POTENTIATING MICONAZOLE ACTIVITY WITH CLOVE OIL AND CHITOSAN IN MICROEMULSION BASED GEL FOR TREATMENT OF FUNGAL INFECTION

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (4) ◽  
pp. 74-77
Author(s):  
Durga Pandey ◽  
◽  
Rajni Rajak ◽  
Alok Mahor ◽  
Surendra Jain ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Fungal Infections ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Clove Oil ◽  
In Vitro Drug Release ◽  
Micron Size ◽  
Microemulsion Based Gel ◽  
Spherical Droplets

The study aimed to investigate the in vitro antifungal activity of miconazole entrapped in microemulsion based gel with clove oil as permeation enhancer and chitosan as antifungal agent. SEM confirmed spherical droplets of microemulsion in the 2 micron size range. The viscosity of emugel was 2251 cP, excellent spreadability 31.27 ±0.219 g.cm/cc as compared to marketed formulation. pH was 5.528 ± 0.032, homogeneity was excellent and drug content was 98 % in optimized batch. No drug-excipients interaction was reported in FTIR spectroscopy. In vitro drug release showed 94.8 % in 6 h. Ex vivo skin permeation showed higher steady state flux than conventional cream. Antifungal activity on Candida albicans showed a zone of inhibition more than that of marketed preparation. Thus, it can be concluded that the formulation may hold some promise for the treatment of severe fungal infections.

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.

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.

Preparation, characterizations and in vitro evaluation of Econazole-Btamethasone loaded solid lipid nanoparticles (SLNs)

2021 ◽  
pp. 1-12
Author(s):  
Kamran Khan ◽  
Shefaat Ullah Shah ◽  
Yusuf S. Althobaithi ◽  
Kifayat Ullah Shah ◽  
Aman Ullah ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Side Effects ◽  
Drug Release ◽  
Oral Delivery ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
Ex Vivo ◽  
Sem Images ◽  
Drug Content

Tremendous increase of fungal infections in hospitalized or immune compromised patients has been reported from the last two decades. These infections are commonly treated using econazole and miconazole that have shorter half-life and produce severe side effects. All such issues can be addressed using targeted drug delivery. We developed SNLs based formulation for the treatment of mycosis. The high pressure homogenization method was employed for formulation followed by characterization, assay for antifungal activity, in vitro drug release and ex vivo permeation. The particle size of Econazole-Betamethasone-loaded SLNs, Econazole-loaded SLNs, Betamethasone-loaded SLNs and Blank SLNs were 377.4±23 nm, 298.7±9 nm, 177.7±15 nm and 113.4±6 nm respectively. The SEM images displayed that droplets are uniform and spherical in shape which ranged from 113.4±6 to 377.4±23 nm. In DSC, the SLNs formulation showed endothermic peak at 185.2 °C±0.9. Drug content of Econazole loaded SLNs was 82±0.1 and its entrapment efficiency was approximately 90.4±0.2. Betamethasone SLNs displayed highest drug content which was 83.5±0.4 while encapsulation efficiency of same formulation was 94.2±0.4. The Econazole and Betamethasone combined SLNs exhibited drug content of 80±0.3 while its encapsulation efficiency was 93.1±0.5. E-SLNs have significantly high drug release (p <  0.05) as compared to other formulation B-SLNs and EB-SLNs.The Econazole loaded formulations displayed antifungal activity with no synergistic or antagonistic effect with each other. Drug permeation from Econazole SLNs, Betamethasone SLNs and combined Econazole and Betamethasone SLNs was 45%, 40% and 38% respectively. Overall, SLN’s are an effective carrier for topical delivery of antifungals agents and that may be helpful in bypassing the serious side effects associated with oral delivery.

scholarly journals FORMULATION OF KETOCONAZOLE LOADED NANO DISPERSIVE GEL USING SWOLLEN MICELLES TECHNIQUE AND ITS IN VITRO CHARACTERIZATION

2018 ◽  
Vol 10 (3) ◽  
pp. 162
Author(s):  
Mohammad Irshad Reza ◽  
Divya Goel ◽  
Rahul Kumar Gupta ◽  
Musarrat Hussain Warsi
Keyword(s):  
Antifungal Activity ◽  
Drug Release ◽  
Ex Vivo ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Permeation Study ◽  
Ex Vivo Permeation ◽  
Enhanced Solubility ◽  
Ex Vivo Permeation Study

