scholarly journals Thermoreversible Gel-Loaded Amphotericin B for the Treatment of Dermal and Vaginal Candidiasis

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 312 ◽  
Author(s):  
Lilian Sosa ◽  
Ana Cristina Calpena ◽  
Marcelle Silva-Abreu ◽  
Lupe Carolina Espinoza ◽  
María Rincón ◽  
...  
Keyword(s):  
Drug Release ◽  
Amphotericin B ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Vaginal Candidiasis ◽  
Vaginal Mucosa ◽  
High Porosity ◽  
Candida Spp ◽  
Thermoreversible Gel ◽  
Antifungal Efficacy

The present study was designed to develop a thermoreversible gel of Pluronic (P407) loaded amphotericin B (AmB-gel) for the dermal and vaginal treatment of candidiasis. P407 was used as a copolymer to exploit potential advantages related to increasing drug concentration in the tissue layer in order to provide a local effect. Parameters including internal structure, swelling, porosity, and short-term stability were determined. In addition, drug release profile and ex vivo skin and vaginal permeation studies were carried out. Antifungal efficacy was evaluated against strains of Candida spp. and atomic force microscopy (AFM) supported the results. The tolerance of AmB-gel was studied by evaluating biomechanical properties of skin and determining the irritation level in scarified rabbit skin supported by histological analysis. Results confirmed the development of a thermoreversible AmB-gel with high porosity exhibiting Newtonian behavior at 4 °C and pseudoplasticity at 32 °C as well as optimal stability for at least 90 days. The Amb-gel provided a sustained drug release following a Boltzmann sigmoidal model. Non permeation was observed in skin and vaginal mucosa, showing a high retained amount of AmB of 960.0 and 737.3 µg/g/cm2, respectively. In vitro antifungal efficacy showed that AmB-gel was more effective than Free-AmB in inhibiting strains of Candida spp. and these results were corroborated by AFM. Finally, tolerance studies showed that its application did not induce skin irritation nor alter its biophysical properties. Together, these results confirmed that AmB-gel could be proposed as a promising candidate for the clinical status in the treatment of skin and vaginal candidiasis.

scholarly journals Polishing the Therapy of Onychomycosis Induced by Candida spp.: Amphotericin B–Loaded Nail Lacquer

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 784
Author(s):  
Aleph M. S. Souza ◽  
Renato C. A. Ribeiro ◽  
Gleyse K. L. O. Pinheiro ◽  
Francisco I. Pinheiro ◽  
Wógenes N. Oliveira ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Ex Vivo ◽  
Drug Loading ◽  
Drug Bioavailability ◽  
Candida Spp ◽  
Drying Time ◽  
Analytical Method Validation ◽  
Nail Lacquer ◽  
In Vitro Adhesion

Onychomycosis induced by Candida spp. has several limitations regarding its treatment. Nail lacquers display the potential to overcome these drawbacks by providing therapeutic compliance and increasing local drug bioavailability. Thus, this work aimed to produce a nail lacquer loaded with Amphotericin B (AmB) and evaluate its performance. The AmB-loaded nail lacquer was produced and preliminarily characterized. An AmB quantification method was developed. Stability, drug release, permeability and anti-Candida activity assays were conducted. The analytical method validation met the acceptance criteria. The drug loading efficiency was 100% (0.02 mg/g of total product), whereas the AmB stability was limited to ≅ 7 days (≅ 90% remaining). The nail lacquer displayed a drying time of 187 s, non-volatile content of around 20%w/w, water-resistance of approximately 2%w/w of weight loss and satisfactory in vitro adhesion. Moreover, the in vitro antifungal activity against different Candida spp. strains was confirmed. The AmB release and the ex vivo permeability studies revealed that AmB leaves the lacquer and permeates the nail matrix in 47.76 ± 0.07% over 24 h. In conclusion, AmB-loaded nail lacquer shows itself as a promising extemporaneous dosage form with remarkable anti-Candida activity related to onychomycosis.

