scholarly journals FORMULATION AND EVALUATION OF TOPICAL ANTIFUNGAL GEL CONTAINING ITRACONAZOLE

2018 ◽  
Vol 10 (4) ◽  
pp. 71
Author(s):  
Poonam Madhukar Kasar ◽  
Kalyanisundarrao Kale ◽  
Dipti Ganesh Phadtare
Keyword(s):  
Side Effects ◽  
Drug Release ◽  
Rheological Properties ◽  
Skin Irritation ◽  
Scale Up ◽  
In Vitro Drug Release ◽  
Systemic Fungal Infection ◽  
Topical Gel ◽  
Gel Preparation

Objective: The present research has been undertaken with the aim to develop a topical gel formulation of Itraconazole. Itraconazole is an imidazole derivative and used for the treatment of local and systemic fungal infection. The oral use of Itraconazole is not much recommended as it has many side effects. Commercially Itraconazole topical gel preparation are not available in the market, thus this formulation is made for better patient compliance and to reduce the dose of the drug and to avoid the side effects like liver damage and kidney damage.Methods: The gel was formulated by changing the polymer ratio. Various formulation (F1, F2, F3, F4, F5) were developed by using a suitable polymer (carbopol 934p and HPMC). The formulation was evaluated for % yield, spreadability, extrudability, wash ability and viscosity in vitro drug release study, skin irritation study, stability testing.Results: Viscosity studies of various formulations revealed that formulation F3 was better to compare to others. From among all the developed formulation, F3 shows better drug diffusion, did good Rheological properties. pH of the F3 formulation is sufficient enough to treat the skin infections. Results indicated that the concentration of carbopol-934 and HPMC K4M significantly affects drug release and rheological properties of the gels.Conclusion: It was concluded that formulation F3 was the best formulation among this formulation. Hence formulation F3 should be further developed for scale-up to industrial production.

scholarly journals SOLUBILITY ENHANCEMENT OF CELECOXIB BY SOLID DISPERSION TECHNIQUE AND INCORPORATION INTO TOPICAL GEL

2019 ◽  
pp. 294-300
Author(s):  
AMRIN SHAIKH ◽  
PRASHANT BHIDE ◽  
REESHWA NACHINOLKAR
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
In Vitro Drug Release ◽  
Peg 6000 ◽  
Topical Gel ◽  
Drug Content ◽  
Vitro Release

Objective: The aim of the present investigation was to design gels for the topical delivery of celecoxib and evaluate with an aim to increase its penetration through the skin and thereby its flux. Method: The solubility of celecoxib is shown to be increased by preparing solid dispersions (SDs) using carriers such as mannitol, polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG) 6000 and urea by solvent evaporation, fusion, and coevaporation methods. In vitro release profile of all SD was comparatively evaluated and studied against the pure drug. The prepared SD was subjected for percent practical yield, drug content, infrared spectroscopy, differential scanning calorimetry analysis, X-ray diffraction studies, and scanning electron microscopy (SEM) imaging. The celecoxib gel was prepared using hydroxypropyl methyl cellulose (HPMC) and Carbopol containing a permeation enhancer dimethyl sulfoxide (DMSO) at different proportions and evaluated for drug content, pH, viscosity, spreadability, extrudability, stability, and in vitro drug release. Results: Faster dissolution rate was exhibited by SD containing 1:5 ratio of celecoxib: PVP K-30 prepared by coevaporation method. In vitro drug release of celecoxib, gels revealed that formulation with HPMC has higher drug release as compared to Carbopol. Conclusion: The increase in dissolution rate for SD is observed in the following order of PVP K-30>urea>mannitol>PEG 6000. The CPD5 gel containing a SD CP5 and 20% DMSO showed the best in vitro release 74.13% at the end of 6 h.

scholarly journals CURCUMIN LOADED CHITOSAN NANOPARTICLES FOR TOPICAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES

2021 ◽  
Vol 10 (2) ◽  
pp. 48-52
Author(s):  
J Adlin Jino Nesalin ◽  
Preethi Raj M N
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Topical Gel

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive nanoparticles and to design an innovative topical delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated nanoparticles were prepared by ionic gelation method. The nanoparticles were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected nanoparticles formulation (FS5, containing drug: polymer ratio 1:5) was incorporated into gels with a bio adhesive polymer. The Nanoencapsulated topical gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected Nanoencapsulated bio adhesive topical gel (FS3 gel, containing 1 % w/w of drug loaded nanoparticles and 0.6 % w/w of Carbopol 934) was found to control curcumin release over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of Nanoencapsulated topical gel study may be adopted for a successful delivery of Curcumin for topical use.

