scholarly journals Formulation and Evaluation of Topical Microemulgel Containing Terbinafine Hydrochloride

2021 ◽  
pp. 794-803
Author(s):  
Zingade Sarika G. ◽  
Nagoba Shivappa N. ◽  
Agwane Shanta G. ◽  
Swami Avinash B.
Keyword(s):  
Fungal Infections ◽  
Tween 20 ◽  
Application Site ◽  
Pharmaceutical Sciences ◽  
Terbinafine Hydrochloride ◽  
Delivery Technique ◽  
Carbopol 940 ◽  
Diffusion Studies ◽  
Transdermal Permeability

The purpose of this study is to create and test a Terbinafine hydrochloride microemulgel. Terbinafine hydrochloride is an FDA-approved antifungal medication used to treat fungal infections on the skin. It's a BCS class II medication with little bioavailability. In the realm of pharmaceutical sciences, microemulgel has evolved into one of the most intriguing topical preparations. Microemulgel as a delivery technique has several advantages over simple traditional formulations, including simplicity of administration, increased residence duration at the application site, consistent drug release with improved bioavailability, superior thermodynamic stability, and excellent transdermal permeability. Terbinafine hydrochloride microemulgels were made with carbopol 940 and HPMC as gelling agents, oleic acid as an oil, parabens as a preservative, and tween 20 as an emulgent and penetration enhancer. The appearance, spreadability, homogeneity, viscosity, pH, percent drug content, and in vitro diffusion studies of the generated microemulgel formulation were all visually checked. The findings show that developing a terbinafine-containing microemulgel is more effective, but clinical efficacy must be determined through clinical trials.

scholarly journals FORMULATION AND EVALUATION OF ANTIFUNGAL CREAM OF CHLORPHENESIN

2021 ◽  
pp. 76-81
Author(s):  
VEENA S. ◽  
SURINDER KAUR ◽  
GURURAJ KULKARNI
Keyword(s):  
Fungal Infections ◽  
Dosage Forms ◽  
Skin Infections ◽  
Topical Drug Delivery ◽  
Cream Formulation ◽  
Diffusion Studies ◽  
In Vitro Diffusion ◽  
Materials Used ◽  
Routes Of Drug Administration

Objective: The main aim of our research was to develop an Antifungal cream formulation consisting of Chlorphenesin for the treatment of Fungal infections. Topical route is the most suitable route for skin infections. Methods: The development of topical drug delivery systems designed to have systemic effects appears to be beneficial for a number of drugs on account of several advantages over conventional dosage forms(or) routes of drug administration. An Antifungal cream formulation consisting of Chlorphenesin was prepared. Results: The formulation was subjected to in vitro diffusion studies. Microbiological studies were performed to find out the safety of materials used in the formulation. Conclusion: The developed cream consisting of Cholrphnesin was found to be safe and effective for the treatment of fungal infection.

scholarly journals Formulation and Evaluation of Galantamine Hydrobromide Proniosome Gel for Alzheimer’s disease

2020 ◽  
Vol 10 (2-s) ◽  
pp. 68-74
Author(s):  
Mohammed Sarfaraz ◽  
Tanvi Goel ◽  
H. Doddayya
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Phase Separation ◽  
Oral Delivery ◽  
Tween 80 ◽  
Separation Method ◽  
Tween 20 ◽  
Drug Diffusion ◽  
Diffusion Studies

Galantamine hydrobromide is formulated in tablets and capsules prescribed through oral delivery for the treatment of Alzheimer’s disease. However, oral delivery of drugs can cause severe side effects such as nausea, vomiting, and gastrointestinal disturbance. In the present research work, Galantamine hydrobromide is formulated as proniosome gel by Coacervation phase separation method using different surfactants such as Tweens and Spans. Overall eight formulations were developed and evaluated for various parameters. The prepared gels were viewed by naked eye to observe the colour of gel. Microscopical observations of the gels showed vesicles of optimum size from 3.030 mm (P2) - 3.735 mm (P5). The gel also showed optimum rate of spontaneity in the range 9.60 mm3x1000 (P7) to 11.80 mm3x1000 (P4) and entrapment efficiency of vesicles in the range 66.15% (P5) to 86.92% (P3). The gels had pH in suitable range of skin (5.92-6.9). The in vitro drug diffusion studies revealed that the drug diffusion was affected by the various surfactants used. The rank order of surfactant effect on in-vitro drug diffusion was Tween 80 > Tween 60 > Tween 40 >Tween 20 > Span 80 > Span 60 > Span 40 > Span 20. The proniosomal gel containing Tween 80 showed maximum drug diffusion (99.24%) and the gel containing Span 20 showed minimum drug diffusion (71.74%). FT-IR studies of optimized proniosome gel P8 revealed the absence of any chemical interactions between drug and carriers used. Keywords: Galantamine hydrobromide, Proniosome gel, Coacervation phase separation method,   Surfactants, in vitro drug diffusion studies.