Transdermal Delivery of Ondansetron HCl from Thermoreversible Gel Containing Nanocomposite

2019 ◽  
Vol 4 (2) ◽  
pp. 137-147 ◽  
Author(s):  
Rabinarayan Parhi ◽  
Surya Santhosh Reddy ◽  
Suryakanta Swain
Keyword(s):  
Drug Release ◽  
Mechanical Strength ◽  
Ex Vivo ◽  
Poloxamer 407 ◽  
Gelation Temperature ◽  
Permeation Study ◽  
Ex Vivo Permeation ◽  
Model Animal ◽  
Ex Vivo Permeation Study ◽  
Thermoreversible Gel

Background: Application of thermoreversible gel can be a solution to the low residence time of the topical dosage forms such as normal gel, ointment and cream on the skin surface. Addition of another polymer and a nanocomposite can improve the poor mechanical strength and fast drug release of poloxamer 407 (POL 407) gel. Therefore, it is essential to add xanthan gum (XG) and graphene oxide (GO, thickness 1-2 nm, lateral dimension 1-5 µm) to POL 407 gel to enhance the mechanical strength and to sustain the drug release from the gel. Methods: Thermal gel of ondansetron hydrochloride (OSH) containing nanocomposite was prepared by adopting cold method. Interaction between drug and polymers was studied using FTIR method, morphological investigation was carried out by optical and scanning electron microscopy method, and rheological study was performed employing rotational rheometer equipped with a cone/plate shear apparatus, gelation temperature by glass bottle method and ex vivo permeation study was performed with cylindrical glass diffusion cell. Skin irritation potential was measured using rat as a model animal. Results: The FTIR spectrum of the selected gel showed that there is shifting of O-H stretching vibration of a hydroxyl group from 3408.72 to 3360.49 cm-1 and appearance of a new band at 1083.01 cm-1. The spectrum of the selected gel also showed the absence of characteristic peaks of GO at 1625.49 cm- 1. This result indicated that there may be an interaction between OSH and GO and hydrogen bonding between XG and POL 407. The gelation temperature was found to be decreased with the increase in GO content from 14.1±1.21°C 13±0.97°C. SEM micrograph demonstrated the uniform dispersion and intercalation of GO sheets in the gel. All the gel formulations showed a pseudo-plastic flow. Ex vivo permeation study (for 24 hr) exhibited highest (6991.425 µg) and lowest (2133.262 µg) amount of drug release, for OG1 and OG5, respectively. This is attributed to an increase in viscosity which led to a decrease in drug permeation across the abdominal skin of rats. The OG1 formulation (without GO) showed the highest flux of 76.66 µg/cm2/h, permeability coefficient (Kp) of 5.111× 10-3 cm/h and enhancement ratio of 3.277 compared to OG5 containing highest amount (9% w/w) of GO. The selected gel was found to be physically stable and there was minimum irritation score. Conclusion: All the above results indicated that thermal gel containing nanocomposite sustained the drug release and can be considered as an alternative to the orally administered tablet of OSH.

scholarly journals Comparison of Rheological, Drug Release, and Mucoadhesive Characteristics upon Storage between Hydrogels with Unmodified or Beta-Glycerophosphate-Crosslinked Chitosan

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Emilia Szymańska ◽  
Anna Czajkowska-Kośnik ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Physicochemical Characteristics ◽  
Vaginal Mucosa ◽  
Drug Release Profile ◽  
Modified Chitosan ◽  
Long Term Storage ◽  
Crosslinked Chitosan ◽  
Chitosan Hydrogels ◽  
The Impact

The physicochemical characteristics of beta-glycerophosphate-crosslinked chitosan hydrogels were investigated upon long-term storage at ambient, accelerated, and refrigerated conditions and compared to unmodified chitosan formulations. Additionally, the impact of chitosan modification on the ex vivo mucoadhesive performance in contact with porcine vaginal mucosa and on the drug release profile from hydrogels was evaluated. Viscosity and mechanical properties of formulations with unmodified chitosan decreased significantly upon storage regardless of tested conditions as a result of hydrolytic depolymerization. Introduction of ion crosslinker exerted stabilizing effect on physicochemical performance of chitosan hydrogels but only upon storage at refrigerated conditions. Beta-glycerophosphate-modified chitosan formulations preserved organoleptic, rheological behavior, and hydrogel structure up to 3-month storage at 4 ± 2°C. Viscosity variations upon storage influenced markedly mucoadhesive properties and drug release rate from hydrogels.

