scholarly journals Formulation and Evaluation of Miconazole Nitrate Loaded Nanoparticles for Topical Delivery

2021 ◽  
pp. 102-123
Author(s):  
Ashish Y. Pawar ◽  
Khanderao R. Jadhav ◽  
Komal D. Ahire ◽  
Tushar P. Mahajan
Keyword(s):  
Particle Size ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Topical Administration ◽  
Hair Follicles ◽  
Systemic Delivery ◽  
Mean Particle Size ◽  
Miconazole Nitrate

The aim of the present work was to formulate and evaluate Miconazole nitrate (MN) polymeric nanoparticles (NPs) for systemic delivery of the active ingredient after topical administration. The Solvent evaporation approach was used to make nanoparticles for topical delivery of MN. Particle size, entrapment efficiency and SEM were all measured in MN-SLN. A consistent size distribution (PI 0.300) was used to generate aqueous NPs dispersions with a mean particle size less than 250 nm. After 3 months of storage, the produced semi-solid systems had a mean particle size of less than 250 nm and a PI of less than 0.500. The F5 formulation was been chosen as the model formulation from among the nine nanoparticle formulations developed (F1 to F9). The reason for this was that, according to the ICH stability guidelines, formulation F5 was judged to be optimal and stable. The F5 formulations of miconazole nanoparticles shows the highest entrapment efficiency (93.28%) and drug loading (86.64%). In conclusion, there are two major advantages of using miconazole nanoparticle drug delivery systems. i.e., they are topical preparations that assemble in the hair follicles and wrinkles to produce a systemic and local action. It is possible that nanoparticles will be the most effective treatment for fungal skin infections.

scholarly journals FORMULATION AND EVALUATION OF ETHAMBUTOL POLYMERIC NANOPARTICLES

2020 ◽  
pp. 207-217
Author(s):  
MONOWAR HUSSAIN ◽  
ANUPAM SARMA ◽  
SHEIKH SOFIUR RAHMAN ◽  
ABDUL MATIN SIDDIQUE ◽  
TANUKU PAVANI EESWARI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Compatibility Study ◽  
Bacterial Disease ◽  
Dose Frequency

Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency. Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics. Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h. Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.

scholarly journals Formulation Optimization of Erythromycin Solid Lipid Nanocarrier Using Response Surface Methodology

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Anil Kumar Sahu ◽  
Tekeshwar Kumar ◽  
Vishal Jain
Keyword(s):  
Particle Size ◽  
Response Surface Methodology ◽  
Response Surface ◽  
Chemical Interaction ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Concentration ◽  
Total Period ◽  
Mean Particle Size ◽  
Solid Lipid

In present work response surface methodology (RSM) using the miscellaneous design model was used to optimize formulations of erythromycin solid lipid nanocarriers (ERY-SLN). Two-factor three level factorial design was considered for optimization. There were three parameters, drug entrapment efficiency (EE), drug loading (DL) percentage, and mean particle size of ERY-SLN, considered for investigating the optimal formulation with respect to two independent variables, including lipid concentration (X1) and surfactant : cosurfactant ratio (X2). The result showed that the optimal ERY-SLN was composed of lipid concentration (X1) 15 mg/mL and surfactant : cosurfactant ratio (X2) 1 : 1 with %EE of 88.40 ± 2.09%, DL of 29.46 ± 0.69%, mean particle size of 153.21 ± 2.31 nm, polydispersity index (PDI) of 0.026 ± 0.008, and zeta potential value of −15.18 ± (−5.53)  mV. DSC and TEM study showed that there was no chemical interaction between ERY and lipid (GMS) and the ERY-SLN particles are nonspherical, respectively. The drug release experiments exhibited a sustained release over during 24 h, up to 66.26 ± 2.83%. Accelerated stability studies showed that there was no significant change occurring in the responses after storage condition for a total period of 3 months.