Objective: The objective of the present work was to formulate and characterize nano dispersive gel (NDG) for topical delivery of water-insoluble antifungal agent ketoconazole in order to enhance its solubility, penetration through the skin and antifungal activity.Methods: Nano dispersion of the drug was first prepared by swollen micelles technique (SMT) using tween 80 and chloroform which is then incorporated into the gel using carbopol 934. Ten formulations of ketoconazole loaded NDG was prepared and characterized for different physicochemical parameters like homogeneity, pH, spreadability, extrudability, practical yield, drug content, in vitro drug release, ex vivo permeation study, and biological parameter antifungal activity.Results: The formulated topical preparation exhibit pH in the range of 6.5 to 7.4, and unveiled excellent homogeneity, spreadability and extrudability. Out of 10 formulations, formulation F4 showed maximum drug content of 95.56±1.13% and practical yield of 97.23±0.51%. The in vitro drug release studies were performed using pH 7.4 phosphate buffer. Formulation F4 showed best in vitro drug release 96.52±0.52% at the end of 24 h of study. Ex vivo permeation study of formulation F4 carried out using franz diffusion cell, also manifested good permeation and flux of drug across the chicken skin. Antifungal activity test of formulation F4 was carried out by the cup plate method using Aspergillus niger strain against marketed ketoconazole unveiled higher antifungal activity than marketed one.Conclusion: The study confirmed formulation F4 to be an optimized and promising formulation for the effective treatment of topical fungal infections with enhanced solubility and penetration through the skin.

scholarly journals Glimepiride-Loaded Nanoemulgel; Development, In Vitro Characterization, Ex Vivo Permeation and In Vivo Antidiabetic Evaluation

Cells ◽  
2021 ◽  
Vol 10 (9) ◽  
pp. 2404
Author(s):  
Fizza Abdul Razzaq ◽  
Muhammad Asif ◽  
Sajid Asghar ◽  
Muhammad Shahid Iqbal ◽  
Ikram Ullah Khan ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
Tween 80 ◽  
Hypoglycemic Activity ◽  
Clove Oil ◽  
Promising Alternative ◽  
In Vitro Skin Permeation ◽  
Nano Emulsion

Glimepiride (GMP), an oral hypoglycemic agent is extensively employed in the treatment of type 2 diabetes. Transdermal delivery of GMP has been widely investigated as a promising alternative to an oral approach but the delivery of GMP is hindered owing to its low solubility and permeation. The present study was designed to formulate topical nanoemulgel GMP system and previously reported solubility enhanced glimepiride (GMP/βCD/GEL-44/16) in combination with anti-diabetic oil to enhance the hypoglycemic effect. Nanoemulsions were developed using clove oil, Tween-80, and PEG-400 and were gelled using xanthan gum (3%, w/w) to achieve the final nanoemulgel formulations. All of the formulations were evaluated in terms of particle size, zeta potential, pH, conductivity, viscosity, and in vitro skin permeation studies. In vivo hypoglycemic activity of the optimized nanoemulgel formulations was evaluated using a streptozocin-induced diabetes model. It was found that a synergistic combination of GMP with clove oil improved the overall drug permeation across the skin membrane and the hypoglycemic activity of GMP. The results showed that GMP/βCD/GEL-44/16-loaded nanoemulgel enhanced the in vitro skin permeation and improved the hypoglycemic activity in comparison with pure and marketed GMP. It is suggested that topical nano emulsion-based GMP gel and GMP/βCD/GEL-44/16 could be an effective alternative for oral therapy in the treatment of diabetes.

