scholarly journals Formulation development and evaluation of Glibenclamide loaded Eudragit RLPO microparticles

2013 ◽  
Vol 2 (12) ◽  
pp. 196-201 ◽  
Author(s):  
Balagani Pavan Kumar ◽  
Irisappan Sarath Chandiran ◽  
Korlakunta Narasimha Jayaveera
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Release Studies ◽  
Vitro Release ◽  
Eudragit Rlpo

The objective of the present investigation was to formulate and evaluate microencapsulated Glibenclamide produced by the emulsion – solvent evaporation method. Microparticles were prepared using Eudragit RLPO by emulsion solvent evaporation method and characterized for their micromeritic properties, encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis. In vitro release studies were performed in phosphate buffer (pH 7.4). Stability studies were conducted as per ICH guidelines. The resulting microparticles obtained by solvent evaporation method were free flowing in nature. The mean particle size of microparticles ranges from 134.49 – 179.72 µm and encapsulation efficiency ranges from 92.30-98.32%. The infrared spectra and differential scanning calorimetry thermographs confirmed the stable character of Glibenclamide in the drug-loaded microparticles. Scanning electron microscopy revealed that the microparticles were spherical in nature. In vitro release studies revealed that the drug release was sustained up to 12 hrs. The release kinetics of Glibenclamide from optimized formulation followed zero-order and peppas mechanism. The mechanism of drug release from the microparticles was found to be non-Fickian type. Eudragit RLPO microparticles containing Glibenclamide could be prepared successfully by using an emulsion solvent evaporation technique, which will not only sustain the release of drug but also manage complicacy of the diabetes in a better manner.DOI: http://dx.doi.org/10.3329/icpj.v2i12.17016 International Current Pharmaceutical Journal, November 2013, 2(12): 196-201

Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

1970 ◽  
Vol 1 (3) ◽  
pp. 257-266
Author(s):  
Nagda C. D. ◽  
Chotai N. P. ◽  
Patel S. B. ◽  
Soni T. J ◽  
Patel U. L
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Phenyl Acetic Acid ◽  
Solvent Evaporation Method ◽  
Elimination Half ◽  
Release Studies ◽  
Differential Scanning Colorimetry ◽  
Polymer Interactions ◽  
Vitro Release

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.

Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Size Distribution ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Glycol Succinate ◽  
Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

scholarly journals Development of nitazoxanide-loaded colon-targeted formulation for intestinal parasitic infections: centre composite design-based optimization and characterization

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Charu Bharti ◽  
Upendra Nagaich ◽  
Jaya Pandey ◽  
Suman Jain ◽  
Neha Jain
Keyword(s):  
Particle Size ◽  
Desirability Function ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Percentage Yield ◽  
Vitro Release ◽  
Selection Of

Abstract Background The current investigation is focused on the development and characterization of Eudragit S100 coated nitazoxanide-loaded microbeads as colon-targeted system utilizing central composite design (CCD) and desirability function. The study initiated with the selection of a BCS class II drug nitazoxanide and its preformulation screening with excipients, selection of polymer and identification of concentration for CCD, selection of optimized formulation based on desirability function, and in vitro release studies in simulated gastric and colonic media and stability studies. A two-factor, three-level CCD was employed with two independent variables, i.e. X1 (chitosan % w/v) and X2 (sodium tripolyphosphate % w/v), and three dependent variables, i.e. Y1 (particle size in micrometres), Y2 (percentage yield) and Y3 (percent entrapment efficiency), were chosen. Additionally, surface morphology, mucoadhesion and in vitro drug release studies were also conducted. Result Chitosan concentration showing maximum entrapment and optimum particle size was selected to formulate chitosan beads. The polynomial equation and model graphs obtained from the Design-Expert were utilized to examine the effect of independent variables on responses. The effect of formulation composition was found to be significant (p ˂ 0.05). Based on the desirability function, the optimized formulation was found to have 910.14 μm ± 1.03 particle size, 91.84% ± 0.64 percentage yield and 84.75% ± 0.38 entrapment efficiency with a desirability of 0.961. Furthermore, the formulations were characterized for in vitro drug release in simulated colonic media (2% rat caecal content) and have shown a sustained release of ∼ 92% up to 24 h as compared to in vitro release in simulated gastric fluid. Conclusion The possibility of formulation in enhancing percentage yield and entrapment efficiency of nitazoxanide and the utilization of CCD helps to effectively integrate nitazoxanide microbeads into a potential pharmaceutical dosage form for sustained release.

