scholarly journals Synthesis and Characterization of Polyfumarateurethane Nanoparticles for Sustained Release of Bupivacaine

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 281
Author(s):  
Soo-Yong Park ◽  
Jiin Kang ◽  
Ji-Young Yoon ◽  
Ildoo Chung
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Loading ◽  
Double Emulsion ◽  
Fluorescein Isothiocyanate ◽  
Hexamethylene Diisocyanate ◽  
Polymer Backbone ◽  
Oil In Water

Biodegradable polyfumarateurethane (PFU) for use as a bupivacaine delivery vehicle, synthesized using di-(2-hydroxypropyl fumarate) (DHPF), polyethylene glycol (PEG) and 1,6-hexamethylene diisocyanate (HMDI), was designed to be degradable through the hydrolysis and enzymatic degradation of the ester bonds in its polymer backbone. Using a water-in-oil-in-water double emulsion techniques, nanoparticles encapsulating water or fluorescein isothiocyanate (FITC) were fabricated to avoid the immune system owing to the presence of PEG on their surface. The morphologies of these nanoparticles were characterized by DLS, TEM, FE-SEM, and fluorescent microscopies. The present study explored the encapsulation, loading efficiency and in vitro drug release of bupivacaine encapsulated with biodegradable PFU nanoparticles for the treatment of local anesthesia. Various concentrations of bupivacaine were encapsulated into nanoparticles and their encapsulation efficiencies and drug loading were investigated. Encapsulation efficiency was highest when 2.5% bupivacaine was encapsulated. Drug release behavior from the bupivacaine-loaded PFU nanoparticles followed a sustained release profile.

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

scholarly journals FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

2018 ◽  
Vol 8 (5) ◽  
pp. 465-474
Author(s):  
S PADMA PRIYA ◽  
AN Rajalakshmi ◽  
P Ilaveni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Loading ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Polyvinyl Pyrrolidone ◽  
Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods:  Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine  formulations were formulated and  evaluated for  possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro  drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

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 Effect of cross-linked biodegradable polymers on sustained release of sodium diclofenac-loaded microspheres

2013 ◽  
Vol 49 (4) ◽  
pp. 873-888 ◽  
Author(s):  
Avik Kumar Saha ◽  
Sarbani Dey Ray
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Differential Scanning Calorimetric ◽  
Prolonged Release ◽  
Easy Method ◽  
Calorimetric Analysis ◽  
Sodium Diclofenac

The objective of this study was to formulate an oral sustained release delivery system of sodium diclofenac(DS) based on sodium alginate (SA) as a hydrophilic carrier in combination with chitosan (CH) and sodium carboxymethyl cellulose (SCMC) as drug release modifiers to overcome the drug-related adverse effects and to improve bioavailability. Microspheres of DS were prepared using an easy method of ionotropic gelation. The prepared beads were evaluated for mean particle size, entrapment efficiency, swelling capacity, erosion and in-vitro drug release. They were also subjected to various studies such as Fourier Transform Infra-Red Spectroscopy (FTIR) for drug polymer compatibility, Scanning Electron Microscopy for surface morphology, X-ray Powder Diffraction Analysis (XRD) and Differential Scanning Calorimetric Analysis (DSC) to determine the physical state of the drug in the beads. The addition of SCMC during the preparation of polymeric beads resulted in lower drug loading and prolonged release of the DS. The release profile of batches F5 and F6 showed a maximum drug release of 96.97 ± 0.356% after 8 h, in which drug polymer ratio was decreased. The microspheres of sodium diclofenac with the polymers were formulated successfully. Analysis of the release profiles showed that the data corresponds to the diffusion-controlled mechanism as suggested by Higuchi.

5-Fluorouracil-Impregnated PLGA Coated Gold Nanoparticles for Augmented Delivery to Lung Cancer: in vitro Investigations

2021 ◽  
Vol 22 ◽  
Author(s):  
Rashmi Gupta ◽  
Leena Vishwakarma ◽  
Sunil Kant Guleri ◽  
Gourav Kumar
Keyword(s):  
Lung Cancer ◽  
Gold Nanoparticles ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
A549 Cells ◽  
Double Emulsion ◽  
Zero Order Release ◽  
Reduced Toxicity

