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.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Studies ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

PREPARATION AND CHARACTERIZATION OF GLYCYRRHETINIC ACID-MODIFIED POLOXAMER 188/CHITOSAN NANOPARTICLES

NANO ◽  
2013 ◽  
Vol 08 (04) ◽  
pp. 1350042 ◽  
Author(s):  
JING WANG ◽  
LI GUO ◽  
LI FANG MA
Keyword(s):  
High Performance ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Spherical Shape ◽  
Glycyrrhetinic Acid ◽  
Poloxamer 188 ◽  
H Nmr ◽  
Ft Ir

In this paper, we firstly synthesized glycyrrhetinic acid-modified double amino-terminated poloxamer 188 (GA–NH–POLO–NH–GA). The structure of the synthesized compound was confirmed by 1H-NMR and Fourier transform infrared (FT-IR) spectroscopy. Then the nanoparticles composed of GA–NH–POLO–NH–GA/chitosan (GA–NH–POLO–NH–GA/CTS) were prepared by an ionic gelation process. The characterization of the nanoparticles was measured by dynamic light scattering (DLS) and scanning electron microscope (SEM). The results showed that the nanoparticles were well dispersed with a spherical shape and the particle size was distributed between 100 nm and 300 nm. The cytotoxicity based on MTT assay against cells (QGY-7703 cells and L929 cells) showed that the nanoparticles had low toxicity and good biocompatibility. The encapsulation efficiency and drug loading of 5-fluorouracil-loaded nanoparticles (5-FU nanoparticles) were measured by high-performance liquid chromatography (HPLC) and fluorescence spectroscopy, ultraviolet-visible (UV-vis) absorbance. The encapsulation of 5-Fu-loaded CTS nanoparticles was 12.8% and the drug loading was 2.9%, while the encapsulation of 5-Fu-loaded GA–NH–POLO–NH–GA/CTS nanoparticles was 20.9% and the drug loading was 3.36%. The release profile showed that the GA–NH–POLO–NH–GA/CTS nanoparticles were available for sustained release of 5-Fu. The GA–NH–POLO–NH–GA/CTS nanoparticles have a higher affinity to the QGY-7703 cells, so indicated that the GA–NH–POLO–NH–GA/CTS nanoparticles have the capacity of liver-targeting in vitro.

scholarly journals Thermosensitive Chitosan Hydrogels Containing Polymeric Microspheres for Vaginal Drug Delivery

2017 ◽  
Vol 2017 ◽  
pp. 1-12 ◽  
Author(s):  
Ting-Ting Yang ◽  
Yuan-Zheng Cheng ◽  
Meng Qin ◽  
Yong-Hong Wang ◽  
Hong-Li Yu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Delivery System ◽  
Drug Loading ◽  
Great Promise ◽  
Burst Release ◽  
Bletilla Striata ◽  
Vaginal Drug Delivery ◽  
Thermosensitive Hydrogels

Thermosensitive hydrogels have increasingly received considerable attention for local drug delivery based on many advantages. However, burst release of drugs is becoming a critical challenge when the hydrogels are employed. Microspheres- (MS-) loaded thermosensitive hydrogels were thus fabricated to address this limitation. Employing an orthogonal design, the spray-dried operations of tenofovir (TFV)/Bletilla striata polysaccharide (BSP)/chitosan (CTS) MS were optimized according to the drug loading (DL). The physicochemical properties of the optimal MS (MS F) were characterized. Depending on the gelation temperature and gelating time, the optimal CTS-sodium alginate- (SA-) α,β-glycerophosphate (GP) (CTS-SA-GP) hydrogel was obtained. Observed by scanning electron microscope (SEM), TFV/BSP/CTS MS were successfully encapsulated in CTS-SA-GP. In vitro releasing demonstrated that MS F-CTS-SA-GP retained desirable in vitro sustained-release characteristics as a vaginal delivery system. Bioadhesion measurement showed that MS-CTS-SA-GP exhibited the highest mucoadhesive strength. Collectively, MS-CTS-SA-GP holds great promise for topical applications as a sustained-release vaginal drug delivery system.

scholarly journals PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

2018 ◽  
Vol 10 (6) ◽  
pp. 57
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
N. N. Bala
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Ropinirole Hydrochloride