scholarly journals Application of Molecularly Structured Ben Oil in Gentamicin Entrapped Lipospheres

2019 ◽  
pp. 262-270 ◽  
Author(s):  
Salome A. Chime ◽  
Ikechukwu V. Onyishi ◽  
Ifeoma O. Eze
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Moringa Oleifera ◽  
Extended Release ◽  
In Vitro Release ◽  
Antimicrobial Studies ◽  
Microbial Inhibition ◽  
Vitro Release ◽  
Moringa Oleifera Seed

Objective: To formulate extended release gentamicin-entrapped lipospheres using natural lipids from Irvingia wombolu (IWF) and Moringa oleifera seed (MO) popularly known as Ben oil. Methods: Different lipid combinations including IWF and Phospholipon 90H (P90H) and IWF and MO were employed in the formulation of lipospheres. The formulations were analysed for particle size, encapsulation efficiency (EE), pH stability and antimicrobial studies amongst other tests. Also the in vitro release properties were studied in Phosphate buffer pH 7.2. Results: High EE of up to 90 % were obtained for the various LM combinations. The pH was stable over 30 days and the formulations showed about 93 % release of gentamicin at 12 h. Lipospheres formulated with MO matrices showed synergism in the microbial inhibition than other formulations. Conclusion: Natural lipids from Irvingia wombolu and Moringa oleifera seed could be used in formulating oral extended release gentamicin lipospheres.

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 AND IN VITRO EVALUATION OF CURCUMIN LOADED JACKFRUIT SEED STARCH NANOPARTICLES

2020 ◽  
pp. 32-35
Author(s):  
JUNMONI NATH
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Infrared Studies ◽  
Drug Entrapment Efficiency ◽  
Starch Nanoparticles ◽  
Vitro Release

Objectives: To meet the above aim the following objectives are undertaken: (1) Isolation of starch from jackfruit seeds and formulation of curcumin loaded jackfruit seed starch nanoparticles (2) In vitro evaluations of the drug loaded nanoparticles Methods: Jackfruit seed starch nanoparticles were prepared by Nanoprecipitation technique. In this technique, jackfruit seed starch was mixed with curcumin and acetone solution using a magnetic stirrer at 600 rpm. To the above solution, water were added dropwise and stirred at room temperature until acetone was completely vaporized. Nanoparticles were separated by centrifugation at 4000 rpm after 40 min. Results: Particle size of prepared nanoparticle formulations was found to be 371 to 411.72 nm with PDI of 0.148 to 0.356. The maximum % drug entrapment was found to be 57.34 % with formulation F5. In vitro release studies showed sustained release of drug till 12 h. Conclusion: The prepared nanoparticles were evaluated for its particle size, drug entrapment efficiency, in vitro drug release study, and surface morphology studies by scanning electron microscopy. The results of Fourier transform infrared studies of 1:1 physical mixture of drug and excipients confirmed the absence of incompatibility. Thus, the study concludes that curcumin loaded jackfruit seed starch nanoparticles were developed successfully by nanoprecipitation, which is expected to enhance the oral bioavailability of curcumin.

