Preparation and Characterisation of TAM-PLGA Microspheres by Solvent Evaporation

2011 ◽  
Vol 194-196 ◽  
pp. 558-561
Author(s):  
Bai Li Shu ◽  
Xu Ming Xue ◽  
Qi Meng Zhang ◽  
Ying Li Liu ◽  
Zong Hui Ma ◽  
...  
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Size Distribution ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
Plga Microspheres ◽  
Sphere Size ◽  
Particle Size Analyzer ◽  
Release In Vitro

Uniformly sized microspheres of poly(d, l-lactic-co-glycolic) (PLGA) encapsulating tamoxifen(TAM) were successfully prepared by solvent evaporation. In this study three different polylactide-co-glycolides were used with differing lactide-glycolide ratios (50:50, 75:25, and 85:15, respectively). The sphere size distribution and morphology was analyzed using Laser Particle Size Analyzer and SEM. The drug loading and release in vitro of the microspheres were also investigated. The result showed that the microspheres have good spherical and better sustained release.

Formulation optimization and in vitro characterization of granisetron-loaded polylactic-co-glycolic acid microspheres prepared by a dropping-in-liquid emulsification technique

2021 ◽  
Vol 18 ◽  
Author(s):  
Atef Mohammed Qasem Ahmed ◽  
Li-Qing Chen ◽  
Huan-Huan Du ◽  
Wei Sun ◽  
Qing-Ri Cao
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Molecular Interactions ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Plga Microspheres ◽  
Scanning Calorimetry ◽  
Medium Ph ◽  
Hardening Process

Purpose: Traditional dosage forms of granisetron (GRN) decrease patient compliance associated with repeated drug administration because of the short half-life of the drug. Methods: In this study, novel GRN-loaded polylactic-co-glycolic acid (PLGA) sustained release microspheres were prepared for the first time via a dropping-in-liquid emulsification technique. The effect of various factors, such as pH of the outer phase, Tween80, polyvinyl alcohol (PVA) concentrations, and hardening process, on the encapsulation efficiency (EE), drug loading (DL), and particle size of microspheres were extensively studied. The physicochemical properties, including drug release, surface morphology, crystallinity, thermal changes, and molecular interactions, were also studied. Results: GRN has a pH-dependent solubility and showed a remarkably high solubility under an acidic condition. The EE of the alkaline medium (pH 8) was higher than that of the acidic medium (pH 4.0). EE and DL decreased in the presence of Tween80 in the outer phase, whereas EE significantly increased during hardening. The particle size of microspheres was not affected by PVA and Tween80 concentrations, but it was influenced by PVA volume and hardening. X-ray diffraction and differential scanning calorimetry results showed that the physical state of the drug changed from a crystalline form to an amorphous form, thereby confirming that the drug was encapsulated into the PLGA matrix. Fourier transform-infrared spectroscopy confirmed that some molecular interactions occurred between the drug and the polymer. GRN-loaded PLGA microspheres showed sustained release profiles of over 90% on week 3. Conclusion: GRN-loaded PLGA microspheres with sustained release were successfully prepared, and they exhibited a relatively high EE without Tween 80 as an emulsifier and with hardening process.

scholarly journals BIODEGRADABLE POLYMER: A NOVEL PHARMACEUTICAL CARRIER FOR SUSTAINED RELEASE OF METRONIDAZOLE

2017 ◽  
Vol 10 (10) ◽  
pp. 136
Author(s):  
Gayathri Hariharan ◽  
Priyanka Sinha
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Biodegradable Polymer ◽  
Drug Loading ◽  
Cross Linking ◽  
Loading Capacity ◽  
Flow Properties ◽  
Chitosan Microspheres

Objective: To optimize and evaluate the formulation of metronidazole (MT)-loaded chitosan microspheres and to investigate the efficiency of biodegradable polymer in developing sustained release formulation of MT to prolong the action of drug.Methods: MT microspheres were prepared using emulsion cross-linking method. Polymer-drug compatibility study was done using Fourier transform infrared. Physical characteristics were evaluated by particle size,SEM, flow properties etc. In vitro studies for evaluating drug release for MT-loaded chitosan microspheres were done by dissolution study.Results: Particle size of the formulated microspheres was found to be within the range of 110-130 μm. Flow properties of F1-F7 such as angle of repose, bulk density, and tapped density were found to be within limits. Drug entrapment efficiency was found to be better for all the formulations within the range of 74.82-84.32% w/w. Drug loading capacity was found to be in the range of 56-83.2% w/v. In vitro drug release was found to be in the range of 81.32-96.23% w/v.Conclusion: In spite of all the above results, we conclude that F5 formulation was optimized depending on the data obtained from the drug loading capacity and percentage drug release studies. F5 formulation is formulated with drug-polymer ratio 1:2 with 1% of di octyl sodium sulfo succinate and 8 ml of glutaraldehyde as a cross-linking agent.

