scholarly journals Development and Characterization of Metronidazole Loaded Microsponges for the Management of Diabetic Foot

2021 ◽  
Vol 8 (10) ◽  
pp. 440-457
Author(s):  
Ponni Sujathan ◽  
Umesh Kumar Sharma
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Diabetic Foot ◽  
Particle Size Analysis ◽  
Diffusion Method ◽  
Size Analysis ◽  
Poly Vinyl Alcohol ◽  
Scanning Calorimetry ◽  
Solvent Diffusion

The objective of present work was formulation and evaluation of Metronidazole loaded microsponges for the management of diabetic foot ulcer via topical application and to reduce side effects. The microsponges were prepared by quasi-emulsion solvent diffusion method using different concentrations of Ethyl cellulose and Poly vinyl alcohol. The prepared microsponges were evaluated for particle size analysis, SEM, % production yield, % drug entrapment efficiency, in-vitro drug release studies, DSC and antimicrobial studies. FTIR studies shown that there was no interaction between drug and polymers. The optimum sustained release of drug around a period of 12hrs was shown by formulation F8. The n value of optimized formulation indicated that the drug release followed zero order kinetics. It was confirmed from the stability studies that the optimized formulation remained stable at 45±2℃ and 70±5% relative humidity. Keywords: Microsponges, Metronidazole, Diabetic Foot, Quasi-emulsion solvent diffusion, Sustained release, Scanning electron microscopy, Differential scanning calorimetry.

scholarly journals PREPARATION AND EVALUATION OF PARECOXIB MICROSPONGE HYDROGEL SUSTAINED RELEASED TABLET

2019 ◽  
Vol 8 (3) ◽  
Author(s):  
Maruthi. N ◽  
Lakshmi Radhika G
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Production Yield ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Solvent Diffusion ◽  
Dissolution Studies ◽  
Emulsion Solvent Diffusion Method

Microsponges are the polymeric drug delivery systems composed of porous microspheres. They are tiny sponge like spherical particles that consists of myriad of inter-connecting voids within a non-collapsible structure with a large porous surface. The present work is to formulate and evaluate the Parecoxib Microsponge Hydrogel Sustained Release Tablet. The Microsponges of Parecoxib is prepared by Quasi-emulsion solvent diffusion method using Ethyl cellulose and Eudragit RS100 as polymers and Di-butyl phthalate as Plasticizer. And they are characterized for FTIR studies, production yield, particle size analysis, DSC and SEM. The production yield of formulations was from 77.77 to 82.75. FTIR and DSC studies are revealed that the drug and polymer are compatible with each other during preparation. The average diameter of Microsponge is ranged from 536.9 nm to 489.7. Parecoxib Microsponge hydrogel were prepared as sustained release tablets by using sustained release polymers like MCC, Magnesium stearate, Lactose and talc. Preformulation of Microsponge granules were carried out by various parameters and post formulation were carried out by In-vitro dissolution studies, hardness, friability and weight variation tests. Formulation F3 shows good results for the drug release kinetics as controlled release and F6 formulation shows good results for the in-vitro dissolution studies for sustained release. Key words: Microsponge hydrogel drug delivery, Parecoxib, Sustained drug release tablets, quasi emulsion solvent diffusion method.

scholarly journals Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

2012 ◽  
Vol 62 (4) ◽  
pp. 529-545 ◽  
Author(s):  
Anuj Chawla ◽  
Pooja Sharma ◽  
Pravin Pawar
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Naproxen Sodium ◽  
Drug Loading ◽  
Size Analysis ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
S 100 ◽  
Eudragit S 100

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

scholarly journals FORMULATION AND CHARACTERIZATION OF SUSTAINED RELEASE COATED MATRIX GRANULES OF METFORMIN HYDROCHLORIDE

2018 ◽  
Vol 11 (7) ◽  
pp. 387
Author(s):  
Radha Rani Earle ◽  
Kiran Kumar Bandaru ◽  
Lakshmi Usha A
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Diabetes Mellitus Type Ii ◽  
Drug Content ◽  
Percentage Yield