scholarly journals SIMULTANEOUS ESTIMATION OF DRUGS PRESENT IN MICROBEADS FOR COLON-TARGETED DRUG DELIVERY SYSTEM

2019 ◽  
pp. 122-125
Author(s):  
ABHISHEK KUMAR ◽  
MEENAKSHI BHARKATIYA
Keyword(s):  
Particle Size ◽  
Drug Loading ◽  
Morphological Characteristics ◽  
Entrapment Efficiency ◽  
Operating Conditions ◽  
Simultaneous Estimation ◽  
Compatibility Study ◽  
Physicochemical Interaction ◽  
Mean Particle Size ◽  
Drug Entrapment Efficiency

Objectives: The present study was aimed to develop Eudragit S100 coated colon-targeted sustained-release formulations of alginate-pectin and alginate-hydroxypropyl methylcellulose microbeads containing norfloxacin (NF) and tinidazole (TZ) for the treatment of amebiasis which was simultaneous estimated. Methods: Taguchi L9 orthogonal array design has been used to optimize the composition and operating conditions for the preparation of formulations. Nine batches (P1-H5) were prepared by taking three independent variables (X1 – drug:polymer ratio, X2 – concentration of sodium alginate, and X3 – curing time) at three levels (1, 2, and 3). Response variables studied for batches (P1-H5) were mean particle size (μm) (Y1), drug entrapment efficiency (% w/w) (Y2), and drug loading (% w/w) (Y3). NF and TZ were simultaneous estimated by ultraviolet spectrophotometric method. Drug-polymer compatibility study was carried out by differential scanning calorimetry and Fourier-transform infrared spectroscopy and indicates no physicochemical interaction. Results: Microbeads were analyzed for morphological characteristics, mean particle size, drug entrapment efficiency, drug loading, and in vitro drug release. The average size of optimized alginate-pectin microbeads was found to be 881±0.05 μm with an entrapment efficiency of 78.50±0.28% (NF) and 86.50±0.32% (TZ) which was simultaneous estimated. Conclusion: The studies concluded that formulated enteric-coated alginate-pectin microbeads after enteric coating can be used effectively for the delivery of NF and TZ to colon.

scholarly journals CENTRAL COMPOSITE DESIGN FOR FORMULATION AND OPTIMIZATION OF LONG-ACTING INJECTABLE (LAI) MICROSPHERES OF PALIPERIDONE PALMITATE

2021 ◽  
pp. 87-98
Author(s):  
SANDIP MALI ◽  
NISHANT OZA
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Central Composite Design ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Paliperidone Palmitate ◽  
Burst Release ◽  
Mean Particle Size ◽  
Long Acting ◽  
Central Composite

Objective: The aim of the present study was to optimize long-acting injectable (LAI) microspheres of Paliperidone palmitate (PP) for treatment of schizophrenia using face-centered central composite design (FC-CCD). Methods: In this study, poly lactic-co-glycolic acid (PLGA) based LAI microspheres of paliperidone palmitate (PP) were formulated by using FC-CCD. LAI microspheres were developed by using oil in water (O/W) emulsion solvent evaporation technique. On the basis of preliminary trials, FC-CCD was employed to check effect of independent variables such as drug polymer ratio (X1), homogenization speed (X2) and rate of addition (X3). While mean particle size (Y1), drug loading (Y2), entrapment efficiency (Y3), burst release (Y4), and drug release on day 60 (Y5) were considered as dependent variables and statistically evaluation performed by using design expert 12 software. Morphology of prepared microspheres was studied by using the scanning electron microscopy (SEM) technique, while particle size was analyzed by laser diffraction technique. In vitro drug release studies were performed using a controlled temperature shaking water bath apparatus. Fourier transforms infrared spectroscopy (FTIR) and differential scanning calorimetric (DSC) study were performed to analyze any changes in crystal behavior or to detect any chemical bonding between ingredients. 13C NMR and 1H NMR techniques were used to analyze end-capping and monomer ratio in developed microspheres. Results: The factorial batches mean particle size was found to be 38 µm to 104 µm and drug loading were found between 27.2 % to 47.2%. Mathematical modelling of drug release kinetics revealed that near zero-order drug release of checkpoint formulations. Endcap analysis and molar ratio of formulated microspheres were found to be ester end cap and ~75:25, respectively. Morphologically all the prepared samples were found to be spherical in shape and smooth surface. FTIR data showed no significant interactions occurred between drug and excipients. The actual responses of checkpoint formulations were observed within 5% variation of predicted values. Conclusion: The prepared microspheres showed promising results of morphology, particle size, drug loading, entrapment efficiency, burst release and drug release on day 60. The successful predictive designs models were achieved from employed FC-CCD.

