scholarly journals Development and Evaluation of Nanoparticles Based Topical Gel Containing Antifungal Drug Fluconazole

2021 ◽  
Vol 01 (09) ◽  
Author(s):  
Misbah Khanum ◽  
Keyword(s):  
Drug Release ◽  
Ph Value ◽  
Fungal Infections ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Topical Gel ◽  
Drug Content ◽  
Zero Order Release ◽  
The Stability

The objective of this work was to prepare Fluconazole nanoparticles, and then incorporated into the freshly prepared gel for transdermal delivery, reducing the oral side effects of the drug and forenhancing stability. Fluconazole is commonly used antifungal agents for the treatment of local and systemic fungal infections. In this study Fluconazole nanoparticles was prepared by using Eudragit RL 100 by nanoprecipitation method with different drugs to polymer (1:1, 1:2 and 1:3) and stabilizer (Poloxamer 188) ratios (0.5%, 0.75% and 1%) and evaluated for various parameters. Drug-excipients compatibility was performed by FTIR study. The particle size, polydispersity index, Zeta potential, % Entrapment efficiency and % drug content of all the formulations were found in the range of 16.8 to 48.9nm, 0.229 to 0.558, -11.6 to -26.6 mv, 28.41% to 95.78% and 59% to 97.38%. From SEM studies it was revealed that Fluconazole nanoparticles particles are spherical in shape and without any agglomeration. From the in-vitro drug release study, it was revealed that sustained release of same formulation last up to 12 hours. From the stability study, it was revealed that the F5 formulation was stable at 40°C ± 2°C /75% ± 5%RH and 4°C. The optimised formulation F5 was selected to prepare Fluconazole loaded nanoparticles based topical gels using different concentration of Carbopol 934 and 940 and characterized for pH, spreadability, drug content, viscosity and in-vitro drug diffusion. Among the five formulations, G5 was selected as the best formulation. The pH of all formulations was found near to the skin pH value. The in-vitrodiffusion study of Fluconazole gel (G5) showed 94.75%. The optimized formulation G5 was checked for mechanism and kinetics of drug release. It is found it following Zero order release and non-Fickian mechanism. The selected Gel formulation G5 was found to be stable at 40°C ± 2°C /75% ± 5%RH and 4°C, it is clear that the formulation did not undergo any chemical changes found more stable at room temperature

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

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.

scholarly journals Development of Fast Dissolving Oral Films Containing Vitamin B6 for Nausea and Vomiting of Pregnancy (NVP)

2019 ◽  
Vol 9 (3) ◽  
pp. 51-59
Author(s):  
JESINDHA BEYATRICKS ◽  
, Dhananjaya
Keyword(s):  
Drug Release ◽  
Vitamin B6 ◽  
Stability Study ◽  
Infrared Study ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Folding Endurance ◽  
The Fourier Transform ◽  
The Stability

The aim of this study was to formulate and evaluate the oral fast-dissolving film of Vitamin B6 for the effective management of motion sickness and vomiting during pregnancy. Fast-dissolving films were prepared by the solvent-casting method using different polymers, HPMC-15 and Pullulan, along with Propylene glycol as a plasticizer. The Fourier-transform infrared study for the drug-polymer interaction was carried out. Evaluation of physical parameters such as physical appearance, surface texture, uniformity of weight, uniformity of strip thickness, surface pH, folding endurance, uniformity of drug content and percentage of moisture absorption were performed. Kinetic data analysis for the release study and the stability study were also performed. Results of uniformity of weight, thickness, folding endurance, surface pH, percentage drug content, tensile strength and percentage elongation of all the films were found to be satisfactory. The Fourier-transform infrared study indicated that there was no interaction between the drug and the polymers. The in-vitro drug release study showed that a better rate of drug release was achieved by formulations F4 and F8 compared with other formulations. The stability study did not show any significant difference in the external appearance, the drug content and the in-vitro drug release. In conclusion present study suggested that fast dissolving films has a better ability to cross the sublingual barrier at a faster rate, and hence the delivery system was found to be promising as it has the potential of overcoming the drawbacks associated with tablet formulations available in the market presently. Keywords: Fast-dissolving film, Vitamin B6, HPMC-15, Pullulan gum, Mango peel pectin, Crospovidone, solvent casting

scholarly journals Formulation and in-vitro evaluation of Glipizide (Anti diabetic drug) Liposphere