Objective: Metformin hydrochloride is a biguanide antihyperglycemic agent which is a generally recommended first-line drug for the treatment of diabetes mellitus (Type II). The purpose of this investigation is to prepare sustained release matrix granules of metformin hydrochloride which are coated to extend the drug release over a longer time period.Methods: Metformin hydrochloride granules were prepared by mixing all the dry powders in a V-cone blender and wetting the powder mix with aqueous solution of hydroxypropyl methyl cellulose K100. The prepared granules (MG1-MG5) were investigated for drug release. The batch of granules which exhibited extended release for up to 4 h was coated in a standard coating pan with blends of Eudragit RS and RL to further enhance release period. These were marked as coated metformin granules (CMG3) and CMG4 which were later filled into empty capsules. The granules were characterized for micromeritic properties, percentage yield, particle size distribution, percentage of drug content, and in vitro release of the drug.Results: All the formulations showed percentage yield in the range of 77.66–82.86% and drug content in the range of 78.23–96.62%. CMG3 showed drug release of 97.02% for 12 h. Fourier-transform infrared spectroscopy and differential scanning calorimetry studies indicated that no possible interaction existed between the drug and the polymers used. Scanning electron microscopy images revealed that the granules were spherical in shape with smooth surface and completely covered with a coating of polymer. Kinetic analysis of drug release confirmed that drug release followed zero-order kinetics where it is independent of the concentration.Conclusion: From the results, it was analyzed that design of coated granules employing the polymers used in the present work can produce a sustained release of the drug over a period of 12 h.

scholarly journals CURCUMIN LOADED CHITOSAN NANOPARTICLES FOR TOPICAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES

2021 ◽  
Vol 10 (2) ◽  
pp. 48-52
Author(s):  
J Adlin Jino Nesalin ◽  
Preethi Raj M N
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Topical Gel

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive nanoparticles and to design an innovative topical delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated nanoparticles were prepared by ionic gelation method. The nanoparticles were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected nanoparticles formulation (FS5, containing drug: polymer ratio 1:5) was incorporated into gels with a bio adhesive polymer. The Nanoencapsulated topical gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected Nanoencapsulated bio adhesive topical gel (FS3 gel, containing 1 % w/w of drug loaded nanoparticles and 0.6 % w/w of Carbopol 934) was found to control curcumin release over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of Nanoencapsulated topical gel study may be adopted for a successful delivery of Curcumin for topical use.

scholarly journals PREPARATION, CHARACTERIZATION AND EVALUATION OF CELECOXIB LOADED NANOSPONGES FOR THE TREATMENT OF PSORIATIC ARTHRITIS

2019 ◽  
Vol 3 (12) ◽  
Author(s):  
G. Ravi ◽  
P. Subhash Chandra Bose ◽  
Valluru Ravi ◽  
Damineni Sarita
Keyword(s):  
Particle Size ◽  
Psoriatic Arthritis ◽  
Drug Release ◽  
Particle Size Analysis ◽  
Joint Disease ◽  
Size Analysis ◽  
Sem Images ◽  
Melting Technique ◽  
Low Solubility

Psoriatic arthritis is a chronic inflammatory joint disease which is one of the types of psoriasis. 25% of all psoriasis patients develop psoriatic arthritis. It is characterised with innate and adaptive immune responses. The main objective of the present work was to prepare characterization and evaluate the Celecoxib nanosponges for the treatment of Psoriatic Arthritis. It is a non-steroidal anti-inflammatory drug (NSAID) having low solubility and low bioavailability. In order to increase the solubility, this drug was incorporate in nanosponges by melting technique. The prepared formulation was evaluated for different parameters. SEM images confirm that the prepared formulation was spherical and porous in nature. Particle size analysis shows that as the cross-linker ratio increases, there is increase in the particle size of nanosponges. Particle size was in the size range of 201.69 nm. The in vitro studies were carried out for prepared nanosponges which showed drug release of 89.69% in 24 h. Keywords: Nanosponges, Psoriatic arthritis, NSAID, Drug release

scholarly journals FORMULATION AND EVALUATION OF GLICLAZIDE NANOSPONGES

2019 ◽  
pp. 181-189
Author(s):  
RAHUL S. SOLUNKE ◽  
UDAY R. BORGE ◽  
KRISHNA MURTHY ◽  
MADHURI T. DESHMUKH ◽  
RAJKUMAR V. SHETE
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Production Yield ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Average Particle ◽  
Dissolution Profile ◽  
Solvent Diffusion ◽  
Emulsion Solvent Diffusion Method

