scholarly journals Study of Ethyl Cellulose Based Sustained Release Microspheres of Naproxen Sodium

2012 ◽  
Vol 10 (2) ◽  
pp. 123-129 ◽  
Author(s):  
Kowshik Sarkar ◽  
Sams Mohammad Anowar Sadat ◽  
Md Saiful Islam ◽  
Reza-ul Jalil

The present study was conducted to prepare sustained release microspheres of naproxen sodium using ethyl cellulose (Ethocel 20 cps) polymer. Three different plasticizers namely polyethyleneglycol 600   (PEG 600), polyethyleneglycol 6000 (PEG 6000) and triethyl citrate (TEC) were used at 10% (wt/wt) and 40% (wt/wt) level of the drug content. Prepared microspheres were characterized with respect to drug loading,   microsphere particle size, microsphere surface morphology and release behavior. Surface morphology of the microspheres was examined in a scanning electron microscope. Drug release was observed in phosphate buffer   solution of pH 6.8 for 8 hours. At 10% level of the plasticizers, percent release was 93.36%, 93.02% and   92.67% for PEG 600, PEG 6000 and TEC respectively after 8 hours. On the other hand, at 40% level, percent   release was 81.12%, 70.06% and 51.12% for PEG 600, PEG 6000 and TEC respectively after the same   duration. Release mechanisms followed case I or fickian model   DOI: http://dx.doi.org/10.3329/dujps.v10i2.11792   Dhaka Univ. J. Pharm. Sci. 10(2): 123-129, 2011 (December)  

2012 ◽  
Vol 482-484 ◽  
pp. 2605-2608 ◽  
Author(s):  
Li Li Ruan ◽  
Da Xin Wang ◽  
You Wei Zhang ◽  
Jiong Xin Zhao ◽  
Xiu Fang Zhang ◽  
...  

In this paper we study in vitro release of paclitaxel-loade polycaprolactone sustained-release microspheres. Different pH values release medium is used to simulate pH conditions in different parts of body, and determination the paclitaxel in Microspheres by High Performance Liquid Chromatography according Chinese Pharmacopoeia 2010. The experimental results indicate that the microspheres release rates of same drug loading content in buffer solution of pH 7.35 is the fastest, and in the pH 1.2 is the slowest. The drug release behavior according to the first-order model and it is not affected by drug loading rate of microspheres. The prepared paclitaxel-loade polycaprolactone sustained-release microspheres has good sustained release effect in different release media, and the results can provide references for further study of in vivo release.


2013 ◽  
Vol 22 ◽  
pp. 31-40
Author(s):  
Jin Qiao Xu ◽  
Hai Xing Xu ◽  
Zubad Newaz ◽  
Ran Li ◽  
Yu Zhang ◽  
...  

A new method of reversible association of melphalan (MEL) to magnetic Fe3O4 nanoparticles preparing MEL magnetic microspheres was developed for magnetically targeted chemotherapy. The efficacy of this approach was evaluated in terms of encapsulation efficiency (EE), drug loading content (DLC), delivery properties and cytotoxicity in vitro. Magnetic Fe3O4 nanoparticles were synthesized by co-precipitation methods and characterized by X-ray diffraction (XRD), fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM) and magnetization measurements. The MEL magnetic microspheres were obtained through emulsion cross-linking method and characterized by FTIR, magnetization measurements and scan electron microscopy (SEM). The EE and DLC were determined using a Spectro Vision DB-18805 spectrophotometer. The MEL magnetic microspheres showed good EE values, between 60.6% and 75.6%, as well as good DLC values, between 16.7% and 32.2%, and the magnetic properties were not significantly affected by incorporation of the drug. The in vitro drug release study was carried out in phosphate buffer solution (PBS), simulating physiologic body fluid conditions at 37o C with pH = 7.4. The release profiles showed an initial fast release rate, which decreased as time progressed; about 60% of the drug was released in the first 4 h, and about 78.23 % had been released after 24 h. The results indicated that the prepared magnetic microspheres may be useful for potential applications of MEL for magnetically targeted chemotherapy.


2015 ◽  
Vol 13 (2) ◽  
pp. 149-166 ◽  
Author(s):  
Navid Jubaer Ayon ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza

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)


2017 ◽  
Vol 872 ◽  
pp. 178-182
Author(s):  
Feng Fen Zhang ◽  
Chun Lin Xie ◽  
Xiao Juan Yang ◽  
Xiu Feng Xiao

In this work, vertically aligned titania nanotube arrays (TNTs) were fabricated on Ti surface in fluoride-containing electrolytes by anodization. TNTs were treated by hydrothermal treatment in the saturated solution of [Cu(NH3)4 (H2O)2]2+. Different hydrothermal treatment conditions were studied to obtain the best modification effect in the experiment. The TNTs were loaded with alendronate and ibuprofen via vacuum drying method and the release properties from the nanotubes were detected in phosphate buffer solution (PBS). The samples were characterized by field emission scanning electron microscopy, X-ray diffraction, and UV-Vis spectrophotometer. The data show that copper is successfully doped to the nanotube surface by hydrothermal treatment, and the optimum hydrothermal treatment conditions are 200°C, 0.5h. The drug loading capacity of the modified sample increased obviously, whether it was hydrophilic or hydrophobic. Meanwhile, the modified nanotubes release more slowly in the later stage. This approach provides an alternative to tailor the surface of TNTs and offer considerable propects for diverse biomedical applications.