scholarly journals Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

Molecules ◽  
2019 ◽  
Vol 24 (17) ◽  
pp. 3139 ◽  
Author(s):  
Pradeep Kumar Bolla ◽  
Carlos A. Meraz ◽  
Victor A. Rodriguez ◽  
Isaac Deaguero ◽  
Mahima Singh ◽  
...  
Keyword(s):  
Fungal Infections ◽  
Entrapment Efficiency ◽  
Tape Stripping ◽  
X Ray Diffraction ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Topical Bioavailability ◽  
Diffusion Studies ◽  
Permeation Studies

Global incidence of superficial fungal infections caused by dermatophytes is high and affects around 40 million people. It is the fourth most common cause of infection. Clotrimazole, a broad spectrum imidazole antifungal agent is widely used to treat fungal infections. Conventional topical formulations of clotrimazole are intended to treat infections by effective penetration of drugs into the stratum corneum. However, drawbacks such as poor dermal bioavailability, poor penetration, and variable drug levels limit the efficiency. The present study aims to load clotrimazole into ufosomes and evaluate its topical bioavailability. Clotrimazole loaded ufosomes were prepared using cholesterol and sodium oleate by thin film hydration technique and evaluated for size, polydispersity index, and entrapment efficiency to obtain optimized formulation. Optimized formulation was characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). Skin diffusion studies and tape-stripping were performed using human skin to determine the amount of clotrimazole accumulated in different layers of the skin. Results showed that the optimized formulation had vesicle size <250 nm with ~84% entrapment efficiency. XRD and DSC confirmed the entrapment of clotrimazole into ufosomes. No permeation was observed through the skin up to 24 h following the permeation studies. Tape-stripping revealed that ufosomes led to accumulation of more clotrimazole in the skin compared to marketed formulation (Perrigo). Overall, results revealed the capability of ufosomes in improving the skin bioavailability of clotrimazole.

Formulation Development of Diclofenac Sodium Emulgel Using Aloe vera Gel for Transdermal Drug Delivery System

2017 ◽  
Vol 10 (5) ◽  
pp. 3858-3865 ◽  
Author(s):  
Thanushree H.R. ◽  
Kiran Kumar G B ◽  
Ankit Acharya
Keyword(s):  
Side Effects ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Aloe Vera ◽  
Tween 20 ◽  
Release Kinetic ◽  
Formulation Development ◽  
Diffusion Studies ◽  
In Vitro Diffusion

Diclofenac sodium has many side effects like nausea, vomiting, GIT disorders. These side effects can be reduced by converting into emulgel formulations. The emulgel formulation of Diclofenac Sodium was prepared by incorporation method, using span 20 and tween 20 as non-ionic surfactants, clove oil and cinnamon oil as penetration enhancers, Aloe vera as a gel base and sesame oil as a solvent. The prepared emulgel formulations were evaluated for compatibility study, physical examination, viscosity, spreadability, in vitro diffusion studies, various release kinetic studies and stability studies. In vitro diffusion studies were carried out using cellophane membrane, results showed that emulgel formulations (F2-F7) showed higher cumulative percent drug release (49-65%) compared to normal gel (48%) and marketed gel (35%). Results of in vitro diffusion studies showed that formulation F3 and F6 exhibited 64% and 65% drug release respectively over a period of 6 hrs. In conclusion, a physiochemical stable diclofenac emulgel was formulated, which could deliver significant amount of drug across the skin in steady-state manner for the prolong period of time in the treatment of osteoarthritis.

scholarly journals Preparation and characterizations of glyceryl oleate ufasomes of terbinafine hydrochloride: a novel approach to trigger Candida albicans fungal infection

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Sankha Bhattacharya
Keyword(s):  
Antifungal Activity ◽  
Zeta Potential ◽  
Fungal Infection ◽  
Fungal Infections ◽  
Skin Permeation ◽  
Morphological Characteristics ◽  
Terbinafine Hydrochloride ◽  
Novel Approach ◽  
In Vitro Antifungal Activity