2018 ◽  
Vol 8 (6-s) ◽  
pp. 116-119
Author(s):  
Sarika Saini ◽  
Aman Mittal
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Paraffin Wax ◽  
Drug Content ◽  
Dissolution Apparatus ◽  
Dispersion Technique

Objective- The aim of the present study was to formulate and in- vitro study of glipizide liposphere by using melt dispersion technique. Methods- Glipizide Liposphere system composed of paraffin wax, Stearic acid as lipid phase and sodium lauryl sulphate as surfactant. Glipizide lipospheres were prepared by using melt dispersion technique. Formulation of Glipizide was evaluated such as organoleptic properties, particle size, drug content, entrapment efficiency in-vitro study and stability of the lipospheres. Result- The formation of glipizide lipospheres by using melt dispersion technique was done successfully. All the formulations have off- white in colour, characteristic odour and spherical shape. The formulation A4 has particle size 19.65 μm, drug content 84.93 %, entrapment efficiency 80.75 % and the percentage drug release was carried out by using USP type 2 dissolution apparatus in 6.8 pH phosphate buffer solution and drug release of glipizide lipospheres within 12 hrs was found to be 74.06 %.stability study of glipizide lipospheres revealed that the formulation was stable at 5oC ± 3oC. Keywords- Lipospheres, Glipizide, Paraffin wax, Melt dispersion method, Dissolution Apparatus, Stability study

scholarly journals EVALUATION OF STABILITY OF ROPINIROLE HYDROCHLORIDE AND PRAMIPEXOLE DIHYDROCHLORIDE MICROSPHERES AT ACCELERATED CONDITION

2018 ◽  
Vol 10 (4) ◽  
pp. 82
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
Gouranga Nandi
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Shelf Life ◽  
Stability Study ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Ropinirole Hydrochloride ◽  
Pramipexole Dihydrochloride

Objective: The objective of the present work was to conduct accelerated stability study as per international council for harmonisation (ICH) guidelines and to establish shelf life of controlled release dosage form of ropinirole hydrochloride and pramipexole dihydrochloride microspheres for a period of 6 mo.Methods: Most optimized batch of ropinirole hydrochloride and pramipexole dihydrochloride (F12 and M12 respectively) were selected and subjected to exhaustive stability testing by keeping the sample in stability oven for a period of 3 and 6 mo. Various parameters like surface morphology, particle size, drug content, in vitro drug release and shelf life were evaluated at 3 and 6 mo period. The surface morphology of the formulated microspheres was determined by scanning electron microscopy (SEM). The particle size of the microspheres was estimated by optical microscopy method. The drug content was assayed by the help of ultra-violet spectrophotometer (UV). The in vitro drug release was performed by using Paddle II type dissolution apparatus and the filtrate was analyzed by UV spectrophotometer. The shelf life of the optimized microspheres was calculated by using the rate constant value of the zero-order reaction.Results: A minor change was recorded in average particle size of F12 and M12 microspheres after storage for 6 mo. For F12 and M12, initially the particle size was 130.00 µm and 128.92 µm respectively and after 6 mo it was found to be 130.92 µm and 128.99 µm respectively. There was no change in surface morphology of F12 and M12 microspheres after 6 mo of storage. The shape of microspheres remained spherical and smooth after 6 mo. An insignificant difference of drug content was recorded after 6 mo compared to the freshly prepared formulation. For F12 and M12, 94.50% and 93.77% of the drug was present initially and after 6 mo 94.45% and 93.72% of the drug was recorded. In vitro drug release was recorded after 6 mo for F12 and M12. Initially, 97.99% and 97.69% of the drug was released till 14th hour respectively for F12 and M12. After 6 mo, 98.23% and 97.99% of the drug was released respectively. The percentage residual drug content revealed that the degradation of microspheres was low. Considering the initial percentage residual drug content as 100%, 99.94% of the drug was recorded for both F12 and M12. The shelf life for F12 and M12 was found to be 10 y 52 d and 10 y 70 d respectively which were determined by the zero-order kinetic equation.Conclusion: A more or less similar surface morphology, particle size, drug content and percent of drug release before and after stability study confirmed the stability of F12 and M12 microspheres after storage for 6 mo and prove the efficacy of the microspheres in the site-specific delivery of drugs in Parkinson’s disease.

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

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.