2015 ◽  
Vol 645-646 ◽  
pp. 1374-1382 ◽  
Author(s):  
Rui Hua Zhang ◽  
Li Qin Li ◽  
Chen Wang ◽  
Xiao Jing Lu ◽  
Tong Shi ◽  
...  

Huperzine A (HupA), an alkaloid isolated from theChinese club moss, is a reversible inhibitor of cholinesterases which cross the blood-brain barrier and show high specificity for acetylcholinesterase (AChE). However, HupA induces unwanted side effects in an effective dose against nerve agent poisoning. In the present study, HupA–loaded poly (lactide-co-glycolide) nanoparticles (HupA-PLGA-NP) were prepared using the O/W emulsion solvent evaporation method. The results of SEM demonstrated that HupA-PLGA-NP had an spherical shape and a smooth surface without pores. It’s mean diameter and PDI were 208.5±3.6nm and 0.09±0.01 respectively. The Zeta potential was-35.3±1.8mV and the drug loading was 2.86±0.6%.In vitrodrug release studies showed that HupA-PLGA-NP had a sustained-release behavior in phosphate buffer solution, The accumulated amount of HupA was about 72.1% at 48h with a low burst release within 30min. The LD50values of HupA and HupA-PLGA-NP were 1.40 and 4.85mg/kg respectively, showing that the toxicity of HupA was reduced by 3.5 times. We evaluated the protective efficacy for different doses of HupA or HupA-PLGA-NP against 1.0×LD95(143.0μg/kg) soman toxicity. The results confirmed that HupA (0.3~0.5mg/kg) or HupA-PLGA-NP (0.5~1.5mg/kg) could ensure animals survive. However, about 10% of the animals injected with HupA (0.8mg/kg) died, while no animals died when injected with HupA-PLGA-NP (1.5mg/kg). Aim to 100% survival rate, the effective protective time (12h) of HupA-PLGA-NP (0.5mg/kg,iv) against 1.0×LD95soman toxicity in mice was significantly prolonged compared with that of HupA (4h). The study of AChE activity showed that whole-blood and supernatant of brain diluted by 80-fold and 10-fold respectively were optimum in this study. AChE inhibition after administration of HupA and HupA-PLGA-NP (0.5mg/kg,iv) was recorded and analyzed, The peak values of AChE inhibition in whole-blood and brain by HupA-PLGA-NP (17.6% and 21.8%) were lower than those by HupA (33.7% and 31.9%) and AChE inhibition time by HupA-PLGA-NP was longer than that by HupA. These data confirmed that HupA-PLGA-NP had less toxic and more longer time than HupA against 1.0×LD95soman poisoning and warrant further development as a potent medical countermeasure against chemical warfare nerve agents (CWNAs) poisoning.


2021 ◽  
Vol 89 (2) ◽  
pp. 25
Author(s):  
Adejumoke Lara Ajiboye ◽  
Uttom Nandi ◽  
Martin Galli ◽  
Vivek Trivedi

The aim of this study was to understand the effect of high shear homogenization (HSH) and ultrasonication (US) on the physicochemical properties of blank and olanzapine loaded nanostructured lipid carriers (NLCs) along with their drug loading potential and drug release profiles from formulated particles. NLCs were prepared with different ratios of Compritol and Miglyol as the solid and liquid lipids, respectively, under changing HSH and US times between 0 to 15 minutes. The surfactants (Poloxamer 188 (P188) and tween 80) and the drug content was kept constant in all formulations. The prepared NLCs were evaluated for particle size, polydispersity index, zeta potential, drug crystallinity and chemical interactions between lipids and OLZ. The in-vitro drug release was performed using dialysis tube method in phosphate buffer solution (PBS) at pH 7.4. The formulated NLCs were negatively charged, spherically shaped and monodisperse, with particle sizes ranging from 112 to 191 nm. There was a significant influence of US time on the preparation of NLCs in comparison to HSH, where a significant reduction in the mean particle diameter was seen after 5 min of sonication. An increase of Miglyol content in NLCs led to an increase in particle size. In general, application of US led to decrease in particle size after HSH but an increase in particle diameter of low Miglyol containing preparation was also observed with longer sonication time. OLZ was successfully encapsulated in the NLCs and a total release of 89% was achieved in 24 hours in PBS at pH 7.4.


