scholarly journals Evaluation of the Influence of Stirring Speed on the Release Kinetics of Fexofenadine HCl Polymeric Microspheres

2021 ◽  
Vol 18 (4) ◽  
pp. 733-741 ◽  
Author(s):  
Paroma Arefin ◽  
Md Shehan Habib ◽  
Mohammad Mostafa ◽  
Dipankar Chakraborty ◽  
Sreebash Chandra Bhattacharjee ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Stirring Rate ◽  
The Impact ◽  
Fexofenadine Hcl

Microspheres, a potential drug delivery approach, has opened a new era for attaining versatile release patterns needed. By optimizing the formulation variables, they can be prepared to obtain targeted release, immediate release, sustained release patterns. The release of the active drug material depends upon a number of formulation parameters such as polymers, stirring speed (rpm), methodology, surfactants, etc. Fexofenadine hydrochloride (HCl) is a second generation antihistamine. Our present research has explored the effects of using different rpm (600- 1000 rpm) in preparing fexofenadine hydrochloride (HCl) microspheres by emulsion solvent evaporation method. The formulation is aimed to provide sustained release for the required long period with a high margin of safety. We used a blended mixture of Hydroxy Propyl Methyl Cellulose (HPMC) K 100 MCR and Eudragit RL100 polymers to have sustained-release microspheres. The impact of different rpm on Yield, drug encapsulation efficiency, flow properties, and dissolution pattern were appraised. We observed the release of the drug for 10 hours in phosphate buffer (pH 6.8) and evaluated the drug release spectrophotometrically. Our study finds that the release of fexofenadine HCl from the microspheres was significantly increased with drug loading. We found the dosage forms to follow Higuchi release kinetics and Hixson-Crowell release kinetics the most, indicating successful achievement of sustained-release pattern in the dosage form. The change in drug release rate was statistically significant for variation in the stirring rate. We found that 600 rpm was the most optimized stirring rate for preparing microspheres in the emulsion solvent evaporation method.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF CIPROFLOXACIN BY SOLVENT EVAPORATION METHOD USING DIFFERENT POLYMERS

2021 ◽  
pp. 101-108
Author(s):  
KAUSLYA ARUMUGAM ◽  
PAYAL D. BORAWAKE ◽  
JITENDRA V. SHINDE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Angle Of Repose ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time. Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies). Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h. Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency.

scholarly journals Development and In-Vitro Evaluation of Betahistine Hydrochloride microspheres by Emulsification Solvent Evaporation Method

1970 ◽  
Vol 7 (5) ◽  
pp. 30-36
Author(s):  
Sandeep A Wathore
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Tween 80 ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Ftir Studies ◽  
Emulsification Solvent Evaporation ◽  
Polymer Ratio

The formulation of floating microspheres of Betahistine hydrochloride by the o/w emulsification and solvent evaporation method in the presence of tween 80 as an emulsifying agent. The influence of formulation factor Drug: Polymer ratio on particle size, encapsulation efficiency and invitro release characteristics of the microspheres were investigated. The microspheres have been analyzed for their size, drug loading capacity and drug release study. Spherical and smooth surfaced microspheres with desired encapsulation efficiencies were obtained. Slow drug release from microspheres observed up to 12 h. for formulation F4, F5. Optimized formulation F4 was evaluated for FTIR, DSC, SEM. DSC and FTIR studies showed that the nature of pure drug Betahistine hydrochloride remains unaffected till the completion of process of microspheres formation. SEM photographs showed that the Floating microspheres were spherical in nature with smooth surface and uniform distribution of the drug within the microsphere. Keywords: 

scholarly journals FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

2018 ◽  
Vol 8 (5) ◽  
pp. 465-474
Author(s):  
S PADMA PRIYA ◽  
AN Rajalakshmi ◽  
P Ilaveni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Loading ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Polyvinyl Pyrrolidone ◽  
Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods:  Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine  formulations were formulated and  evaluated for  possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro  drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

scholarly journals PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

2018 ◽  
Vol 10 (6) ◽  
pp. 57
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
N. N. Bala
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Ropinirole Hydrochloride

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

scholarly journals ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF IBUPROFEN BY SOLID DISPERSION TECHNIQUE AND FORMULATION OF SUSTAINED RELEASE TABLETS CONTAINING THE OPTIMISED BATCH OF SOLID DISPERSION

2017 ◽  
pp. 37-44
Author(s):  
ABHIK KAR ◽  
ABDUL BAQUEE AHMED
Keyword(s):  
Sustained Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Sustained Release Tablets