Design and Development of Clobetasol Propionate Topical Gel Thickened with Novel Copolymer

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
Kumar Pawan ◽  
Shailendra Kumar Singh
Keyword(s):  
Drug Release ◽  
Water Solubility ◽  
In Vitro Release ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
Promising Alternative ◽  
Topical Gel ◽  
Release Studies ◽  
Photo Stability

Topical delivery of clobetasole propionate (CP) offers several formulation related problems due to poor water solubility and photo degradation property. In the present investigation, topical gel of CP was formulated using Acrylamide/ Sodium Acryloyldimethyl taurate copolymer (SEPINEO™ P 600) as a gelling agent and evaluated with respect to different physicochemical parameters such as pH, viscosity, bio-adhesivity, spreadability, in vitro drug release and photo stability. Permeation of CP gel was studied using freshly excised pig ear skin for 24 h. The cumulative permeation of drug through excised rat skin was 3.0 ± 1.2 mg cm-2 with the corresponding flux value of 0.24 ± 0.09 mg cm-2 h -1 . The in vitro release studies showed 101.43±1.12 % drug release over 10 h. The selected formulation was found to be effective with respect to percent drug content, permeation characteristics, pH, viscosity, and photostability. Therefore, CP gel could be very promising alternative for the topical drug delivery.

Formulation and Evaluation of Nanosponges loaded Bifonazole for Fun-gal Infection

2020 ◽  
Vol 18 ◽  
Author(s):  
Amaravathi Murali Krishna ◽  
Venkatesh Dinnekere Putte Gowda ◽  
Roopa Karki
Keyword(s):  
Drug Release ◽  
Fungal Infections ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Three Dimensional ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Model Stability ◽  
Novel Approach

Background: Nanosponges is a novel approach of topical drug delivery, especially for the fungal infections. Nanosponges are a unique class of nanoparticles with three-dimensional nanostructure in nanometers wide cavities, which can encapsulate both hydrophilic and lipophilic substances, will provide increased efficacy and safety. Objective: To formulate and evaluate Bifonazole loaded nanosponges in hydrogels for the treatment of fungal diseases. Methods: Bifonazole-loaded nanosponges to be formulated using emulsion solvent diffusion technique. Interaction of drugethyl cellulose polymer along with other excipients’ was done by using FTIR as well as DSC. The nanosponges formulations were evaluated with different parameters. Results: Bifonazole loaded nanosponges’ particle size and zeta potential for formulations were between the range of 183.7 to 560.2 nm and –17.77 to –21.9 mV, respectively. Surface morphology of nanosponges by SEM disclosed that it was spherical and porous in nature. Drug entrapment efficiency was found to be 45.44 to 79.71%. The drug release study was done by using phosphate buffer pH 6.8. Further in vitro release data is fitted in to kinetic models. The optimized formulation M6 has incorporated hydrogels, further evaluated skin irritation, in vitro drug release, viscosity and pH using a rat model. Stability studies of hydrogel formulation MH2 revealed that no changes in in-vitro drug release, pH and drug content study at the completion of 6 months. Conclusion: Thus, it indicated that the prepared Bifonazole loaded nanosponges into hydrogel was stable. Hence, it could be a suitable dosage form for the cure of fungal infections in the skin.

scholarly journals Antielastase Activity of Macassar Kernels (Rhus javanica) Stem Extract and Skin Elasticity Evaluation of Its Topical Gel Formulation

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Nadia Bunga Anggraini ◽  
Berna Elya ◽  
Iskandarsyah Iskandarsyah
Keyword(s):  
Skin Irritation ◽  
Test Methods ◽  
Homogeneity Test ◽  
Skin Elasticity ◽  
Topical Gel ◽  
Safety Test ◽  
Stem Extract ◽  
Microplate Reader ◽  
Gel Preparation

Background. Macassar kernels (Rhus javanica L.) has potential as an antiaging agent as it has antielastase activity, especially its stem extract which has best percent inhibition compared to its leaves and fruit extract. Moreover, the antiaging agent can be commonly used in the form of gel for topical applications. Hence, formulation of HEC-based topical gel from the stem extract of Macassar kernels was conducted. This study aims to determine the antielastase activity of the stem extract of Macassar kernels and evaluate the skin elasticity of its topical gel formulation by conducting dermatological safety and skin antiaging efficacy test. Methods. The stem extract was in vitro tested for antielastase activity using a microplate reader. Then, a formulation of a topical gel containing Rhus javanica stem extract was made. Five stages of quality control, which consisted of an organoleptic test, homogeneity test, pH measurement, viscosity measurement, and physicochemical stability test, were conducted to ensure the quality of topical gel formulation. Last, clinical studies were conducted to evaluate the dermatological safety and antiaging efficacy of gel preparation containing stem extract of Rhus javanica. Results. The stem extract provided antielastase activity (IC50 = 245.68 μg/mL), and its polyphenol was valued at 23.28 ± 1.52 mg GAE/g). The gel containing 10% stem extract had better stability than the gel containing 5% stem extract. The dermatology safety test and efficacy test results indicated that the topical gel containing 10% Rhus javanica stem extract did not cause any skin irritation and significantly improved skin elasticity p < 0.05 . In the treatment group, the moisture parameter was significantly changed on day 14 p < 0.0001 , day 21 p < 0.0001 , and day 29 p < 0.0001 . The elasticity parameter was also changed significantly on day 14 p = 0.0485 , day 21 p = 0.0537 , and day 29 p = 0.0002 . Conclusion. The stem extract of Rhus javanica has potential antielastase activity. The topical gel containing Rhus javanica stem extract also has potential antielastase activity by increasing the skin moisture and enhancing skin elasticity.

