Preparation, Cytotoxicity and Degradability of Chitosan-Based Thermosensitive Hydrogels as Drug Delivery System

2009 ◽  
Vol 79-82 ◽  
pp. 1531-1534 ◽  
Author(s):  
Hui Yun Zhou ◽  
Jian Wang ◽  
Wei Fen Zhang ◽  
Ye Wang ◽  
Xi Guang Chen

A new thermosensitive hydrogel had been prepared that could be transformed into gel at 37 °C from chitosan and a mixture of α- and β-glycerophosphate (αβ-GP). The appearance of hydrogel was compact and corrugated. There was little granule in the appearance of gel loaded with adriamycin and the granules might be crystals of the added model drug. In vitro cytotoxicity of the hydrogel was tested by the MTT method using mouse embryonic fibroblasts (MEF). MEF cultured with leachates of CS-αβ-GP were investigated and the relative growth rate (RGR) was calculated and the cytotoxicity was graded by generally accepted standard. The study of in vitro degradation of CS-αβ-GP hydrogels included hydrolysis and degradation by lysozyme. The CS-αβ-GP thermosensitive hydrogel was degradable in vitro and the degradation rate was faster in lysozyme solution than that in the medium of PBS. So the CS-αβ-GP system had good cell biocompatibility and biodegradability which provided possibilities and foundations for the further research.

Author(s):  
Kumbakonam Balachandran Ilango ◽  
Senguttuvan Gowthaman ◽  
Kumbakonam Ilango Seramaan ◽  
Kumarappan Chidambaram ◽  
Mohammad F Bayan ◽  
...  

Mucilage from Coccinia grandis was extracted, isolated by maceration technique and precipitated, accordingly. The mucilage was evaluated for its physicochemical, binding, and disintegrant properties in tablets using paracetamol as a model drug. The crucial physicochemical properties such as flow properties, solubility, swelling index, loss on drying, viscosity, pH, microbial load, cytotoxicity were evaluated and the compatibility was analysed using sophisticated instrumental methods (TGA, DTA, DSC, and FTIR). The binding properties of the mucilage were used at three different concentrations and compared with starch and PVP as standard binders. The disintegrant properties of mucilage were used at two different concentrations and compared with standard disintegrants MCCP, SSG, and CCS. The wet granulation technique was used for the preparation of granules and was evaluated for the flow properties. The tablets were punched and evaluated for their hardness, friability, assay, disintegration time, in vitro dissolution profiles. In vitro cytotoxicity study of the mucilage was performed in human embryonic kidney (HEK) cell line using cytotoxic assay by MTT method. The outcome of the study indicated that the mucilage had good performance when compared with starch and PVP. Further, the mucilage acts as a good disintegrant than MCCP, SSG and CCS to paracetamol tablets. Moreover, the in vitro cytotoxicity evaluation results demonstrated that the mucilage is non-cytotoxic to human cells and is safe.


2019 ◽  
Vol 2019 ◽  
pp. 1-9
Author(s):  
Chang-Yuan Zhang ◽  
Yi-Ling Cheng ◽  
Xin-Wen Tong ◽  
Hao Yu ◽  
Hui Cheng

The aim of the present study was to evaluate the in vitro cytotoxicity of self-adhesive dual-cured resin cement (SADRC) polymerized beneath three different cusp inclinations of zirconia with different light curing time. A commercial SADRC (Multilink Speed) was polymerized beneath zirconia (ZrO2) with three different cusp inclinations (0°, 20°, and 30°) for 20 s or 40 s. After being stored in light-proof box for 24 h, the ZrO2-SADRC specimens were immersed in DMEM for 72 h and then we got the extract solution, cultured the human gingival fibroblasts (HGF, 8 × 103 per well) with 100% or 50% concentrations of the extract solution for 24 h, 72 h, and 120 h, respectively, and evaluated cytotoxicity of the polymerized SADRC with CCK-8 assay in optical density (OD) values, relative growth rates (RGR), and cytotoxicity grades. Statistical analysis was conducted using a two-way ANOVA followed by post hoc Student–Newman–Keuls test. The OD values varied from 0.8930 to 3.2920, the RGR varied from 33.93% to 98.68%, and the cytotoxicity grades varied from 0 to 2. There was significant difference in the OD values among the different cusp inclinations of zirconia (P < 0.001), and there was significant difference in the OD values between the different light curing times in some situations (P < 0.05). The cusp inclination of zirconia affects the in vitro cytotoxicity of SADRC. Prolonging the light curing time from 20 s to 40 s can reduce the in vitro cytotoxicity of SADRC when the cusp inclination of zirconia is smaller than 20°.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 413 ◽  
Author(s):  
Hsiu-Chao Lin ◽  
Madonna Rica Anggelia ◽  
Chih-Chi Cheng ◽  
Kuan-Lin Ku ◽  
Hui-Yun Cheng ◽  
...  

