Alginate–Chitosan Nanocapsules for Controlled Release of Low Molecular Drugs Tegafur and DHAD

2013 ◽  
Vol 647 ◽  
pp. 264-268 ◽  
Author(s):  
Yuan Gang Liu ◽  
Hong Hao Mao ◽  
Shi Bin Wang ◽  
Qing Qing Sun
Keyword(s):  
Controlled Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Burst Release ◽  
Two Stage ◽  
Cumulative Release ◽  
Stage Process

Alginate–chitosan nanocapsules (Alg-CS NCs) were prepared by a two-stage process. The NCs were loaded with two low molecular drugs-tegafur and Mitoxantrone Hydrochloride(DHAD). Results revealed that these two drugs exhibited different drug loading and release characteristics. The drug loading and encapsulation efficiency of tegafur (<1%) were both lower than those of DHAD with the drug loading at about 20%~60% and encapsulation efficiency over 90%. However, tegafur showed a visible burst release phenomenon and the cumulative release rate of tegafur was much higher than that of DHAD.

Gemcitabine Nanoparticles Improve the Activity of Ovarian Cancer Cells by Inhibiting CA-125 and Apoptosis-Related Proteins

2021 ◽  
Vol 11 (7) ◽  
pp. 1400-1405
Author(s):  
Sisi Yi ◽  
Chen Feng ◽  
Xiaohua Hu
Keyword(s):  
Ovarian Cancer ◽  
Cell Viability ◽  
Release Rate ◽  
Inhibitory Action ◽  
Encapsulation Efficiency ◽  
Slow Release ◽  
Drug Loading ◽  
Ca 125 ◽  
Ovarian Cancer Cells ◽  
Related Proteins

In recent years, the risk of ovarian cancer (OC) has become increasingly prevalent. Gemcitabine (GE) provides excellent inhibitory action on some solid tumors, but how it affects OC remains elusive. In the present research, we prepared GE nanoparticles (GEN) and analyzed OC cell viability under its intervention, hoping to conceive novel ideas for future clinical treatment of OC. Through experiments, we observed that the encapsulation efficiency and drug loading of GEN were observably higher than those of GE alone, and the release rate presented a stable slow release state. Under GEN intervention, the viability of OC cells was decreased, the apoptosis rate was elevated, and the apoptosis-related proteins were activated, while CA-125 was suppressed. Therefore, we can see that GEN exert favorable inhibitory action on OC cell viability, whose mechanism may be achieved through activating apoptosis-related proteins and inhibiting CA-125, which may be a new scheme for OC treatment in the future.

scholarly journals Inulin-Grafted Stearate (In-g-St) as the Effective Self-Assembling Polymeric Micelle: Synthesis and Evaluation for the Delivery of Betamethasone

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Gholamabbas Chehardoli ◽  
Parham Norouzian ◽  
Farzin Firozian
Keyword(s):  
Zeta Potential ◽  
Sustained Release ◽  
Targeted Delivery ◽  
Encapsulation Efficiency ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Polymeric Micelle ◽  
Water Soluble ◽  
Burst Release ◽  
Potential Measurement

Background. Betamethasone as a corticosteroid drug is commonly used for the treatment of rheumatoid arthritis. Unfortunately, betamethasone is a low water-soluble drug and its efficacy is low. So an attractive strategy is the targeted delivery of betamethasone to the damaged joint using polymeric micelle-based carriers. Methods. Inulin-grafted stearate (In-g-St) was synthesized via the reaction of stearoyl chloride and inulin, then characterized by FT-IR and H-NMR. In-g-St forms micelles in the presence of betamethasone. The prepared polymeric micelles were characterized for size, zeta potential, drug loading, particles’ morphology, critical micelle concentration (CMC), and encapsulation efficiency. So sustained release polymeric micelles of betamethasone were developed by employing In-g-St. Results. The measurement of particle size showed a mean diameter of 60 and 130 nm for 10% and 20% drug-loaded micelles, respectively, and SEM showed that the particle’s morphologies are spherical. Zeta potential measurement for the drug-containing micelles showed a value of -11.8 mV. Drug loading efficiency and the encapsulation efficiency were 6.36% and 63.6%, as well as 18.97% and 94.88% for 10% and 20%, respectively. 20% drug-loaded polymer showed a small burst release of betamethasone at the first 3 h which was followed by sustained release in the next 24 h. Furthermore, the formula with 10% exhibited good sustained release properties except for the minor initial burst release. Conclusion. Data from the zeta potential, CMC, drug loading capacity, and in vitro drug release studies indicated that In-g-St polymeric micelles can be suitable candidates for the efficient delivery of hydrophobic drugs like betamethasone.

