scholarly journals Semi-Crystalline Copolymer Hydrogels as Smart Drug Carriers: In Vitro Thermo-Responsive Naproxen Release Study

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 158
Author(s):  
Snežana Ilić-Stojanović ◽  
Ljubiša Nikolić ◽  
Vesna Nikolić ◽  
Slobodan Petrović ◽  
Violeta Oro ◽  
...  
Keyword(s):  
Drug Carrier ◽  
Drug Carriers ◽  
Xrd Analysis ◽  
Hplc Method ◽  
Potential Candidate ◽  
Swelling Kinetic ◽  
Model Drug ◽  
Xrd Techniques ◽  
Responsive Hydrogels

In this study, poly(N-isopropylacrylamide-co-2-hydroxypropyl methacrylate) hydrogels were synthesized using free radical initiated copolymerization method. Four hydrogels with different cross-linker concentrations were prepared. Semi-crystalline, cross-linked copolymer networks were confirmed by FTIR, SEM and XRD analysis. Variation of swelling behaviour was monitored gravimetrically and thermo-responsiveness has been noticed. An application of synthesized thermo-responsive hydrogels as carriers for the modulated release of anti-inflammatory model drug was investigated. Moreover, naproxen loading into these hydrogels was also determined using FTIR, SEM and XRD techniques and release was analyzed using HPLC method at simulated physiological conditions. Swelling kinetic and mechanism of water transport, as well as diffusion of naproxen through the hydrogels were analyzed. Thus, the aim of this work was to study various compositions of obtained hydrogels and their possibility of application as a thermo-responsive carrier for prolonged naproxen release in order to evaluate as a potential candidate for drug carrier in future pharmaceutical applications.

Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

2018 ◽  
Vol 18 (2) ◽  
pp. 302-311
Author(s):  
Shulin Dai ◽  
Yucheng Feng ◽  
Shuyi Li ◽  
Yuxiao Chen ◽  
Meiqing Liu ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Anti Cancer ◽  
Physical Interactions

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

Preparation and Characterization of Biopolymeric Nanoparticles as Drug Delivery Vehicles

2017 ◽  
pp. 225-246
Author(s):  
Sai S. Sagiri ◽  
Suraj K. Nayak ◽  
S. Lakshmi ◽  
Kunal Pal
Keyword(s):  
Drug Delivery ◽  
Salicylic Acid ◽  
Drug Release ◽  
Chitosan Nanoparticles ◽  
Xrd Analysis ◽  
Gelatin Nanoparticles ◽  
Drug Delivery Vehicles ◽  
Model Drug ◽  
Bioactive Agents

In recent years, the use of biopolymeric nanoparticles as vehicles for drug delivery has increased exponentially. In the present study, chitosan and gelatin nanoparticles were prepared by ionic gelation and desolvation methods, respectively. Salicylic acid was used as the model drug. The nanoparticles were characterized using SEM, XRD analysis and FTIR spectrophotometric studies. In vitro drug release experiments were carried out to understand the mechanism of drug release. SEM micrographs showed the formation of spherical nanoparticles. XRD studies indicated a higher crystalline nature of the chitosan nanoparticles as compared to the gelatin nanoparticles. FTIR studies indicated the presence of salicylic acid within the drug- loaded nanoparticles. Drug release studies indicated that the developed nanoparticles may be used as carriers for various bioactive agents.

scholarly journals A Facile Route to Fabricate CS/GO Composite Film for the Application of Therapeutic Contact Lenses

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Pin Chen ◽  
Xin Wang ◽  
Jingyang Kong ◽  
Xiaohong Hu
Keyword(s):  
Composite Film ◽  
Contact Lenses ◽  
Umbilical Vein ◽  
Drug Carriers ◽  
Diffusion Method ◽  
Swelling Ratio ◽  
Significant Difference ◽  
Ophthalmic Drug ◽  
Model Drug