scholarly journals Encapsulation of metronidazole in polycaprolactone microspheres

2019 ◽  
Vol 9 (1) ◽  
pp. 190-194
Author(s):  
Rima Kassab ◽  
Dima Moussa ◽  
Cherine Saliba ◽  
Paolo Yammine
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
Compatibility Study ◽  
Drug Encapsulation ◽  
Evaporation Technique ◽  
Ft Ir ◽  
Ir Study

Non-aqueous oil-in-oil solvent evaporation technique is used for the preparation of polycaprolactone microspheres loaded with the antibiotic metronidazole by introducing different masses for the drug. The prepared microspheres are characterized by calculating drug encapsulation and drug loading percentages, measuring the corresponding particle size, performing FT-IR polymer-drug compatibility study and in vitro drug release. Moderate drug encapsulation values with a maximum of 34% are observed due to the low molecular weight of the drug. Microspheres had a particle size ranging between 130 and 280 µm with a spherical profile and porous structure. FT-IR study showed no interactions between the drug and the polymer. Drug release studies showed fast release rates for all the formulations with the slowest release for the highest drug loading. Keywords: polycaprolactone, metronidazole, targeted drug delivery, solvent evaporation.

scholarly journals Preparation and characterization of Gliclazide incorporated Cellulosic Microspheres: studies on drug release, compatibility and micromeritics

2015 ◽  
Vol 13 (2) ◽  
pp. 149-166 ◽  
Author(s):  
Navid Jubaer Ayon ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Sustained Release ◽  
Release Rate ◽  
Drug Loading ◽  
Angle Of Repose ◽  
Flow Properties ◽  
Dissolution Apparatus

Polymeric microspheres of gliclazide were prepared to provide sustained release delivery of gliclazide to aid in continuous therapy with high margin of safety. Gliclazide was microencapsulated with different polymers namely HPMC K100LV, Ethocel (20 cps) and HPMC K100M by emulsion solvent evaporation technique using acetone as internal phase and liquid paraffin as external phase. Seventeen formulations were prepared using different drug loading and polymeric ratio of which nine formulations were prepared by a 32 full factorial design. Each formulation was evaluated for flow properties, particle size, surface morphology, drug entrapment efficiency, drug release and compatibility. Yield (%) for every batch of microspheres was measured. Flow properties of the microspheres were examined by determining bulk density, tapped density, Carr’s compressibility index, Hausner ratio and angle of repose. Particle size distribution was examined by sieving and particle size analyzer. Surface morphology was determined by scanning electron microscopy (SEM). In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) for a period of 8 hours at 37°C using phosphate buffer ( pH 7.4). FTIR and DSC studies established compatibility of the drug with the polymers. Microspheres prepared with Ethocel (20 cps) and HPMC K100M were free flowing than those prepared only with HPMC K100LV. Entrapment efficiencies were within 75.88-99.69%. Microspheres prepared with Ethocel (20 cps) and HPMC K100M showed more sustained release when compared to microspheres prepared with HPMC K100LV only. Increase in drug loading resulted in increased drug release for the microspheres. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranging from diffusion controlled to anomalous type. Ethocel and HPMC K100M in a ratio of 1:3 exhibited better sustained release properties than 1:1 and 3:1 ratios. The release rate of gliclazide from microspheres prepared with Ethocel (20 cps) and HPMC K100M was less than the release rate of gliclazide from microspheres prepared with HPMC K100LV, demonstrating Ethocel and HPMC K100M as suitable polymeric blend for preparing the controlled release formulation for gliclazide whereas, HPMC K100LV was found not suitable candidate when used alone as a polymer. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21893 Dhaka Univ. J. Pharm. Sci. 13(2): 149-166, 2014 (December)

scholarly journals Development of Indomethacin Sustained Release Microcapsules using Ethyl Cellulose and Hydroxy Propyl Methyl Cellulose Phthalate by O/W Emulsification