Abstract Background Worldwide fungal infection cases are increasing by leaps and bounds. The patients who are immunocompromised, i.e., cancer and AIDS, are more susceptible to different types of fungal infections like cutaneous candidiasis and its associate infections. The available treatment for such a disease is creams, gels, etc. However, due to the lack of penetrability and higher systematic absorption, these formulations have reported many side effects. To overcome such challenges, various novel drug delivery systems were introduced. The present research focused on the preparation of glyceryl oleate ufasomes of terbinafine hydrochloride using the film hydration method. Result The prepared formulations were characterized for globular size (nm), zeta potential (mV), PDI, morphological characteristics, thermal behavior, in vitro drug release, in vitro antifungal activity, and in vitro skin permeation retention studies. After suitable formulation optimization using thin-film hydration method, 3:7 drug to glyceryl oleate ratio, UF3 formulation was found to produce higher drug entrapment efficacy (52.45 ± 0.56%), stable anionic zeta potential (− 33.37 ± 0.231 mV), desired globular size (376.5 ± 0.42 nm), and decent polydispersity index (0.348 ± 0.0345). Diffusion-controlled and zero-order sustained release profile was observed in the optimized UF3 batch. From the 5 days in vitro antifungal activity studies, it confirmed that UF3 ufasomes possessed good applicability in more prolonged therapy. Conclusion From the current investigation, it can be concluded that glyceryl oleate ufasomes of terbinafine hydrochloride could be an excellent approach to treat topical fungal infections.

Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Size Distribution ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Glycol Succinate ◽  
Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

Potential of Nanoparticles in Combating Candida Infections

2019 ◽  
Vol 16 (5) ◽  
pp. 478-491 ◽  
Author(s):  
Faizan Abul Qais ◽  
Mohd Sajjad Ahmad Khan ◽  
Iqbal Ahmad ◽  
Abdullah Safar Althubiani
Keyword(s):  
Targeted Delivery ◽  
Recent Progress ◽  
Antifungal Agents ◽  
Fungal Infections ◽  
Fold Increase ◽  
Antifungal Drugs ◽  
Low Toxicity ◽  
Candida Infections ◽  
Made In

Aims: The aim of this review is to survey the recent progress made in developing the nanoparticles as antifungal agents especially the nano-based formulations being exploited for the management of Candida infections. Discussion: In the last few decades, there has been many-fold increase in fungal infections including candidiasis due to the increased number of immunocompromised patients worldwide. The efficacy of available antifungal drugs is limited due to its associated toxicity and drug resistance in clinical strains. The recent advancements in nanobiotechnology have opened a new hope for the development of novel formulations with enhanced therapeutic efficacy, improved drug delivery and low toxicity. Conclusion: Metal nanoparticles have shown to possess promising in vitro antifungal activities and could be effectively used for enhanced and targeted delivery of conventionally used drugs. The synergistic interaction between nanoparticles and various antifungal agents have also been reported with enhanced antifungal activity.

Smart Gn-Keto Nanohybrid Embedded Topical System for Effective Management of Dermatophytosis

2019 ◽  
Vol 9 (1) ◽  
pp. 21-28
Author(s):  
Nisha Sharma ◽  
Shashikiran Misra
Keyword(s):  
Antifungal Activity ◽  
Fungal Infections ◽  
High Surface ◽  
High Surface Area ◽  
Vital Role ◽  
Common Disease ◽  
Microdilution Method ◽  
Enhanced Solubility ◽  
Bioactive Agents