scholarly journals Accuracy in clinical examinations for the diagnosis of vulvovaginitis by CANDIDA SPP. and IN VITRO susceptibility to the main antifungals

2020 ◽  
Vol 49 (3) ◽  
Author(s):  
Andressa Santana Santos ◽  
Ana Laura Sene Amancio Zara ◽  
Fábio Silvestre Ataídes ◽  
Elisangela Gomes da Silva ◽  
Vivianny Aparecida Queiroz Freitas ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Clinical Diagnosis ◽  
High Resistance ◽  
Antifungal Susceptibility ◽  
Vulvovaginal Candidiasis ◽  
Vaginal Mucosa ◽  
Candida Spp ◽  
In Vitro Susceptibility ◽  
Gynecology And Obstetrics

Vulvovaginal candidiasis (VVC) is a common infection. This work aims to determine the positive predictive value (PPV) of the clinical diagnosis of VVC and to characterize Candida species isolated from the vaginal mucosa. This cross-sectional study was conducted from February 2016 to February 2017 at the Gynecology and Obstetrics Outpatient Clinic of the Hospital das Clínicas, in Goiânia, Goiás State, Brazil. The study included samples of vaginal secretion from 55 women who complained of vaginal discharge and itching as their main symptoms. The PPV of the clinical diagnosis of VVC was estimated in comparison to the laboratory culture method. The phenotypic methods and molecular tests were performed to identify Candida spp. In vitro susceptibility of Candida spp. isolates to fluconazole, itraconazole, clotrimazole, nystatin, and amphotericin B was determined using the broth microdilution assay. Yeast growth using the enzymes protease, phospholipase, and hemolysin was carried out in media containing respectively bovine albumin, egg yolk, and sheep erythrocytes. A PPV of 61.8% (34/55) was determined. Among the 55 vulvovaginal samples collected, we identified 36 isolates in whichC. albicans was the most common species. High resistance to fluconazole and low minimal inhibitory concentration (MIC) values for clotrimazole, nystatin and amphotericin B were observed. All isolates were proteinase and hemolysin producers, while seven strains were phospholipase negative. The clinical diagnosis of VVC presented a moderate PPV, which meant that cultures had to be conducted in the laboratory to confirm infection. The high resistance to fluconazole and itraconazole indicated the importance of the in vitro susceptibility test.KEY WORDS: Vulvovaginal candidiasis; antifungal susceptibility; enzymatic activity

scholarly journals FORMULATION AND EVALUATION OF METRONIDAZOLE MICROSPHERES-LOADED BIOADHESIVE VAGINAL GEL

2017 ◽  
Vol 10 (3) ◽  
pp. 418
Author(s):  
Banasmita Kalita ◽  
Kritika Saikia ◽  
Bhupen Kalita
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Spherical Particles ◽  
Vaginal Fluid ◽  
Vaginal Mucosa ◽  
Scanning Calorimetry ◽  
Vaginal Gel ◽  
Study Results