Background and Objective: The study aimed to investigate the augmented cytotoxic effects of polymer-coated (poly-lactic-co-glycolic acid-PLGA) gold nanoparticles (GNPs) carrying 5-fluorouracil (5-FU) in the management of lung cancer. Materials and Methods: In this study, several formulations were prepared using a double emulsion (water-oil-water) method and evaluated for drug release behavior, compatibility, cell line toxicity (A549), and apoptosis assessment. Results: Characterization results showed spherical polydispersed particles with size 29.11-178.21 nm, polydispersity index (PDI) 0.191-292, and zeta potential (ZP) 11.19-29.21 (-mV), respectively. The optimized polymer-coated 5-FU loaded gold nanoparticles (PFGNPs) illustrated a maximum drug loading (93.09 ± 10.75%) compared to others. The percent cumulative drug release of polymer-coated 5-FU loaded nanoparticles (PFNPs), 5-FU loaded gold nanoparticles (FGNPs), (PFGNPs) and 5-FU solution were 47.87± 1.5, 41.09±1.8, 56.31±1.05, and 98.8±4.2%, respectively, over 10 h. following zero-order release kinetics (except 5-FU solution). From the MTT results, the cytotoxic effect of PFGNPs on the A549 cells was 82.89 % compared to the 5-FU solution (74.91 %). EGFR and KRAS gene expression analysis under the influence of PFNPs, FGNPs, PFGNPs, and 5-FU was studied and observed maximum potency for PFNPs. Conclusion: PLGA coated biogenic gold nanoparticles have a combined effect to achieve high drug loading, sustained delivery, improved efficacy, and enhanced permeation. Conclusively, the approach may be promising to control lung cancer with reduced toxicity and improved efficacy.

Preparation of Targeted Mitochondrion Nanoscale-Release Peptides and Their Efficiency on Eukaryotic Cells

2021 ◽  
Vol 17 (8) ◽  
pp. 1679-1689
Author(s):  
Yuan He ◽  
Zhuoya Quan ◽  
Ruixue Zhang ◽  
Beilei He ◽  
Yun Xu ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Sustained Release ◽  
Mtt Assay ◽  
Drug Loading ◽  
Fluorescein Isothiocyanate ◽  
Medical Application ◽  
Eukaryotic Cells ◽  
Loading System ◽  
High Level

We established a self-decomposable SiO2 encapsulated mitochondrial targeting short peptide SS31 drug loading system (SiO2@SS31) to determine its nano-sustained release characteristics in eukaryotic cells. We explored the protection of SiO2@SS31 on the 661W cells after oxidative injury by H2O2. After the drug loading, we detected the morphology of SiO2@SS31 by transmission electron microscopy (TEM). Moreover, high-pressure liquid chromatography (HPLC) was used to determine the drug capacity and encapsulation efficiency of the nanoparticles. Then, the release curve in vitro was drawn. The 661W cells were cultured in vitro to allow the detection of cytotoxicity by the MTT assay. The SS31loaded nanoscale microspheres labeled with fluorescein isothiocyanate (SiO2@FITC-SS31) were prepared, and their sustained release effect was detected with intracellular endocytosis, using confocal microscopy and flow cytometry. Within 15 days, the SiO2@SS31 nanoparticles were completely decomposed and simultaneously released the SS31 peptide in deionized water and normal saline. Nonetheless, the process was faster in simulated body fluid and serum. The MTT assay suggested that SiO2@SS31 has sustained protection compared with SS31 in the 661W cells at 48 h. Flow cytometry proved SiO2@FITC-SS31 could maintain a high level and last longer after 24 h. The SS31 peptide, which has excellent medical application prospects, can be slowly and continuously released from self-decomposable SiO2 and targeted to concentrate on mitochondria.

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)

Preparation and Characterization of Cyclophosphamide-Loaded Chitosan Microspheres

2012 ◽  
Vol 621 ◽  
pp. 130-133
Author(s):  
Yi Lin Ding ◽  
Su Su Ding ◽  
Guo Fang Ding
Keyword(s):  
Drug Release ◽  
Anticancer Agent ◽  
Loading Rate ◽  
Drug Loading ◽  
Average Diameter ◽  
Uv Spectrophotometry ◽  
Chitosan Microspheres ◽  
Dialysis Bag

Chitosan microspheres were prepared by using a cross linking agent combined with an emulsion technique. Cyclophosphamide was loaded as an anticancer agent. Obtained microspheres were spherical and regular, with a smooth surface morphology, having an average diameter of 15.7±9.0μm. After preparation, the drug-loading rate and entrapment rate of cyclophosphamide was investigated by UV spectrophotometry. Drug release was tested in vitro in a dynamic dialysis system with a dialysis bag. The chitosan microspheres prepared were proved to have good drug release profiles.

scholarly journals Formulation And Characterization of Carageenan Gels Encapsulating Amphotericin B And Lactobacillus acidophilus Against Candidal Vaginitis

