the polymers. Nine formulations were formulated according to design. The prepared formulations were evaluated for various physical and chemical parameters. In-vitro drug permeation study was carried out for 6 hrs. The formulation OLP-4 was given as best batch by the design expert software. The formulation OLP-4 showed the 34.47% permeation in 6 hrs and permeation flux435.74 μg/cm2/hr. The best fit model for optimized batch OLP4 is zero order model with highest r2 value of (r2 = 0.9641) and the mechanism of release was fickian diffusion mediated. Statistical optimization proved to be very useful in the subsequent formulation development work following preliminary evaluations. Thus, the design of experiment with response surface method is an efficient tool to determine and optimize formulation conditions within experimental conditions.

Formulation and Evaluation of Transdermal patch of Arnica montana

Formulation and Evaluation of Transdermal patch of Arnica montana

Development and Evaluation of Transdermal Patches containing Carvedilol and Effect of Penetration Enhancer on Drug Release

Adhesiveness, as well as permeation of drug presents a significant challenge for the acceptability of transdermal patches. The current investigation deals with the development of pressure-sensitive based drug in transdermal patches containing Carvedilol with four different grades of acrylic polymer Duro-Tak 87- 4098, Duro-Tak 387-2051, Duro-Tak 387-2052 and Duro-Tak 87-2510 (a pressure-sensitive adhesive). Despite of the functionality or non functionality of these polymers, an attempt has been made to increase their permeability by using three distinct permeation enhancer individually, non ionic surfactant Span 80,oleic acid and a terpene farnesol. Transdermal patches containing Carvedilol were prepared by spreading method by using a fixed concentration of various grades of acrylic polymer; drug and penetration enhancers. The patches were evaluated for different physical parameters with Ex-vivo permeation studies. Skin irritation studies are conducted by using Albino Rats. Ex-vivo permeation across excised rat skin from these formulated carvedilol patches were found to be sustained over 12 h and followed the zero-order model with Fickian diffusion mechanism. The effect of permeation enhancers was in order: Span 80> farnesol >oleic acid. The skin irritation test demonstrated absence of any sign of skin irritation.

Design and Evaluation of Transdermal Patches Containing Risperidone

Transdermal drug delivery systems are also known as patches, containing dispersed or dissolved drug with plasticizers, polymers, etc. are intended to deliver a therapeutically effective amount of drug across the skin. In the present work, Transdermal drug delivery of Risperidone were formulated in different concentration (10%, 20% and 30%) of glycerine and polyethylene glycol 400 as plasticizer and a blend of two in different concentrations of polymers (PVPK30, HPMC, PVA and Eudragit RS 100) were formulated by solvent casting method. Drug polymer interaction study was carried out using FTIR and DSC studies. In this study the results indicates, as increase in the concentration of glycerine and Polyethylene glycol increases the diffusion rate of Risperidone patches. The physico-chemical parameters like weight variation, thickness, folding endurance. Percentage Flatness and Water vapour transmission of the Risperidone patches were evaluated. All the physico chemical parameters were found to be satisfactory. Risperidone patches formulated by using 30% glycerine 30% PEG400shows enhanced rate of diffusion than the patches prepared with 10% and 20% glycerine10% and 20% PEG400 respectively. Risperidone patches formulated with 20% glycerine 20% PEG400 had enhanced rate than the patches prepared with 10%glycerine/10% PEG400 respectively. Among polymers, combination of HPMC and Eudragit had enhanced diffusion rate than the combination of HPMC and PVPK30 in all formulations formulated by using glycerine as plasticizer. The polymers, combination of PVPK30 and Eudragit had enhanced diffusion rate than the combination of PVPK30 and PVA in all formulations formulated by using PEG400 as plasticizer. The Risperidone transdermal patches shows greater diffusion rate when formulated with higher concentration of plasticizer hence the 30% of glycerine and PEG 400 had shown a values higher than 20 and 10% glycerine and PEG 400. The kinetic study and mechanism for the diffusion of Risperidone transdermal patches obeys higuchi, peppas model. The correlation coefficient (R2) values were greater, indicating from the analysis of diffusion data as per above models. The T50 and T80 values for Risperidone patches formulated with glycerine and PEG 400 are exhibited good results. The SEM films indicating uniform distribution of the drug with polymers and plasticizers.

Formulation and Evaluation of Transdermal Patch Containing Sibutramine

Sibutramine is a serotonin-norepinephrine reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. The oral administration of sibutramine is followed by its dose-related side effects. In this study, sibutramine was formulated into drug in adhesive (DIA) patches in an attempt to overcome these problems. The effects of different formulation variables including pressure-sensitive adhesive (PSA), loading amount of drug, thickness of matrix and enhancer on the skin permeation of the drug were evaluated using excised hairless mouse skin. In the acrylic adhesive with carboxyl functional group, low release of sibutramine was observed due to the strong interaction between carboxyl group of adhesive and amine group of sibutramine. The acrylic adhesive without functional group provided good adhesion force and allowed high drug loading. Changing drug load as well as thickness of the matrix was found to alter permeation rate. PK40 and A40, were found to be effective enhancers for sibutramine. The optimized patch contained 20% sibutramine, and 5% A40 as permeation enhancer, in thick Duro- 87-9301 matrix.

Formulation and evaluation of transdermal patches of papaverine hydrochloride

Formulation and evaluation of transdermal patches of papaverine hydrochloride

Formulation and In Vitro Evaluation of Transdermal Patches of Melatonin

The present study was undertaken to prepare and evaluate monolithic drug‐in‐adhesive type transdermal patches of melatonin containing penetration enhancers such as fatty alcohols, fatty acids, and terpenes. The patches were prepared using Eudragit® E 100 as the adhesive polymer. The release profile of melatonin from control as well as enhancer‐containing patches showed an initial burst of melatonin release for up to 4 hours and then a plateau after 8 hours. The release profiles of melatonin from patches containing various enhancers were similar to the control patch. However, the addition of enhancers in the patch increased the permeation of melatonin through hairless rat skin. The flux values of patches containing octanol, nonanoic acid, and myristic acid were higher than the control patch (no enhancer), but the differences were not statistically significant (P > 0.05). Decanol, myristyl alcohol, and undecanoic acid at 5% concentrations showed significantly higher flux values through hairless rat skin (enhancement ratios 1.7, 1.5, and 1.6 for decanol, myristyl alcohol, and undecanoic acid, respectively) (P < 0.05). Menthol and limonene at 5% w/w showed maximum permeation of melatonin among all enhancers studied (enhancement ratios = 2.1 and 2.0 for menthol and limonene, respectively) (P < 0.001). In general, there was about 4–6 hours of lag time observed before a steady state flux of melatonin was achieved. Though the flux of melatonin observed in the present study is 5–10 times higher than the required delivery rate in humans, it must be noted that the present study was performed using hairless rat skin, which is generally more permeable compared to human skin. Further studies using human skin would prove the usefulness of these patches.