Preparation and evaluation of an oral mucoadhesive gel containing nystatin-loaded alginate microparticles

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
S. Mohammadi Samani ◽  
S. Karimaddini ◽  
Z. Sobhani ◽  
F. Ahmadi
Keyword(s):  
Calcium Chloride ◽  
Encapsulation Efficiency ◽  
Bitter Taste ◽  
Drug Loading ◽  
Dosage Forms ◽  
Release Profile ◽  
Burst Release ◽  
Carbopol Gel ◽  
Alginate Concentration ◽  
Preparation And Evaluation

Abstract Nystatin is an antifungal agent used for prophylaxis and treatment of candidiasis, especially oral mycosis. Efficacy of nystatin conventional dosage forms is limited by the short residence time and bitter taste of the drug. This research aims at designing an optimized formulation of oral mucoadhesive gel of nystatin-loaded alginate microparticles, which can be retained in the mouth. Sodium alginate solution containing nystatin was added to the solution of calcium chloride under stirring. Microparticles containing nystatin were incorporated into the Carbopol gel. Size, loading, and release profile and mucoadhesion were investigated. The most suitable microparticles with particle size of < 250 μm were prepared with alginate concentration of 1%(w/v), calcium chloride of 1%(w/v), drug:polymer concentration 1%, and ratio of alginate solution:calcium chloride of 1:10. This formulation showed 49.1% drug loading and 98.2% encapsulation efficiency. Carbopol 934 gel provided optimal mucoadhesive properties. Release profile proved a burst release, which can be attributed to the surface associated drug, followed by a slower sustained release phase for all microparticles. The developed system with ability to adhere to the oral mucosa has great appeal for treatment of localized infections and can mask bitter taste of the drug and be retained in the mouth for long periods.

scholarly journals Comparing Microspheres with Different Internal Phase of Polyelectrolyte as Local Drug Delivery System for Bone Tuberculosis Therapy

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Gang Wu ◽  
Long Chen ◽  
Hong Li ◽  
Chun-Ling Deng ◽  
Xiao-Feng Chen
Keyword(s):  
Release Rate ◽  
Drug Loading ◽  
Double Emulsion ◽  
Particle Size Analysis ◽  
Local Drug Delivery ◽  
Size Analysis ◽  
Burst Release ◽  
Water Solvent ◽  
Internal Phase ◽  
Local Drug Delivery System

We use hydrophobic poly(lactic-co-glycolic) acid (PLGA) to encapsulate hydrophilic ofloxacin to form drug loading microspheres. Hyaluronic acid (HA) and polylysine (Pls) were used as internal phase additives to see their influences on the drug loading and releasing. Double emulsion (water-in-oil-in-water) solvent extraction/evaporation method was used for the purpose. Particle size analysis display that the polyelectrolytes have low impact on the microsphere average size and distribution. Scanning electron microscope (SEM) pictures show the wrinkled surface resulted by the internal microcavity of the microspheres. Microspheres with HA inside have higher drug loading amounts than microspheres with Pls inside. The loading drug amounts of the microspheres increase with the HA amounts inside, while decreasing with the Pls amounts inside. All the polyelectrolytes adding groups have burst release observed in experiments. The microspheres with Pls internal phase have faster release rate than the HA groups. Among the same polyelectrolyte internal phase groups, the release rate increases with the amounts increasing when Pls is inside, while it decreases with the amounts increasing when HA is inside.