ABSTRACTObjectives: The objective of the present work is to develop and characterize metronidazole microsphere-loaded bioadhesive vaginal gel to ensurelonger residence time at the infection site, providing a favorable release profile for the drug.Methods: Microsphere was prepared by solvent evaporation method in various ratios of metronidazole to poly-ε-caprolactone (PCL). Physicochemicalevaluation of microspheres includes determination of solubility in simulated vaginal fluid, partition coefficient (n-octanol/citrate phosphatebuffer pH 4.5), particle size distribution, entrapment efficiency, X-ray diffraction, and surface morphology by scanning electron microscopy (SEM).Drug excipient compatibility was established by Fourier transform infrared and differential scanning calorimetry studies. Bioadhesive gel wasprepared using Carbopol 934P and HPMC K4M in various concentrations, and methyl paraben was used as a preservative. The pH was adjustedwith triethanolamine which resulted in a translucent gel. The optimized metronidazole microsphere formulation was dispersed into the gel base.Microspheres in gel formulations were evaluated for pH, viscosity, spreadability, drug content, and gelling strength. Ex vivo mucoadhesive strength ofthe gel was determined on goat vaginal mucosa. In vitro drug release study was performed using cellophane membrane.Results: The optimized batch of microsphere F4 (drug-polymer ratio 1:4) showed entrapment efficiency of 72.62±3.66%, solubility of 1.5 mg/ml, andpartition coefficient of 0.12. Particle size of all the formulations was observed below 100 μm. Regular and spherical particles were observed in theSEM photomicrographs. The optimized gel formulation G5 (Carbopol and HPMC at 1: 0.25 ratio) showed viscosity of 7538 cps at 100 RPM, gel strengthrecorded as 35 secobds for a 1000.00 mg load, and spreadability of 4.6 g.cm/seconds. G5 showed 82.4% drug release at 10.0 hrs and mucoadhesivestrength of 6.5±1.2 g.Conclusion: The study results suggest that metronidazole-loaded PCL microsphere in mucoadhesive gel would provide a mean for sustainedtreatment of vaginal infections.Keywords: Microsphere, Metronidazole, Bioadhesive vaginal gel.

FORMULATION AND EVALUATION OF DARIFENACIN HYDROBROMIDE TRANSDERMAL PATCH

2021 ◽  
pp. 12-14
Author(s):  
Aparna Reddy K ◽  
Latha K ◽  
Naseeb Basha Shaik ◽  
Sushma B ◽  
Haritha T ◽  
...  
Keyword(s):  
Drug Release ◽  
Physicochemical Properties ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Drug Level ◽  
Immediate Release ◽  
Tween 20 ◽  
Transdermal Patch ◽  
Weight Variation

The aim of present study is to formulate and characterize darifenacin hydrobromide transdermal patch and the effects of non-ionic surfactants span 20 and tween 20 on drug permeation were studied. Transdermal patches were prepared by solvent casting method using PVA, PVP, HPMC E5, HPMC E15 polymers. Propylene glycol and Glycerol were used as plasticizers and Span 20 and Tween 20 were used as permeation enhancers. The prepared patches were evaluated for physicochemical properties like drug content, thickness, weight variation, folding endurance, moisture uptake, watervapour transmission studies. Physicochemical properties have shown better. Drug release studies by in-vitro diffusion, ex-vivo permeation as well as skin irritation. Formulations DPAT2, DPLT3 showed better drug release rate, ux and Q when compared to DPAS2, DPLS2. From the results it was concluded that darifenacin hydrobromide transdermal patch 24 (DPAT2) formulation would reduce the administration frequency, side effects and may avoid uctuations of drug level in the blood in comparison to immediate release formulations which might enhance the patient compliance.

scholarly journals DESIGN OF DERMA STICKS OF ANDROGAPHIS PANICULATA FOR THE TREATMENT OF GYNAECOLOGICAL SKIN DISORDERS

2018 ◽  
Vol 10 (1) ◽  
pp. 8
Author(s):  
Savita Sonawane K. ◽  
Purushotham Rao
Keyword(s):  
Skin Irritation ◽  
Phase Iii ◽  
Vaginal Candidiasis ◽  
Vaginal Mucosa ◽  
Skin Disorders ◽  
Healthy Human ◽  
Phase Ii Studies ◽  
Human Volunteers ◽  
Phase Iii Studies

