scholarly journals Synthesis of Ester-linked Taxol-glycoside Conjugate and Its Application to Drug Delivery System Using Immunoliposome Targeted with Trastuzumab and Cetuximab

2018 ◽  
Vol 13 (7) ◽  
pp. 1934578X1801300
Author(s):  
Hiroki Hamada ◽  
Shouta Okada ◽  
Noriyoshi Masuoka ◽  
Hatsuyuki Hamada ◽  
Kei Shimoda ◽  
...  

Synthesis of ester-linked glycoside prodrug of taxol, i.e., 7-glycolyltaxol 2″- O-α-D-glucopyranoside, was investigated by chemical synthetic procedure. The encapsulation efficiency and loading efficiency of taxol for liposomes was much improved by modification with glucosyl ester group. The immunoliposomes containing the glycoside prodrug of taxol, i.e., 7-glycolyltaxol 2″- O-α-D-glucopyranoside, exhibited effective anti-tumor activities.

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3580
Author(s):  
Chuda Chittasupho ◽  
Jakrapong Angklomklew ◽  
Thanu Thongnopkoon ◽  
Wongwit Senavongse ◽  
Pensak Jantrawut ◽  
...  

A hydrogel scaffold is a localized drug delivery system that can maintain the therapeutic level of drug concentration at the tumor site. In this study, the biopolymer hydrogel scaffold encapsulating doxorubicin was fabricated from gelatin, sodium carboxymethyl cellulose, and gelatin/sodium carboxymethyl cellulose mixture using a lyophilization technique. The effects of a crosslinker on scaffold morphology and pore size were determined using scanning electron microscopy. The encapsulation efficiency and the release profile of doxorubicin from the hydrogel scaffolds were determined using UV-Vis spectrophotometry. The anti-proliferative effect of the scaffolds against the lung cancer cell line was investigated using an MTT assay. The results showed that scaffolds made from different types of natural polymer had different pore configurations and pore sizes. All scaffolds had high encapsulation efficiency and drug-controlled release profiles. The viability and proliferation of A549 cells, treated with gelatin, gelatin/SCMC, and SCMC scaffolds containing doxorubicin significantly decreased compared with control. These hydrogel scaffolds might provide a promising approach for developing a superior localized drug delivery system to kill lung cancer cells.


2012 ◽  
Vol 600 ◽  
pp. 137-143
Author(s):  
Jing Hui ◽  
Xiao Jie Yu ◽  
Yue Zhang ◽  
Feng Qing Hu

Poly (3-hydroxybutyrate-co-3-hydroxyhexanoate) (PHBHHx) is one of the components of polyhydroxyalkanoates (PHAs) and some of its mechanical properties have been shown to improve over poly (3-hydroxybutyrate) (PHB) and poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV). The investigation of PHBHHx microspheres as a drug delivery system was prepared by emulsion-solvent evaporation method for the sustained release of anti-cancer drug 5-fluorouracil (5-FU) and cyclosporin A (CsA). The mean diameter of the PHBHHx microspheres ranged from 5.24 to 22.10 μm dependent on the different processing parameters. The PHBHHx concentration, emulsifier concentration, anti-cancer drug dosage, and agitation speed, were optimized according to the encapsulation efficiency of 4% PHBHHx, 0.5% SDS, 10 mg anti-cancer drug, and 500 rpm. Under optimized conditions, the encapsulation efficiency of 5-FU and CsA microspheres were 7.19% and 96.44%, respectively. The morphologies of scanning electron microscope (SEM) suggested that PHBHHx microspheres were relatively smooth that provided better dispersion compared to PHB microspheres. The in vitro release profiles indicated 32.42% of 5-FU and 30.61% of CsA were released from PHBHHx microspheres during the initial burst phase, and the drug release from PHBHHx microsphere could be detected even after one month. The characteristics of PHBHHx microspheres demonstrated the feasibility of PHBHHx microsphere as a novel matrix for drug release system. With positive maintenance of the therapeutic concentrations of the drug, side effects can be reduced and patient compliance can be improved.


2013 ◽  
Vol 829 ◽  
pp. 247-250 ◽  
Author(s):  
Negar Motakef-Kazemi ◽  
Seyed Abbas Shojaosadati ◽  
Ali Morsali

Porous metal organic framework (MOF) {Zn2(1,4-bdc)2(dabco)}n synthesized under solvothermal conditions. The MOF was used as the carrier matrices for drug delivery system. The ibuprofen as analgesic and anti-inflammatory drug with 0.6 nm molecule size as a model was entrapped into this new carrier with pores distribution of 1.85 nm. The ibuprofen loading efficiency was obtained by thermogravimetric analysis. The ibuprofen loading efficiency of 22% (w/w) was obtained for this MOF. The entrapped ibuprofen was released over several days by soaking the sample in the simulated body fluid (pH 7.4) at 37 °C. The ibuprofen concentrations were analyzed using UV-vis Spectrophotometer at a wavelength of 260 nm. The result of release reveals that this {Zn2(1,4-bdc)2(dabco)}n is suitable as drug delivery system.


2021 ◽  
Vol 16 (1) ◽  
pp. 1934578X2095365
Author(s):  
Yuya Fujitaka ◽  
Hiroki Hamada ◽  
Hatsuyuki Hamada ◽  
Kohji Ishihara ◽  
Takafumi Iwaki ◽  
...  

Synthesis of the ester-linked glucoside conjugate of paclitaxel, 7-propionylpaclitaxel 3″- O-β-d-glucopyranoside, was carried out by chemoenzymatic procedures. The encapsulation efficiency (EE) values for hybrid-bio-nanocapsules of the compound were much improved in comparison with those of paclitaxel. The hybrid-bio-nanocapsules targeted with trastuzumab, which contained 7-propionylpaclitaxel 3″- O-β-d-glucopyranoside, showed high anticancer activity.


2020 ◽  
Vol 977 ◽  
pp. 178-183
Author(s):  
Findi Citra Kusumasari ◽  
Lukmanul Hakim Samada ◽  
Emil Budianto

Simvastatin is a cholesterol-lowering agent that inhibits the microsomal activity of 3-hydroxy-3-methylglutaril-CoA-reductase (HMG-CoA reductase), enzyme that contributes in biosynthesis cholesterol. Simvastatin has short half-life elimination about 2 hours and low solubility, this condition makes its bioavailability to be quite small. Simvastatin has adverse effect such as myopathy and rhabdomyolysis because of higher dose consumption of simvastatin. Controlled drug delivery system is needed to reduce the adverse effect. One of method that is used in drug delivery system is encapsulation using biodegradable polymer such as poly(L-lactic acid) and poly(ɛ-caprolactone). PLLA and PCL was blended with fix composition PLLA : PCL 60 : 40 (%w/w) by solvent evaporation technique using Tween 80 and Span 80 as emulsifier. Based on the optimization, the best encapsulation efficiency microcapsules were obtained at concentration of Tween 80 0.025% (v/v), Span 80 1% (v/v) with stirring speed at 900 rpm for 1 hour. The encapsulation efficiency was 83.67%. The best microcapsules were dissolved in dissolution media to get drug release profile. The percentage of drug release at pH 1.2 was 0.86% for 3 hours and in the phosphate buffer solution pH 7.4 for 12.22% for 52 hours.


Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
AR Bilia ◽  
G Capecchi ◽  
MC Salvatici ◽  
B Isacchi ◽  
MC Bergonzi

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