Preliminary studies on optimization of anti-parkinson drug loaded lipid nanoparticles enriched hydrogel formulations for management of Parkinson’s disease

2021 ◽  
Vol 11 ◽  
Author(s):  
Kumara Swamy ◽  
Ramesh Alli ◽  
Thirupathi Gorre
Keyword(s):  
Parkinson’S Disease ◽  
Particle Size ◽  
Parkinson's Disease ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Release Studies ◽  
Lipid Nanocarriers ◽  
Vitro Release

Purpose: Ropinirole (RP), is a selective dopamine agonist that is used alone or with other medications to treat the symptoms of Parkinson’s disease (PD). RP has low bioavailability of only about 50% due to the first-pass metabolism, and it requires frequent dosing during oral administration. Aim: The objective of the current research was to develop RP loaded solid lipid nanoparticles (RP-SLNs), nanostructured lipid carriers (RP-NLCs), and their corresponding hydrogels (RP-SLN-C and RP-NLC-C) that could enhance RP therapeutic outcomes during PD treatment. Methods: RP nanoparticles were prepared by homogenization followed by probe sonication and optimized based on particle size, polydispersity index (PDI), zeta potential (ZP), % assay, % entrapment efficiency, and in vitro release studies. Optimized formulations were converted to hydrogel formulations using Carbopol 934 as a gelling polymer and optimized based on rheological and release characteristics. Optimized formulations were further evaluated using differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), freeze-drying, and stability study at refrigerated and room temperatures. Results: The optimized RP-SLN formulation showed particle size and entrapment efficiency of 213.5±3.8 nm and 77.9±3.1% compared to 190.6±3.7 nm and 85.7±1.7% for optimized RP-NLC formulation. PXRD supplemented and confirmed DSC results, RP was entrapped in a molecularly dispersed state inside the core of the lipid nanocarrier. Furthermore, RP loaded lipid nanocarriers revealed a spherical shape in SEM images. In vitro release studies demonstrated sustained release profiles for RP from SLNs, NLCs, and their hydrogels over 24 h. Optimized SLN, NLC, and nanocarrier loaded hydrogel formulations were stable over three months at 4ºC and 25ºC storage conditions. Conclusion: Overall, the results demonstrated that lipid nanocarriers and their corresponding hydrogel formulations can be considered as a topical drug delivery vehicle for RP during the treatment of PD.

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

scholarly journals Preparation, In Vitro characterization and stability studies of ropinirole lipid nanoparticles enriched hydrogel for treatment of neurodegeneration diseases

2021 ◽  
Vol 11 (2-S) ◽  
pp. 66-75
Author(s):  
Kumara Swamy Samanthula ◽  
Ramesh Alli ◽  
Thirupathi Gorre
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Solid Lipid ◽  
Release Studies ◽  
Vitro Release

Ropinirole (RP), is a selective dopamine agonist that is used alone or with other medications to treat the symptoms of Parkinson’s disease (PD). RP has low bioavailability of only about 50% due to the first-pass metabolism, and it requires frequent dosing during oral administration. The objective of the current research was to develop RP loaded solid lipid nanoparticles (RP-SLNs), nanostructured lipid carriers (RP-NLCs), and their corresponding hydrogels (RP-SLN-C and RP-NLC-C) that might improve efficacy in PD treatment. RP nanoparticles were prepared by homogenization aided probe sonication method and optimized based on particle size, polydispersity index (PDI), zeta potential (ZP), assay, entrapment efficiency, and in vitro release studies. Optimized formulations were converted to hydrogel formulations using Carbopol 934 as a gelling polymer and optimized based on rheological and release characteristics. Optimized formulations were further evaluated using differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), freeze-drying, and stability study at refrigerated and room temperatures. The optimized RP-SLN formulation showed particle size and entrapment efficiency of 213.5±3.8 nm and 77.9±3.1% compared to 190.6±3.7 nm and 85.7±1.7% for optimized RP-NLC formulation. PXRD supplemented and confirmed DSC results, RP was entrapped in a molecularly dispersed state inside the core of the lipid nanocarrier. Furthermore, RP loaded lipid nanocarriers revealed a spherical shape in SEM images. In vitro release studies demonstrated sustained release profiles for RP from SLNs, NLCs, and their hydrogels over 24 h and were stable over three months at 4ºC and 25ºC storage conditions. Keywords: Parkinson’s disease, Ropinirole, Solid lipid nanoparticles, Nanostructured lipid carriers, Hydrogel.

Sign in / Sign up

Export Citation Format

Share Document