scholarly journals Design, fabrication and evaluation of clotrimazole loaded polymeric microsphere based in situ ophthalmic gel

2021 ◽  
Vol 12 (2) ◽  
pp. 1003-1008
Author(s):  
Manish Kumar Gupta ◽  
Vipul Sansare ◽  
Birendra Shrivastava ◽  
Santosh Jadhav
Keyword(s):  
Particle Size ◽  
Antifungal Activity ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
Methyl Cellulose ◽  
Polymeric Microsphere ◽  
In Vitro Antifungal Activity

The present study was started with aim to design clotrimazole loaded polymeric microsphere based in situ  ophthalmic gel for management of corneal fungal infections. The clotrimazole loaded microsphere was fabricated using various percentage of polylactide-co-glycolide polymer by solvent evaporation technique and evaluated for particle size, zeta potential and encapsulation efficiency. The polyvinyl alcohol was used as stabilizer. The formulation batch which showed good particle size and entrapment efficiency was selected for further study. The in situ  ophthalmic gel of optimized drug loaded microsphere was formulated using various ratios of sodium alginate and hydroxy propyl methyl cellulose. The formulated gel was evaluated with respect to pH, in vitro gelling capacity, clarity, viscosity, in vitro  antifungal activity and in vitro transcorneal permeation behavior. The fabricated drug loaded microspheres revealed acceptable particle size, zeta potential and encapsulation efficiency. The prepared in situ  gels were clear and exhibited acceptable pH, rheological properties and in vitro  gelation. The drug loaded microsphere based gel revealed superior in vitro  antifungal activity against Aspergillus niger  than conventional formulation and sufficient drug permeation across goat cornea. Thus, formulated clotrimazole loaded microsphere based in situ gel based systems can be a promising approach for sustained ophthalmic delivery of antifungal agents.

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.

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.

scholarly journals FORMULATION AND EVALUATION OF CURCUMIN LOADED LIPOSOME AND ITS BIO-ENHANCEMENT

2019 ◽  
Vol 9 (4-A) ◽  
pp. 425-437
Author(s):  
Khushboo Verma ◽  
Jhakeshwar Prasad ◽  
Suman Saha ◽  
Surabhi Sahu
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
High Performance ◽  
Encapsulation Efficiency ◽  
Mean Particle Size ◽  
Liposome Formulation

The aim of this work was to develop and evaluate curcumin loaded liposome and its bio- enhancement. Curcumin was selected as a natural drug for liposome formulation. Curcumin show variety of biological activity but it also shows poor bioavailability due to low aqueous solubility (1 µg/ml), poor absorption and rapid metabolism so that piperine was selected as bio enhancer to improve curcumin bioavailability. Soy lecithin and cholesterol were used to prepared curcumin and curcumin-piperine loaded liposome at different ratio by thin film hydration method because of easy to perform, and high encapsulation rates of lipid. The all liposome formulations (F1-F5) were evaluated by mean particle size, polydispersity index, zeta potential, encapsulation efficiency and drug release. Bioavailability was also determined on rat. Blood samples were collected at specific intervals, and plasma was separated by ultracentrifugation. Plasma was analyzed by high-performance liquid chromatography at 425 nm taking acetonitrile: water (75:25 v/v) acidified with 2% acetic acid as a mobile phase at a flow rate of 0.5 ml/min using C18 column. The mean particle size was found in the range between 800-1100 that indicate liposome are large unilamellar vesical types. By zeta potential study its conform that the all formulation was stable. The encapsulation efficiency of all liposome formulation are varied between 59-67%. In vitro drug release was analyse in 7.4 pH phosphate buffer, the maximum %CDR observed at the 12 hrs., and formulation are follow sustained release thus they reduce metabolism, good absorption rate which improve bioavailability of drug. From in-vivo study, it is clear that curcumin-piperine liposomal formulation, increases Cmax, area under the curve, and mean residence time significantly as compared to pure curcumin and pure curcumin liposome. Keywords: liposome; Curcumin; Piperine, Thin film hydration method; Bioavailability

scholarly journals SYNTHESIS, SPECTRAL CHARACTERIZATION AND ANTIFUNGAL STUDIES ON LANTHANUM (III) AND PRASEODYMIUM (III) COMPLEXES WITH N2O2DIAZADIOXAMACROCYCLES

2020 ◽  
Vol 8 (11) ◽  
pp. 01-10
Author(s):  
Priti Tripathi ◽  
◽  
Akhilesh Kumar Srivastava ◽  
Om Prakash Pandey ◽  
Soumitra Kumar Sengupta ◽  
...  
Keyword(s):  
Particle Size ◽  
Biological Activity ◽  
Antifungal Activity ◽  
Schiff Bases ◽  
Lanthanide Complexes ◽  
Scherrer Formula ◽  
In Vitro Antifungal Activity ◽  
Nm Range