1970 ◽  
Vol 7 (1) ◽  
pp. 83-88 ◽  
Author(s):  
Md Abu Hena Mostafa Kamal ◽  
Maruf Ahmed ◽  
Mir Imam Ibne Wahed ◽  
Md Shah Amran ◽  
Sharif Md Shaheen ◽  
...  
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Release Rate ◽  
Ethyl Cellulose ◽  
Methyl Cellulose ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Key Words Indomethacin ◽  
Emulsification Solvent Evaporation

Indomethacin (IM) sustained release microcapsules were successfully prepared using ethyl cellulose (EC) and hydroxy propyl methyl cellulose phthalate (HPMCP) by o/w emulsification-solvent evaporation technique. The prepared microcapsules were evaluated for size, shape, drug content and in vitro drug release. The microcapsules show sustained release curves at pH 7.2 phosphate buffer for up to 6 h. The data obtained from the dissolution profiles were compared in the light of different kinetics models and the regression coefficients were compared. The in vitro dissolution study confirmed the Higuchi-order release pattern. Particle size and release data analysis from five consecutive batches prepared in the laboratory indicated suitable reproducibility of the solvent evaporation process. The release rate increased exponentially with the addition of HPMCP in EC. IM release rate was observed highest with the highest concentration of HPMCP (3:7 ratio of EC:HPMCP), used in the present studies. On the other hand, IM release rate was lowest when EC and HPMCP combination was used at the ratio of 10:0. When percent of HPMCP was increased, the particle size of microcapsules was decreased. Key words: Indomethacin, sustained release, microcapsule, HPMCP, EC, Higuchi-order  DOI = 10.3329/dujps.v7i1.1223 Dhaka Univ. J. Pharm. Sci. 7(1): 83-88, 2008 (June)

Electronic particle size measurements of platelet aggregates formed in vitro

1975 ◽  
Vol 38 (4) ◽  
pp. 739-744 ◽  
Author(s):  
R. T. Solis ◽  
C. B. Wright ◽  
M. B. Gibbs
Keyword(s):  
Particle Size ◽  
Size Distribution ◽  
Adenosine Diphosphate ◽  
Human Platelets ◽  
Time Dependent ◽  
Experimental Conditions ◽  
Particle Size Analyzer ◽  
Platelet Aggregates ◽  
The Individual

The aggregation of human platelets induced by adenosine diphosphate (ADP) was used to evaluate electronic particle size analyzer measurements of platelet aggregates in plasma. As platelets began to clump in plasma, the total volume and the diameter of individual aggregates increased; after a time dependent on experimental conditions, the diameter increased but the total volume remained unchanged. Similar but opposite changes in size distribution occurred during platelet deaggregation. The total volume of aggregates formed in plasma varied (linear correlation coefficient = 0.99) with the total volume of platelets which were available to clump and with simultaneous changes in optical density. The diameter of the aggregates varied with the concentration of, and time of exposure to, ADP and with the total volume of platelets and aggregates in plasma was not different from that of control platelets in untreated plasma, the individual platelets aggregated without an accompanying increase in size. This study demonstrates that platelet aggregation can be characterized by electronic measurements of the size distribution of platelet aggregates.

scholarly journals Development of Oral Sustained Release Rifampicin Loaded Chitosan Nanoparticles by Design of Experiment

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Bhavin K. Patel ◽  
Rajesh H. Parikh ◽  
Pooja S. Aboti
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Design Of Experiment ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Kinetic

Objective. The main objective of the present investigation was to develop and optimize oral sustained release Chitosan nanoparticles (CNs) of rifampicin by design of experiment (DOE). Methodology. CNs were prepared by modified emulsion ionic gelation technique. Here, inclusion of hydrophobic drug moiety in the hydrophilic matrix of polymer is applied for rifampicin delivery using CN. The 23 full-factorial design was employed by selecting the independent variables such as Chitosan concentration (X1), concentration of tripolyphosphate (X2), and homogenization speed (X3) in order to achieve desired particle size with maximum percent entrapment efficiency and drug loading. The design was validated by checkpoint analysis, and formulation was optimized using the desirability function. Results. Particle size, drug entrapment efficiency, and drug loading for the optimized batch were found to be 221.9 nm, 44.17 ± 1.98% W/W, and 42.96 ± 2.91% W/W, respectively. In vitro release data of optimized formulation showed an initial burst followed by slow sustained drug release. Kinetic drug release from CNs was best fitted to Higuchi model. Conclusion. Design of Experiment is an important tool for obtaining desired characteristics of rifampicin loaded CNs. In vitro study suggests that oral sustained release CNs might be an effective drug delivery system for tuberculosis.