Preparation of Zingiber officinale Extract Loaded Solid Lipid Nanoparticles

2012 ◽  
Vol 506 ◽  
pp. 389-392 ◽  
Author(s):  
N. Ratcharin ◽  
P. Wongtrakul ◽  
Ratana Indranupakorn
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Loading Capacity ◽  
Ginger Extract ◽  
Mean Particle Size ◽  
Solid Lipid ◽  
The Mean

Solid lipid nanoparticles (SLNs) loaded ginger extract were prepared by microemulsion technique. The nanoparticles were composed of stearic acid as solid lipids, Cremophor RH 40 as surfactant and ethanol as co-surfactant. It was found that variation in the amount of surfactant and co-surfactant had profound effects on the mean particle size, the drug entrapment efficiency and loading capacity. Transmission electron microscope (TEM) revealed the spherical nature of the particles. The mean particle size of SLNs ranging between 453.1 and 551.7 nm were measured by dynamic light scattering (DLS). The entrapment efficiency (EE) and drug loading capacity (LC) determined by high performance liquid chromatography (HPLC) found to be in the range of 85.2390.07% and 1.411.49%, respectively.

Development of pH-Dependent Nanospheres for Nebulisation- In vitro Diffusion, Aerodynamic and Cytotoxicity Studies

Drug Research ◽  
2018 ◽  
Vol 68 (12) ◽  
pp. 680-686 ◽  
Author(s):  
Pradum Ige ◽  
Sagar Pardeshi ◽  
Raju Sonawane
Keyword(s):  
Particle Size ◽  
Beclomethasone Dipropionate ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
In Vitro Cytotoxicity ◽  
Mean Particle Size ◽  
Cytotoxicity Studies ◽  
In Vitro Diffusion ◽  
Ph Dependent

AbstractThe aim of this work was to evaluate the in vitro performance of nebulized nanosuspension formulation when nebulized using ultrasonic nebulizer. The present investigation deals with successful formulation of Beclomethasone dipropionate loaded HPMCP nanospheres prepared by solvent evaporation technique using PEG 400 as a stabilizer. Beclomethasone dipropionate is a water insoluble drug molecule was encapsulated in HPMCP nanospheres to have pH dependent solubility at basic pH for targeted drug delivery in lung and studied for in vitro cytotoxicity and immediate release capability. The synthesized nanospheres were characterized through drug excipient compatibility, surface topography; mean particle size , zeta potential, PDI, entrapment efficiency and drug loading, in vitro diffusion, aerodynamic, in vitro cytotoxicity and stability studies. The mean particle size and PDI of the optimized batch (F1) had 197.6±0.40 nm and 0.324 ±0.35, respectively. The % entrapment efficiency and % drug loading was found to be 86.56±1.32 and 8.30±0.27, respectively. The optimized batch F1 showed % cumulative drug release 94.77±0.24 at 1 h. The formulation showed cell viability up to 91.28%. It can be concluded that, Beclomethasone dipropionate loaded HPMCP nanospheres was found to be safe, stable with significant increase in solubility and bypass the liver.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