Background and Objectives: Dermatophytosis (topical fungal infection) is the 4th common disease in the last decade, affecting 20-25% world’s population. Patients of AIDS, cancer, old age senescence, diabetes, cystic fibrosis become more vulnerable to dermatophytosis. The conventional topical dosage proves effective as prophylactic in preliminary stage. In the advanced stage, the therapeutics interacts with healthy tissues before reaching the pathogen site, showing undesirable effects, thus resulting in pitiable patient compliance. The youngest carbon nano-trope “Graphene” is recently used to manipulate bioactive agents for therapeutic purposes. Here, we explore graphene via smart engineering by virtue of high surface area and high payload for therapeutics and developed graphene–ketoconazole nanohybrid (Gn-keto) for potent efficacy towards dermatophytes in a controlled manner. </P><P> Methods: Polymethacrylate derivative Eudragit (ERL100 and ERS 100) microspheres embedded with keto and Gn-keto nanohybrid were formulated and characterized through FTIR, TGA, and SEM. In vitro drug release and antifungal activity of formulated Gn-keto microspheres were assessed for controlled release and better efficacy against selected dermatophytes. </P><P> Results: Presence of numerous pores within the surface of ERL100 microspheres advocated enhanced solubility and diffusion at the site of action. Controlled diffusion across the dialysis membrane was observed with ERS100 microspheres owing to the nonporous surface and poor permeability. Antifungal activity against T. rubrum and M. canis using microdilution method focused on a preeminent activity (99.785 % growth inhibition) of developed nanohybrid loaded microspheres as compared to 80.876% of keto loaded microspheres for T. rubrum. The culture of M. canis was found to be less susceptible to formulated microspheres. Conclusion: Synergistic antifungal activity was achieved by nanohybrid Gn-Keto loaded microspheres against selected topical fungal infections suggesting a vital role of graphene towards fungi.

Recent Advances in Curcumin Nanocarriers for the Treatment of Different Types of Cancer with Special Emphasis on In Vitro Cytotoxicity and Cellular Uptake Studies

2020 ◽  
Vol 10 (5) ◽  
pp. 577-590
Author(s):  
Jai B. Sharma ◽  
Shailendra Bhatt ◽  
Asmita Sharma ◽  
Manish Kumar
Keyword(s):  
Cancer Cells ◽  
Cellular Uptake ◽  
Anticancer Agents ◽  
Targeted Delivery ◽  
In Vitro Cytotoxicity ◽  
Curcumin Nanoparticles ◽  
Cytotoxicity Studies ◽  
Delivery Technique ◽  
Different Types

Background: The potential use of nanocarriers is being explored rapidly for the targeted delivery of anticancer agents. Curcumin is a natural polyphenolic compound obtained from rhizomes of turmeric, belongs to family Zingiberaceae. It possesses chemopreventive and chemotherapeutic activity with low toxicity in almost all types of cancer. The low solubility and bioavailability of curcumin make it unable to use for the clinical purpose. The necessity of an effective strategy to overcome the limitations of curcumin is responsible for the development of its nanocarriers. Objective: This study is aimed to review the role of curcumin nanocarriers for the treatment of cancer with special emphasis on cellular uptake and in vitro cytotoxicity studies. In addition to this, the effect of various ligand conjugated curcumin nanoparticles on different types of cancer was also studied. Methods: A systematic review was conducted by extensively surfing the PubMed, science direct and other portals to get the latest update on recent development in nanocarriers of curcumin. Results: The current data from recent studies showed that nanocarriers of curcumin resulted in the targeted delivery, higher efficacy, enhanced bioavailability and lower toxicity. The curcumin nanoparticles showed significant inhibitory effects on cancer cells as compared to free curcumin. Conclusion: It can be concluded that bioavailability of curcumin and its cytotoxic effect to cancer cells can be enhanced by the development of curcumin based nanocarriers and it was found to be a potential drug delivery technique for the treatment of cancer.

scholarly journals Conifers Phytochemicals: A Valuable Forest with Therapeutic Potential

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3005
Author(s):  
Kanchan Bhardwaj ◽  
Ana Sanches Silva ◽  
Maria Atanassova ◽  
Rohit Sharma ◽  
Eugenie Nepovimova ◽  
...  
Keyword(s):  
Experimental Data ◽  
Potential Role ◽  
Therapeutic Potential ◽  
Fungal Infections ◽  
Cell Damage ◽  
Cancer Growth ◽  
Naturally Occurring ◽  
Antioxidant Effects

Conifers have long been recognized for their therapeutic potential in different disorders. Alkaloids, terpenes and polyphenols are the most abundant naturally occurring phytochemicals in these plants. Here, we provide an overview of the phytochemistry and related commercial products obtained from conifers. The pharmacological actions of different phytochemicals present in conifers against bacterial and fungal infections, cancer, diabetes and cardiovascular diseases are also reviewed. Data obtained from experimental and clinical studies performed to date clearly underline that such compounds exert promising antioxidant effects, being able to inhibit cell damage, cancer growth, inflammation and the onset of neurodegenerative diseases. Therefore, an attempt has been made with the intent to highlight the importance of conifer-derived extracts for pharmacological purposes, with the support of relevant in vitro and in vivo experimental data. In short, this review comprehends the information published to date related to conifers’ phytochemicals and illustrates their potential role as drugs.

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