Nanostructured lipid carrier-incorporated gel for efficient topical delivery of fluconazole

2021 ◽  
Author(s):  
Archana Patil ◽  
Vedangi Tuencar ◽  
Anand Gadad ◽  
Panchaxari Dandagi ◽  
Rajashree Masareddy
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carrier ◽  
Topical Drug Delivery ◽  
In Vitro Drug Release ◽  
Drug Permeability ◽  
Permeation Studies

Background: Nanostructured lipid carriers (NLCs) of fluconazole were prepared to improve permeability and thereby effective topical drug delivery. Materials and method: NLCs were prepared and evaluated, and then the optimized NLC suspension was incorporated into a gel that was further evaluated for topical drug delivery. Results and discussion: F-2 NLC formulation was optimized based on results of particle size (161.3 ± 1.385 nm), polydispersity index (0.401), zeta potential (-33 ± 0.46), entrapment efficiency (82.26 ± 0.91%) and in vitro drug release (76.40 ± 0.21%). Ex vivo skin permeation studies showed flux of F-2 gel and the comparison marketed gel as 0.21 and 0.18 mg/cm2/h, respectively. The in vitro antifungal study revealed significantly better activity compared with the marketed gel. Conclusion: Fluconazole NLCs increase drug permeability and proved to be effective in topical drug delivery.

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.

Formulation and Evaluation of Carbopol Gel Containing Liposomes of Ketoconazole. (Part-II)

2009 ◽  
Vol 1 (2) ◽  
Author(s):  
Rakesh Patel ◽  
Hardik Patel ◽  
Ashok Baria
Keyword(s):  
Antifungal Activity ◽  
Rat Skin ◽  
Albino Rat ◽  
In Vitro Drug Release ◽  
Carbopol Gel ◽  
Liposomal Formulations ◽  
Release Drug ◽  
In Vitro Permeation ◽  
In Vitro Antifungal Activity

The aim of this work was to prepare and evaluate the topical carbopol gel formulation containing ketoconazole encapsulated liposomes. Ketoconazole loaded liposomes were prepared by thin film hydration technique. The prepared liposomes were incorporated into 1% carbopol gel, and the systems were evaluated for in-vitro drug release, drug retention into skin and in-vitro antifungal activity. The in-vitro permeation of ketoconazole using wistar albino rat skin from liposomal gel was compared with that of plain drug gel and also with plain drug cream containing 2% w/w of ketoconazole. The release of ketoconazole from liposomal gel was much slower than from non liposomal formulations. Gel containing liposomal ketoconazole showed maximum antifungal activity after 30 hours over plain ketoconazole gel and cream formulations.

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.

scholarly journals Botanical Control of Citrus Green Mold and Peach Brown Rot on Fruits Assays Using a Persicaria acuminata Phytochemically Characterized Extract

Plants ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 425
Author(s):  
Melina G. Di Liberto ◽  
Gisela M. Seimandi ◽  
Laura N. Fernández ◽  
Verónica E. Ruiz ◽  
Laura A. Svetaz ◽  
...  
Keyword(s):  
Ecological Model ◽  
Fungal Infections ◽  
Ex Vivo ◽  
Central Area ◽  
Brown Rot ◽  
Phytopathogenic Fungi ◽  
Perennial Herb ◽  
Huh7 Cells ◽  
Gas Chromatography Mass Spectroscopy

Persicaria acuminata (Polygonaceae) is a perennial herb that grows in the central area of Argentina and it is commonly used by native populations to heal infected wounds and other conditions related to fungal infections. In this article, we explored the in vitro antifungal activity of its ethyl acetate extract against a panel of three fruit phytopathogenic fungi including: Penicillium digitatum, P. italicum, and Monilinia fructicola. The sesquiterpenes isolated from the extract were also evaluated against these strains, demonstrating that the dialdehyde polygodial was the responsible for this activity. In order to encourage the use of the extract rather than the pure compound, we displayed ex vivo assays using fresh oranges and peaches inoculated with P. digitatum and M. fructicola, respectively, and subsequently treated by immersion with an extract solution of 250 and 62.5 µg/mL, respectively. There were no statistically significant differences between the treatments with commercial fungicides and the extract over the control of both fruit rots. The concentration of the active compound present in the extract used on fruit experiments was determined by Gas Chromatography-Mass Spectroscopy. Finally, cytotoxicity evaluation against Huh7 cells showed that P. acuminata extract was less cytotoxic than the commercial fungicides at the assayed concentrations. After these findings we could conclude that a chemically characterized extract of P. acuminata should be further developed to treat fungal diseases in fruits from an agro-ecological model.

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