A novel series of N2O2diazadioxamacrocyclic complexes of type [Ln(mac)Cl3] has been synthesized via the condensation reactions of a 3-(phenyl/substituted phenyl)-4-amino-5-hydrazino-1,2,4-triazoles with salicylaldehyde and 1,4-dibromobutane in the presence of lanthanum(III) chloride and praseodymium(III) chloride in ethanol. All the newly synthesized compounds were characterized by elemental analysis, electronic absorption, IR, 1HNMR. The particle size of the complexes have been calculated from XRD spectral using Debye-Scherrer formula and these are found to be in 29-31 nm range. In order to evaluate the biological activity of Schiff bases and to assess the role of Ln(III) and Pr(III) metal on biological activity, the hydrazine triazole Schiff bases and their lanthanide complexes have been studies for in vitro antifungal activity against Fusariumoxysporum, CurvularialunataandColletotrichumfalcatum.

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.

Antifungal action of chlorogenic acid against pathogenic fungi, mediated by membrane disruption

2010 ◽  
Vol 82 (1) ◽  
pp. 219-226 ◽  
Author(s):  
Woo Sang Sung ◽  
Dong Gun Lee
Keyword(s):  
Antifungal Activity ◽  
Chlorogenic Acid ◽  
Mode Of Action ◽  
Fungal Infections ◽  
Pathogenic Fungi ◽  
Membrane Dynamics ◽  
Independent Manner ◽  
Antifungal Action ◽  
In Vitro Antifungal Activity

Chlorogenic acid is a polyphenol compound, derived from several fruit and plants. The aim of this study was to assess the in vitro antifungal activity of chlorogenic acid and its mode of action. The results indicate that chlorogenic acid exhibits antifungal activities against certain pathogenic fungi in an energy-independent manner, without any hemolytic effect on human erythrocytes. To elucidate the antifungal mode of action of chlorogenic acid, flow cytometry analysis by using DiBAC4(3) and changes in membrane dynamics using 1,6-diphenyl-1,3,5-hexatriene (DPH) were performed with Candida albicans. The results suggest that chlorogenic acid may exert antifungal activity by disrupting the structure of the cell membrane. It is demonstrated that chlorogenic acid is a valid lead compound for the development of bioactive alternatives for treatment of fungal infections.

scholarly journals Formulation and in vitro Characterization of Donepezil-loaded Chitosan Nanoparticles

2020 ◽  
pp. 10-16
Author(s):  
Muhammad Wahab Amjad ◽  
Nawaf Mohamed Alotaibi
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Sonication Time ◽  
In Vitro Characterization ◽  
Constant Rate

Millions of people are affected globally by alzheimer’s disease and it is regarded as a dangerous progressive medical and socio-economic burden. The drug delivery to brain is hindered due to the presence of blood brain barrier. Nanoparticle mediated drug delivery is a promising approach in this regard. Chitosan is a hydrophilic polysaccharide polymer of N-acetylglycosamine and glucosamine. Owing to its biodegradability, nontoxicity and biocompatibility it is regarded as a safe excipient. The aim of the study was to fabricate donepezil-loaded sustained release chitosan nanoparticles as a simple way to deliver nano-drugs to the brain. The nanoparticles were fabricated using ionic gelation method using different concentrations of Sodium tripolyphosphate (TPP) and chitosan. The fabricated nanoparticles were assessed for particle size, zeta potential, encapsulation efficiency and in vitro drug release. The effect of sonication time on the particle size of nanoparticles was also studied. The nanoparticles exhibited mean particle size (between 135-1487 nm) and zeta potential (between +3.9-+38mV) depending on chitosan and TPP concentration used. The rise in the sonication time from 25 to 125 sec exhibited a decrease in particle size. The encapsulation efficiency was found to be in the range of 39.1-74.4%. Sustained and slow release of donepezil at a constant rate was exhibited from nanoparticles. The nanoparticles show potential to deliver donepezil to brain with enhanced encapsulation efficiency.

SYNERGISTIC EFFECT OF NIGELLA OIL AND CLOTRIMAZOLE AS ETHOSOMAL GEL FOR IMPROVED TREATMENT OF FUNGAL INFECTIONS

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (04) ◽  
pp. 45-49
Author(s):  
M Momin ◽  
K. Butte ◽  
A. D’Souza ◽  
Keyword(s):  
Thin Film ◽  
Antifungal Activity ◽  
Fungal Infections ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Synergistic Action ◽  
Physiochemical Parameters ◽  
Anti Fungal ◽  
In Vitro Antifungal Activity