Formulation and Evaluation of DHA Oil based Nicotinamide Nanoemulsion Gel for Treating Atopic Dermatitis

2020 ◽  
Vol 10 (6) ◽  
pp. 892-901
Author(s):  
Gayathri P. Pradeep ◽  
Vidya Viswanad
Keyword(s):  
Drug Release ◽  
Cell Line ◽  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Nanoemulsion Gel ◽  
Permeation Studies ◽  
Franz Diffusion Cells

Background: Atopic dermatitis (or eczema) can be defined as a chronic inflammatory condition accompanied by severe pruritus. Objective: The prepared gel was evaluated for in vitro drug release, in vitro occlusion studies, transepidermal water loss studies, skin permeation studies, in vitro skin irritation studies and antiinflammatory cell line studies. Methods: In vitro drug release studies were performed using Franz diffusion cells. The in vitro occlusion studies were carried out by the procedure reported by Wissing et al. TEWL determination was done by the method proposed by Reiger. The skin permeation studies were carried out using porcine skin using Franz diffusion cells. In vitro skin irritation study was carried out using HETCAM (Hen’s Egg Test on the Chorioallantoic Membrane) method. Anti-inflammatory cell line studies were carried out using RAW 264.7 cell lines. Results: In vitro drug release studies,drug release of nicotinamide from nanoemulsion gel was found to be more than marketed gel. Kinetic modelling showed a higuchi model with non-fickian diffusion. In vitro occlusion study showed the percentage of evaporated water from prepared nanoemulsion formulation after 72 h is very less compared with the other formulations. The TEWL measurement shows the reduction in TEWL has more in prepared nanoemulsion gel than other formulations. Anti-inflammatory cell line studies proved that the nanoemulsion gel has inhibition capacity on COX activity, LOX activity, Inducibe nitric oxide synthase and cellular nitrate levels. Conclusion: DHA oil based nicotinamidenanoemulsion gel were prepared successfully and the evaluation of prepared gel showed better drug release and skin permeation with better antiinflammatory activity.

Design and Characterization of Nanostructure Lipid Carrier for Transdermal Delivery of Pioglitazone

2018 ◽  
Vol 11 (4) ◽  
pp. 4185-4195
Author(s):  
Niket N Garude ◽  
Rachel B Geevarghese
Keyword(s):  
Drug Release ◽  
Transdermal Delivery ◽  
High Speed ◽  
Drug Loading ◽  
Skin Irritation ◽  
Systemic Availability ◽  
Transdermal Patch ◽  
Drug Release Profile ◽  
In Vitro Drug Release

Nanostructure Lipid Carrier (NLC) is one of the lipid-based drug delivery systems that are used as carrier for delivery of drugs. NLC are composed of mixture of solid lipid and liquid lipid, which form imperfect type of lipid matrix with improved drug loading capacity, drug release profile and stability. The aim of the present study was to develop and characterize nanostructure lipid carrier for transdermal delivery of pioglitazone (PZ) to overcome the problems related with oral route of administration and to improve systemic availability. NLC’s were prepared by high-speed homogenization method. Optimized NLC formulation was evaluated for particle size, percentage entrapment efficiency, surface morphology, DSC analysis, in-vitro drug release etc. The optimized NLC formulation was formulated as a transdermal patch and evaluated for in vitro drug release study and primary skin irritation study. In vivo hypoglycaemic activity of pioglitazone -NLC loaded transdermal patch was studied in comparison with its orally administered suspension. PZ- NLC loaded transdermal patch was found to be non-irritant and showed reduction in blood glucose level in a controlled manner up to 24 hrs.    

scholarly journals FORMULATION OPTIMIZATION AND EVALUATION OF FLURBIPROFEN EMULGEL