Tacrolimus is an immunosuppressive agent for acute rejection after allotransplantation. However, the low aqueous solubility of tacrolimus poses difficulties in formulating an injection dosage. Polypeptide thermosensitive hydrogels can maintain a sustained release depot to deliver tacrolimus. The copolymers, which consist of poloxamer and poly(l-alanine) with l-lysine segments at both ends (P–Lys–Ala–PLX), are able to carry tacrolimus in an in situ gelled form with acceptable biocompatibility, biodegradability, and low gelling concentrations from 3 to 7 wt %. By adding Pluronic F-127 to formulate a mixed hydrogel system, the drug release rate can be adjusted to maintain suitable drug levels in animals with transplants. Under this formulation, the in vitro release of tacrolimus was stable for more than 100 days, while in vivo release of tacrolimus in mouse model showed that rejection from skin allotransplantation was prevented for at least three weeks with one single administration. Using these mixed hydrogel systems for sustaining delivery of tacrolimus demonstrates advancement in immunosuppressive therapy.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 726
Author(s):  
Kuldeep Kumar Bansal ◽  
Ezgi Özliseli ◽  
Gaurav Kumar Saraogi ◽  
Jessica M. Rosenholm

Biodegradable polymers from renewable resources have attracted much attention in recent years within the biomedical field. Lately, poly(δ-decalactone) based copolymer micelles have emerged as a potential drug delivery carrier material as a sustainable alternative to fossil-based polymers. However, their intracellular drug delivery potential is not yet investigated and therefore, in this work, we report on the synthesis and cellular uptake efficiency of poly(δ-decalactone) based micelles with or without a targeting ligand. Folic acid was chosen as a model targeting ligand and Rhodamine B as a fluorescent tracer to demonstrate the straightforward functionalisation aspect of copolymers. The synthesis of block copolymers was accomplished by a combination of facile ring-opening polymerisation and click chemistry to retain the structure uniformity. The presence of folic acid on the surface of micelles with diameter ~150 nm upsurge the uptake efficiency by 1.6 fold on folate receptor overexpressing MDA-MB-231 cells indicating the attainment of targeting using ligand functionality. The drug delivery capability of these carriers was ascertained by using docetaxel as a model drug, whereby the in vitro cytotoxicity of the drug was significantly increased after incorporation in micelles 48 h post incubation. We have also investigated the possible endocytosis route of non-targeted micelles and found that caveolae-mediated endocytosis was the preferred route of uptake. This work strengthens the prospect of using novel bio-based poly(δ-decalactone) micelles as efficient multifunctional drug delivery nanocarriers towards medical applications.


1998 ◽  
Vol 3 (1) ◽  
pp. 49-53 ◽  
Author(s):  
J. Enrico Lazaro ◽  
Frederick Gay

The microculture tetrazolium assay using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) was used to estimate the 50% inhibitory concentration of chloroquine, quinine, artemisinin, and atovaquone using a Plasmodium falciparum in vitro culture system. The MTT assay was compared to the standard tritiated hypoxan-thine assay and to a previously described method, the 2,2′-di-p-nitrophenyl-5,5′-diphenyl-3,3′-[3,3′-dimethoxy-4,4′-diphenylenel-ditetrazolium chloride (NBT) assay. In general, the results show that the three assays generate comparative results. The results of this study suggest that the MTT method is able to give a profile of cytotoxic dose response effects over a wide range of concentrations of a drug. The method may be used in work that does not require extreme pre-cision and sensitivity, for instance, as a portable rapid screen to assay natural products for in vitro cytotoxic ac-tivity against Plasmodium falciparum.


2020 ◽  
Author(s):  
Deng Linxin ◽  
Li Song ◽  
Xuehua Sun

Abstract The ligands of (E)-bis(p-3-nitrobenzoic acid) vinyl (C16H10N2O8) were synthesized in three steps, and then the MOF-Zn2(EBNB)2(BPY)2·2H2O was synthesized by solvothermal method. This structure was characterized by X-ray single crystal diffraction, SEM and TG. The drug loading and in vitro release of Zn2(EBNB)2(BPY)2·2H2O were also studied with Methadone as model drug. The result shows that the highest loading amount of Zn2(EBNB)2(BPY)2·2H2O to Methadone was 0.256g/g, and the drug delivery system was a two-phase mode. The results of in vitro cytotoxicity test shows that Zn2(EBNB)2(BPY)2·2H2O has good biocompatibility.