Fabrication of Vesicular Drug Delivery of Niosomal Topical Formulation for the Effective Treatment of Osteoarthritis

2016 ◽  
Vol 12 ◽  
pp. 1-8
Author(s):  
S. Nagalakshmi ◽  
T. Sandeep ◽  
S. Shanmuganathan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Lipid Vesicles ◽  
Tween 20 ◽  
Injection Method ◽  
Topical Gel ◽  
Release Studies

Delivery of drug through topical route, delivers most convenient and novel approach. The Skin can offer several advantages as a route of drug administration although its barrier nature makes it difficult for most drugs to penetrate in to and permeate through it. During the past decades there has been a lot of interest in lipid vesicles as a tool to improve topical drug delivery. Vesicular system such as liposomes, niosomes, ethosomes and elastic deformable vesicles provide an alternative for improved skin drug delivery. In fact vesicles can act as drug carriers controlling drug release. The Research findings were intended to develop sustained release of aceclofenac niosomes formulations in order to reduce gastrointestinal disturbances and to provide better effect when applied topically. Niosomes of aceclofenac was prepared by modified ether injection method using different ratio of surfactants (Tween 20, 40, 60 & 80) with cholesterol and drug. The developed formulations were optimized based on the high entrapment efficiency and in-vitro release studies. Optimized batch was selected and made in to topical niosomal gel using gelling agents like carbopol and sodium carboxy methyl cellulose. Formulation were evaluated for various parameters like vesicle shape, vesicle size, entrapment efficiency, drug content, compatibility studies, in-vitro release studies and stability studies. Ether injection method was found to be most satisfactory in terms of niosome particle size, drug entrapment efficiency was found to be 88.68 ±0.64 % and in-vitro release studies showed 40% of sustain drug release at the end of 8 hrs of study when compared with marketed formulation. Hence, the formulated niosomal topical gel was found to be a better alternative when compared to the marketed formulation in terms of better efficacy, bioavailability and permeation.

scholarly journals FORMULATION AND EVALUATION OF KETOCONAZOLE NIOSOMAL GEL

2018 ◽  
Vol 6 (5) ◽  
pp. 71-75
Author(s):  
Paninder Kaur ◽  
J.S Dua ◽  
D.N Prasad
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Drug Content ◽  
Novel Drug Delivery System ◽  
Niosomal Gel ◽  
Span 60 ◽  
Novel Drug ◽  
Rotary Vacuum

ABSTRACT   In recent years, treatment of infectious disease through Novel Drug delivery system (NDDS) has undergone a revolutionary shift. Niosomes are a Novel Drug Delivery system which has potential application to treat infectious disease topically. Niosomes are non-ionic surfactant vesicles, in which medication is encapsulated in a vesicle for controlled drug release. Ketoconazole niosomes were prepared by using Cholesterol, Span 60/ Span 40 as surfactants, chloroform, and diethyl ether using rotary vacuum evaporator method. Formulation was then evaluated for particle size, drug content, entrapment efficiency, and in-vitro drug release studies. The Entrapment efficiency and drug content were calculated at 225nm using UV spectrophotometer. The drug content was found to be 70.37% for Span 40 and 72.81% for Span 60.The percentage of drug entrapment in niosomes was 60.3 % for Span 40 and 62.21 % for Span 60. FT-IR studies for niosomes containing Span 40 shows -CH stretching (Aliphatic) at 2891 cm-1and2925 cm-1 for niosomes containing Span 60. Ketoconazole niosomal gel was prepared using Carbopol 940, glycerol, Triethanolamine and distilled water. Evaluation of niosomal gel was determined by Physical appearance, pH, viscosity, drug content, entrapment efficiency and In-vitro diffusion studies.The percentage of the drug release from the niosomal gel was found to be 40.78 % for Span 40 and 33.75% for Span 60 . This delivery system is cost effective and simple to prepare as only the prepared gel of niosomes was introduced in Rotary vacuum evaporator for solvent evaporation.    

scholarly journals DIACEREIN-LOADED NIOSOMES (DC-NS): A NEW TECHNIQUE TO SUSTAIN THE RELEASE OF DRUG ACTION

2022 ◽  
pp. 156-163
Author(s):  
RASHAD M. KAOUD ◽  
EMAN J. HEIKAL ◽  
TAHA M. HAMMADY
Keyword(s):  
Physical Stability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Molar Ratios ◽  
Tween 40 ◽  
A New Technique ◽  
The Stability ◽  
Tween 60

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate.

Sign in / Sign up

Export Citation Format

Share Document