Objective: Vaginal candidiasis are often painful and uncomfortable and can include intense itching, irritation, vaginal discharge and dysuria. Gynaecological skin disorders referring to inflammatory and infectious conditions affecting the vaginal mucosa and vulvitis often accompanies vagina pain, itching and burning sensation. Herbal therapy is gaining popularity of women on account of it’s reduced side effect and restoration of the normal vaginal flora. Plants reported to possess activity or used in traditional systems of medicine for prevention and treatment of vaginitis. Therefore, it was found essential to find an alternative to counter all the above disadvantages effectively and hence in the present work, formulation and development of medicated sticks has been planned with the herbal drug Androgaphis Paniculata which is very well known for the anti bacterial and anti fungal activity.Methods: The preparation and characterization of medicated sticks was carried out in four phases. Phase I studies includes preparation of medicated derma sticks using the ointment bases with varied concentrations of waxes. Phase II studies involves characterization of prepared medicated derma sticks like weight, thickness and length. Phase III studies involves stability studies of prepared formulations. Phase IV Studies involves anti microbial studies by zone inhibition method. .Phase V: Primary skin irritation studies carried out on rabbits and guinea pigs and in healthy human volunteers showed no sensitization and edema on skin after 72 h of application.Results: The results of present study revealed that the prepared medicated sticks of Androgaphis Paniculata are convenient, equally effective, without any contamination chances on application and free from skin irritation.Conclusion:The present work is a unique piece of contribution to the drug industry. The results will be useful to industry RandD for further investigations. The continuation of these work clinical studies is in progress.Objective: Vaginal candidiasis are often painful and uncomfortable and can include intense itching, irritation, vaginal discharge and dysuria. Gynaecological skin disorders referring to inflammatory and infectious conditions affecting the vaginal mucosa and vulvitis often accompanies vagina pain, itching and burning sensation. Herbal therapy is gaining popularity of women on account of its reduced side effect and restoration of the normal vaginal flora. Plants reported to possess activity or used in traditional systems of medicine for prevention and treatment of vaginitis. Therefore, it was found essential to find an alternative to counter all the above disadvantages effectively and hence in the present work, formulation and development of medicated sticks have been planned with the herbal drug Androgaphis Paniculata which is very well known for the antibacterial and antifungal activity.Methods: The preparation and characterization of medicated sticks were carried out in four phases. Phase I studies include preparation of medicated derma sticks using the ointment bases with varied concentrations of waxes. Phase II studies involve characterization of prepared medicated derma sticks like weight, thickness and length. Phase III studies involves stability studies of prepared formulations. Phase IV Studies involves antimicrobial studies by zone inhibition method. .Phase V: Primary skin irritation studies carried out on rabbits and guinea pigs and in healthy human volunteers showed no sensitization and edema on the skin after 72 h of application. Results: The results of present study revealed that the prepared medicated sticks of Androgaphis Paniculata are convenient, equally effective, without any contamination chances on the application and free from skin irritation. Conclusion: The present work is a unique piece of contribution to the drug industry. The results will be useful to industry R&D for further investigations. The continuation of these work clinical studies is in progress.

scholarly journals Vaginal delivery of clotrimazole by mucoadhesion for treatment of candidiasis

2021 ◽  
Vol 11 (6) ◽  
pp. 6-14
Author(s):  
Monica RP Rao ◽  
Gajanan Paul
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Solid Dispersions ◽  
Vaginal Candidiasis ◽  
Wet Granulation ◽  
Vaginal Fluid ◽  
Eudragit L100 ◽  
Mucoadhesive Polymers ◽  
Weight Variation

The aim of this study was to prepare mucoadhesive vaginal tablets of clotrimazole for treatment of vaginal candidiasis. A combination of mucoadhesive polymers like HPMC K100M, Sodium CMC, and Eudragit L100 were used in different ratios prepare solid dispersions to enhance its solubility. Tablets were prepared by the wet granulation method. Solid dispersions were evaluated for saturation solubility. All tablet batches were evaluated for weight variation, hardness, friability, drug content, swelling index, in vitro drug release study, ex vivo diffusion and mucoadhesive strength. FTIR spectra showed there was no interaction between the drug and the excipients. HPMC K100 M increased the solubility of clotrimazole in simulated vaginal fluid at pH 4.5. Eudragit L100 was shown to increase the swelling and mucoadhesive strength of the tablet, i.e., 3.03 and 3.29 g. The in vitro and ex vivo release of all 9 batches showed between 61 to 78% release in 8h. Ex vivo diffusion studies using sheep vaginal membrane showed 43 to 59% in 6h in simulated vaginal fluid. The release and flux were nearly comparable to marketed tablet i.e., Candid-V6. The drug release of all batches followed the Korsmeyer-Peppas kinetic model, and the mechanism was found to be non‐Fickian/anomalous. Keywords: Clotrimazole, solid dispersion, HPMC K100M, Eudragit L100, Sodium CMC.

