scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCH OF PLUMBAGIN FOR ANTI-FUNGAL ACTIVITIES

2021 ◽  
Vol 12 (2) ◽  
pp. 23-28
Author(s):  
Aman Sharma ◽  
Abhinav Agarwal

The objective of the current study is to improve the patient compliance and sustained drug release action by herbal medicine which can be achieved by developing alternative drug delivery system. The matrix type transdermal patches containing plumbagin were prepared by solvent evaporation method with different ratios of polymers (HPMC 50cps, PVP K29-32 and EUDRAGIT RS-100). In these matrix type transdermal patches, the PEG (Polyethylene glycol) was used as plasticizer and DMSO (Dimethyl sulfoxide) used as a penetration enhancer. The formulated patches were evaluated for physicochemical parameters like thickness, weight variation, % moisture content, % moisture uptake, % flatness, folding endurance and drug content. In vitro drug release studies were carried out by using the Franz diffusion cell. The cumulative % of drug released in 10 hours from the six batch formulations were 95.66%, 94.2%, 97.33%, 90.13%, 83.75% and 85.71%, respectively. On the basis of in-vitro drug release, formulation (HE-2) was found to be better than other formulation and these were selected for further evaluation such as anti-fungal activity and stability studies.

Author(s):  
J. R. D. Gupta ◽  
R. Irchhiaya ◽  
N. Garud ◽  
Priyanka Tripathi ◽  
Prashant Dubey ◽  
...  

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.


Author(s):  
Ningule Ganesh M. ◽  
Nagoba Shivappa N. ◽  
Shaikh Atiya L. ◽  
Wadulkar Raghunath D. ◽  
Deshmukh Aditye Y.

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.


Author(s):  
Lama Hamdan ◽  
Jamila Husian

  Objective: Transdermal patches of Ketotifen fumarate (KT) were developed for prolonged effect of the drug, and to protect the patient from allergic symptoms associated with asthma and other allergic diseases.Methods: Matrix type patches were prepared by solvent casting technique using different types of polymers: Hydroxy propyl methyl cellulose (HPMC K15M) and ethyl cellulose to formed the matrix of the patch in different ratios, emulsifying agents were added as a penetration enhancers (Span 60, Tween 60, Cremophor EL) in a ratio 0.025% w/v to the matrix, 10% v/v of glycerin was added as plasticizer to 10 ml of chloroform:methanol (1:1). The drug matrix film was casted on a polyvinyl alcohol backing membrane. All patches were evaluated for physical proprieties, thickness uniformity, folding endurance, moisture uptake, moisture content, drug content, uniformity of weight, content uniformity, in vitro drug release, and kinetic models. Differential scanning calorimetry was used to characterize physical mixtures of KT and the different used excipients.Results: The results showed that the prepared patches had acceptable physical properties. The drug substance was released well. Adding the penetration enhancers delayed the release of the drug from the matrix in all the prepared formulas, formula A2 that having no enhancer, showed maximum amounts of drugs release (90.06±0.9)% for 24 hrs. However, adding penetration enhancers decreased the amount of the drug release, formula B2 having Tween 60 as a penetration enhancer, showed the maximum release of the drug (87.78±0.88)%, and formula B3 having Cremophor EL showed the minimum release of the drug (79.13±1.58) at the end of 24 hrs dissolution study. The release of the drug from all formulations was followed by Korsmeyer-Peppas pattern with n>0.45 indicating that drug release from matrix was mainly happened by swallowed and diffusion (non- Fickian pattern).Conclusion: Optimized formula A2 containing the maximum amounts of HPMC K15M showed a controlled release of the drug over 12 hrs, and it identified as a successful formulation for this study.


Author(s):  
Swati Hardainiyan ◽  
Krishan Kumar ◽  
Bankim Chandra Nandy ◽  
Richa Saxena

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.


Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.


Author(s):  
Dillip Kumar Behera ◽  
Kampal Mishra ◽  
Padmolochan Nayak

In this present work, chitosan (CS) crosslink with polyaniline (PANI) with montmorilonite (MMT) called as (CSPANI/MMT) and CS crosslink with PANI without MMT called as (CS-PANI) were prepared by employing the solution casting method. Further the formation of nanocomposites CS-PANI/MMT and CS-PANI were investigated using XRD, FTIR, SEM and tensile strength. Water uptake and swelling ratio of the CS-PANI and CS-PANI/MMT were found to decrease with increase in concentration of clay. Mechanical properties of the CS-PANI and CS-PANI/MMT were assessed in terms of tensile strength and extensibility using texture analyzer. Increase in tensile strength and reduction in extensibility was reported with increase in the nanoclay content. In vitro drug release study on CS-PANI and CS-PANI/MMT indicated pronounced sustained release of doxorubicin by the incorporation of clay particles in the CS polymer matrix. Overall CSPANI/MMT nanocomposite films exhibited improved mechanical and sustained drug release properties than CS-PANI.


Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate theintragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulationswere formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration ofdrug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitrobuoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimizedformulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMCK100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studiesand was found to be stable as no significant change was observed in various evaluated parameters of the formulation.Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach toincrease gastric residence time, thereby improving its bioavailability.Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P,Xanthan gum.


2017 ◽  
Vol 16 (10) ◽  
pp. 2325-2330
Author(s):  
Qiong Jin ◽  
Wei Chen ◽  
Wan Wu

Purpose: To develop mucoadhesive tablets containing miconazole (MCZ) for the treatment of oropharyngeal candidiasis, using chitosan and hydroxypropyl methylcellulose (HPMC) as mucoadhesive polymers.Methods: Mucoadhesive tablets were formulated and optimized using a 23 factorial design and direct compression method. The independent variables were compression force and concentrations of chitosan and HPMC, while mucoadhesion time and in vitro drug release were dependent variables. Tablet characterization was carried out by evaluating hardness, thickness, tablet weight variation, content uniformity, friability and in vitro drug release at salivary pH (pH 6.8).Results: The tablets showed good mucoadhesion for an extended period (8 h), and their physical characteristics were within acceptable ranges. Drug release ranged from 60.5 % to 80.8 %.Conclusion: These results indicate that the mucoadhesive MCZ tablets formulated with chitosan and HPMC possess potential for the development of therapeutic preparations for management of oropharyngeal candidiasis.Keywords: Miconazole, Oropharyngeal candidiasis, Factorial design, Mucoadhesion, Chitosan, Drug release


Author(s):  
Pratik Swarup Das ◽  
Puja Saha

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.


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