2020 ◽  
Author(s):  
Deng Linxin ◽  
Li Song ◽  
Xuehua Sun

Abstract The ligands of (E)-bis(p-3-nitrobenzoic acid) vinyl (C16H10N2O8) were synthesized in three steps, and then the MOF-Zn2(EBNB)2(BPY)2·2H2O was synthesized by solvothermal method. This structure was characterized by X-ray single crystal diffraction, SEM and TG. The drug loading and in vitro release of Zn2(EBNB)2(BPY)2·2H2O were also studied with Methadone as model drug. The result shows that the highest loading amount of Zn2(EBNB)2(BPY)2·2H2O to Methadone was 0.256g/g, and the drug delivery system was a two-phase mode. The results of in vitro cytotoxicity test shows that Zn2(EBNB)2(BPY)2·2H2O has good biocompatibility.


2014 ◽  
Vol 893 ◽  
pp. 56-59 ◽  
Author(s):  
Eko Pujiyanto ◽  
Pringgo Widyo Laksono ◽  
Joko Triyono

This study prepared hydroxyapatite powder that synthesized from natural gypsum rock and find out physicalchemical and cytotoxicity properties. The synthesis realized by reacting natural gypsum powder with 1M of (NH4)2HPO4 solutions using a microwave. Characterizations of natural gypsum powder and hydroxyapatite powder were conducted by XRD, XRF and SEM. In vitro cytotoxicity testings of hydroxyapatite powder were conducted by MTT method using vero cells. XRD patterns of gypsum powder closed to JCPDF 33-0311 (gypsum standard). Characteristics of gypsum powder i.e. contained 41.72% CaO, level of purity 91,6 % and crystal size 7,147 nm. Charateristic of hydroxyapatite powder that synthesized from natural gypsum powder i.e. contained 46.91% CaO and 40.20% P2O5, XRD patern closed to JCPDF 09-432 (hydroxyapatite standard), level of purity 99 % and crystal size 1.243 nm. There were not significantly difference in cytotoxicity properties of hydroxyapatite powder that synthesized from natural gypsum rock and commercial hydroxyapatite powder (p= 0.086). These results indicated hydroxyapatite powder that synthesized from natural gypsum rock possible to be used as bone substitutes.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1672
Author(s):  
Sabrina Sciabica ◽  
Giovanni Tafuro ◽  
Alessandra Semenzato ◽  
Daniela Traini ◽  
Dina M. Silva ◽  
...  

Hyaluronic acid (HA), an excellent biomaterial with unique bio properties, is currently one of the most interesting polymers for many biomedical and cosmetic applications. However, several of its potential benefits are limited as it is rapidly degraded by hyaluronidase enzymes. To improve the half-life and consequently increase performance, native HA has been modified through cross-linking reactions with a natural and biocompatible amino acid, Ornithine, to overcome the potential toxicity commonly associated with traditional linkers. 2-chloro-dimethoxy-1,3,5-triazine/4-methylmorpholine (CDMT/NMM) was used as an activating agent. The new product (HA–Orn) was extensively characterized to confirm the chemical modification, and rheological analysis showed a gel-like profile. In vitro degradation experiments showed an improved resistance profile against enzymatic digestions. Furthermore, in vitro cytotoxicity studies were performed on lung cell lines (Calu-3 and H441), which showed no cytotoxicity.


Gels ◽  
2022 ◽  
Vol 8 (1) ◽  
pp. 44
Author(s):  
Jomarien García-Couce ◽  
Miriela Tomás ◽  
Gastón Fuentes ◽  
Ivo Que ◽  
Amisel Almirall ◽  
...  

Intra-articular administration of anti-inflammatory drugs is a strategy that allows localized action on damaged articular cartilage and reduces the side effects associated with systemic drug administration. The objective of this work is to prepare injectable thermosensitive hydrogels for the long-term application of dexamethasone. The hydrogels were prepared by mixing chitosan (CS) and Pluronic-F127 (PF) physically. In addition, tripolyphosphate (TPP) was used as a crosslinking agent. Chitosan added to the mix increased the gel time compared to the pluronic gel alone. The incorporation of TPP into the material modified the morphology of the hydrogels formed. Subsequently, MTS and Live/Dead® experiments were performed to investigate the toxicity of hydrogels against human chondrocytes. The in vitro releases of dexamethasone (DMT) from CS-PF and CS-PF-TPP gels had an initial burst and took more time than that from the PF hydrogel. In vivo studies showed that hydrogels retained the fluorescent compound longer in the joint than when administered in PBS alone. These results suggest that the CS-PF and CS-PF-TPP hydrogels loaded with DMT could be a promising drug delivery platform for the treatment of osteoarthritis.


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