2020 ◽  
pp. 49-54
Author(s):  
DIKSHA S. CHODANKAR ◽  
SACHI S. KUDCHADKAR ◽  
RAJASHREE S. GUDE ◽  
PRERANA D. NAVTI ◽  
SANAM M. SAWANT
Keyword(s):  
Side Effects ◽  
Drug Release ◽  
Stability Study ◽  
Water Soluble ◽  
Gelling Agent ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Dermal Delivery

Objective: The objective of the present study was to formulate flurbiprofen (FLB) emulgel, evaluation of the formulations and the selection of an optimized formulation through in vitro drug release and drug content studies. Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) requiring frequent administration and its chronic intake can lead to systemic side effects like gastric irritation and GI bleeding. The development of a dermal drug delivery system can overcome these side effects. Methods: The emulgel formulations were produced using different combinations of oil and emulsifying agents. Carbopol 940 was used as a gelling agent. The prepared emulgels were evaluated for general appearance, pH, spreadability, extrudability, drug content, in vitro drug release, average globule size and viscosity. Results: Optimized formulation F7 showed a better in vitro drug release compared to the marketed gel preparation. The stability study for the optimized formulation was carried out at 25 °C/60 % RH for 3 mo and the emulgel was found to be stable concerning the physical appearance, pH and drug content. Conclusion: The study revolved around the formulation of emulgel containing Flurbiprofen for dermal delivery of the drug. Emulgel was formulated with the purpose to enhance the permeation of poorly water-soluble drug FLB. The study concluded that the optimized emulgel containing FLB exhibited better in vitro drug release profile compared to the marketed formulation.

scholarly journals Formulation and Evaluation of Transdermal Topical Gel of Ibuprofen

2020 ◽  
Vol 10 (2) ◽  
pp. 20-25
Author(s):  
Ankita Kashyap ◽  
Asha Das ◽  
Abdul Baquee Ahmed
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Research Work ◽  
Physical Mixture ◽  
Compatibility Study ◽  
Topical Gel ◽  
Carbopol 940 ◽  
Egg Membrane ◽  
Gel Preparation

The present research work is based on the formulation and evaluation of topical gel of Ibuprofen where Carbopol 940 is used as the polymer. Gels were prepared by dispersing the polymers  in a mixture of water and glycerol with methyl paraben as the preservative and the varying amount of ibuprofen, being kept under magnetic stirring until the homogeneous dispersion was formed. The dispersion was then neutralized and made viscous by the addition of triethanolamine. The Carbopol gels of Ibuprofen were found to be homogenous with good drug loading. The pH of all the gel formulations was found within the neutral pH range which is compatible with skin. And the viscosity of the formulations was found to be feasible for topical drug delivery. The drug content of the three formulations was found in the range of 87.56% to 90.45% which shows efficient drug loading. Results of In vitro drug release study showed that F5 formulation has better diffusion of drug through egg membrane and hence further permeation studies were carried out through rat epidermis. The compatibility study showed that the major peaks in FTIR spectra of the pure drug were found to be intact in their physical mixture. Hence there is no interaction between drug and Carbopol in their physical mixture. Carbopol can be effectively used as the polymer for topical gel preparation. And F5 formulation containing 0.5 % w/w Carbopol 940 may be effectively used as topical transdermal delivery for Ibuprofen. Keywords: Ibuprofen, Transdermal Gel, Drug release, Compatibility study

scholarly journals DESIGN, DEVELOPMENT, AND CHARACTERIZATION OF TOPICAL GEL CONTAINING ITRACONAZOLE - ANTIFUNGAL AGENT

2018 ◽  
Vol 11 ◽  
Author(s):  
Pavithra K
Keyword(s):  
Drug Release ◽  
Fungal Infections ◽  
Gelling Agent ◽  
Compatibility Study ◽  
In Vitro Drug Release ◽  
Topical Gel ◽  
Drug Content ◽  
Release Studies ◽  
Ft Ir

Objective: The main purpose of this study was to develop a topical delivery of itraconazole to reduce the dose of the drug, to improve patient compliance, and to avoid the side effects. Itraconazole is a triazole derivative to treat antifungal and antiprotozoal infections. Methods: Topical gel formulations of itraconazole were prepared using Carbopol 940 as a gelling agent with different concentrations. Four different formulations were prepared and evaluated with respect to color, spreadability, viscosity measurement, determination of pH, drug content, in vitro drug release studies, zeta potential studies, and stability studies. Compatibility study was carried out by Fourier-transform infrared (FT-IR) spectral analysis. Results: FT-IR study revealed that there were no significant interaction between the drug and polymers. All the prepared formulations show acceptable physical properties. The drug content and percentage yield were higher for F1 formulation among all formulation F1 shows better drug release. Stability study of best formulation shows that there was no difference in drug content and in vitro drug release studies. Conclusion: From the above observation results that this formulation may be more encouraging topical substitute for the healing of fungal infections in the skin.

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