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جستجوی مقالات مرتبط با کلیدواژه « copolymer » در نشریات گروه « پزشکی »

  • Ashkan Mohammad Sadeghi, Fatemeh Farjadian, Shohreh Alipour *
    Objective(s)
    Ocular inserts are usually polymeric thin films with increased ocular residence time and sustained drug release capacity. Sodium alginate is a biocompatible and biodegradable carrier; however, initial burst release of encapsulated drug within it, is recognized as a challenge. Grafting –addition of functional moieties to a polymer– is a technique to modify polymers’ physicochemical properties, including higher ability to control drug release. Linezolid (LNZ) solution is used in consecutive doses in treatment of antibiotic-resistant Gram-positive bacterial infections especially induced by methicillin resistant Staphylococcus aureus (MRSA).
    Materials and Methods
    Grafted alginate copolymers were synthesized using butyl methacrylate (BMC) and lauryl methacrylate (LMC) at two different reaction times (12 hr and 24 hr). Copolymerization was evaluated by 1H-NMR, Ft-IR, and TGA. Copolymer safety was examined by cytotoxicity test against HEK-293 cell. Linezolid inserts were prepared using optimized copolymers and characterized.
    Results
    1H-NMR, Ft-IR, and TGA confirmed the successful grafting of alginate copolymers. ALG-B24 and ALG-L12 showed the highest safety against HEK-293 cell line comparing with intact alginate. Linezolid insert characterization results indicated a slower linezolid release profile related to creation of a lipophilic structure. A better strength property for linezolid loaded ALG-B24 and ALG-L12 inserts was obtained while ALG-L12 showed a stronger adhesive force compared with intact alginate. Antibacterial efficacy on clinical isolated MRSA after 24 hr was similar to linezolid solution.
    Conclusion
    Lipophilic alginate copolymer (ALG-L12) showed a sustained release capability while retaining its main feature in strong film forming ability so it seems to be a promising safe carrier.
    Keywords: Copolymer, Grafting, Linezolid, Ocular insert, Sodium alginate}
  • Zeinolabedin Sharifian, Batool Hashemibeni, Majid Pourentezari*, Ali Valiani, Mohammad Mardani, Mohammad Zamani Rarani, Hamidreza Pourentezari
    Background and Aims

    Tissue engineering is a relatively novel field that has been intensely developing during recent years and has shown to be excessively promising when used for cartilage regeneration. Scaffolds represent important components for tissue engineering.

    Materials and Methods

    The Poly Lactic-Co-Glycolic Acid (PLGA) impregnated with fibrin and hyaluronic acid (HA) produce hybrid scaffolds. human adipose-derived stem cells (hADSCs) were seeded in scaffolds and cultured in chondrogenic media. The viability of cells in different groups was assessed by MTT. The expression of chondrogenic related genes [Sox9, type II collagen (Col II), Aggrecan(AGG)] and type X collagen (Col X) was quantified by real-time polymerase chain reaction.

    Results

    The results of the real-time PCR showed SOX9, AGG and Col X gene expression in the control groups being significantly lower than the other groups (p≤0.05). It also demonstrated Col II gene expression in the control group being significantly lower than the PLGA/Fibrin and PLGA/Fibrin/HA groups (p≤0.05). The Col X gene expression of cells in PLGA/HA and PLGA/Fibrin/HA groups significantly decreased in comparison with the PLGA/Fibrin group (p≤0.05).

    Conclusions

    These conclusions indicate that administration of PLGA/ Fibrin and PLGA/HA scaffolds, particularly PLGA/Fibrin/ HA, motivates chondrogenesis in hADSCs. This can be diminished by decreasing hypertrophic markers and increasing characteristic markers of hyaline cartilage.

    Keywords: Copolymer, Hyaluronic acid, Mesenchymal stem cells, Polylactic acid-polyglycolic acid, Tissue scaffolds}
  • Ashkan Hassankhani Rad, Farshid Asiaee, Sevda Jafari, Ali Shayanfar, Afsaneh Lavasanifar, OmmoleilaMolavi*
    Introduction

    Silibinin is a naturally occurring compound with known positive impacts on prevention and treatment of many types of human illnesses in general and cancer in particular. Silibinin is poorly water soluble which results in its insufficient bioavailability and lack of therapeutic efficacy in cancer. Here, we proposed to examine the potential of micelles composed of poly(ethylene glycol) (PEG) as the hydrophilic block and poly(ε-caprolactone) (PCL), poly(α-benzylcarboxylate-ε-caprolactone) (PBCL), or poly(lactide)-(PBCL) (PLA-PBCL) as hydrophobic blocks for enhancing the water solubility of silibinin and its targeted delivery to tumor.

    Methods

    Co-solvent evaporation method was used to incorporate silibinin into PEG-PCL based micelles. Drug release profiles were assessed using dialysis bag method. MTT assay also was used to analyze functional activity of drug delivery in B16 melanoma cells.

