scholarly journals Noncytotoxic polycaprolactone-polyethyleneglycol-ε-poly(l-lysine) triblock copolymer synthesized and self-assembled as an antibacterial drug carrier

RSC Advances ◽  
2017 ◽  
Vol 7 (63) ◽  
pp. 39718-39725 ◽  
Author(s):  
Chuncai Zhou ◽  
Xinyu Zhou ◽  
Xiaokai Su
Keyword(s):  
Antibacterial Activity ◽  
Drug Release ◽  
Triblock Copolymer ◽  
Drug Carrier ◽  
Antibacterial Drug ◽  
Self Assembled ◽  
Low Cytotoxicity

The PCL35-b-PEG45-b-EPL23 vesicles perform well in vitro drug release and antibacterial activity against Gram− and Gram+ bacteria with low cytotoxicity.

scholarly journals Hydroxyapatite/nifuroxazide conjugate: Characterization, drug release and antimicrobial activity

2021 ◽  
pp. 40-40
Author(s):  
Zeljko Radovanovic ◽  
Katarina Mihajlovski ◽  
Lidija Radovanovic ◽  
Djordje Janackovic ◽  
Rada Petrovic
Keyword(s):  
Drug Release ◽  
Raw Materials ◽  
Drug Carrier ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Antibacterial Drug ◽  
Stomach Acid ◽  
Poorly Soluble ◽  
Good Biocompatibility

Synthetic hydroxyapatite (Ca10(PO4)6(OH)2, HAp) is very similar to the inorganic part of the bones and teeth of mammals. It is a well-known biomaterial with good biocompatibility, osteoconductivity and bioactivity. Nifuroxazide (C12H9N3O5, NFX) is a broad-spectrum antibacterial drug and poorly soluble in water. In order to increase the solubility of NFX, nanosized HAp powder and raw NFX drug were mixed giving, as a result, HAp/NFX conjugate. Characterization of the raw materials and the obtained conjugate confirmed the integration of NFX on the HAp surface. The in vitro study of drug release in simulated stomach acid and intestinal fluid showed a much faster release of NFX from HAp surface than those of raw drug. HAp/NFX conjugate showed an excellent inhibitory effect against Gram-positive bacterium Staphylococcus aureus, Gram-negative bacterium Escherichia coli and yeast Candida albicans, proving the nanosized HAp powder as a promising drug carrier.

Preparation of poly(sebacic anhydride) and polylactic acid pills used as drug carrier for levofloxacin controlled release

2013 ◽  
Vol 33 (7) ◽  
pp. 659-664 ◽  
Author(s):  
Zhuan Zhang ◽  
Liao-Bing Chen ◽  
Jie Gao ◽  
Feng Bao ◽  
Jing Yin ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Controlled Release ◽  
Drug Release ◽  
Polylactic Acid ◽  
Release Rate ◽  
Drug Carrier ◽  
Antibacterial Drug ◽  
Molecular Weights ◽  
Zero Order Release

Abstract A biodegradable local drug release system consisting of poly(sebacic anhydride) and polylactic acid was developed for the purpose of osteomyelitis therapy. Five kinds of poly(sebacic anhydride) with different molecular weights were synthesized, and levofloxacin was chosen as a model antibacterial drug in the in vitro release within 38 days. As the molecular weight of poly(sebacic anhydride) increased, the melting point (Tm) of the matrices increased and the surface morphology became smoother. Consequently, the initial burst effect was reduced and the release rate significantly decreased. In addition, the kinetics of pills containing poly(sebacic anhydride) (Mw=13,000) were close to zero order release. The release profile reveals that the thermodynamic properties and morphology of these matrices, which are affected by the molecular weight, are essential for developing controllable delivery systems. The drug release rate could be easily controlled by the molecular weight of the poly(sebacic anhydride). Finally, these prospective results allow the biodegradable controlled release systems to be employed as carriers for the treatment of chronic osteomyelitis, as well as for other medical applications.

scholarly journals Assessment of a mathematical model considering the effect of flow rate on in-vitro drug-release from PLGA films