In vitro drug release and antibacterial activity evaluation of silk fibroin coated vancomycin hydrochloride loaded poly (lactic-co-glycolic acid) (PLGA) sustained release microspheres

2022 ◽  
pp. 088532822110640
Author(s):  
Shengtang Li ◽  
Xuewen Shi ◽  
Bo Xu ◽  
Jian Wang ◽  
Peng Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Burst Release ◽  
Plga Microspheres ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Initial Burst Release

Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.

scholarly journals Formulation and In vitro Evaluation of Eudragit RL 100 Loaded Fexofenadine HCl Microspheres

2016 ◽  
Vol 19 (1) ◽  
pp. 58-67
Author(s):  
Paroma Arefin ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Release Kinetics ◽  
Drug Loading ◽  
Release Mechanism ◽  
Order Release ◽  
Eudragit Rl ◽  
Fexofenadine Hcl

The present study deals with the formulation and evaluation of Fexofenadine hydrochloride (HCl) loaded sustained release microspheres by emulsion solvent evaporation method with Eudragit RL 100. The effects of percent drug loading on drug encapsulation efficiency, drug content and drug release rate were assessed. In vitro dissolution study was performed spectrophotometrically according to USP paddle method using phosphate buffer (pH 6.8) for 10 hours. The release rate of Fexofenadine HCl from the microspheres was significantly increased with the increase of drug loading. The drug release patterns were simulated in different kinetic orders such as zero order release kinetics, first order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism and Higuchi release kinetics was found to be the predominant release mechanism. Morphological changes due to different drug loading were assessed by scanning electron microscopic (SEM) technique. Differential scanning calorimetry and fourier transform infra-red (FT-IR) spectroscopy was performed to evaluate compatibility of drug with the polymer. A statistically significant variation indrug encapsulation efficiency and release rate was observed for variation in drug loading.Bangladesh Pharmaceutical Journal 19(1): 58-67, 2016

scholarly journals Fabrication of Bio-Nanocomposite Based on HNT-Methionine for Controlled Release of Phenytoin

Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2576
Author(s):  
Majid Abdouss ◽  
Nastaran Radgoudarzi ◽  
Alireza Mohebali ◽  
Elaheh Kowsari ◽  
Mojtaba Koosha ◽  
...  
Keyword(s):  
Controlled Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Release Profile ◽  
Burst Release ◽  
Loading Efficiency ◽  
Phenytoin Sodium ◽  
Good Potential ◽  
Ft Ir

In this study, a novel promising approach for the fabrication of Halloysite nanotube (HNT) nanocomposites, based on the amino acid named Methionine (Met), was investigated. For this purpose, Met layered on the outer silane functionalized surface of HNT for controlled release of Phenytoin sodium (PHT). The resulting nanocomposite (MNT-g-Met) was characterized by FTIR, XRD, Zeta potential, TGA, TEM and FE-SEM. The FT-IR results showed APTES and Met peaks, which proved the modification of the HNTs. The zeta-potential results showed the interaction between APTES (+53.30) and Met (+38.80) on the HNTs (−30.92). The FE-SEM micrographs have displayed the grafting of Met on the modified HNTs due to the nanotube conversion to a rough and indistinguishable form. The amount of encapsulation efficiency (EE) and loading efficiency (LE) of MNT-g-Met was 74.48% and 37.24%, while pure HNT was 57.5%, and 28.75%, respectively. In-vitro studies showed that HNT had a burst release (70% in 6 h) in phosphate buffer while MNT-g-Met has more controlled release profile (30.05 in 6 h) and it was found to be fitted with the Korsmeyer-Peppas model. Due to the loading efficiency and controlled release profile, the nanocomposite promote a good potential for drug delivery of PHT.

scholarly journals Preparation, Characteristics, and Controlled Release Efficiency of the Novel PCL-PEG/EM Rod Micelles

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
Huiling Song ◽  
Yu Yin ◽  
Jiahui Peng ◽  
Zixiu Du ◽  
Wei Bao
Keyword(s):  
Staphylococcus Aureus ◽  
Controlled Release ◽  
Encapsulation Efficiency ◽  
Orthogonal Design ◽  
Drug Loading ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Average Particle ◽  
Model Drug