Objective: The present study was aimed to enhance the solubility of poorly water soluble drug Ibuprofen using solid dispersion technique and to develop sustained release tablets containing solid dispersion granules of the optimized batch. Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-inflammatory propertiesMethods: Solid dispersions of Ibuprofen were prepared by using PEG 20000 and Poloxamer 407 in different weight ratios by fusion and solvent evaporation method. Drug-carrier physical mixtures were also prepared. Solid dispersions were characterized by saturation solubility, drug content, in vitro dissolution, FTIR and DSC analysis. Solid dispersion formulation, SDF9 (PEG 20000 and Poloxamer 407, 1:3:3) prepared by solvent evaporation method was considered as the optimized batch. Sustained release tablets containing the solid dispersion granules of the optimized batch were prepared by direct compression method using HPMC K100M at three concentrations (10%, 14%, 18% w/w). The prepared formulations were evaluated for hardness, thickness, weight variation, friability, in vitro dissolution studies and release kinetics modelling.Results: Solid dispersion formulation, SDF9showed 95.09% drug release in 60 min and considered as the optimized batch. Tablet formulation, FT3 (HPMC K100M 18% w/w) showed 96% drug release for 12 h.Conclusion: Solid dispersions of ibuprofen using a combination of PEG 20000 and poloxamer 407 by solvent evaporation method may result in higher aqueous solubility of the drug. Also sustained release tablets containing solid dispersion granules of ibuprofen, using HPMC K100M may be a promising approach to extend the release rate of the drug from the solid dispersion for 12 h.

A Novel Antimicrobial Nano-Composite Porous Material for Bone Repair

2011 ◽  
Vol 695 ◽  
pp. 517-520
Author(s):  
Pei Pei Luo ◽  
Ji Dong Li ◽  
Yi Zuo ◽  
Xia Wu ◽  
Yu Bao Li
Keyword(s):  
Bone Repair ◽  
Drug Loading ◽  
Continuous Phase ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Technological Parameters ◽  
Nano Composite ◽  
Evaporation Method ◽  
Hydrophilic Drugs ◽  
Oil In Water

In this paper, isoniazid (INH)-loaded poly (ε-caprolactone) microspheres with a special microporous surface and relatively high drug loading were fabricated by an oil-in-oil (O/O) solvent evaporation method. Meanwhile the microspheres were produced by an oil-in-water (O/W) method for comparison. The technological parameters such as the concentration of surfactant, the volume of continuous phase and the quantity of the drug were investigated systematically. The microspheres morphology, their size distribution and the viscosity of both the dispersed and continuous phase were characterized. The results indicate that the O/O solvent evaporation method is a feasible approach to encapsulate micromolecular and hydrophilic drugs in PCL. This opens the door for INH-loaded microspheres able to release drugs and thereby improve the therapy of tuberculosis of bones and joints in the future.

scholarly journals Formulation Development and Evaluation of Sustained Release Microsphere of Levetiracetam

2021 ◽  
Vol 71 (2) ◽  
Author(s):  
Dinesh V. Panpaliya ◽  
Atish Y. Sahare ◽  
Priyanka Lanje ◽  
Pooja Dhoke
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Solvent Evaporation Method ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Evaporation Method

The aim of the present work was to develop and evaluate of oral microsphere of Levetiracetam to reduce the frequency of dosing by achieving 12 hours sustained drug release. The microsphere formed will also mask the bitter taste of the drug and thus increase the compatibility of the drug with the patients. Levetiracetam is a second-generation anti-epileptic agent useful in the treatment of partial onset and monoclinic seizures. It has a short half life of 7 hours and its recommended dose is 500 mg twice a daily. Microspheres are suitable drug delivery system for such drug candidate. For these reasons it is must to formulate a suitable dosage form by which it will be easier to administer the dose and also to get a sustained drug release hence microsphere was prepared using solvent evaporation method. Preformulation studies were carried out to rule out any drug polymer interaction by FTIR technique. In this study formulation was done solvent evaporation method using different percentage of HPMC– K 100, HPMC- K 15 and coated with Eudragit S100. Drug, polymer and physical mixture were evaluated for in compatibility study by Fourier transforms infrared spectroscopy. All the batches of microsphere (F1 to F5) were subjected for in vitro dissolution. Microsphere was evaluated for surface morphology, micromeritics properties, entrapment efficiency and in vitro drug release. The entrapment efficiency of microsphere ranged from 71.16%-73.66%. The size of the prepared microsphere ranges between 42.8 µm to 55.64 µm which was found to increase with increase in RPM at same polymer ratio. Micromeritics studies showed good flow properties. Among the microsphere batches, F5 was observed as an optimized batch as its formulation with polymer i.e. Eudragit-S 100 and HPMC-K 100 was found to be release in sustained manner. The F-5 batch shows is 79.45% drug release at the end of 7 hrs and its stability study indicate that these microspheres were stable at selected temperature and humidity

scholarly journals Improvement of Drug Release and Compatibility between Hydrophilic Drugs and Hydrophobic Nanofibrous Composites