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

scholarly journals Development and Evaluation of Matrices Composed of β-cyclodextrin and Biodegradable Polyesters in the Controlled Delivery of Pindolol

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 500
Author(s):  
Agnieszka Lis-Cieplak ◽  
Filip Charuk ◽  
Marcin Sobczak ◽  
Anna Zgadzaj ◽  
Agata Drobniewska ◽  
...  
Keyword(s):  
Heart Diseases ◽  
Coupling Reaction ◽  
Magic Angle Spinning ◽  
Burst Release ◽  
Magic Angle ◽  
Chemical Structures ◽  
Drug Conjugates ◽  
Flight Mass Spectrometry ◽  
Angle Spinning

Polymer-drug conjugates are currently being more widely investigated for the treatment of hypertension. In view of the above, in the first stage of our work, we used nontoxic β-cyclodextrin (β-CD) as effective, simple, inexpensive, and safe for the human body initiator for the synthesis of biocompatible and biodegradable functionalized polymers suitable for the medical and pharmaceutical applications. The obtained polymeric products were synthesized through a ring-opening polymerization (ROP) of ε-caprolactone (CL), d,l-, and l,l-lactide (LA and LLA). The chemical structures of synthesized materials were elucidated based on 1H NMR and solid-state carbon-13 cross-polarization/magic angle spinning nuclear magnetic resonance (13C CP/MAS NMR) analysis, while the incorporation of β-CD molecule into the polymer chain was confirmed by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS). Furthermore, molecular modeling has been applied to investigate the intrachain rigidities and chain architectures for several representative structures. The obtained and thoroughly characterized branched matrices were then used to generate the first β-cyclodextrin/biodegradable polymer/β-blocker conjugate through the successful conjugation of pindolol. The conjugates were fabricated by carbodiimide-mediated coupling reaction. The branched biodegradable materials released the drug in vitro in a sustained manner and without “burst release” and thus have the ability to treat different heart diseases.

Drug release profile and reduction in the in vitro burst release from pectin/HEMA hydrogel nanocomposites crosslinked with titania

RSC Advances ◽  
2016 ◽  
Vol 6 (23) ◽  
pp. 19060-19068 ◽  
Author(s):  
Elisangela P. da Silva ◽  
Marcos R. Guilherme ◽  
Francielle P. Garcia ◽  
Celso V. Nakamura ◽  
Lucio Cardozo-Filho ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Profile ◽  
Burst Release ◽  
Drug Release Profile ◽  
Initial Release ◽  
Hydrogel Nanocomposites

Hydrogel nanocomposites of pectin, HEMA and titania for Vit-B12 controlled release with reduced initial release burst were prepared. A reduction of up to ca. 60% was observed.

scholarly journals Microwave assisted the short time clean synthesis of 1,3-Diketones as Building Blocks in Heterocyclic Synthesis: A Facile Synthesis and Antimicrobial Evaluation of New Dihydropyridine, 4H-Pyrane, Dihydropyridazine, Pyrimidine and Pyrazole derivatives

2019 ◽  
Author(s):  
mohamed ahmed abdelreheim ◽  
Ibrahim Saad Abdel Hafiz ◽  
Hend Saad Eldin Abdel Rady
Keyword(s):  
Antimicrobial Activity ◽  
Wide Spectrum ◽  
Building Blocks ◽  
Mycelial Fungi ◽  
Mass Spectral ◽  
H Nmr ◽  
Chemical Structures ◽  
Short Time ◽  
Anti Fungal

Abstract Background: According to literature survey, the compounds bearing naphthalene moiety can be used as medical preparations because of their wide spectrum of biological activity and low toxicity. In this study, a new series of azoles or azines were synthesized from the reaction of the key intermediate 1-(1-hydroxynaphthalen-2-yl)-3-phenylpropane-1,3-dione 3 with a variety of electrophilic and nucleophilic reagents under a variety of mild conditions. Results: The chemical structures of these compounds were confirmed by various spectroscopic methods such as (IR, 1H-NMR, 13C-NMR, mass spectral data and elemental analyses). Conclusions: The prepared compounds were screened in vitro for their antimicrobial activity against some species of Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) and Gram-negative bacteria (Escherichia coli and Pseudomonas aeuroginosa). Anti-fungal activities of the compounds were tested against yeast and mycelial fungi,Candida albicans and Aspergillus flavus. The antimicrobial activity of this series was showed either weak or moderate activities.