In order to achieve sustained and controlled release of the hydrophobic cargoes, improve the bioavailability, and reduce the side effects of antibiotics, the model drug erythromycin (EM) was used to prepare polycaprolactone-polyethylene glycol (PCL-PEG)/EM micelles. PCL-PEG, a biocompatible and biodegradable amphiphilic polymer, was used as carrier material of micelles to optimize the formulation and preparation process by orthogonal design. The morphology, stability, drug loading, and encapsulation efficiency and the in vitro release behavior of the micelles were investigated. In addition, activity assays of anti-Staphylococcus aureus were performed. The results indicated that PCL-PEG/EM were rod-like micelles with an average particle size of 220 ± 2.6  nm and a zeta potential of +19 mV. The average drug loading and encapsulation efficiency were approximately 6.5% and 97.0%, respectively. The micelles were stable in the serum within three days. At the effective concentration of the drug, the formulation indicated no apparent toxicity to the cells. The micelles were able to rapidly enter Staphylococcus aureus (S. aureus) and to provide sustained release cargoes that effectively inhibited S. aureus proliferation. The present study provided a new platform for the rational and effective use of hydrophobic antibiotics to treat infections.

scholarly journals Synthesis and Controlled Release Behavior of Biodegradable Polymers with Pendant Ibuprofen Group

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Heying Deng ◽  
Jihua Song ◽  
Akoda Komlan Elom ◽  
Junlian Xu ◽  
Zhihui Fan ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Loading ◽  
Burst Release ◽  
Polymer Carriers ◽  
H Nmr ◽  
Chemical Structures ◽  
Angle Measurements ◽  
High Level ◽  
Continuous Use

The continuous use of nonsteroidal anti-inflammatory drugs such as ibuprofen frequently leads to some serious side-effects including stomach ulcers and bleeding. In this paper, two kinds of new biocompatible polyesters (PIGB, PIGH) and polyester-amide (PIGA) comprising biodegradable components (L-glutamic acid,1,4-butanediol, and1,6-hexanediol and6-amino hexanol) and ibuprofen as pendant group have been prepared by the melting polycondensation. The chemical structures of the monomer and polymers are characterized by FTIR,1H NMR spectrum, GPC, and contact angle measurements. The drug loading of ibuprofen reaches very high level (35–37%) for PIGB, PIGH, and PIGA carriers. The free ibuprofen molecules are releasedin vitrofrom polymer carriers in a controlled manner without a burst release, different from the release pattern observed in the other drug-encapsulated systems. It is also found that the different hydrophilicity among PIGB, PIGH, and PIGA plays a key role in the time-controlled release of ibuprofen. In addition, the viability of HeLa cells after 48 h of incubation reaches more than 100%, indicating no cytotoxicity for PIGB, PIGH, and PIGA carriers.

Preparation of Epidermal Growth Factor-Modified Targeted Doxorubicin Nanoliposomes and Therapy of Liver Cancer

2021 ◽  
Vol 21 (9) ◽  
pp. 4565-4572
Author(s):  
Yongan Chen ◽  
Lei Cheng ◽  
Dan Yu ◽  
Jie Shen ◽  
Zhengrong Zhou ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Hepatoma Cells ◽  
Average Particle ◽  
Therapeutic Effects ◽  
Drug Release Rate

The objective of this study was to prepare doxorubicin-loaded EGF modified PEG-nanoparticles and evaluate its targeting capability and therapeutic effects with EGFR-expressing hepatocellular carcinoma cells. The morphology, particle size distribution, and doxorubicin content of the nanoparticles were measured, and the drug loading and encapsulation efficiency were calculated. The doxorubicin nanoparticles prepared were regular circular, with good dispersibility, no adhesion, and the average particle size was (136.7±9.3) nm. The average encapsulation efficiency was (76.67±8.63)%, the average drug loading was (3.86±0.55)%; the drug release rate of doxorubicin was 100% for 12 h, and the doxorubicin nanometer was loaded. The drug release rate of the granules was 52.9% at 24 h and 81.2% at 144 h. The inhibition rate of the proliferation of hepatocarcinoma cells by the doxorubicin-containing nanoparticles was slower than that of doxorubicin, and the IC50 of the two cells was 1.844 and 0.345 μg/mL, respectively. At the same time, apoptosis and cycle analysis showed that the doxorubicin nanoparticles could significantly inhibit the cell cycle of hepatoma cells and promote the apoptosis of hepatoma cells. This study successfully produced nanoparticles loaded with doxorubicin targeting EGFR, which has a good sustained release effect, and its antitumor effect is stronger than free doxorubicin.

Sign in / Sign up

Export Citation Format

Share Document