Author(s):  
MONISHA BANSAL ◽  
MANPREET KAUR WALIA ◽  
GURFATEH SINGH ◽  
S. L. HARIKUMAR

Objective: The objective of the present investigation was to design and evaluate a gel containing lycopene loaded colloidal microparticles. Methods: The lycopene loaded colloidal microparticles were successfully prepared by Cloud point technique to form colloids using Tween 40 and Tween 60 surfactant solution and then incorporated into microparticles by solvent evaporation method using polymer like HPMC and ethyl cellulose. These colloidal microparticles were evaluated for particle size (PS), drug loading (DL), entrapment efficiency (EE), Scanning Electron Microscopy (SEM). Further, these colloidal microparticles were incorporated into a topical formulation i.e., gel. This topical formulation was then evaluated for macroscopic examination, viscosity, drug content, spreadability, antioxidant activity, in vitro permeation and release kinetics. Results: Colloidal microparticles were successfully prepared and the particle size, drug loading and entrapment efficiency were found to be 249.45±14.2 μm, 49.8±0.96 % and 93.4±0.26 % respectively. FTIR study depicted no chemical interaction between pure drug lycopene and other excipients. The topical formulation showed sustained release and followed Korsmeyer-Peppas release kinetics model. Conclusion: The sustained release topical formulation of lycopene was successfully prepared using Tween 40 and Tween 60 surfactant solution and combination of HPMC and ethyl cellulose and evaluated for several parameters.


2012 ◽  
Vol 538-541 ◽  
pp. 68-71 ◽  
Author(s):  
Jian Xiang Yu ◽  
Tai Qi Liu

In his paper, polylactic acid ultra- thin fibers membrane carried rifampicin were prepared by electrospinning technology, and release experiment of polylactic acid super thin fiber membrane with rifampicin were carried out in PBS solution. The resulted ultra-fine fibers membrane of polylactic acid membrane were characterized through scanning electron microscopy to decided the morphology, the results showed that the drug-loaded polylactic acid membrane contained microfiber in a range of 1μm-8μm in diameter; polylactic acid fiber diameter distribution was affected by molecular weight of polylactic acid, concentration of polylactic acid, quantity of drug loaded and spinning parameters such as voltage, the average fiber diameter increased when improved the mass fraction of PLA solution, the diameter of PLA ultra-fine fibers loaded rifampicin was thiner than PLA ultra-fine fibers. The performance of controlled release in phosphate buffer solution (PBS) was detected by UV, and their delivery rate was calculated by the detected result. The sustained release effect of polylactic acid Molecular with weight of 150,000 loaded rifampicin was better than polylactic acid ultra-fine fibers with the molecular weight of 100,000, the addition of lipase can improve release rate of rifampicin.


2020 ◽  
Vol 12 (10) ◽  
pp. 1476-1484
Author(s):  
Jun Zhao ◽  
Longbiao Xu ◽  
Ming Zhao ◽  
Chao Wei

The polylactic acid/glycolic acid (PLGA) sustained-release microspheres are used as the main material for local sustained-release in the study. Ultrasonic emulsification-solvent evaporation method is applied to combine the sustained-release microspheres material with temozolomide to form a composite sustained-release microsphere (TMZ-PLGA-W). The ratio of lactic acid (LA) and glycolic acid (GA) was adjusted so as to test the morphological characteristics of TMZ-PLGA-W at different ratios. The amount of drug released and the encapsulation rate of the material at different time periods were calculated. The C6 glioma system was implanted into the right caudate nucleus of Wistar rats to obtain a rat intracranial glioma model. The models were divided into 5 groups according to different sustained-release materials, and each group had 10 rats. The brain tumor at different times were compared and the survival time of rats was statistically calculated. The TMZ-PLGA-W sustained-release microsphere material with LA/GA ratio of 25%/75% was selected and placed in C6 cells culturing incubator according to different drug loadings. The cell activity according to the culture time was observed. The results showed that the TMZ-PLGA-W sustained-release microspheres prepared in the study were stable in structure, uniform in size, and free of cracks. At the same time, the sustained-release curve showed that the microsphere material conformed to the biodynamic law, which could reduce the burst effect and prolong the sustained release of the drug. The application of TMZ-PLGA-W sustained-release microspheres can effectively inhibit the increase in the area of brain tumors in rats, and at the same time improve the survival rate of rats. The increase in the drug loading of the microspheres can further inhibit the growth of glioma cells.


2011 ◽  
Vol 335-336 ◽  
pp. 1469-1472 ◽  
Author(s):  
Chun Yan Wang ◽  
Xiu Feng Xiao ◽  
Dan Mao ◽  
Hai Zhen Tang ◽  
Rong Fang Liu

TiO2 nanotube arrays possess regular hollow structure, large specific surface area and good biocompatibility, which are good for filling with drugs. In this paper, a vertically aligned nanotube arrays of titanium oxide was fabricated on the surface of titanium substrate in fluoride-containing electrolytes by anodization. The TiO2 nanotube arrays were loaded with alendronate via vacuum drying method and the release of alendronate from the nanotubes were detected in phosphate buffer solution(PBS). The samples were characterized by scanning electronic microscope(SEM), X-ray diffraction(XRD), Fourier transform infrared(FTIR), Thermogravimetric analysis (TG) and visible ultraviolet spectrophotometer(UV-vis). The data showed that the release of alendronate from the nanotubes includes two stages: burst release and sustained release, the result indicated that the drug loaded in the TiO2 nanotubes has a certain amounts of sustained-release effect.


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