scholarly journals Development and In Vitro/In Vivo Evaluation of pH-Sensitive Polymeric Nanoparticles Loaded Hydrogel for the Management of Psoriasis

Nanomaterials ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 3433
Author(s):  
Muhammad Imran Asad ◽  
Dildar Khan ◽  
Asim ur Rehman ◽  
Abdelhamid Elaissari ◽  
Naveed Ahmed
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Topical Formulation ◽  
Sustained Drug Release ◽  
In Vivo Evaluation ◽  
Ex Vivo Permeation ◽  
Pasi Score

Methotrexate (MTX), the gold standard against psoriasis, poses severe problems when administered systemically viz increased toxicity, poor solubility and adverse reactions. Hence, a topical formulation of MTX for the management of psoriasis can be an effective approach. The present study aimed to develop an MTX based nanoparticle-loaded chitosan hydrogel for evaluating its potential efficacy in an imiquimod-induced psoriatic mice model. MTX-NPs loaded hydrogel was prepared and optimized using the o/w emulsion solvent evaporation method. Particle size, zeta potential, entrapment efficiency, in vitro drug release, ex vivo permeation, skin irritation and deposition studies were performed. Psoriatic Area and Severity Index (PASI) score/histopathological examinations were conducted to check the antipsoriatic potential of MTX-NPs loaded hydrogel using an imiquimod (IMQ)-induced psoriatic model. Optimized MTX-NPs showed a particle size of 256.4 ± 2.17 nm and encapsulation efficiency of 86 ± 0.03%. MTX-NPs loaded hydrogel displayed a 73 ± 1.21% sustained drug release in 48 h. Ex vivo permeation study showed only 19.95 ± 1.04 µg/cm2 of drug permeated though skin in 24 h, while epidermis retained 81.33% of the drug. A significant decrease in PASI score with improvement to normalcy of mice skin was observed. The developed MTX-NPs hydrogel displayed negligible signs of mild hyperkeratosis and parakeratosis, while histopathological studies showed healing signs of mice skin. So, the MTX-NPs loaded hydrogel can be a promising delivery system against psoriasis.

Potential Ganciclovir Liposomal Thermoreversible Gel for Ophthalmic Delivery Using Box-Behnken Statistical Design and Efficacy Assessment Study in Rabbit Model

2019 ◽  
Vol 9 (7) ◽  
pp. 950-957
Author(s):  
Yanjuan Sheng ◽  
Yanni Zhu
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Rabbit Model ◽  
Methyl Cellulose ◽  
Temperature Sensitive ◽  
Potential Candidate ◽  
Core System ◽  
Thermoreversible Gel

The present study focuses on development of novel thermoreversible ophthalmic drug delivery system using Ganciclovir as potential candidate for treatment of various ocular infections. The formulation was prepared for thermoreversible gel which incorporates liposomes of Ganciclovir as core system. Thermoreversible gel prolongs delivery of drug with use of combination of polymers like Poloxamer, Hydroxypropyl methyl cellulose. The Poloxamer used here serves as temperature sensitive polymer. Thus prepared system was evaluated for various parameters. Liposomes found to be complies with basic requirement like non-leak ability, high in-vitro drug release with optimum encapsulation efficiency. The results obtained showed that the in situ gel is clear and transparent (prime requirement for ophthalmic product) with high gelling capacity and moderately viscous liquid (1454 cp), highest bioadhesive strength (Dyne/cm2). The ex-vivo study was also done and compared with marketed eye drop formulation. The results showed superiority of in situ gel formulation over eye in sustaining the drug release over prolong period of time. The haemolytic study performed proved the non-haemolytic nature of formulation.

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