SCREENING OF BIODEGRADABLE POLYMER AND MOST EFFECTIVE VARIABLES IN PREPARATION OF ESSENTIAL OIL LOADED NANO PARTICLES FOR PULMONARY DELIVERY USING TAGUCHI DESIGN

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (02) ◽  
pp. 68-75
Author(s):  
Avani Khristi ◽  
Lalit L. Jha ◽  
Abhay Dharamsi ◽  
Keyword(s):  
Particle Size ◽  
Essential Oil ◽  
Biodegradable Polymers ◽  
Drug Loading ◽  
Pulmonary Inflammation ◽  
Pulmonary Delivery ◽  
Entrapment Efficiency ◽  
Nano Particles ◽  
Favorable Conditions ◽  
Insoluble Polymers

The biodegradability of inhalable nanoparticles (NPs) is an important criterion in prevention of lung toxicity due to NPs which have been taken to cure the condition. Pulmonary inflammation may result due to non-biodegradation or insoluble polymers used to produce NPs. Biodegradable polymers are widely used for manufacturing safe drug-entrapped inhalable NPs for pulmonary delivery. Here in this study, for preparing ajwain essential oil loaded NPs for pulmonary delivery, biodegradable polymers chitosan, gelatin and alginic acid have been evaluated for suitability. Based on the results of trial batches prepared from each polymer, the responses particle size and entrapment efficiency were measured and compared. Out of the three polymers, chitosan was having very good entrapment efficiency, poly dispersive index, drug loading and zeta potential-favorable conditions for pulmonary delivery of essential oils. Further screening of most effective variables in manufacturing nano particles using chitosan, eight batches of nano particles have been prepared as per taguchi orthogonal 2 level array L8 experimental design (Design expert software, version 7.0) where two responses, particle size and entrapment efficiency, have been observed. Based on the results of eight batches, standard effects have been calculated and significant variables identified, for both particle size and entrapment efficiency, for further optimization under design of experiment.

scholarly journals FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN

2021 ◽  
pp. 216-226
Author(s):  
GEETHA V. S. ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Crude Protein ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Sustained Drug Delivery ◽  
Drug Loading Efficiency

Objective: To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design. Methods: 5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and in vitro drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process. Results: 5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%), in vitro drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer. Conclusion: The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.

scholarly journals FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE LOADED FLOATING MICROSPHERES

2019 ◽  
pp. 74-82
Author(s):  
SHIKHA KESHARVANI ◽  
PANKAJ KUMAR JAISWAL ◽  
ALOK MUKERJEE ◽  
AMIT KUMAR SINGH
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Compatibility Study ◽  
Specific Drug ◽  
Site Specific

Objective: The main objective of this study was to develop and evaluate the eudragit and HPMC coated metformin hydrochloride floating microspheres, in which HPMC helps in floating and eudragit as a coating material for a site-specific drug release in a controlled manner and the active moiety metformin used as anti-hyperglycemic agent. Methods: The floating microsphere was prepared by the solvent evaporation method incorporating metformin as a model drug. The prepared floating microsphere were characterized for particle size, %yield, drug loading and entrapment efficiency, compatibility study, %buoyancy, surface morphology and In vitro drug release and release kinetics. Results: The result metformin loaded floating microsphere was successfully prepared and the particle size range from 397±23.22 to 595±15.82 µm, the entrapment efficiency range from 83.49±1.33 to 60.02±1.65% and drug loading capacity range from 14.3±0.54 to 13.31±0.47% and %buoyancy range from 85.67±0.58 to 80.67±1.15%. The FT-IR and X-RD analysis confirmed that no any interaction between drug and excipient, and surface morphology confirmed those particles are sphere. The floating microsphere show maximum 96% drug release in pH 0.1N HCL and follow the Korsmeyer peppas model of the super case-2 transport mechanism. Conclusion: These results suggest that metformin loaded floating microspheres could be retain in stomach for long time and give site specific drug release in controlled manner.

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