    Results

    Silibinin encapsulated micelles were shown to be less than 60 nm in size. Among different structures under study, the one with PEG-PBCL could incorporate silibinin with the highest encapsulation efficiency being 95.5%, on average. PEG-PBCL micelles could solubilize 1 mg silibinin in 1 mL water while the soluble amount of silibinin was found to be 0.092 mg/mL in the absence of polymeric micelles. PEG-PBCL micelles provided the sustained release of silibinin indicated with less than 30% release of silibinin within 24 hours. Silibinin encapsulated in PEG-PBCL micelles resulted in growth inhibitory effect in B16 cancer cells which was significantly higher than what observed with free drug.

    Conclusion

    Our findings showed that PEG-PBCL micellar nanocarriers can be a useful vehicle for solubilization and targeted delivery of silibinin.

    Keywords: Silibinin, Micelle, Copolymer, PEG-PCL, Melanoma}
  • بررسی تخریب پذیری و سمیت سلولی کوپلیمرهای دوتایی mPEG-PCL و سه تایی PCL-PEG-PCL بر روی سلولهای نرمال کلیه
    حمیدرضا خیری منجیلی، حسین دانافر *، علی شرفی
    سابقه و هدف
    در سیستم های دارورسانی با استفاده از کوپلیمرها دانستن میزان تخریب پذیری و زیست سارگاری پلیمرها از اهمیت ویژه ای برخوردار است.
    روش بررسی
    در این پروژه ابتدا کوپلیمرهای PCL-PEG-PCL و کوپلیمرهای mPEG-PCLبه روش پلیمریزاسیون حلقه گشایی سنتز و از تکنیکهای مختلفی همچون GPC، HNMR، FT-IR، و DSC برای تایید سنتز موفقیت آمیز و تعیین ویژگی های آنها استفاده گردید.تخریب پذیری کوپلیمرها با استفاده از تکنیک GPC و از روی میزان کاهش جرم و زیست سازگاری کوپلیمرها با استفاده از سمیت سلولی این کوپلیمرها با استفاده از MTT assay بر روی سلولهای نرمال کلیه(HEK 293) انجام گرفت.
    یافته ها
    نتایج HNMR وFTIR صحت تشکیل کوپلیمرهای سه تایی و دوتایی سنتز شده را تایید نموده و با استفاده از تکنیک DSC نقطه ذوب کوپلیمرهای سه تایی و دوتایی به ترتیب در55 0C و °C 68/58می باشد و همچنین این کوپلیمرها به ترتیب ارای جرم مولکولی میانگین 16000و12223 دالتون می باشد. تخریب پذیری این کوپلیمرها در محیط بافری صورت گرفت که در انتهای روز 31 جرم مولکولی پلیمردوتایی و کوپلیمر سه تایی به ترتیب در حدود 7852 و 9586 دالتون می باشد. از روی میزان IC50 محاسبه برای هرترکیب بر روی سلولهای کلیه(HEK 293) نشان داده شده که کوپلیمرهای دو تایی و سه تایی هیچ گونه سمیتی نداشته اند و کاملا زیست سازگار هستند.
    نتیجه گیری
    این کوپلیمرهای سه تایی و دوتایی زیست تخریب پذیری بالایی داشتند و همچنین با توجه به نداشتن هیچ گونه سمیت سلولی روی سلولهای نرمال کلیه از لحاظ زیستی نیز زیست سازگار می باشند.
    کلید واژگان: کوپلیمر, زیست سازگاری, زیست تخریب پذیری, سمیت سلولی}
    Assessment of biodegradability and cytotoxicity of mPEG-PCL diblock copolymers and PCL-PEG-PCL tri block copolymers on HEK293 cells
    Dr Hamidreza Kheiri Manjilli, Dr Hossein Danafar *, Dr Ali Sharafi
    Background And Aim
    Knowledge of biodegradability and biocompatibility rate in drug delivery systems is very important.
    Material and
    Method
    This study PCL–PEG–PCL and MPEG-PCL copolymers were synthesized by ring-opening copolymerization. HNMR, FTIR, DSC and GPC techniques were used to confirm successful synthesis and determination of the characteristics of the copolymers. We evaluated biocompatibility by MTT assay on the basis of cytotoxicity effect of these copolymers on HEK293 cells. Biodegradation was evaluated by GPC technique.
    Results
    The results of HNMR and FTIR confirmed synthesis of diblock and tri block copolymers. Using DSC technique, melting point of tri block and diblock copolymers were 55 °C and 58.68°C and also the average molecular weights of these copolymers were 16,000 and 12,223 Dalton, respectively. The degradation of these copolymers were performed in buffer solution and at the end of the 31st day, molecular weights of diblock and tri block Copolymers were 7852 and 9586 Dalton respectively. Based on IC50 , diblock and tri block copolymers had no toxic effects on HEK293 cells and are biocompatibile .
    Conclusion
    diblock and tri block copolymers had high rates of biodegradability and because of not having toxic effects on normal renal cells, they were biocompatible.
    Keywords:
    Keywords: Copolymer, Cytotoxicity, Biocompatibility, Biodegradability}
  • Mitra Alami-Milani, Parvin Zakeri-Milani, Hadi Valizadeh, Roya Salehi, Sara Salatin, Ali Naderinia, Mitra Jelvehgari*