The aim of this research work was to develop an ethosomal gel containing nigella oil encapsulated with clotrimazole (CLT) for improved antifungal activity. The ethosomes were prepared using soya lecithin (SpC) and Nigella oil (NO) as lipids by thin film hydration and they exhibited a particle size of 136±69 nm with an entrapment efficiency of 65.44±1.08 %. CLT ethosomal gel exhibited controlled release of CLT with a steady flux of 7.20mcg/cm2/h across cellophane membrane. The ethosomal gel was stable for 180 days with no significant change in physiochemical parameters. In vitro antifungal activity demonstrated a synergistic action of CLT and NO against the fungal strains compared to plain CLT and NO. This signifies that the combination of NO and CLT in an ethosomal gel has tremendous potential to serve as a synergistic topical anti-fungal preparation than simple ethosomal formulation of CLT.

scholarly journals COMPARATIVE MUCOPENETRATION ABILITY OF METRONIDAZOLE LOADED CHITOSAN AND PEGYLATED CHITOSAN NANOPARTICLES

2017 ◽  
Vol 10 (6) ◽  
pp. 125
Author(s):  
Sukhbir Kaur ◽  
Chawla V ◽  
Narang R K ◽  
Aggarwal G
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Chitosan Nanoparticles ◽  
Methyl Cellulose ◽  
Fluorescein Isothiocyanate ◽  
Entrapment Efficiency ◽  
Spherical Particles ◽  
Detachment Force

Objective: The objective of this study is to compare the mucopenetration ability of metronidazole loaded chitosan (CS) and pegylated CS nanoparticles.Methods: Nanoparticles were prepared by ionic gelation technique using negatively charged pH sensitive polymer, hydroxyl propyl methyl cellulose phthalate with positively charged CS and methoxy polyethylene glycol-grafted-CS (mPEG-g-CS). mPEG-g-CS was synthesized by formaldehyde linkage method and characterized by Fourier transform infrared spectroscopy. The optimized formulations were compared for morphology, particle size, polydispersity index (PDI), entrapment efficiency, bioadhesion detachment force, in vitro and in vivo mucopenetration for CS-mPEG-g-CS nanoparticles.Results: The morphological assessment revealed smooth spherical particles with uniform dispersions. The optimized formulations particle size was found to be 202.7±27 nm and 294.1±46 nm, zeta potential 26.94±2.4 mV and 6.0±1.3 mV. PDI 0.231 and 0.268, entrapment efficiency 79.8±5.4% and 83.6±9.7%, bio-adhesion detachment force 14.98*103 dyne/cm2 and 10.67*103 dynes/cm2, in vitro mucopenetration 78% and 98% for CS-mPEG-g-CS, respectively. The qualitative in vivo mucopenetration result confirms retention of fluorescein isothiocyanate (FITC) labeled mPEG-g-CS nanoparticles till 24 hrs.Conclusion: Nanoparticles with lesser zeta potential and mucoadhesion showed higher mucosal penetration which is evident from FITC labeled histopathological mucus penetration test. Studies thus provided evidence that planned pharmaceutical strategies open new vistas for effective treatment of mucosal infections.

scholarly journals Design and Evaluation of Natamycin Nanocrystals Loaded In Situ Gel for Ophthalmic Administration

2021 ◽  
pp. 307-324
Author(s):  
Roshni Das ◽  
Marina Koland ◽  
S. M. Sindhoor
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Ex Vivo Permeation

Background: Natamycin belongs to a large group of naturally occurring polyene antifungal antibiotics derived from Streptomyces natalensis. Natamycin has a restrictive pharmaceutical role because of its extremely low aqueous solubility, which severely reduces the bioavailability of the drug. To improve the absorption of the drug, nanocrystals of natamycin were prepared and incorporated into in situ gel. Aim: To improve the solubility and absorption of natamycin nanocrystals by preparing nanocrystal in situ gel of natamycin for ophthalmic delivery Methodology: Natamycin nanocrystal was prepared using Sono-Precipitation method. Box-Behnken approach was employed to assess the influence of independent variables, namely concentration of stabilizer, sonication time and amplitude on particle size and zeta potential of the prepared nanocrystal. Optimized natamycin nanocrystal in situ gel formulations was characterized for various parameters like pH, viscosity, drug content, in vitro drug release and ex vivo permeation studies. Results: The optimized formulation of natamycin nanocrystal with a particle size of  293.9nm and zeta potential -14.6mV was incorporated into in situ gels. The pH triggered in situ gel was prepared using Carbopol and Hydroxypropyl methylcellulose (HPMC)., which showed clear preparation, pH of the formulation was closed to the pH of tear fluid, i.e., 7.4, viscosity showed pseudoplastic behaviour with immediate gelation remained for an extended period, and the drug content was around 99.70%. From the characterizations given above, PF-4 was optimized and evaluated for In vitro drug release showing slow and sustained release when compared to the marketed formulation and followed first-order kinetics with the diffusion-controlled mechanism. Ex vivo permeation through goat's cornea of PF-4 showed better permeation than marketed formulation. The stability studies of PF-4 showed that formulation was stable at the appropriate condition. Conclusion: Nanocrystals formulations of natamycin was successfully formulated and incorporated into in situ gels. Further in vivo studies need to be carried out for confirmation of pharmacological activity

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