scholarly journals Topical Chitosan-Based Thermo-Responsive Scaffold Provides Dexketoprofen Trometamol Controlled Release for 24 h Use

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2100
Author(s):  
Luis Castillo-Henríquez ◽  
Pablo Sanabria-Espinoza ◽  
Brayan Murillo-Castillo ◽  
Gabriela Montes de Oca-Vásquez ◽  
Diego Batista-Menezes ◽  
...  
Keyword(s):  
Controlled Release ◽  
Kinetic Models ◽  
In Vitro Release ◽  
Solution Temperature ◽  
Burst Release ◽  
Release Studies ◽  
Dexketoprofen Trometamol ◽  
Ft Ir ◽  
Healing Wounds

Chronic and non-healing wounds demand personalized and more effective therapies for treating complications and improving patient compliance. Concerning that, this work aims to develop a suitable chitosan-based thermo-responsive scaffold to provide 24 h controlled release of Dexketoprofen trometamol (DKT). Three formulation prototypes were developed using chitosan (F1), 2:1 chitosan: PVA (F2), and 1:1 chitosan:gelatin (F3). Compatibility tests were done by DSC, TG, and FT-IR. SEM was employed to examine the morphology of the surface and inner layers from the scaffolds. In vitro release studies were performed at 32 °C and 38 °C, and the profiles were later adjusted to different kinetic models for the best formulation. F3 showed the most controlled release of DKT at 32 °C for 24 h (77.75 ± 2.72%) and reduced the burst release in the initial 6 h (40.18 ± 1.00%). The formulation exhibited a lower critical solution temperature (LCST) at 34.96 °C, and due to this phase transition, an increased release was observed at 38 °C (88.52 ± 2.07% at 12 h). The release profile for this formulation fits with Hixson–Crowell and Korsmeyer–Peppas kinetic models at both temperatures. Therefore, the developed scaffold for DKT delivery performs adequate controlled release, thereby; it can potentially overcome adherence issues and complications in wound healing applications.

Azacitidine Loaded PLGA Nanoparticles and their Dual Release Mechanism

2020 ◽  
Vol 10 (3) ◽  
pp. 280-289
Author(s):  
Kanchan Kashyap ◽  
Mayank Handa ◽  
Rahul Shukla
Keyword(s):  
Glioblastoma Multiforme ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Plga Nanoparticles ◽  
Current Therapy ◽  
Release Mechanism ◽  
Burst Release ◽  
In Vivo Evaluation ◽  
Dual Release

Background: Glioblastoma multiforme (GBM) is a belligerent brain tumor constituting about 67% of primary brain tumours. The current therapy for glioblastoma multiforme is surgery, radiations and chemotherapy though the success rate is quite limited. Azacitidine is a hydrophilic anti-cancer agent which acts by demethylation and is used in the treatment of both acute and chronic myelomonocytic leukaemia along with GBM. Objective: Formulation of stable Azacitidine loaded poly-lactide-co-glycolide (PLGA) nanoparticles (NPs) with tailor-made release profiles. Methods: Preparation of Azacitidine loaded PLGA nanoparticles was done by double emulsion (w/o/w) solvent evaporation technique. PLGA was used in the formulation, as it is biocompatible and biodegradable. Polyvinyl alcohol worked as an emulsifier while Span 80 decreased the interfacial tension among two immiscible phases (aqueous and organic), resulting in increased stability of the formulation. Results: Polymer concentration was directly proportional to the entrapment and drug loading and inversely proportional to particle size. Azacitidine loaded PLGA NPs showed a biphasic release model. At the first stage, burst release was observed, followed by sustained release. About 43.93 ± 0.69% drug was released in 1 hour and the remaining drug was released in 48 hours. Conclusion: Dual release behavior first delivered an ample amount of dose which provided cytotoxic dose, followed by the maintenance dose for sustaining the cytotoxic drug levels. Future prospective requires In-vitro cell viability evaluation of tailor-made polymeric nanoparticles along with In-vivo evaluation for therapeutic intervention in a glioblastoma tumor model.

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.

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