2017 ◽  
Vol 4 (1) ◽  
pp. 37-49
Author(s):  
R Kaur ◽  
M Khurana ◽  
M Bindal ◽  
A Sharma
Keyword(s):  
Candida Albicans ◽  
Drug Release ◽  
Sustained Release ◽  
Amphotericin B ◽  
Lactobacillus Acidophilus ◽  
Drug Carriers ◽  
In Vitro Drug Release ◽  
Antimicrobial Studies

The present study is concerned with the development and characterization of bioadhesive carageenan gel encapsulating Amphotericin B and Lactobacillus acidophillus, prepared by graft co-polymeriztion against Candidal vaginitis. Intravaginal gel systems based on bioadhesive polymer (carrageenan) were characterized with respect to swelling index, bioadhesive strength, percent encapsulation and in vitro drug release antimicrobial studies. A marked increase in swelling index of gel encapsulating Lactobacillus was found to be 1.9±0.35. The percent encapsulation of drug was found to be 98.63%±.0.2% and that of Lactobacillus was 91.81 ±0.01. The viability was observed for interval of 6 hrs on trypton soya agar and showed that viability was highly conserved till 4 hrs. The antimicrobial study of gels encapsulating Amphotericin B and Lactobacillus showed that carageenan gel can inhibit Candida albicans upto a maximum extent. Bioadhesivity study also conducted for gels that showed a bioadhesivity of 84.66% ±.0.5% with drug, 88.66% ±.02% with Lactobacillus. In-vitro drug release showed a sustained type release of drug from the polymer i.e. there was initial burst of Amphotericin B up to 5 hours, after which there was a sustained release upto 10 days. Thus it has been concluded from the present study that bioadhesive gels encapsulating Amphotericin B can act as promising drug carriers along with Lactobacillus against candidal vaginitis.

Development and Evaluation of Ropivacaine Loaded Poly(Lactic-Co-Glycolic Acid) Microspheres with Low Burst Release

2019 ◽  
Vol 16 (6) ◽  
pp. 490-499 ◽  
Author(s):  
Xiqing Zhao ◽  
Yue Gao ◽  
Xuemei Tang ◽  
Wei Lei ◽  
Yang Yang ◽  
...  
Keyword(s):  
Postoperative Pain ◽  
Pain Relief ◽  
Sustained Release ◽  
Drug Loading ◽  
Postoperative Pain Relief ◽  
Burst Release ◽  
Anesthetic Drugs ◽  
Oil In Water

Background: The local anesthetic drugs, especially ropivacaine, were considered favorable analgesia for postoperative management because of their effective local pain relief and low adverse effects. However, the short half-life and the resulting in bolus doses lead to the indistinctive improvement of these drugs in postoperative pain relief. Therefore, the ropivacaine microspheres with sustained release and low initial burst release were anticipated. Methods: Three methods including oil in water (O/W), water in oil in water (W/O/W), and solid in oil in water (S/O/W) emulsion solvent evaporation method were used to optimize the ropivacaine loaded PLGA microspheres. The microspheres were evaluated both in vitro and in rats. The in vitro-in vivo correlation (IVIVC) was also investigated. Results: The microspheres prepared by O/W method showed more satisfactory properties and the microspheres used for evaluation were prepared by O/W method. The particle size, drug loading, encapsulation efficiency and burst release were 11.19±1.24 µm, 28.37±1.15%, 98.15±3.98%, and 10.96±5.37% for microspheres with PLGA of 12 kDa, and 6.64±0.61 μm, 19.62±0.89%, 92.74±4.21%, and 18.42±5.12% for microspheres with PLGA of 8 kDa, respectively. These microspheres were also injected into rats by subcutaneous, intramuscular and intraperitoneal route, respectively. It was indicated that the detectable concentration of ropivacaine could last for at least 20 days for both kinds of microspheres in spite of injection routes. The low burst releases at 1 d were also manifested in rats and they were 6.62%, 6.99%, 6.48% for the microspheres with PLGA of 12 kDa, and 4.72%, 4.33%, 4.48% for the microspheres with PLGA of 8 kDa by intraperitoneal, intramuscular and subcutaneous route, respectively. A linear relationship between the in vitro release and the in vivo adsorption of ropivacaine from microspheres was also established. Conclusion: The ropivacaine microspheres with sustained release and low burst release were acquired, which indicated that the postoperative pain relief might last longer and the side effects might get lower. Therefore, the ropivacaine microspheres prepared in this paper have great potential for clinical use.

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