Traditional contact lenses bring convenience for ophthalmic drug delivery. However, either as contact lenses or as drug carriers, traditional materials have still some drawbacks in the field. Therefore, a transparent film was designed and investigated for the application of therapeutic contact lenses. Chitosan (CS)/graphene oxide (GO) composite film and CS film were fabricated with acceptable transparent and tensile properties by simple casting flow method. Although swelling ratio of CS/GO composite film was higher than that of CS film with significant difference, both formed films had suitable swelling ratio for contact lens application. Both CS/GO composite film and CS film exhibited typical CS infrared characteristic peaks. CS/GO composite film had significant greater breaking strength than CS film, but its elongation at break was a little lower than CS film. Either CS/GO composite film or CS film exhibited good hydrophilic property with a contact angle of around 20 degree. Ofloxacin as a model drug was loaded into films by adsorption diffusion method. Loaded drug amount in CS/GO composite film was a little larger than that in CS film, but without significant difference. The drug release behaviors from CS/GO composite film or CS film were investigated and revealed that the loaded drug could be controlled to release in the first hour. Two kinds of cells were used to evaluate the biocompatibility of films by in vitro method. It was found that both CS/GO composite film and CS film could support human umbilical vein endothelial cell (HUVEC) growth. But for human epidermal fibroblasts (HSF) cells, CS/GO composite film could promote HSF cells growth and proliferation much better than CS film.

scholarly journals Discovery of a New Xanthone against Glioma: Synthesis and Development of (Pro)liposome Formulations

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 409 ◽  
Author(s):  
Ana Alves ◽  
Marta Correia-da-Silva ◽  
Claúdia Nunes ◽  
João Campos ◽  
Emília Sousa ◽  
...  
Keyword(s):  
Potent Inhibitor ◽  
Drug Carrier ◽  
Drug Carriers ◽  
Current Treatment ◽  
Tumor Cell Growth ◽  
Drying Method ◽  
New Agents ◽  
Liposome Formulation ◽  
Growth Activity

Following our previous work on the antitumor activity of acetylated flavonosides, a new acetylated xanthonoside, 3,6-bis(2,3,4,6-tetra-O-acetyl-β-glucopyranosyl)xanthone (2), was synthesized and discovered as a potent inhibitor of tumor cell growth. The synthesis involved the glycosylation of 3,6-di-hydroxyxanthone (1) with acetobromo-α-d-glucose. Glycosylation with silver carbonate decreased the amount of glucose donor needed, comparative to the biphasic glycosylation. Xanthone 2 showed a potent anti-growth activity, with GI50 < 1 μM, in human cell lines of breast, lung, and glioblastoma cancers. Current treatment for invasive brain glioma is still inadequate and new agents against glioblastoma with high brain permeability are urgently needed. To overcome these issues, xanthone 2 was encapsulated in a liposome. To increase the well-known low stability of these drug carriers, a proliposome formulation was developed using the spray drying method. Both formulations were characterized and compared regarding three months stability and in vitro anti-growth activity. While the proliposome formulation showed significantly higher stability, it was at the expense of losing its biocompatibility as a drug carrier in higher concentrations. More importantly, the new xanthone 2 was still able to inhibit the growth of glioblastoma cells after liposome formulation.

scholarly journals Sustained Release and Cytotoxicity Evaluation of Carbon Nanotube-Mediated Drug Delivery System for Betulinic Acid

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Julia M. Tan ◽  
Govindarajan Karthivashan ◽  
Palanisamy Arulselvan ◽  
Sharida Fakurazi ◽  
Mohd Zobir Hussein
Keyword(s):  
Carbon Nanotubes ◽  
Cell Line ◽  
Drug Carrier ◽  
Drug Loading ◽  
Fibroblast Cell ◽  
Xrd Analysis ◽  
Prolonged Release ◽  
Loading Capacity ◽  
Cytotoxicity Studies