2021 ◽  
Vol 321 ◽  
pp. 04011
Author(s):  
Navideh Abbasnezhad ◽  
Farid Bakir ◽  
Stéphane Champmartin ◽  
Mohammadali Shirinbayan
Keyword(s):  
Mathematical Model ◽  
Drug Release ◽  
Flow Rate ◽  
Drug Carrier ◽  
Diclofenac Sodium ◽  
Drug Eluting Stents ◽  
In Vitro Drug Release ◽  
Drug Eluting ◽  
Release Profiles

Drug-eluting stents implanted in blood vessels are subject to various dynamics of blood flow. In this study, we present the evaluation of a mathematical model considering the effect of flow rate, to simulate the kinetic profiles of drug release (Diclofenac Sodium (DS)) from in-vitro from PLGA films. This model solves a set of non-linear equation for modeling simultaneously the burst, diffusion, swelling and erosion involved in the mechanisms of liberation. The release parameters depending on the flow rate are determined using the corresponding mathematical equations. For the evaluation of the proposed model, test data obtained in our laboratory are used. To quantify DS release from drug-carrier PLGA films, we used the flow-through cell apparatus in a closed-loop. Four flow rate values are applied. For each value, the model-substance liberation kinetics showed an increase in drug released with the flow rate. The simulated release profiles show good agreement with the experimental results. Therefore, the use of this model could provide a practical tool to assess in-vitro drug release profiles from polymer matrices under continuous flow rate constraint, and could help improve the design of drug eluting stents.

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals Facile Construction of Functionalized GO Nanocomposites with Enhanced Antibacterial Activity

Nanomaterials ◽  
2019 ◽  
Vol 9 (7) ◽  
pp. 913 ◽  
Author(s):  
Lei Jiang ◽  
Zhongjie Zhu ◽  
Yanyi Wen ◽  
Shan Ye ◽  
Chen Su ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Drug Release ◽  
Drug Carrier ◽  
Diffusion Method ◽  
Release Mechanism ◽  
Order Kinetic ◽  
Sustained Drug Release ◽  
Disk Diffusion Method ◽  
Antimicrobial Materials ◽  
Inhibition Performance

The development of antimicrobial materials with sustained drug release performance is of great importance. Graphene oxide (GO) is considered to be an ideal drug carrier. In this study, tetracycline hydrochloride (TC) was loaded onto polyethyleneimine-functionalized GO (PG) to fabricate TC/PG nanocomposites. The success of the fabrication was confirmed by zeta potential, TEM, FTIR, and Raman analyses. The TC/PG nanocomposites showed a controlled and sustained drug release behavior, and a pseudo second order kinetic model was employed to illustrate the release mechanism. The antibacterial activity was studied using the disk diffusion method against Escherichia coli and Staphylococcus aureus. The TC/PG nanocomposites exhibited great bacterial inhibition performance. The results indicate that the fabricated TC/PG nanocomposites with effective antibacterial activity have great potential in antibacterial applications.

scholarly journals Polycaprolactone-Based Mimetic Antimicrobial Peptide Copolymers Vesicles as an Effective Drug-Carrier for Cancer Therapy

Polymers ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 1783 ◽  
Author(s):  
Yusheng Qian ◽  
Xinyu Zhou ◽  
Jing He ◽  
Chuncai Zhou
Keyword(s):  
Cancer Therapy ◽  
Drug Release ◽  
Antimicrobial Peptide ◽  
Drug Carrier ◽  
Uniform Size ◽  
Vesicular Structure ◽  
Transmission Electron ◽  
Low Concentrations ◽  
Carrier Systems

A novel series of amphiphilic mimicking antimicrobial peptide copolymers PCL16-b-Kn can assemble in water to form uniform vesicles. Transmission electron microscopy was used to observe the vesicular structure of the nanoparticles, and dynamic light scattering revealed their uniform size and narrow dispersion. Critical vesiculation concentrations were also tested, revealing that these vesicles can exist at low concentrations. Furthermore, in vitro and intracellular drug release of doxorubicin(DOX)-vesicles were conducted. These vesicles could encapsulate DOX and achieve efficient intracellular drug release. Overall, these copolymer vesicles exhibit potential application value as multifunctional drug-carrier systems with antibacterial capability in cancer therapy.