scholarly journals Development of Curcumin loaded Nanostructured Lipid Carriers: Preparation, Characterization and In-vitro Evaluation of Anti-cancer Activity Against A-549 Human Lung Cancer Cell Line

2021 ◽  
pp. 66-88
Author(s):  
Shoaib Patel ◽  
Jinal Shah ◽  
Srinivas Bhairy ◽  
Rajashree Hirlekar
Keyword(s):  
Lung Cancer ◽  
Particle Size ◽  
Zeta Potential ◽  
Surface Morphology ◽  
Size Distribution ◽  
Human Lung ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Human Lung Cancer

Aims: The present study was aimed at preparing stable lyophilized curcumin loaded nanostructured lipid carriers (NLCs). The optimized lyophilized curcumin loaded NLCs were characterized and evaluated for various quality control parameters. Methodology: The optimized curcumin loaded NLCs were prepared by modified hot emulsification using compritol 888 ATO (CMPR), capmul MCM C8 EP (CAP) as solid and liquid lipids respectively. The combination of tween 80 (T80) and solutol HS 15 (SHS) were used as an emulsifier. The NLCs dispersion was lyophilized into powder form to improve the thermodynamic stability of the formulation. The lyophilized curcumin loaded NLCs were evaluated for particle size, size distribution, zeta potential, entrapment efficiency (EE), drug loading, assay, in-vitro drug release, crystallinity, thermal behavior and surface morphology studies. Results: The optimized lyophilized curcumin loaded NLCs have a mean particle size of 332.88 ± 5.9 nm with a size distribution of 0.350 ± 0.007, a zeta potential of 0.098 ± 0.019 mV with high entrapment of 97.64 ± 1.59% and drug loading of 2.50 ± 0.16%. The X-ray diffraction and endothermic peaks confirmed the maximum encapsulation of curcumin in lipid matrices. The particles were spherical with smooth surface morphology. In-vitro release studies showed sustained release for up to 24 h. The cytotoxicity against human lung cancer line A-549 for curcumin loaded NLCs was confirmed with positive control adriamycin (ADR). Conclusion: Curcumin loaded NLCs prepared had a nanosize particle distribution with maximum entrapment efficiency. Dispersion stability was increased by the lyophilization process. The solid lyophilized powder is reconstituted for oral delivery.

scholarly journals In-vitro study of formulation and evaluation of nanosuspension of tamoxifen

2018 ◽  
Vol 7 (5) ◽  
pp. 926
Author(s):  
Somasekhar M. Reddy ◽  
Navispaul N. Sriganth ◽  
Chandra S. Kumar ◽  
Santosh C. Gursale ◽  
Vijay V. Ragavan
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Size Distribution ◽  
Drug Loading ◽  
Polarized Light ◽  
Scanning Calorimetry ◽  
High Drug ◽  
Dissolution Properties ◽  
High Drug Loading

Background: Nanosuspension technology has been developed as a promising candidate for efficient delivery of hydrophobic drugs. It could maintain the required crystalline state of the drug with reduced particle size, leading to an increased reporting on dissolution rate and therefore improved bioavailability.Methods: In this paper, we report on the preparation of Tamoxifen nanosuspension by high-pressure homogenization (HPH). The aim is to obtain a stable nanosuspension with an increased drug saturation solubility and dissolution velocity. The morphology and particle size distribution of the modified nanosuspensions were characterized by the means of several analyses that included: transmission electron microscopy (TEM), polarized light microscopy (PLM), scanning electron microscopy, differential scanning calorimetry (DSC) and powder X- ray diffractometry (XRD).Results: HPH was employed to produce aqueous drug nanosuspensions with fine solubility and dissolution properties, which render the produced particles stable up to one month. In addition, the prepared nanosuspensions possessed a high drug-loading efficiency (10%). The recoded zeta potential values (≈ -27 mV) indicated that the prepared nanosuspensions possess a higher degree of long-term stability. TEM data showed narrow size distribution with average size 322.7 nm. Morphologically, as indicated from results, the produced nanosuspensions have a homogenous distribution even after redispersion, indicating the stability of the product.Conclusions: It was possible to obtain Tamoxifen nanosuspensions with fine solubility and dissolution properties. Nanosuspensions possessed a high drug- loading (10%), which could reduce the dosage administration and gastrointestinal side effects. HPH can be employed to produce aqueous drug nanosuspensions that are stable up to one month. Aqueous nanosuspension can be converted to dry nanocrystals by lyophilization which offer superior physicochemical properties.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

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