Carbon nanotubes (CNTs) have been widely utilized as a novel drug carrier with promising future applications in biomedical therapies due to their distinct characteristics. In the present work, carboxylic acid-functionalized single-walled carbon nanotubes (f-SWCNTs) were used as the starting material to react with anticancer drug, BA to produce f-SWCNTs-BA conjugate viaπ-πstacking interaction. The conjugate was extensively characterized for drug loading capacity, physicochemical properties, surface morphology, drug releasing characteristics, and cytotoxicity evaluation. The results indicated that the drug loading capacity was determined to be around 20 wt% and this value has been verified by thermogravimetric analysis. The binding of BA onto the surface of f-SWCNTs was confirmed by FTIR and Raman spectroscopies. Powder XRD analysis showed that the structure of the conjugate was unaffected by the loading of BA. The developed conjugate was found to release the drug in a controlled manner with a prolonged release property. According to the preliminaryin vitrocytotoxicity studies, the conjugate was not toxic in a standard fibroblast cell line, and anticancer activity was significantly higher in A549 than HepG2 cell line. This study suggests that f-SWCNTs could be developed as an efficient drug carrier to conjugate drugs for pharmaceutical applications in cancer chemotherapies.

Enzyme-Resistant Starch for Oral Colon-Targeting Drug Delivery System

2005 ◽  
Vol 288-289 ◽  
pp. 129-132 ◽  
Author(s):  
Ling Chen ◽  
Xiao Xi Li ◽  
Lin Li ◽  
Bing Li
Keyword(s):  
Drug Delivery ◽  
Resistant Starch ◽  
Drug Carriers ◽  
Enzymatic Digestion ◽  
Oral Route ◽  
X Ray Diffraction ◽  
Colon Targeting ◽  
Potential System ◽  
Model Drug

Colon-targeting drug delivery systems (CDDSs) are employed to improve the bioavailability of protein and peptide drugs through the oral route. So it is important to prepare the drug carriers for oral CDDS. In this study, the Enzyme-Resistant starch (RS) was studied for use as a vehicle in oral colon-targeting drug delivery. The characteristics of RS powders were investigated by X-ray diffraction, polarizing microscopy, DSC and SEM, and their film were examined by enzymatic digestion test. The results showed that RS could be a promising film-former for pharmaceutical coatings, having good stability to enzymatic digestion. Furthermore, a novel peroral formulation using RS coating and bovine serum albumin as a model drug was studied for colon-specific drug delivery in vitro. Drug release studies have shown that RS coating could delivery the drug to the colon and the release rate in simulated colonic fluids was dependent on the biodegradation of RS and its coatings. It is indicated that the RS coated tablet is a potential system for oral CDDS.

scholarly journals Preparation and in vitro release kinetics of nitrendipine-loaded PLLA–PEG–PLLA microparticles by supercritical solution impregnation process

RSC Advances ◽  
2019 ◽  
Vol 9 (28) ◽  
pp. 16167-16175 ◽  
Author(s):  
Shiping Zhan ◽  
Jingchang Wang ◽  
Weijing Wang ◽  
Liyun Cui ◽  
Qicheng Zhao
Keyword(s):  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Impregnation Process ◽  
Supercritical Solution ◽  
Model Drug ◽  
Polymer Microparticles ◽  
Kinetics Of ◽  
Vitro Release

In this work, drug-loaded polymer microparticles were prepared by a supercritical solution impregnation (SSI) process with nitrendipine as the model drug and PLLA–PEG–PLLA as the drug carrier.

scholarly journals Temperature-Responsive Molecular Assemblies Using Oligo(Ethylene Glycol)-Attached Polyamidoamine Dendron Lipids and their Functions as Drug Carriers

2020 ◽  
Vol 11 (1) ◽  
pp. 16
Author(s):  
Takuya Hashimoto ◽  
Yuji Hirai ◽  
Eiji Yuba ◽  
Atsushi Harada ◽  
Kenji Kono
Keyword(s):  
Ethylene Glycol ◽  
Drug Carrier ◽  
Drug Carriers ◽  
Head Group ◽  
Stimuli Responsive ◽  
Alkyl Chains ◽  
Temperature Responsive ◽  
Poly Ethylene ◽  
External Stimuli