scholarly journals Synthesis and In Vitro Antibacterial Activity of Quaternized 10-Methoxycanthin-6-one Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1553 ◽  
Author(s):  
Na Li ◽  
Dan Liu ◽  
Jiang-Kun Dai ◽  
Jin-Yi Wang ◽  
Jun-Ru Wang
Keyword(s):  
Antibacterial Activity ◽  
Seed Germination ◽  
Pathogenic Bacteria ◽  
Dilution Method ◽  
Highly Active ◽  
Structure Activity ◽  
In Vitro Antibacterial Activity ◽  
Potential Activity ◽  
Low Cytotoxicity

Background: Based on our previous work, we found that 10-methoxycanthin-6-one displayed potential antibacterial activity and quaternization was an available method for increasing the antibacterial activity. Here, we explored the antibacterial activity of quaternized 10-methoxy canthin-6-one derivatives. Methods and Results: Twenty-two new 3-N-benzylated 10-methoxy canthin-6-ones were designed and synthesized through quaternization reaction. The in vitro antibacterial activity against three bacteria was evaluated by the double dilution method. Moreover, the structure–activity relationships (SARs) were carefully summarized in order to guide the development of antibacterial canthin-6-one agents. Two highly active compounds (6p and 6t) displayed 8-fold superiority (MIC = 3.91 µg/mL) against agricultural pathogenic bacteria R. solanacearum and P. syringae compared to agrochemical streptomycin sulfate, and showed potential activity against B. cereus. Moreover, these two compounds exhibited good “drug-like” properties, low cytotoxicity, and no inhibition on seed germination. Conclusions: This work provides two new effective quaternized canthin-6-one derivatives as candidate bactericide, promoting the development of natural-sourced bactericides and preservatives.

scholarly journals Preparation, in vitro and in vivo evaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysis

2010 ◽  
Vol 60 (3) ◽  
pp. 255-266 ◽  
Author(s):  
Santanu Chakraborty ◽  
Madhusmruti Khandai ◽  
Anuradha Sharma ◽  
Nazia Khanam ◽  
Ch. Patra ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Drug Carrier ◽  
Polymer Concentration ◽  
Multiple Comparison ◽  
Prolonged Release ◽  
Comparison Analysis ◽  
Significant Difference

Preparation,in vitroandin vivoevaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysisIonotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigatedin vitrofor possible sustained drug release and their usein vivoas a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunnet's multiple comparison analysis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.

scholarly journals Formulation and evaluation of chitosan films containing sparfloxacin for the treatment of periodontitis

2019 ◽  
Vol 9 (1) ◽  
pp. 38-45 ◽  
Author(s):  
Santoshi Naik ◽  
Prasiddhi Raikar ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
Antibacterial Activity ◽  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Periodontal Pocket ◽  
Content Uniformity ◽  
Burst Release ◽  
In Vitro Antibacterial Activity ◽  
Chitosan Films

In the present study an attempt has been made to formulate and evaluate a sustained release periodontal film of Sparfloxacin with biodegradable, cost effective polymer Chitosan. The objective of the study was to formulate intra-pocket periodontal films, which could be easily placed into the periodontal pocket, and thus be capable of delivering therapeutic concentrations of drug. Sparfloxacin is an antibiotic, showing wide spectrum antibacterial activity against a number of periodontal pathogens. Hence Sparfloxacin is selected as model for site specific delivery, i.e., into periodontal pocket for the treatment of periodontitis. In the present investigation Chitosan films containing Sparfloxacin were prepared by solution casting method using acetic acid. The copolymers HPMC K4M, Sodium CMC and Eudragit RL 100 in the concentrations of 10%, 20% and 30% w/w of Chitosan were added into the polymeric solution. Propylene glycol was used as plasticizer. FT-IR and UV spectroscopic methods revealed no interaction between Sparfloxacin and polymers. The drug loaded films were evaluated for their thickness, weight variation, content uniformity, tensile strength, percent elongation, percentage moisture loss, surface pH, folding endurance, in- vitro drug release studies, in - vitro antibacterial activity and stability studies. Periodontal films showed initial burst release of drug on 1st day and then the release was sustained for a period of 8 days. In – vitro antibacterial activity was carried out on staphylococcus aureus and the antibacterial activity was retained for 96 hours. In - vitro release from periodontal films was fit to kinetic models to reveal drug release kinetics. Keywords: Periodontitis, Sparfloxacin, Bio-adhesive polymers.

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