Materials ◽  
2021 ◽  
Vol 14 (18) ◽  
pp. 5344
Author(s):  
Hazim J. Haroosh ◽  
Yu Dong ◽  
Shaimaa Jasim ◽  
Seeram Ramakrishna
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Halloysite Nanotubes ◽  
Polymer Processing ◽  
Hydrophilic Drugs ◽  
Drug Release Kinetics ◽  
Flexible Polymer ◽  
The Impact

Electrospinning is a flexible polymer processing method to produce nanofibres, which can be applied in the biomedical field. The current study aims to develop new electrospun hybrid nanocomposite systems to benefit the sustained release of hydrophilic drugs with hydrophobic polymers. In particular, electrospun hybrid materials consisting of polylactic acid (PLA):poly(ε-caprolactone) (PCL) blends, as well as PLA:PCL/halloysite nanotubes-3-aminopropyltriethoxysilane (HNT-ASP) nanocomposites were developed in order to achieve sustained release of hydrophilic drug tetracycline hydrochloride (TCH) using hydrophobic PLA:PCL nanocomposite membranes as a drug carrier. The impact of interaction between two commonly used drugs, namely TCH and indomethacin (IMC) and PLA:PCL blends on the drug release was examined. The drug release kinetics by fitting the experimental release data with five mathematical models for drug delivery were clearly demonstrated. The average nanofiber diameters were found to be significantly reduced when increasing the TCH concentration due to increasing solution electrical conductivity in contrast to the presence of IMC. The addition of both TCH and IMC drugs to PLA:PCL blends reduced the crystallinity level, glass transition temperature (Tg) and melting temperature (Tm) of PCL within the blends. The decrease in drug release and the impairment elimination for the interaction between polymer blends and drugs was accomplished by mobilising TCH into HNT-ASP for their embedding effect into PLA:PCL nanofibres. The typical characteristic was clearly identified with excellent agreement between our experimental data obtained and Ritger–Peppas model and Zeng model in drug release kinetics. The biodegradation behaviour of nanofibre membranes indicated the effective incorporation of TCH onto HNT-ASP.

scholarly journals Formulation and evaluation of floating microspheres of losartan potassium using sodium alginate and HPMC by solvent evaporation method

2019 ◽  
Vol 9 (1-s) ◽  
pp. 60-66 ◽  
Author(s):  
Kapil Purohit ◽  
Navneet Garud
Keyword(s):  
Drug Release ◽  
Solvent Evaporation ◽  
Losartan Potassium ◽  
Solvent Evaporation Method ◽  
In Vitro Drug Release ◽  
Evaporation Method ◽  
Sustained Action ◽  
Improve Patient

Hollow multі-unіt mіcrospheres were prepared by a solvent dіffusіon technіque іn emulsіon wіth a drug and an acrylіc polymer. These were dіssolved іn a mіxture of ethanol-dіchloromethane and poured іnto an aqueous solutіon of PVA wіth stіrrіng to form emulsіon droplets. The rate of drug release іn mіcro balloons was controlled by changіng the ratіo of polymer to drug. The mіcroballoons were floatіng іn vіtro for 12-24 hours when submerged іn aqueous medіa. Radіographіc studіes showed that mіcroballons admіnіstered orally to humans were dіspersed іn the upper part of the stomach and were held there for 3 hours agaіnst perіstaltіc movement. Floating Microspheres of Losartan potassium were formed by Solvent Evaporation method .The formulas LP7 of Losartan Potassium Floating Microspheres shows a very good drug release profiles and shown better sustained action till the end of last hour (24th hrs). It will improve patient compliance and increase in bioavailability which give better approach to treat hypertensive condition and the angiotensin receptor blocking action of Losartan lower the long term complications of Hypertension and reduce the risk of heart failure, CHF, Myocardial Infarction and also vascular damage in blood vessels and kidney. Keywords: Losartan Potassium, Floating microspheres, Drug Entrapment, In-vitro drug release.

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