Temperature-responsive nanocarrier systems using external stimuli are one of the most widely investigated stimuli-responsive strategies because heat is easy and safe to use for hyperthermia and controlled drug delivery. Polyamidoamine dendron lipids (PAMAM-DLs) composed of PAMAM dendron as head group and two alkyl chains can exhibit temperature-responsive morphological change through the attachment of suitable moieties to terminal of PAMAM dendron. In this study, oligo(ethylene glycol)s including ethoxy- or methoxy-diethylene glycols were attached to the terminals of PAMAM-DL, and temperature-responsive properties of their self-assemblies were evaluated by calorimetric and turbidity measurements. In the evaluation of temperature-responsive properties, ethoxy diethylene glycol (EDEG)-attached PAMAM-DL composed of two saturated alkyl chains and PAMAM dendron with 1st generation had lipid bilayer structure and suitable cloud point for the application as drug carrier. In vitro performances of the assemblies combining EDEG-attached PAMAM-DLs with cholesteryl-oxy-poly(ethylene glycol) (PEG-Chol) was evaluated using doxorubicin (DOX) as an anticancer drug. Cellular uptake of DOX-loaded EDEG-attached PAMAM-DL/PEG-Chol assemblies was promoted at 42 °C rather than 37 °C, resulting in an effective decrease in cell viability.

Synthesis and characterization of an amphiphilic methoxy poly(l-lactide)-block-poly(glycidylmethacrylate) copolymer as a drug nanocarrier

e-Polymers ◽  
2012 ◽  
Vol 12 (1) ◽  
Author(s):  
Massoumeh Bagheri ◽  
Forough Motirasoul
Keyword(s):  
Diblock Copolymer ◽  
Ring Opening ◽  
Polymeric Micelles ◽  
Drug Carrier ◽  
Controlled Drug Release ◽  
Transmission Electron ◽  
Model Drug ◽  
Dialysis Bag

AbstractPresent research is a preliminary report on the amphiphilic diblock copolymer (mPLA-b-PGMA) comprising hydrophobic methoxy poly(L-lactide) (mPLA) and hydrophilic poly(glycidyl methacrylate) (PGMA) segments was used as a promising drug carrier. Diblock copolymer was synthesized via ring opening polymerization (ROP) and atom transfer radical polymerization (ATRP) methods. Methanol first initiated ROP of L-lactide in the presence of tin(II)bis(2-ethylhexanoate) (Sn(oct)2) as a catalyst. The resulting monohydroxyl-terminated polylactic acid (mPLA) was subsequently converted to a bromine-ended macroinitiator (mPLA-Br) by esterification with 2-bromisobutyryl bromide. The copolymer mPLA-b-PGMA was synthesized in a subsequent ATRP of GMA. The obtained polymers were characterized by means of 1H NMR, FTIR, DSC and TGA. The copolymer mPLA-b- PGMA self-assembled into nanoscale micelles in aqueous solutions, as investigated by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The TEM image of polymeric micelles showed that the micelles were spherical in shape and that their diameters were in the range of 80-140 nm. Then by using the naproxen as a hydrophobic model drug, the drug-loaded micelles with 81.18 % loading efficiency and 16.24 % loading capacity were prepared. Moreover, in vitro release study of naproxen was performed using dialysis bag in phosphate-buffered solution at 37°C and pH at 7.4. Accordingly, these polymeric micelles may provide as an effective drug carrier for controlled drug release.

Evaluation of surface acetylated and internally quaternized poly(propylene imine) dendrimer as a biocompatible drug carrier for piroxicam as a model drug

RSC Advances ◽  
2015 ◽  
Vol 5 (129) ◽  
pp. 106461-106475 ◽  
Author(s):  
E. Murugan ◽  
V. Yogaraj ◽  
D. P. Geetha Rani ◽  
Alok Kumar Sinha
Keyword(s):  
Drug Carrier ◽  
Drug Carriers ◽  
Model Drug ◽  
Poly Propylene

Two types of new surface acetylated and internally quaternized poly(propylene imine) dendrimers QPPI-NHAc (G2)/(G3) were prepared, characterized and then demonstrated as potential and biocompatible drug carriers using piroxicam as a model drug.

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