Objective: The objective of the present study was to develop and characterize an optimal stable nanosponges of Gliclazide (GLZ) by using the emulsion solvent diffusion method and aimed to increase its bioavailability and release the drug in sustained and controlled manner. Methods: The GLZ nanosponge was prepared by emulsion solvent diffusion method using different drug-polymer ratios (1:1 to 1:5) Eudragit S100 is used as a polymer. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) estimated the compatibility of GLZ with polymer. All formulations evaluated for production yield, entrapment efficiency, in vitro drug release, scanning electron microscopy (SEM) and stability studies. Results: The DSC and FTIR Studies revealed that no interaction between drug and polymer. The Production yield of all batches in the range of 73.8±0.30 to 85.6±0.32. Batch F3 showed the highest production yield, the entrapment efficiency of batch F3 70.6±0.77. The average particle size ranges from 303±2.36 to 680±2.50 nm. By the end of 10th hour F3 formulation shown highest drug release was found to be 94.40±1.12%. The release kinetics of the optimized formulation shows zero-order drug release. The stability study indicates no significant change in the in vitro dissolution profile of optimized formulation. Conclusion: The results of various evaluation parameters, revealed that GLZ nanosponges would be possible alternative delivery systems to conventional formulation to improve its bioavailability, the emulsion solvent diffusion method is best method for preparation of nanosponges and release the drug in sustained and controlled manner.

scholarly journals FABRICATION AND EFFECT OF PROCESS VARIABLES OF SITAGLIPTIN MICROSPHERES

2018 ◽  
Vol 11 (4) ◽  
pp. 291
Author(s):  
Revathi S ◽  
Dhanaraju Md
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Diffusion Path ◽  
Diffusion Method ◽  
Cube Root ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
The Fourier Transform ◽  
Polymer Ratio

 Objective: The study is to formulate and assess the effects of different variables on the release profile of sitagliptin microspheres.Methods: The microspheres were prepared by emulsion-solvent diffusion method and ionotropic gelation method using ethyl cellulose and sodium alginate as the polymers, respectively. The formulations are optimized by applying 23 factorial design based on the drug-polymer ratio, stirring speed, and method of preparation.Results: The drug-polymer interaction was checked by the Fourier-transform infrared spectroscopy and differential scanning calorimetry the results of which indicated no incompatibility. The formulated sitagliptin microspheres were evaluated for shape, morphology, particle size, the degree of swelling, encapsulation efficiency, in vitro drug release studies for 12 h, and kinetics of drug release.Conclusion: The results showed that the drug-polymer ratio and stirring speed affected the particle size and drug release. The release of the drug was found to be sustained, and diffusion path is following cube root law of Hixson-Crowell kinetics. The batch F3 was found to be desirable and was further characterized by scanning electron microscope for morphology.

scholarly journals Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

2013 ◽  
Vol 63 (3) ◽  
pp. 359-372 ◽  
Author(s):  
Naresh Vishal Gupta ◽  
Shirodker Natasha ◽  
Anil Getyala ◽  
Ramnath Sudeendra Bhat
Keyword(s):  
Drug Release ◽  
Chemical Interaction ◽  
Drug Loading ◽  
Particle Size Analysis ◽  
Vaginal Candidiasis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Dsc Studies

Abstract The aim of the present investigation was to prepare and evaluate novel bioadhesive vaginal tablets containing clotrimazole loaded microspheres in order to provide long-term therapeutic activity at the site of infection. Tablets were prepared by incorporating drug loaded microspheres and using bioadhesive polymers hydroxypropylmethylcellulose, sodium carboxymethylcellulose and Carbopol. Microspheres were prepared by the spray drying technique using Eudragit RS-100 and Eudragit RL-100. Microspheres were characterized by SEM, DSC, FTIR, particle size analysis and evaluated for percentage yield, drug loading, encapsulation efficiency and in vitro drug release. To achieve bioadhesion to the mucosal tissue, optimized microspheres were incorporated into bioadhesive tablets and were evaluated for in vitro drug release, in vitro and in vivo mucoadhesion. FTIR and DSC studies showed that no chemical interaction occurred between the drug and polymers. The sphericity factor indicated that the prepared microspheres were spherical. Formulation Mt6 indicated a controlled in vitro drug release and good bioadhesive strength. The in vivo images confirmed the bioadhesion and retention property of tablets up to 24 h. The results indicated that this drug delivery system can be explored for controlled intravaginal drug release.

scholarly journals Enhancement of Solubility and Dissolution Rate of Poorly Soluble Drug Nifedipine by Solid Sedds

