Enhancement of stability and controlled drug release of lipid nanoparticles by modified solvent-evaporation method

2016 ◽  
Vol 508 ◽  
pp. 294-300 ◽  
Author(s):  
Sang-Eun Lee ◽  
Joon-Kyung Lee ◽  
Woo-Suk Jang ◽  
Tae-Hyeon Kim ◽  
Amolnat Tunsirikongkon ◽  
...  
Keyword(s):  
Drug Release ◽  
Controlled Drug Release ◽  
Lipid Nanoparticles ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
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 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 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.

scholarly journals Design and Development of Sustained Release Microspheres of Ibuprofen by Emulsification Solvent Evaporation Method Using Polymeric Blend

2013 ◽  
Vol 16 (1) ◽  
pp. 39-44 ◽  
Author(s):  
Nandini Saha ◽  
Ikramul Hasan ◽  
Mehrina Nazmi ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Fourier Transforms ◽  
In Vitro Release ◽  
Pharmaceutical Journal ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Dissolution Apparatus ◽  
Emulsification Solvent Evaporation

Ibuprofen, a non-steroidal anti-inflammatory drug was formulated as microspheres by using Methocel K4M & Eudragit RSPO. These microspheres were prepared by emulsification solvent evaporation method to provide sustained action and to minimize local side effect of Ibuprofen by avoiding the drug release in the upper gastrointestinal tract. The prepared microspheres were subjected to various evaluation and in-vitro release studies. In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) using Phosphate buffer (pH 7.4) as the dissolution medium at 37.5oC for 6 hours (paddle speed 50 RPM). The release mechanisms were explored and explained with Zero Order, First Order, Higuchi and Korsmeyer-Peppas equations. The correlation coefficients values of the trend lines of the graphs showed that the formulations best fit with Korsmeyer-Peppas release pattern. Microspheres’ morphology and chemical integrity were studied by a scanning electron microscope (SEM) and Fourier transforms infrared spectroscopy (FTIR) respectively. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14489 Bangladesh Pharmaceutical Journal 16(1): 39-44, 2013

Diclofenac sodium-loaded solid lipid nanoparticles prepared by emulsion/solvent evaporation method

2010 ◽  
Vol 13 (6) ◽  
pp. 2375-2386 ◽  
Author(s):  
Dongfei Liu ◽  
Sunmin Jiang ◽  
Hong Shen ◽  
Shan Qin ◽  
Juanjuan Liu ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Diclofenac Sodium ◽  
Lipid Nanoparticles ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Solid Lipid

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 Risperidone Controlled Release Microspheres Based on Poly(Lactic Acid)-Poly(Propylene Adipate) Novel Polymer Blends Appropriate for Long Acting Injectable Formulations

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 130 ◽  
Author(s):  
Stavroula Nanaki ◽  
Panagiotis Barmpalexis ◽  
Alexandros Iatrou ◽  
Evi Christodoulou ◽  
Margaritis Kostoglou ◽  
...  
Keyword(s):  
Lactic Acid ◽  
Controlled Release ◽  
Drug Release ◽  
Polymer Blends ◽  
Solvent Evaporation ◽  
Poly Lactic Acid ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Long Acting ◽  
Poly Propylene

The present study evaluates the preparation of risperidone controlled release microspheres as appropriate long-acting injectable formulations based on a series of novel biodegradable and biocompatible poly(lactic acid)–poly(propylene adipate) (PLA/PPAd) polymer blends. Initially, PPAd was synthesized using a two-stage melt polycondensation method (esterification and polycondensation) and characterized by 1H-NMR, differential scanning calorimetry (DSC), and powder X-ray diffraction (XRD) analyses. DSC and XRD results for PLA/PPAd blends (prepared by the solvent evaporation method) showed that these are immiscible, while enzymatic hydrolysis studies performed at 37 °C showed increased mass loss for PPAd compared to PLA. Risperidone-polyester microparticles prepared by the oil–water emulsification/solvent evaporation method showed smooth spherical surface with particle sizes from 1 to 15 μm. DSC, XRD, and Fourier-transformed infrared (FTIR) analyses showed that the active pharmaceutical ingredient (API) was dispersed in the amorphous phase within the polymer matrices, whereas in vitro drug release studies showed risperidone controlled release rates in all PLA/PPAd blend formulations. Finally, statistical moment analysis showed that polyester hydrolysis had a major impact on API release kinetics, while in PLA/PPAd blends with high PLA content, drug release was mainly controlled by diffusion.

BINARY COMPLEXES OF GLIMEPIRIDE WITH Β-CYCLODEXTRIN FOR IMPROVED SOLUBILITY AND DRUG DELIVERY

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 54-60
Author(s):  
L Adhikari ◽  
M. Semalty ◽  
P. S Naruka ◽  
V. K Aswal ◽  
A Semalty ◽  
...  
Keyword(s):  
Drug Release ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Molar Ratio ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Kneading Method ◽  
Ft Ir

Cyclodextrin complexation is a one of the most investigated techniques of solubility and dissolution enhancement of drugs. In the present study, a poorly water soluble drug glimepiride, was complexed with β-cyclodextrin (βCD) with the aim of improving water solubility and drug dissolution. The complexes were prepared using two different methods (solvent evaporation and kneading) and then characterized by Fourier-transform infrared spectroscopy (FT-IR), powder x-ray diffractometry (X-RD), thermal analysis (DSC),scanning electron microscopy and in-vitro dissolution study. The phase solubility study revealed the most suitable ratio of drug to β CD (1:4 molar ratio). Analysis of various physical and pharmacokinetic parameters for the complex prepared by solvent evaporation method showed better drug content, solubility and drug release profile in comparison to the complex prepared by the kneading method. The complex prepared with solvent evaporation method showed better drug release as compared with that of kneading method and the pure drug. The FT-IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:βCD molar ratio) using solvent evaporation method showed the better improvement in solubility and drug dissolution.

scholarly journals Preparation and Evaluation of Solid Dispersion of Nebivolol Using Solvent Evaporation Method

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
A. Laxmi Raj ◽  
Y. Shravan Kumar
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Enhanced Solubility

Nebivolol is a pharmaceutical drug used for the treatment of Hypertension. It is characterized with poor solubility which limits its absorption and dissolution rate which delays onset of action. In the present study, fifteen formulations of solid dispersions were prepared with 1:1:1, 1:5:2 and 1:3:1.5 ratios of drug: carrier: surfactant by solvent evaporation method. There was significant improvement in the rate of drug release from all 15 solid dispersions and the formulation (SD14) comprising Nebivolol: Kleptose HPB: SLS in 1:5:2 ratio has shown enhanced solubility about 42 folds and significant improvement in the rate of drug release i.e. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Nebivolol has been converted into an amorphous form from crystalline within the solid dispersion formulation. The present study demonstrated that formulation of Nebivolol solid dispersion is a highly effective strategy for enhancing the bioavailability of poorly water soluble drug Nebivolol.

Sign in / Sign up

Export Citation Format

Share Document