    Many studies have focused on how drugs are formulated in the sol state at room temperature leading to the formation of in situ gel at eye temperature to provide a controlled drug release. Stimuli-responsive block copolymer hydrogels possess several advantages including uncomplicated drug formulation and ease of application, no organic solvent, protective environment for drugs, site-specificity, prolonged and localized drug delivery, lower systemic toxicity, and capability to deliver both hydrophobic and hydrophilic drugs. Self-assembling block copolymers (such as diblock, triblock, and pentablock copolymers) with large solubility variation between hydrophilic and hydrophobic segments are capable of making temperature-dependent micellar assembles, and with further increase in the temperature, of jellifying due to micellar aggregation. In general, molecular weight, hydrophobicity, and block arrangement have a significant effect on polymer crystallinity, micelle size, and in vitro drug release profile. The limitations of creature triblock copolymers as initial burst release can be largely avoided using micelles made of pentablock copolymers. Moreover, formulations based on pentablock copolymers can sustain drug release for a longer time. The present study aims to provide a concise overview of the initial and recent progresses in the design of hydrogel-based ocular drug delivery systems.
    Keywords: Penta block, Copolymer, Thermosensetive, Micelle, Self-assembled, Ocular}
  • Leila Barghi, Davoud Asgari, Jaleh Barar, Hadi Valizadeh*
    Purpose
    Polycaprolactone (PCL) is a biodegradable polyester and has attracted attention as a suitable carrier for development of controlled drug delivery due to its non-toxicity and biocompatibility. It has been reported that the biodegradability of PCL can be enhanced by copolymerization with PEG. Molecular weight (Mw) and CL block lengths optimization in a series of synthesized PCEC copolymers was the main purpose of this study.
    Methods
    The composition of copolymers was designed using full factorial methodology. Molecular weight of used PEG (4 levels) and weight ratio of epsilon-caprolactone/PEG (3 levels) were selected as independent variables. The PCEC copolymers were synthesized by ring opening polymerization. Formation of copolymers was confirmed by FT-IR spectroscopy as well as H-NMR. The Mn of PCEC copolymers was calculated from HNMR spectra. The thermal behavior of copolymers was characterized on differential scanning calorimeter.
    Results
    Molecular weight of twelve synthesized copolymers was ranged from 1782 to 9264. In order to evaluate the effect of selected variables on the copolymers composition and Mw, a mathematical model for each response parameter with p-value less than 0.001were obtained. Average percent error for prediction of total Mn of copolymers and Mn of CL blocks were 13.81% and 14.88% respectively.
    Conclusion
    In conclusion, the proposed model is significantly valid due to obtained low percent error in Mn prediction of test sets.
    Keywords: PCEC, Copolymer, Full factorial methodology, Molecular weight}
  • Mitra Jelvehgari, Seyed Montazam
    Background
    Microencapsulation is a useful method to prolong a drug release from dosage forms and to reduce its adverse effect (1) among various available methods. The microencapsulation of hydrophilic active ingredients requires the use of a polar dispersing phase such as a mineral oil. Acetone/paraffin systems are conventionally used..
    Objectives
    The current study aimed to investigate two different microencapsulation techniques comparatively, water in oil in oil (w/o/o) and oil in oil (o/o), for theophylline (TH) loaded ethylcellulose (EC), cellulose acetate butyrate (CAB), Eudragit RS and RL microspheres with regard to loading efficiency, release and degradation kinetics..
    Materials And Methods
    Microspheres were prepared by the emulsification method by solvent diffusion/evaporation technique and different polymers which were incorporated into microspheres to control the release rate of drug. Theophylline (TH) was chosen as a model drug. The emulsion technique was investigated for to prepare theophylline microparticles. EC and CAB and acrylatemethacrylate copolymer corresponding to the above ratios were selected as microparticles wall materials. The effects of type polymers on the physical characteristics and dissolution of the microparticles were also studied. However, the TH loading efficiency (for w/o/o emulsion about 90.64% and o/o emulsion about 73.90/5 to 95.90%) and the TH release kinetics were influenced by the microencapsulation technique..
    Results
    The results demonstrated that the o/o microspheres (containing of CAB) was most appropriate, providing a high encapsulation efficiency (95.90%) and low initial burst release (6.45%). The microspheres prepared with CAB polymer showed faster dissolution rate than other polymers with 0.75: 1 drug to polymer ratio. The double emulsion technique with EC as wall material gave the high dissolution efficiency (80.48%) of microcapsules..
    Conclusions
    Eudragit RS microspheres showed higher yield (90%). The release of TH from CAB and Eudragit RL walled microcapsules was slow whilst the release from those of EC and Eudragit RS were faster. The type of polymer and the drug to polymer ratio were found to be the key factors affecting the release profile which could lead to micro-spheres with desired release behavior.
    Keywords: Drug Componding, Copolymer, Drug Carriers}
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