2020 ◽  
Vol 10 (01) ◽  
pp. 9-15
Author(s):  
Sabitri Bindhani ◽  
Utkalika Mohapatra ◽  
Snehamayee Mohapatra ◽  
Rajat K. Kar
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Particle Size Analysis ◽  
Sem Analysis ◽  
In Vitro Dissolution ◽  
Size Analysis ◽  
Drug Content

Nifedipine is a dihydropyridine calci channel blocking agent belongs to biopharmaceutical classification system (BCS) class-II mainly applied in the treatment of hypertension and angina-pectoris. The objective of this work is to improve the solubility and dissolution rate of nifedipine by formulating into a solid-self micro emulsifying drug delivery system (solid smedds). Methods: Oil, Surfactant, and cosurfactant were selected by solubility screening study. For the determination of the best emulsion region, a pseudo ternary diagram was prepared. Based on solubility castor oil, tween 80 and polyethylene glycol (PEG) 400 was selected in which SCOSmix (a mixture of surfactant and cosurfactant) was 1:1. Thermodynamic stability study was performed for the determination of stable smedds formulation. These formulations were evaluated for self emulsification time, drug content analysis, robustness to dilution test, particle size analysis, and in vitro diffusion study. The optimized formulation was selected for formulating into solid-smedds by using aerosil 200 at a different ratio. SCF9L (0.65:1) was selected due to its good flow property. Then it was evaluated for particle size analysis, drug content study, differential scanning calorimetry (DSC), X-Ray Diffraction study (XRD), fourier transform infrared spectroscopy (FTIR) Scanning Electron Microscopy study (SEM) analysis, and in vitro dissolution study. Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM analysis, the texture of powder showed a uniform granular structure, and there was no incompatibility between drugs. Excipients was observed from ftir study. From the in vitro dissolution study, it improved the dissolution rate of nifedipine, which was 98.68% of drug release, where pure drug release only 6.75%.

scholarly journals FORMULATION AND EVALUATION OF MICROSPONGE GEL FOR TOPICAL DELIVERY OF ANTIFUNGAL DRUG

2017 ◽  
Vol 9 (4) ◽  
pp. 30
Author(s):  
Vishal Yadav ◽  
Prakash Jadhav ◽  
Shailaja Dombe ◽  
Anjali Bodhe ◽  
Pranali Salunkhe
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Delivery System ◽  
Antifungal Drug ◽  
Production Yield ◽  
Diffusion Method ◽  
Conventional Formulation ◽  
Solvent Diffusion ◽  
Emulsion Solvent Diffusion Method

Objective: The purpose of present study aims to design novel drug delivery system containing oxiconazole nitrate microsponges and to prepare microsponge gel. Oxiconazole nitrate is an antifungal drug used in the treatment of fungal infection having a poor aqueous solubility, side effects and adverse reactions. The microsponge delivery system is unique technology for controlled release of active agents. Methods: The microsponges were prepared by quasi-emulsion solvent diffusion method by using polymer eudragit S-100 and eudragit L-100. All the formulated microsponges were subjected for various evaluation parameters such as production yield, encapsulation efficiency, particle size analysis and in vitro drug release study. The optimised microsponge formulation F3 and F9 were further formulated as gel formulation for topical delivery. Prepared gel was evaluated for physical parameters like pH, spreadability, viscosity, drug content and in vitro diffusion study and compared with the marketed formulation.Results: The Fourier transform infrared radiation measurement (FTIR) and Differential scanning colorimetry (DSC) of drug and excipient confirm compatibility. Results revealed that quasi-emulsion solvent diffusion method is a suitable technique for the preparation of microsponges as most of the formulations were discrete and spherical in shape with a good production yield of 61.44% to 80.45% and The highest drug release for F3 and F9 formulation was found to be 87.77 % and 83.24 % respectively for the 8 h. The microsponge gel formulation MGI (F3) showed the controlled release of oxiconazole nitrate for 12 h. The drug release data of optimised batch MGI (F3) were fitted into different kinetic models and showed that the drug release from gel formulation follows zero order release.Conclusion: As compared to conventional formulation, the prepared microsponge gel are expected to remain on the skin for a longer time, gradually releasing their contents over the time. Hence, oxiconazole nitrate microsponges and microsponge gel prepared in this study are promising as being more useful than conventional formulation therapy.

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